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Assay Detail

CHEMBL659698

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

Binding
Inhibition of [3H]CP-55940 binding to cannabinoid receptor 1 in rat brain membranes.
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Subcellular Brain membranes
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Cannabinoid receptor 1 (CHEMBL3571)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Molecular interaction of the antagonist N-(piperidin-1-yl)-5-(4-chlorophenyl)-1- (2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide with the CB1 cannabinoid receptor.
Shim JY, Welsh WJ, Cartier E, Edwards JL, Howlett AC.
J Med Chem (2002) 45 : 1447 -1459
PubMed 11906286 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 35 7.38 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL287610 1 9.00
CHEMBL111 RIMONABANT 4.0 1 8.89
CHEMBL432272 1 8.52
CHEMBL284710 1 8.52
CHEMBL287017 1 8.22
CHEMBL285932 1 8.22
CHEMBL287353 1 8.15
CHEMBL36569 1 8.11
CHEMBL34201 1 7.82
CHEMBL286188 1 7.78
CHEMBL286302 1 7.77
CHEMBL33652 1 7.72
CHEMBL36032 1 7.68
CHEMBL286222 1 7.64
CHEMBL287609 1 7.60
CHEMBL35657 1 7.51
CHEMBL32855 1 7.43
CHEMBL287472 1 7.33
CHEMBL36250 1 7.26
CHEMBL285473 1 7.25
CHEMBL285259 1 7.20
CHEMBL285964 1 7.14
CHEMBL35835 1 7.00
CHEMBL34805 1 6.96
CHEMBL285153 1 6.91
CHEMBL285486 1 6.78
CHEMBL35918 1 6.74
CHEMBL284331 1 6.73
CHEMBL36232 1 6.70
CHEMBL2113343 1 6.63

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL287610 Ki = 1.0 nM 9.00
CHEMBL111 RIMONABANT Ki = 1.3 nM 8.89
CHEMBL432272 Ki = 3.0 nM 8.52
CHEMBL284710 Ki = 3.0 nM 8.52
CHEMBL287017 Ki = 6.0 nM 8.22
CHEMBL285932 Ki = 6.0 nM 8.22
CHEMBL287353 Ki = 7.0 nM 8.15
CHEMBL36569 Ki = 7.85 nM 8.11
CHEMBL34201 Ki = 15.0 nM 7.82
CHEMBL286188 Ki = 16.8 nM 7.78
CHEMBL286302 Ki = 17.1 nM 7.77
CHEMBL33652 Ki = 19.0 nM 7.72
CHEMBL36032 Ki = 21.0 nM 7.68
CHEMBL286222 Ki = 23.0 nM 7.64
CHEMBL287609 Ki = 25.0 nM 7.60
CHEMBL35657 Ki = 31.1 nM 7.51
CHEMBL32855 Ki = 37.0 nM 7.43
CHEMBL287472 Ki = 47.0 nM 7.33
CHEMBL36250 Ki = 55.0 nM 7.26
CHEMBL285473 Ki = 56.0 nM 7.25
CHEMBL285259 Ki = 63.0 nM 7.20
CHEMBL285964 Ki = 72.0 nM 7.14
CHEMBL35835 Ki = 100.0 nM 7.00
CHEMBL34805 Ki = 109.0 nM 6.96
CHEMBL285153 Ki = 123.0 nM 6.91
CHEMBL285486 Ki = 165.0 nM 6.78
CHEMBL35918 Ki = 183.0 nM 6.74
CHEMBL284331 Ki = 187.0 nM 6.73
CHEMBL36232 Ki = 202.0 nM 6.70
CHEMBL2113343 Ki = 232.0 nM 6.63
CHEMBL285026 Ki = 256.0 nM 6.59
CHEMBL432857 Ki = 391.0 nM 6.41
CHEMBL36579 Ki = 746.0 nM 6.13
CHEMBL32929 Ki = 771.0 nM 6.11
CHEMBL36553 Ki = 1360.0 nM 5.87