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Assay Detail

CHEMBL887659

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

Binding
Displacement of [3H]CP-559440 from human CB2 receptor expressed in HEK293 cells
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cannabinoid receptor 2 (CHEMBL253)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Optimization of imidazole amide derivatives as cannabinoid-1 receptor antagonists for the treatment of obesity.
Smith RA, Fathi Z, Achebe F, Akuche C, Brown SE, Choi S, Fan J, Jenkins S, Kluender HC, Konkar A, Lavoie R, Mays R, Natoli J, O'Connor SJ, Ortiz AA, Su N, Taing C, Tomlinson S, Tritto T, Wang G, Wirtz SN, Wong W, Yang XF, Ying S, Zhang Z.
Bioorg Med Chem Lett (2007) 17 : 2706 -2711
PubMed 17383180 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 5.67 6.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL276312 1 6.62
CHEMBL389198 1 5.96
CHEMBL229967 1 5.92
CHEMBL389175 1 5.64
CHEMBL230800 1 5.64
CHEMBL231118 1 5.57
CHEMBL230801 1 5.57
CHEMBL395321 1 5.29
CHEMBL229914 1 5.28
CHEMBL229965 1 5.20
CHEMBL439375 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL276312 Ki = 240.0 nM 6.62
CHEMBL389198 Ki = 1100.0 nM 5.96
CHEMBL229967 Ki = 1200.0 nM 5.92
CHEMBL389175 Ki = 2300.0 nM 5.64
CHEMBL230800 Ki = 2300.0 nM 5.64
CHEMBL231118 Ki = 2700.0 nM 5.57
CHEMBL230801 Ki = 2700.0 nM 5.57
CHEMBL395321 Ki = 5100.0 nM 5.29
CHEMBL229914 Ki = 5300.0 nM 5.28
CHEMBL229965 Ki = 6300.0 nM 5.20
CHEMBL439375 Ki > 1000.0 nM -