|
Inhibition of His-tagged human FAAH N-terminal transmembrane-deleted truncated form expressed in Escherichia coli preincubated for 60 mins before oleamide substrate addition
|
Homo sapiens
|
7.2
nM
|
|
Journal : ACS Med. Chem. Lett.
Title : Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor.
Year : 2011
Volume : 2
Issue : 2
First Page : 91
Last Page : 96
Authors : Johnson DS, Stiff C, Lazerwith SE, Kesten SR, Fay LK, Morris M, Beidler D, Liimatta MB, Smith SE, Dudley DT, Sadagopan N, Bhattachar SN, Kesten SJ, Nomanbhoy TK, Cravatt BF, Ahn K.
Abstract : Fatty acid amide hydrolase (FAAH) is an integral membrane serine hydrolase that degrades the fatty acid amide family of signaling lipids, including the endocannabinoid anandamide. Genetic or pharmacological inactivation of FAAH leads to analgesic and anti-inflammatory phenotypes in rodents without showing the undesirable side effects observed with direct cannabinoid receptor agonists, indicating that FAAH may represent an attractive therapeutic target for the treatment of inflammatory pain and other nervous system disorders. Herein, we report the discovery and characterization of a highly efficacious and selective FAAH inhibitor PF-04457845 (23). Compound 23 inhibits FAAH by a covalent, irreversible mechanism involving carbamylation of the active-site serine nucleophile of FAAH with high in vitro potency (k(inact)/K(i) and IC(50) values of 40300 M(-1) s(-1) and 7.2 nM, respectively, for human FAAH). Compound 23 has exquisite selectivity for FAAH relative to other members of the serine hydrolase superfamily as demonstrated by competitive activity-based protein profiling. Oral administration of 23 at 0.1 mg/kg results in efficacy comparable to that of naproxen at 10 mg/kg in a rat model of inflammatory pain. Compound 23 is being evaluated in human clinical trials.
|
Irreversible inhibition of His-tagged rat FAAH N-terminal transmembrane-deleted truncated form expressed in Escherichia coli preincubated for 60 mins before oleamide substrate addition
|
Rattus norvegicus
|
7.4
nM
|
|
Journal : ACS Med. Chem. Lett.
Title : Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor.
Year : 2011
Volume : 2
Issue : 2
First Page : 91
Last Page : 96
Authors : Johnson DS, Stiff C, Lazerwith SE, Kesten SR, Fay LK, Morris M, Beidler D, Liimatta MB, Smith SE, Dudley DT, Sadagopan N, Bhattachar SN, Kesten SJ, Nomanbhoy TK, Cravatt BF, Ahn K.
Abstract : Fatty acid amide hydrolase (FAAH) is an integral membrane serine hydrolase that degrades the fatty acid amide family of signaling lipids, including the endocannabinoid anandamide. Genetic or pharmacological inactivation of FAAH leads to analgesic and anti-inflammatory phenotypes in rodents without showing the undesirable side effects observed with direct cannabinoid receptor agonists, indicating that FAAH may represent an attractive therapeutic target for the treatment of inflammatory pain and other nervous system disorders. Herein, we report the discovery and characterization of a highly efficacious and selective FAAH inhibitor PF-04457845 (23). Compound 23 inhibits FAAH by a covalent, irreversible mechanism involving carbamylation of the active-site serine nucleophile of FAAH with high in vitro potency (k(inact)/K(i) and IC(50) values of 40300 M(-1) s(-1) and 7.2 nM, respectively, for human FAAH). Compound 23 has exquisite selectivity for FAAH relative to other members of the serine hydrolase superfamily as demonstrated by competitive activity-based protein profiling. Oral administration of 23 at 0.1 mg/kg results in efficacy comparable to that of naproxen at 10 mg/kg in a rat model of inflammatory pain. Compound 23 is being evaluated in human clinical trials.
