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
|
|
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
|
|
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
%
|
|
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
|
|
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
|
|
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
%
|
|
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
%
|
|
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
|
|
Glutamate dehydrogenase-coupled FAAH assay (preincubation time 15 min)
|
Homo sapiens
|
32.4
nM
|
|
Glutamate dehydrogenase-coupled FAAH assay (preincubation time 30 min)
|
Homo sapiens
|
10.7
nM
|
|
Glutamate dehydrogenase-coupled FAAH assay (preincubation time 60 min)
|
Homo sapiens
|
7.4
nM
|
|
Proteaseome
|
Homo sapiens
|
0.0
%
|
|
A1 (h) CEREP ligand profiling
|
Homo sapiens
|
3.0
%
|
|
A2A (h) CEREP ligand profiling
|
Homo sapiens
|
-11.0
%
|
|
alpha1 (non-selective) CEREP ligand profiling
|
None
|
-2.0
%
|
|
alpha2A (h) CEREP ligand profiling
|
Homo sapiens
|
-4.0
%
|
|
alpha2B (h) CEREP ligand profiling
|
Homo sapiens
|
4.0
%
|
|
beta1 (h) CEREP ligand profiling
|
Homo sapiens
|
1.0
%
|
|
beta2 (h) CEREP ligand profiling
|
Homo sapiens
|
-11.0
%
|
|
AT1 (h) CEREP ligand profiling
|
Homo sapiens
|
-10.0
%
|
|
BZD (central) CEREP ligand profiling
|
None
|
15.0
%
|
|
CB1 (h) CEREP ligand profiling
|
Homo sapiens
|
55.0
%
|
|
CB1 (h) CEREP ligand profiling
|
Homo sapiens
|
14.0
µM
|
|
CB2 (h) CEREP ligand profiling
|
Homo sapiens
|
55.0
%
|
|
CB2 (h) CEREP ligand profiling
|
Homo sapiens
|
5.1
µM
|
|
CCKA (h) (CCK1) CEREP ligand profiling
|
Homo sapiens
|
-10.0
%
|
|
CCKB (h) (CCK2) CEREP ligand profiling
|
Homo sapiens
|
-6.0
%
|
|
D1 (h) CEREP ligand profiling
|
Homo sapiens
|
3.0
%
|
|
D2S (h) CEREP ligand profiling
|
Homo sapiens
|
-9.0
%
|
|
D3 (h) CEREP ligand profiling
|
Homo sapiens
|
3.0
%
|
|
GABAA CEREP ligand profiling
|
None
|
-4.0
%
|
|
GABAB(1b) (h) CEREP ligand profiling
|
Homo sapiens
|
-13.0
%
|
|
AMPA CEREP ligand profiling
|
None
|
-8.0
%
|
|
Kainate CEREP ligand profiling
|
None
|
2.0
%
|
|
NMDA CEREP ligand profiling
|
None
|
-3.0
%
|
|
Glycine (strychnine-insensitive) CEREP ligand profiling
|
None
|
-2.0
%
|
|
H1 (h) CEREP ligand profiling
|
Homo sapiens
|
-1.0
%
|
|
H2 (h) CEREP ligand profiling
|
Homo sapiens
|
-6.0
%
|
|
H3 (h) CEREP ligand profiling
|
Homo sapiens
|
10.0
%
|
|
MAO-A CEREP ligand profiling
|
None
|
13.0
%
|
|
M1 (h) CEREP ligand profiling
|
Homo sapiens
|
36.0
%
|
|
M2 (h) CEREP ligand profiling
|
Homo sapiens
|
15.0
%
|
|
M3 (h) CEREP ligand profiling
|
Homo sapiens
|
11.0
%
|
|
N(neuronal) (α-BGTX-insensitive) (α4β2 nicotinic receptor) CEREP ligand profiling
|
None
|
8.0
%
|
|
N (h) (muscle-type) CEREP ligand profiling
|
Homo sapiens
|
-25.0
%
|
|
mu (h) (MOP) (agonist site) CEREP ligand profiling
|
Homo sapiens
|
3.0
%
|
|
delta2 (h) (DOP) CEREP ligand profiling
|
Homo sapiens
|
2.0
%
|
|
kappa (KOP) CEREP ligand profiling
|
None
|
0.0
%
|
|
5-HT1A (h) CEREP ligand profiling
|
Homo sapiens
|
6.0
%
|
|
5-HT1B CEREP ligand profiling
|
None
|
-3.0
%
|
|
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
|
|
5-HT2B (h) (agonist site) CEREP ligand profiling
|
Homo sapiens
|
35.0
%
|
|
5-HT2C (h) (agonist site) CEREP ligand profiling
|
Homo sapiens
|
-3.0
%
|
|
5-HT3 (h) CEREP ligand profiling
|
Homo sapiens
|
-8.0
%
|
|
5-HT4e (h) CEREP ligand profiling
|
Homo sapiens
|
-8.0
%
|
|
5-HT7 (h) CEREP ligand profiling
|
Homo sapiens
|
7.0
%
|
|
Glucocorticoid (h) (GR) CEREP ligand profiling
|
Homo sapiens
|
-25.0
%
|
|
V1a (h) CEREP ligand profiling
|
Homo sapiens
|
8.0
%
|
|
Ca2+ channel (L, DHP site) CEREP ligand profiling
|
None
|
11.0
%
|
|
Ca2+ channel (L, diltiazem site) (benzothiazepines) CEREP ligand profiling
|
None
|
1.0
%
|
|
Ca2+ channel (L, verapamil site) (phenylalkylamines) CEREP ligand profiling
|
None
|
-5.0
%
|
|
Ca2+ channel (N) CEREP ligand profiling
|
None
|
-5.0
%
|
|
Na+ channel (site 2) CEREP ligand profiling
|
None
|
13.0
%
|
|
CI channel CEREP ligand profiling
|
None
|
78.0
%
|
|
CI channel CEREP ligand profiling
|
None
|
3.0
µM
|
|
NE transporter (h) CEREP ligand profiling
|
Homo sapiens
|
-5.0
%
|
|
DA transporter (h) CEREP ligand profiling
|
Homo sapiens
|
-1.0
%
|
|
5-HT transporter (h) CEREP ligand profiling
|
Homo sapiens
|
11.0
%
|
|
GABA transporter CEREP ligand profiling
|
None
|
-1.0
%
|
|
Choline transporter (h) (CHT1) CEREP ligand profiling
|
Homo sapiens
|
18.0
%
|
|
COX2 (h) CEREP ligand profiling
|
Homo sapiens
|
-37.0
%
|
|
PDE 3 (h) CEREP ligand profiling
|
Homo sapiens
|
10.0
%
|
|
PDE 4 (h) CEREP ligand profiling
|
Homo sapiens
|
18.0
%
|
|
ACE (h) CEREP ligand profiling
|
Homo sapiens
|
-15.0
%
|
|
p38alpha kinase (h) CEREP ligand profiling
|
Homo sapiens
|
1.0
%
|
|
FLT-1 (h) (VEGFR1) CEREP ligand profiling
|
Homo sapiens
|
4.0
%
|
|
ATPase (Na+/K+) CEREP ligand profiling
|
None
|
-2.0
%
|
|
Acetylcholinesterase (h) CEREP ligand profiling
|
Homo sapiens
|
10.0
%
|
|