|
Inhibition of electric eel AChE at 2 mg/ml by Ellman's method
|
Electrophorus electricus
|
28.65
%
|
|
Journal : Bioorg. Med. Chem.
Title : Exploration of natural compounds as sources of new bifunctional scaffolds targeting cholinesterases and beta amyloid aggregation: the case of chelerythrine.
Year : 2012
Volume : 20
Issue : 22
First Page : 6669
Last Page : 6679
Authors : Brunhofer G, Fallarero A, Karlsson D, Batista-Gonzalez A, Shinde P, Gopi Mohan C, Vuorela P.
Abstract : The presented project started by screening a library consisting of natural and natural based compounds for their acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activity. Active compounds were chemically clustered into groups and further tested on the human cholinesterases isoforms. The aim of the presented study was to identify compounds that could be used as leads to target two key mechanisms associated with the AD's pathogenesis simultaneously: cholinergic depletion and beta amyloid (Aβ) aggregation. Berberin, palmatine and chelerythrine, chemically clustered in the so-called isoquinoline group, showed promising cholinesterase inhibitory activity and were therefore further investigated. Moreover, the compounds demonstrated moderate to good inhibition of Aβ aggregation as well as the ability to disaggregate already preformed Aβ aggregates in an experimental set-up using HFIP as promotor of Aβ aggregates. Analysis of the kinetic mechanism of the AChE inhibition revealed chelerythrine as a mixed inhibitor. Using molecular docking studies, it was further proven that chelerythrine binds on both the catalytic site and the peripheral anionic site (PAS) of the AChE. In view of this, we went on to investigate its effect on inhibiting Aβ aggregation stimulated by AChE. Chelerythrine showed inhibition of fibril formation in the same range as propidium iodide. This approach enabled for the first time to identify a cholinesterase inhibitor of natural origin-chelerythrine-acting on AChE and BChE with a dual ability to inhibit Aβ aggregation as well as to disaggregate preformed Aβ aggregates. This compound could be an excellent starting point paving the way to develop more successful anti-AD drugs.
|
Inhibition of horse BChE at 2 mg/ml by Ellman's method
|
Equus caballus
|
-0.23
%
|
|
Journal : Bioorg. Med. Chem.
Title : Exploration of natural compounds as sources of new bifunctional scaffolds targeting cholinesterases and beta amyloid aggregation: the case of chelerythrine.
Year : 2012
Volume : 20
Issue : 22
First Page : 6669
Last Page : 6679
Authors : Brunhofer G, Fallarero A, Karlsson D, Batista-Gonzalez A, Shinde P, Gopi Mohan C, Vuorela P.
Abstract : The presented project started by screening a library consisting of natural and natural based compounds for their acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activity. Active compounds were chemically clustered into groups and further tested on the human cholinesterases isoforms. The aim of the presented study was to identify compounds that could be used as leads to target two key mechanisms associated with the AD's pathogenesis simultaneously: cholinergic depletion and beta amyloid (Aβ) aggregation. Berberin, palmatine and chelerythrine, chemically clustered in the so-called isoquinoline group, showed promising cholinesterase inhibitory activity and were therefore further investigated. Moreover, the compounds demonstrated moderate to good inhibition of Aβ aggregation as well as the ability to disaggregate already preformed Aβ aggregates in an experimental set-up using HFIP as promotor of Aβ aggregates. Analysis of the kinetic mechanism of the AChE inhibition revealed chelerythrine as a mixed inhibitor. Using molecular docking studies, it was further proven that chelerythrine binds on both the catalytic site and the peripheral anionic site (PAS) of the AChE. In view of this, we went on to investigate its effect on inhibiting Aβ aggregation stimulated by AChE. Chelerythrine showed inhibition of fibril formation in the same range as propidium iodide. This approach enabled for the first time to identify a cholinesterase inhibitor of natural origin-chelerythrine-acting on AChE and BChE with a dual ability to inhibit Aβ aggregation as well as to disaggregate preformed Aβ aggregates. This compound could be an excellent starting point paving the way to develop more successful anti-AD drugs.
|
Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
106.54
%
|
|
Journal : Mol. Pharmacol.
Title : Structure-based identification of OATP1B1/3 inhibitors.
Year : 2013
Volume : 83
Issue : 6
First Page : 1257
Last Page : 1267
Authors : De Bruyn T, van Westen GJ, Ijzerman AP, Stieger B, de Witte P, Augustijns PF, Annaert PP.