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells at 10 uM after 48 hours by high content imaging
|
Homo sapiens
|
4.58
%
|
|
Title : Identification of inhibitors of SARS-CoV-2 in-vitro cellular toxicity in human (Caco-2) cells using a large scale drug repurposing collection
Year : 2020
Authors : Bernhard Ellinger, Denisa Bojkova, Andrea Zaliani, Jindrich Cinatl, Carsten Claussen, Sandra Westhaus, Jeanette Reinshagen, Maria Kuzikov, Markus Wolf, Gerd Geisslinger, Philip Gribbon, Sandra Ciesek
Abstract : To identify possible candidates for progression towards clinical studies against SARS-CoV-2, we screened a well-defined collection of 5632 compounds including 3488 compounds which have undergone clinical investigations (marketed drugs, phases 1 -3, and withdrawn) across 600 indications. Compounds were screened for their inhibition of viral induced cytotoxicity using the human epithelial colorectal adenocarcinoma cell line Caco-2 and a SARS-CoV-2 isolate. The primary screen of 5632 compounds gave 271 hits. A total of 64 compounds with IC50 <20 µM were identified, including 19 compounds with IC50 < 1 µM. Of this confirmed hit population, 90% have not yet been previously reported as active against SARS-CoV-2 in-vitro cell assays. Some 37 of the actives are launched drugs, 19 are in phases 1-3 and 10 pre-clinical. Several inhibitors were associated with modulation of host pathways including kinase signaling P53 activation, ubiquitin pathways and PDE activity modulation, with long chain acyl transferases were effective viral inhibitors.
|
Inhibition of human transmembrane domain deficient FFAH expressed in Escherichia coli using AAMCA as substrate incubated for 1 min measured for 50 mins by fluorescence assay
|
Homo sapiens
|
1.8
nM
|
|
Journal : Bioorg Med Chem Lett
Title : Discovery and evaluation of novel FAAH inhibitors in neuropathic pain model.
Year : 2019
Volume : 29
Issue : 2
First Page : 238
Last Page : 243
Authors : Bhuniya D, Kharul RK, Hajare A, Shaikh N, Bhosale S, Balwe S, Begum F, De S, Athavankar S, Joshi D, Madgula V, Joshi K, Raje AA, Meru AV, Magdum A, Mookhtiar KA, Barbhaiya R.
Abstract : Conceptual design and modification of urea moiety in chemotype PF-3845/04457845, the bench marking irreversible inhibitor of fatty acid amide hydrolase (FAAH), led to discovery of a novel nicotinamide-based lead 12a having reversible mechanism of action. Focused SAR around the pyridine heterocycle (Ar) in 12a (Tables 1 and 2) resulted into four shortlisted compounds, (-)-12a, (-)-12i, (-)-12l-m. The required (-)-enantiomers were obtained via diastereomeric resolution of a novel chiral dissymmetric intermediate 15. Based on comparative profile of FAAH potency, metabolic stability in liver microsome, liability of inhibiting major hCYP450 isoforms, rat PK, and brain penetration ability, two SAR optimized compounds, (-)-12l and (-)-12m, were selected for efficacy study in rat model of chemotherapy-induced peripheral neuropathy (CIPN). Both the compounds exhibited dose related antihyperalgesic effects, when treated with 3-30 mg/kg po for 7 days. The effects at 30 mg/kg are comparable to that of PF-04457845 (10 mg/kg) and Tramadol (40 mg/kg).
|
Inhibition of rat FFAH expressed in Escherichia coli using AAMCA as substrate incubated for 1 min measured for 50 mins by fluorescence assay
|
Rattus norvegicus
|
5.7
nM
|
|
Journal : Bioorg Med Chem Lett
Title : Discovery and evaluation of novel FAAH inhibitors in neuropathic pain model.
Year : 2019
Volume : 29
Issue : 2
First Page : 238
Last Page : 243
Authors : Bhuniya D, Kharul RK, Hajare A, Shaikh N, Bhosale S, Balwe S, Begum F, De S, Athavankar S, Joshi D, Madgula V, Joshi K, Raje AA, Meru AV, Magdum A, Mookhtiar KA, Barbhaiya R.
Abstract : Conceptual design and modification of urea moiety in chemotype PF-3845/04457845, the bench marking irreversible inhibitor of fatty acid amide hydrolase (FAAH), led to discovery of a novel nicotinamide-based lead 12a having reversible mechanism of action. Focused SAR around the pyridine heterocycle (Ar) in 12a (Tables 1 and 2) resulted into four shortlisted compounds, (-)-12a, (-)-12i, (-)-12l-m. The required (-)-enantiomers were obtained via diastereomeric resolution of a novel chiral dissymmetric intermediate 15. Based on comparative profile of FAAH potency, metabolic stability in liver microsome, liability of inhibiting major hCYP450 isoforms, rat PK, and brain penetration ability, two SAR optimized compounds, (-)-12l and (-)-12m, were selected for efficacy study in rat model of chemotherapy-induced peripheral neuropathy (CIPN). Both the compounds exhibited dose related antihyperalgesic effects, when treated with 3-30 mg/kg po for 7 days. The effects at 30 mg/kg are comparable to that of PF-04457845 (10 mg/kg) and Tramadol (40 mg/kg).
