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Assay Detail

CHEMBL4022829

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [3H]CP55940 from recombinant human CB1 receptor expressed in beta-galactosidase expressing CHOK1 cell membranes after 60 mins by scintillation spectrometry
ChEMBL ↗
46
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
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
Ki 46 9.58 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4062749 — — 2 11.00
CHEMBL4095223 — — 2 10.21
CHEMBL4078689 — — 2 10.00
CHEMBL4094098 — — 2 10.00
CHEMBL4100882 — — 2 10.00
CHEMBL4087520 — — 2 9.96
CHEMBL4068708 — — 2 9.90
CHEMBL4089821 — — 2 9.90
CHEMBL4067800 — — 2 9.90
CHEMBL4086535 — — 2 9.70
CHEMBL4090706 — — 2 9.70
CHEMBL4089947 — — 2 9.70
CHEMBL4093165 — — 2 9.66
CHEMBL4082908 — — 2 9.60
CHEMBL4065097 — — 2 9.60
CHEMBL4066563 — — 2 9.51
CHEMBL4105382 — — 2 9.50
CHEMBL4085407 — — 2 9.50
CHEMBL4063825 — — 2 9.43
CHEMBL4068853 — — 2 9.30
CHEMBL4076020 — — 2 9.10
CHEMBL4072418 — — 2 8.60
CHEMBL4102969 — — 2 8.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4062749 — Ki = 0.01 nM 11.00
CHEMBL4062749 — Ki = 0.027 nM 10.57
CHEMBL4095223 — Ki = 0.062 nM 10.21
CHEMBL4095223 — Ki = 0.1 nM 10.00
CHEMBL4094098 — Ki = 0.1 nM 10.00
CHEMBL4100882 — Ki = 0.1 nM 10.00
CHEMBL4100882 — Ki = 0.1 nM 10.00
CHEMBL4078689 — Ki = 0.1 nM 10.00
CHEMBL4087520 — Ki = 0.11 nM 9.96
CHEMBL4089821 — Ki = 0.1259 nM 9.90
CHEMBL4068708 — Ki = 0.1259 nM 9.90
CHEMBL4067800 — Ki = 0.1259 nM 9.90
CHEMBL4087520 — Ki = 0.1259 nM 9.90
CHEMBL4094098 — Ki = 0.13 nM 9.89
CHEMBL4089821 — Ki = 0.14 nM 9.85
CHEMBL4067800 — Ki = 0.18 nM 9.74
CHEMBL4068708 — Ki = 0.19 nM 9.72
CHEMBL4089947 — Ki = 0.2 nM 9.70
CHEMBL4089947 — Ki = 0.1995 nM 9.70
CHEMBL4090706 — Ki = 0.1995 nM 9.70
CHEMBL4086535 — Ki = 0.1995 nM 9.70
CHEMBL4093165 — Ki = 0.22 nM 9.66
CHEMBL4082908 — Ki = 0.2512 nM 9.60
CHEMBL4065097 — Ki = 0.2512 nM 9.60
CHEMBL4082908 — Ki = 0.27 nM 9.57
CHEMBL4065097 — Ki = 0.28 nM 9.55
CHEMBL4090706 — Ki = 0.3 nM 9.52
CHEMBL4066563 — Ki = 0.31 nM 9.51
CHEMBL4066563 — Ki = 0.3162 nM 9.50
CHEMBL4085407 — Ki = 0.3162 nM 9.50
CHEMBL4105382 — Ki = 0.3162 nM 9.50
CHEMBL4086535 — Ki = 0.32 nM 9.49
CHEMBL4105382 — Ki = 0.32 nM 9.49
CHEMBL4078689 — Ki = 0.34 nM 9.47
CHEMBL4063825 — Ki = 0.37 nM 9.43
CHEMBL4063825 — Ki = 0.3981 nM 9.40
CHEMBL4093165 — Ki = 0.5012 nM 9.30
CHEMBL4068853 — Ki = 0.5012 nM 9.30
CHEMBL4085407 — Ki = 0.52 nM 9.28
CHEMBL4068853 — Ki = 0.6 nM 9.22
CHEMBL4076020 — Ki = 0.7943 nM 9.10
CHEMBL4076020 — Ki = 1.26 nM 8.90
CHEMBL4072418 — Ki = 2.512 nM 8.60
CHEMBL4072418 — Ki = 3.3 nM 8.48
CHEMBL4102969 — Ki = 6.28 nM 8.20
CHEMBL4102969 — Ki = 6.31 nM 8.20