Abstract : Several recent studies show that inhibition of the hepatic transport proteins organic anion-transporting polypeptide 1B1 (OATP1B1) and 1B3 (OATP1B3) can result in clinically relevant drug-drug interactions (DDI). To avoid late-stage development drug failures due to OATP1B-mediated DDI, predictive in vitro and in silico methods should be implemented at an early stage of the drug candidate evaluation process. In the present study, we first developed a high-throughput in vitro transporter inhibition assay for the OATP1B subfamily. A total of 2000 compounds were tested as potential modulators of the uptake of the OATP1B substrate sodium fluorescein, in OATP1B1- or 1B3-transfected Chinese hamster ovary cells. At an equimolar substrate-inhibitor concentration of 10 µM, 212 and 139 molecules were identified as OATP1B1 and OATP1B3 inhibitors, respectively (minimum 50% inhibition). For 69 compounds, previously not identified as OATP1B inhibitors, concentration-dependent inhibition was also determined, yielding Ki values ranging from 0.06 to 6.5 µM. Based on these in vitro data, we subsequently developed a proteochemometrics-based in silico model, which predicted OATP1B inhibitors in the test group (20% of the dataset) with high specificity (86%) and sensitivity (78%). Moreover, several physicochemical compound properties and substructures related to OATP1B1/1B3 inhibition or inactivity were identified. Finally, model performance was prospectively verified with a set of 54 compounds not included in the original dataset. This validation indicated that 80 and 74% of the compounds were correctly classified for OATP1B1 and OATP1B3 inhibition, respectively.
|
Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
103.03
%
|
|
Journal : Mol. Pharmacol.
Title : Structure-based identification of OATP1B1/3 inhibitors.
Year : 2013
Volume : 83
Issue : 6
First Page : 1257
Last Page : 1267
Authors : De Bruyn T, van Westen GJ, Ijzerman AP, Stieger B, de Witte P, Augustijns PF, Annaert PP.
Abstract : Several recent studies show that inhibition of the hepatic transport proteins organic anion-transporting polypeptide 1B1 (OATP1B1) and 1B3 (OATP1B3) can result in clinically relevant drug-drug interactions (DDI). To avoid late-stage development drug failures due to OATP1B-mediated DDI, predictive in vitro and in silico methods should be implemented at an early stage of the drug candidate evaluation process. In the present study, we first developed a high-throughput in vitro transporter inhibition assay for the OATP1B subfamily. A total of 2000 compounds were tested as potential modulators of the uptake of the OATP1B substrate sodium fluorescein, in OATP1B1- or 1B3-transfected Chinese hamster ovary cells. At an equimolar substrate-inhibitor concentration of 10 µM, 212 and 139 molecules were identified as OATP1B1 and OATP1B3 inhibitors, respectively (minimum 50% inhibition). For 69 compounds, previously not identified as OATP1B inhibitors, concentration-dependent inhibition was also determined, yielding Ki values ranging from 0.06 to 6.5 µM. Based on these in vitro data, we subsequently developed a proteochemometrics-based in silico model, which predicted OATP1B inhibitors in the test group (20% of the dataset) with high specificity (86%) and sensitivity (78%). Moreover, several physicochemical compound properties and substructures related to OATP1B1/1B3 inhibition or inactivity were identified. Finally, model performance was prospectively verified with a set of 54 compounds not included in the original dataset. This validation indicated that 80 and 74% of the compounds were correctly classified for OATP1B1 and OATP1B3 inhibition, respectively.
|
Antibacterial activity against Staphylococcus aureus MRSA ATCC 43300 (CO-ADD:GP_020); MIC in CAMBH media, using NBS plates, by OD(600)
|
Staphylococcus aureus subsp. aureus
|
-20.45
%
|
|
|
Antibacterial activity against Escherichia coli ATCC 25922 (CO-ADD:GN_001); MIC in CAMBH media using NBS plates, by OD(600)
|
Escherichia coli
|
7.12
%
|
|
|
Antibacterial activity against Klebsiella pneumoniae MDR ATCC 70063 (CO-ADD:GN_003); MIC in CAMBH media using NBS plates, by OD(600)
|
Klebsiella pneumoniae
|
5.32
%
|
|
|
Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 (CO-ADD:GN_042); MIC in CAMBH media using NBS plates, by OD(600)
|
Pseudomonas aeruginosa
|
2.81
%
|
|
|
Antibacterial activity against Acinetobacter baumannii ATCC 19606 (CO-ADD:GN_034); MIC in CAMBH media using NBS plates, by OD600
|
Acinetobacter baumannii
|
6.43
%
|
|
|
Antifungal activity against Candida albicans ATCC 90028 (CO-ADD:FG_001); MIC in YNB media using NBS plates, by OD630
|
Candida albicans
|
4.46
%
|
|
|
Antifungal activity against Cryptococcus neoformans H99 ATCC 208821 (CO-ADD:FG_002); MIC in YNB media using NBS plates, by Resazurin OD(600-570)
|
Cryptococcus neoformans
|
-1.87
%
|
|
|
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
|
-6.19
%
|
|
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.