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
11.69
%
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
6.349
%
|
|
Title : Identification of inhibitors of SARS-Cov2 M-Pro enzymatic activity using a small molecule repurposing screen
Year : 2020
Authors : Maria Kuzikov, Elisa Costanzi, Jeanette Reinshagen, Francesca Esposito, Laura Vangeel, Markus Wolf, Bernhard Ellinger, Carsten Claussen, Gerd Geisslinger, Angela Corona, Daniela Iaconis, Carmine Talarico, Candida Manelfi, Rolando Cannalire, Giulia Rossetti, Jonas Gossen, Simone Albani, Francesco Musiani, Katja Herzog, Yang Ye, Barbara Giabbai, Nicola Demitri, Dirk Jochmans, Steven De Jonghe, Jasper Rymenants, Vincenzo Summa, Enzo Tramontano, Andrea R. Beccari, Pieter Leyssen, Paola Storici, Johan Neyts, Philip Gribbon, and Andrea Zaliani
Abstract : Compound repurposing is an important strategy being pursued in the identification of effective treatment against the SARS-CoV-2 infection and COVID-19 disease. In this regard, SARS-CoV-2 main protease (M-Pro), also termed 3CL-Pro, is an attractive drug target as it plays a central role in viral replication by processing the viral polyprotein into 11 non-structural proteins. We report the results of a screening campaign involving ca 8.7 K compounds containing marketed drugs, clinical and preclinical candidates, and chemicals regarded as safe in humans. We confirmed previously reported inhibitors of 3CL-Pro, but we have also identified 68 compounds with IC50 lower than 1 uM and 127 compounds with IC50 lower than 5 uM. Profiling showed 67% of confirmed hits were selective (> 5 fold) against other Cys- and Ser- proteases (Chymotrypsin and Cathepsin-L) and MERS 3CL-Pro. Selected compounds were also analysed in their binding characteristics.
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
|
Chlorocebus sabaeus
|
-0.03
%
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
|
Chlorocebus sabaeus
|
-0.18
%
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
|
Chlorocebus sabaeus
|
-0.18
%
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
|
Chlorocebus sabaeus
|
-0.03
%
|
|
Title : Cytopathic SARS-Cov2 screening on VERO-E6 cells in a large repurposing effort
Year : 2020
Authors : Andrea Zaliani, Laura Vangeel, Jeanette Reinshagen, Daniela Iaconis, Maria Kuzikov, Oliver Keminer, Markus Wolf, Bernhard Ellinger, Francesca Esposito, Angela Corona, Enzo Tramontano, Candida Manelfi, Katja Herzog, Dirk Jochmans, Steven De Jonghe, Winston Chiu, Thibault Francken, Joost Schepers, Caroline Collard, Kayvan Abbasi, Carsten Claussen , Vincenzo Summa, Andrea R. Beccari, Johan Neyts, Philip Gribbon and Pieter Leyssen
Abstract : Worldwide, there are intensive efforts to identify repurposed drugs as potential therapies against SARS-CoV-2 infection and the associated COVID-19 disease. To date, the anti-inflammatory drug dexamethasone and (to a lesser extent) the RNA-polymerase inhibitor remdesivir have been shown to be effective in reducing mortality and patient time to recovery, respectively, in patients. Here, we report the results of a phenotypic screening campaign within an EU-funded project (H2020-EXSCALATE4COV) aimed at extending the repertoire of anti-COVID therapeutics through repurposing of available compounds and highlighting compounds with new mechanisms of action against viral infection. We screened 8702 molecules from different repurposing libraries, to reveal 110 compounds with an anti-cytopathic IC50 < 20 µM. From this group, 18 with a safety index greater than 2 are also marketed drugs, making them suitable for further study as potential therapies against COVID-19. Our result supports the idea that a systematic approach to repurposing is a valid strategy to accelerate the necessary drug discovery process.
