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Assay Detail

CHEMBL657911

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

Binding
Evaluated for binding affinity against recombinant human central cannabinoid receptor 1
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

New class of potent ligands for the human peripheral cannabinoid receptor
Gallant M, Dufresne C, Gareau Y, Guay D, Leblanc Y, Prasit P, Rochette C, Sawyer N, Slipetz DM, Tremblay N, Metters KM, Labelle M
Bioorg Med Chem Lett (1996) 6 : 2263 -2268
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 5.51 6.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL274833 1 6.20
CHEMBL73206 1 6.06
CHEMBL307210 1 5.76
CHEMBL73711 1 5.72
CHEMBL72374 1 5.69
CHEMBL307627 1 5.66
CHEMBL72163 1 5.59
CHEMBL75326 1 5.50
CHEMBL308777 1 5.47
CHEMBL75733 1 5.44
CHEMBL72324 1 5.34
CHEMBL307887 1 5.25
CHEMBL421685 1 5.17
CHEMBL72771 1 4.99
CHEMBL75571 1 4.78
CHEMBL73572 1 -
CHEMBL6 INDOMETHACIN 4.0 1 -
CHEMBL72631 INDOMETHACIN MORPHOLINYLAMIDE 1 -
CHEMBL308847 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL274833 Ki = 638.0 nM 6.20
CHEMBL73206 Ki = 877.0 nM 6.06
CHEMBL307210 Ki = 1720.0 nM 5.76
CHEMBL73711 Ki = 1917.0 nM 5.72
CHEMBL72374 Ki = 2043.0 nM 5.69
CHEMBL307627 Ki = 2183.0 nM 5.66
CHEMBL72163 Ki = 2553.0 nM 5.59
CHEMBL75326 Ki = 3193.0 nM 5.50
CHEMBL308777 Ki = 3363.0 nM 5.47
CHEMBL75733 Ki = 3600.0 nM 5.44
CHEMBL72324 Ki = 4610.0 nM 5.34
CHEMBL307887 Ki = 5570.0 nM 5.25
CHEMBL421685 Ki = 6680.0 nM 5.17
CHEMBL72771 Ki = 10253.0 nM 4.99
CHEMBL75571 Ki = 16800.0 nM 4.78
CHEMBL73572 Ki > 20000.0 nM -
CHEMBL6 INDOMETHACIN Ki > 20000.0 nM -
CHEMBL72631 INDOMETHACIN MORPHOLINYLAMIDE Ki > 20000.0 nM -
CHEMBL308847 Ki > 20000.0 nM -