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
2.176
%
|
|
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
|
-0.09
%
|
|
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
|
-0.09
%
|
|
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.
|
Inhibition of human protein kinase A at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of human protein kinase Ca at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of human PDE3A1A at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of human PDE5A1 at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of acetylcholinesterase (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of human NPY2R expressed in CHO-K1 cells at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of human NK1 at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of human ET-A at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of BKR2 (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of human AT1 receptor expressed in CHO-K1 cells at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of human Thromboxane A2 at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of human CYSLTR1 expressed in CHO-K1 cells at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of human BLT expressed in CHO-K1 cells at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of NOS (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of sodium channel site2 (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of human ERG in HEK293 cells at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of Calcium-activated potassium channel channel (unknown origin)
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of GABA receptor chloride/TBOB site (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of L-type calcium channel (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of N-type calcium channel (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of sigma 2 receptor (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of sigma 1 receptor (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of human 5HT-7 receptor at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of human 5HT-6 receptor at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of 5HT-4 (unknown origin) receptor at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of 5HT-3 (unknown origin) receptor at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of human 5HT-2A receptor at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of human 5HT-2C receptor at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of human 5HT-2A receptor expressed in CHO-K1 cells at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of 5HT-1D receptor (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of human 5HT-1a receptor at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of human serotonin transporter expressed in HEK293 cells at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of human Mu-type opioid receptor at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of human delta 2-type opioid receptor at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of nAChR (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of human muscarinic M5 receptor expressed in CHO-K1 cells at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of human muscarinic M4 receptor expressed in CHO-K1 cells at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of human muscarinic M2 receptor expressed in CHO-K1 cells at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of human muscarinic M3 receptor expressed in CHO-K1 cells at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of human muscarinic M1 receptor expressed in CHO-K1 cells at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of human histamine H3 receptor expressed in CHO-K1 cells at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of human histamine H2 receptor expressed in CHO-K1 cells at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of human histamine H1 receptor expressed in CHO-K1 cells at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of Glutamate receptor ionotropic NMDA glycine,strychnine-sensitive site (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of Glutamate receptor ionotropic NMDA phencyclidine site (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of Glutamate receptor ionotropic NMDA agonist site (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of Glutamate receptor ionotropic kainate site (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of Glutamate receptor ionotropic AMPA site (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of human GABA-B1 at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of GABA-A agonist site (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of GABA-A alpha1 BDZ site (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of human dopamine D4.4 receptor expressed in CHO-K1 cells at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of human dopamine D2S receptor expressed in CHO-K1 cells at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of human dopamine D3 receptor expressed in CHO-K1 cells at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of human dopamine D1 receptor at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of human dopamine transporter expressed in CHO-K1 cells at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of human adrenergic receptor beta2 expressed in CHO-K1 cells at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of human adrenergic receptor beta1 expressed in CHO-K1 cells at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of human adrenergic receptor alpha2C expressed in CHO-K1 cells at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of human adrenergic receptor alpha2B expressed in CHO-K1 cells at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of human adenosine receptor A1 expressed in CHO-K1 cells at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of human adenosine transporter at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of human adrenergic receptor alpha2A expressed in CHO-K1 cells at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of human adrenergic receptor alpha1B expressed in CHO-K1 cells at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of human adrenergic receptor alpha1A expressed in CHO-K1 cells at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
|
Inhibition of human adenosine receptor A2A expressed in HEK293 cells at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : Bioorg Med Chem
Title : Pyridine alkaloids with activity in the central nervous system.
Year : 2020
Volume : 28
Issue : 24
First Page : 115820
Last Page : 115820
Authors : Lin SX,Curtis MA,Sperry J
Abstract : This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.