|
GPCRScan assay: inhibition of 5-HT1A
|
Homo sapiens
|
20.19
%
|
|
|
GPCRScan assay: inhibition of 5-HT1B
|
Homo sapiens
|
24.44
%
|
|
|
GPCRScan assay: inhibition of 5-HT1D
|
Homo sapiens
|
42.13
%
|
|
|
GPCRScan assay: inhibition of 5-HT1E
|
Homo sapiens
|
18.99
%
|
|
|
GPCRScan assay: inhibition of 5-HT2A
|
Homo sapiens
|
82.92
%
|
|
GPCRScan assay: inhibition of 5-HT2A
|
Homo sapiens
|
248.71
nM
|
|
GPCRScan assay: inhibition of 5-HT2A
|
Homo sapiens
|
251.19
nM
|
|
|
GPCRScan assay: inhibition of 5-HT2B
|
Homo sapiens
|
55.67
%
|
|
|
GPCRScan assay: inhibition of 5-HT2C
|
Homo sapiens
|
64.56
%
|
|
|
GPCRScan assay: inhibition of 5-HT3
|
Homo sapiens
|
10.69
%
|
|
|
GPCRScan assay: inhibition of 5-HT5A
|
Homo sapiens
|
28.4
%
|
|
|
GPCRScan assay: inhibition of 5-HT6
|
Homo sapiens
|
40.65
%
|
|
|
GPCRScan assay: inhibition of 5-HT7A
|
Homo sapiens
|
37.46
%
|
|
|
GPCRScan assay: inhibition of D1
|
Homo sapiens
|
-3.23
%
|
|
|
GPCRScan assay: inhibition of D2
|
Homo sapiens
|
1.84
%
|
|
|
GPCRScan assay: inhibition of D3
|
Homo sapiens
|
4.08
%
|
|
|
GPCRScan assay: inhibition of D4
|
Homo sapiens
|
-6.93
%
|
|
|
GPCRScan assay: inhibition of D5
|
Homo sapiens
|
29.27
%
|
|
|
GPCRScan assay: inhibition of SERT
|
Homo sapiens
|
20.21
%
|
|
|
GPCRScan assay: inhibition of NET
|
Homo sapiens
|
7.86
%
|
|
|
GPCRScan assay: inhibition of DAT
|
Homo sapiens
|
-30.34
%
|
|
|
GPCRScan assay: inhibition of MOR
|
Homo sapiens
|
17.53
%
|
|
|
GPCRScan assay: inhibition of DOR
|
Homo sapiens
|
12.26
%
|
|
|
GPCRScan assay: inhibition of KOR
|
Homo sapiens
|
30.51
%
|
|
|
GPCRScan assay: inhibition of GABAA
|
Rattus
|
-12.82
%
|
|
|
GPCRScan assay: inhibition of H1
|
Homo sapiens
|
27.24
%
|
|
|
GPCRScan assay: inhibition of H2
|
Homo sapiens
|
17.27
%
|
|
|
GPCRScan assay: inhibition of H3
|
Homo sapiens
|
8.73
%
|
|
|
GPCRScan assay: inhibition of H4
|
Homo sapiens
|
17.33
%
|
|
|
GPCRScan assay: inhibition of Alpha1A
|
Homo sapiens
|
10.35
%
|
|
|
GPCRScan assay: inhibition of Alpha1B
|
Homo sapiens
|
0.4
%
|
|
|
GPCRScan assay: inhibition of Alpha2A
|
Homo sapiens
|
34.45
%
|
|
|
GPCRScan assay: inhibition of Alpha2B
|
Homo sapiens
|
40.05
%
|
|
|
GPCRScan assay: inhibition of Alpha2C
|
Homo sapiens
|
79.3
%
|
|
GPCRScan assay: inhibition of Alpha2C
|
Homo sapiens
|
595.66
nM
|
|
GPCRScan assay: inhibition of Alpha2C
|
Homo sapiens
|
602.56
nM
|
|
|
GPCRScan assay: inhibition of Beta1
|
Homo sapiens
|
16.5
%
|
|
|
GPCRScan assay: inhibition of Beta2
|
Homo sapiens
|
0.51
%
|
|
|
GPCRScan assay: inhibition of M1
|
Homo sapiens
|
29.51
%
|
|
|
GPCRScan assay: inhibition of M2
|
Homo sapiens
|
20.77
%
|
|
|
GPCRScan assay: inhibition of M3
|
Homo sapiens
|
27.49
%
|
|
|
GPCRScan assay: inhibition of M4
|
Homo sapiens
|
7.38
%
|
|
|
GPCRScan assay: inhibition of M5
|
Homo sapiens
|
23.53
%
|
|
|
GPCRScan assay: inhibition of Beta3
|
Homo sapiens
|
0.69
%
|
|
|
GPCRScan assay: inhibition of GABAA/BZP
|
Rattus
|
7.35
%
|
|
|
GPCRScan assay: inhibition of GABA/PBR
|
Rattus
|
59.63
%
|
|
|
GPCRScan assay: inhibition of Alpha1D
|
Homo sapiens
|
3.84
%
|
|
|
GPCRScan assay: inhibition of Sigma 2
|
Homo sapiens
|
91.31
%
|
|
GPCRScan assay: inhibition of Sigma 2
|
Homo sapiens
|
436.72
nM
|
|
GPCRScan assay: inhibition of Sigma 2
|
Homo sapiens
|
436.52
nM
|
|
|
GPCRScan assay: inhibition of Sigma 1
|
Homo sapiens
|
88.52
%
|
|
GPCRScan assay: inhibition of Sigma 1
|
Homo sapiens
|
472.06
nM
|
|
GPCRScan assay: inhibition of Sigma 1
|
Homo sapiens
|
467.74
nM
|
|
|
Glutamate dehydrogenase-coupled FAAH assay (preincubation time 1 min)
|
Homo sapiens
|
50.4
nM
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
Glutamate dehydrogenase-coupled FAAH assay (preincubation time 15 min)
|
Homo sapiens
|
32.4
nM
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
Glutamate dehydrogenase-coupled FAAH assay (preincubation time 30 min)
|
Homo sapiens
|
10.7
nM
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
Glutamate dehydrogenase-coupled FAAH assay (preincubation time 60 min)
|
Homo sapiens
|
7.4
nM
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
Proteaseome
|
Homo sapiens
|
