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Assay Detail

CHEMBL4022834

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Functional
Antagonist activity at recombinant human CB1 receptor expressed in HEK293 cell membranes assessed as inhibition of CP55940-induced [35S]GTPgammaS binding preincubated for 1 hr followed by CP55940 addition and subsequent incubation with [35S]GTPgammaS measured after 30 mins by scintillation spectrometry
ChEMBL ↗
46
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cannabinoid receptor 1 (CHEMBL218) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Affinity Relationships and Structure-Kinetic Relationships of 1,2-Diarylimidazol-4-carboxamide Derivatives as Human Cannabinoid 1 Receptor Antagonists.
Xia L, de Vries H, Lenselink EB, Louvel J, Waring MJ, Cheng L, Pahlén S, Petersson MJ, Schell P, Olsson RI, Heitman LH, Sheppard RJ, IJzerman AP.
J Med Chem (2017) 60 : 9545 -9564
PubMed 29111736 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 46 8.62 9.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4068708 — — 2 9.21
CHEMBL4093165 — — 2 9.20
CHEMBL4087520 — — 2 9.00
CHEMBL4100882 — — 2 8.96
CHEMBL4086535 — — 2 8.92
CHEMBL4095223 — — 2 8.92
CHEMBL4094098 — — 2 8.92
CHEMBL4067800 — — 2 8.90
CHEMBL4089947 — — 2 8.90
CHEMBL4062749 — — 2 8.80
CHEMBL4090706 — — 2 8.80
CHEMBL4089821 — — 2 8.80
CHEMBL4065097 — — 2 8.74
CHEMBL4066563 — — 2 8.70
CHEMBL4068853 — — 2 8.70
CHEMBL4082908 — — 2 8.60
CHEMBL4105382 — — 2 8.51
CHEMBL4063825 — — 2 8.42
CHEMBL4076020 — — 2 8.30
CHEMBL4078689 — — 2 8.22
CHEMBL4085407 — — 2 8.20
CHEMBL4102969 — — 2 7.75
CHEMBL4072418 — — 2 7.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4068708 — IC50 = 0.61 nM 9.21
CHEMBL4068708 — IC50 = 0.631 nM 9.20
CHEMBL4093165 — IC50 = 0.631 nM 9.20
CHEMBL4093165 — IC50 = 0.66 nM 9.18
CHEMBL4087520 — IC50 = 1.0 nM 9.00
CHEMBL4100882 — IC50 = 1.1 nM 8.96
CHEMBL4087520 — IC50 = 1.1 nM 8.96
CHEMBL4095223 — IC50 = 1.2 nM 8.92
CHEMBL4086535 — IC50 = 1.2 nM 8.92
CHEMBL4094098 — IC50 = 1.2 nM 8.92
CHEMBL4086535 — IC50 = 1.259 nM 8.90
CHEMBL4067800 — IC50 = 1.259 nM 8.90
CHEMBL4095223 — IC50 = 1.259 nM 8.90
CHEMBL4089947 — IC50 = 1.259 nM 8.90
CHEMBL4100882 — IC50 = 1.259 nM 8.90
CHEMBL4094098 — IC50 = 1.259 nM 8.90
CHEMBL4089947 — IC50 = 1.3 nM 8.89
CHEMBL4067800 — IC50 = 1.3 nM 8.89
CHEMBL4090706 — IC50 = 1.585 nM 8.80
CHEMBL4062749 — IC50 = 1.585 nM 8.80
CHEMBL4089821 — IC50 = 1.585 nM 8.80
CHEMBL4090706 — IC50 = 1.7 nM 8.77
CHEMBL4089821 — IC50 = 1.7 nM 8.77
CHEMBL4062749 — IC50 = 1.8 nM 8.74
CHEMBL4065097 — IC50 = 1.8 nM 8.74
CHEMBL4065097 — IC50 = 1.995 nM 8.70
CHEMBL4066563 — IC50 = 1.995 nM 8.70
CHEMBL4068853 — IC50 = 1.995 nM 8.70
CHEMBL4066563 — IC50 = 2.2 nM 8.66
CHEMBL4068853 — IC50 = 2.4 nM 8.62
CHEMBL4082908 — IC50 = 2.512 nM 8.60
CHEMBL4082908 — IC50 = 2.7 nM 8.57
CHEMBL4105382 — IC50 = 3.1 nM 8.51
CHEMBL4105382 — IC50 = 3.162 nM 8.50
CHEMBL4063825 — IC50 = 3.8 nM 8.42
CHEMBL4063825 — IC50 = 3.981 nM 8.40
CHEMBL4076020 — IC50 = 5.012 nM 8.30
CHEMBL4076020 — IC50 = 5.6 nM 8.25
CHEMBL4078689 — IC50 = 6.0 nM 8.22
CHEMBL4085407 — IC50 = 6.31 nM 8.20
CHEMBL4078689 — IC50 = 6.31 nM 8.20
CHEMBL4085407 — IC50 = 7.1 nM 8.15
CHEMBL4102969 — IC50 = 18.0 nM 7.75
CHEMBL4102969 — IC50 = 19.95 nM 7.70
CHEMBL4072418 — IC50 = 79.43 nM 7.10
CHEMBL4072418 — IC50 = 83.0 nM 7.08