0.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
A1 (h) CEREP ligand profiling
|
Homo sapiens
|
3.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
A2A (h) CEREP ligand profiling
|
Homo sapiens
|
-11.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
alpha1 (non-selective) CEREP ligand profiling
|
None
|
-2.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
alpha2A (h) CEREP ligand profiling
|
Homo sapiens
|
-4.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
alpha2B (h) CEREP ligand profiling
|
Homo sapiens
|
4.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
beta1 (h) CEREP ligand profiling
|
Homo sapiens
|
1.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
beta2 (h) CEREP ligand profiling
|
Homo sapiens
|
-11.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
AT1 (h) CEREP ligand profiling
|
Homo sapiens
|
-10.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
BZD (central) CEREP ligand profiling
|
None
|
15.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
CB1 (h) CEREP ligand profiling
|
Homo sapiens
|
55.0
%
|
|
CB1 (h) CEREP ligand profiling
|
Homo sapiens
|
14.0
µM
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
CB2 (h) CEREP ligand profiling
|
Homo sapiens
|
55.0
%
|
|
CB2 (h) CEREP ligand profiling
|
Homo sapiens
|
5.1
µM
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
CCKA (h) (CCK1) CEREP ligand profiling
|
Homo sapiens
|
-10.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
CCKB (h) (CCK2) CEREP ligand profiling
|
Homo sapiens
|
-6.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
D1 (h) CEREP ligand profiling
|
Homo sapiens
|
3.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
D2S (h) CEREP ligand profiling
|
Homo sapiens
|
-9.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
D3 (h) CEREP ligand profiling
|
Homo sapiens
|
3.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
GABAA CEREP ligand profiling
|
None
|
-4.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
GABAB(1b) (h) CEREP ligand profiling
|
Homo sapiens
|
-13.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
AMPA CEREP ligand profiling
|
None
|
-8.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
Kainate CEREP ligand profiling
|
None
|
2.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
NMDA CEREP ligand profiling
|
None
|
-3.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
Glycine (strychnine-insensitive) CEREP ligand profiling
|
None
|
-2.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
H1 (h) CEREP ligand profiling
|
Homo sapiens
|
-1.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
H2 (h) CEREP ligand profiling
|
Homo sapiens
|
-6.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
H3 (h) CEREP ligand profiling
|
Homo sapiens
|
10.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
MAO-A CEREP ligand profiling
|
None
|
13.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
M1 (h) CEREP ligand profiling
|
Homo sapiens
|
36.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
M2 (h) CEREP ligand profiling
|
Homo sapiens
|
15.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
M3 (h) CEREP ligand profiling
|
Homo sapiens
|
11.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
N(neuronal) (α-BGTX-insensitive) (α4β2 nicotinic receptor) CEREP ligand profiling
|
None
|
8.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
N (h) (muscle-type) CEREP ligand profiling
|
Homo sapiens
|
-25.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
mu (h) (MOP) (agonist site) CEREP ligand profiling
|
Homo sapiens
|
3.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
delta2 (h) (DOP) CEREP ligand profiling
|
Homo sapiens
|
2.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
kappa (KOP) CEREP ligand profiling
|
None
|
0.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
5-HT1A (h) CEREP ligand profiling
|
Homo sapiens
|
6.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
5-HT1B CEREP ligand profiling
|
None
|
-3.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
5-HT2A (h) (agonist site) CEREP ligand profiling
|
Homo sapiens
|
57.0
%
|
|
5-HT2A (h) (agonist site) CEREP ligand profiling
|
Homo sapiens
|
1.6
µM
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
5-HT2B (h) (agonist site) CEREP ligand profiling
|
Homo sapiens
|
35.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
5-HT2C (h) (agonist site) CEREP ligand profiling
|
Homo sapiens
|
-3.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
5-HT3 (h) CEREP ligand profiling
|
Homo sapiens
|
-8.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
5-HT4e (h) CEREP ligand profiling
|
Homo sapiens
|
-8.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
5-HT7 (h) CEREP ligand profiling
|
Homo sapiens
|
7.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
Glucocorticoid (h) (GR) CEREP ligand profiling
|
Homo sapiens
|
-25.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
V1a (h) CEREP ligand profiling
|
Homo sapiens
|
8.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
Ca2+ channel (L, DHP site) CEREP ligand profiling
|
None
|
11.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
Ca2+ channel (L, diltiazem site) (benzothiazepines) CEREP ligand profiling
|
None
|
1.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
Ca2+ channel (L, verapamil site) (phenylalkylamines) CEREP ligand profiling
|
None
|
-5.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
Ca2+ channel (N) CEREP ligand profiling
|
None
|
-5.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
Na+ channel (site 2) CEREP ligand profiling
|
None
|
13.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
CI channel CEREP ligand profiling
|
None
|
78.0
%
|
|
CI channel CEREP ligand profiling
|
None
|
3.0
µM
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
NE transporter (h) CEREP ligand profiling
|
Homo sapiens
|
-5.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
DA transporter (h) CEREP ligand profiling
|
Homo sapiens
|
-1.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
5-HT transporter (h) CEREP ligand profiling
|
Homo sapiens
|
11.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
GABA transporter CEREP ligand profiling
|
None
|
-1.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
Choline transporter (h) (CHT1) CEREP ligand profiling
|
Homo sapiens
|
18.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
COX2 (h) CEREP ligand profiling
|
Homo sapiens
|
-37.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
PDE 3 (h) CEREP ligand profiling
|
Homo sapiens
|
10.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
PDE 4 (h) CEREP ligand profiling
|
Homo sapiens
|
18.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
ACE (h) CEREP ligand profiling
|
Homo sapiens
|
-15.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
p38alpha kinase (h) CEREP ligand profiling
|
Homo sapiens
|
1.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
FLT-1 (h) (VEGFR1) CEREP ligand profiling
|
Homo sapiens
|
4.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
ATPase (Na+/K+) CEREP ligand profiling
|
None
|
-2.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
|
Acetylcholinesterase (h) CEREP ligand profiling
|
Homo sapiens
|
10.0
%
|
|
Title : Data for DCP probe PF-04457845
Year : 2021
Authors : SGC Frankfurt
Abstract : SGC Frankfurt donated chemical probe project: PF-04457845 was donated by Pfizer. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04457845. Control: PF-04875474. References: 1. Ahn, Kay, Sarah E Smith, Marya B Liimatta, David Beidler, Nalini Sadagopan, David T Dudley, Tim Young, Paul Wren, Yanhua Zhang, Steven Swaney, Keri Van Becelaere, Jacqueline L Blankman, Daniel K Nomura, Shobha N Bhattachar, Cory Stiff, Tyzoon K Nomanbhoy, Eranthie Weerapana, Douglas S Johnson, and Benjamin F Cravatt. 2011. ‘Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain’. The Journal of Pharmacology and Experimental Therapeutics 338(1):114–24. PMID: 21505060. 2. Johnson, Douglas S, Cory Stiff, Scott E Lazerwith, Suzanne R Kesten, Lorraine K Fay, Mark Morris, David Beidler, Marya B Liimatta, Sarah E Smith, David T Dudley, Nalini Sadagopan, Shobha N Bhattachar, Stephen J Kesten, Tyzoon K Nomanbhoy, Benjamin F Cravatt, and Kay Ahn. 2011. ‘Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor’. ACS Medicinal Chemistry Letters 2(2):91–96. PMID: 21666860.
