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Assay Detail

CHEMBL1636582

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

Binding
Displacement of [3H]CP-55,940 from recombinant human CB2 receptor transfected in HEK cells
27
Total Activities
27
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 Autocuration

Target

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

Publication

Synthesis and biological evaluation of new N-alkyl 1-aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamides as cannabinoid receptor ligands.
Silvestri R, Ligresti A, La Regina G, Piscitelli F, Gatti V, Lavecchia A, Brizzi A, Pasquini S, Allarà M, Fantini N, Carai MA, Bigogno C, Rozio MG, Sinisi R, Novellino E, Colombo G, Di Marzo V, Dondio G, Corelli F.
Eur J Med Chem (2010) 45 : 5878 -5886
PubMed 20943290 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 6.62 8.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL381689 SR-144528 1 8.27
CHEMBL1629731 1 8.24
CHEMBL1631294 1 7.84
CHEMBL1631297 1 7.70
CHEMBL1631289 1 7.28
CHEMBL285932 1 6.95
CHEMBL1631298 1 6.92
CHEMBL1631299 1 6.88
CHEMBL1631300 1 6.87
CHEMBL1631301 1 6.79
CHEMBL1631291 1 6.69
CHEMBL1631162 1 6.69
CHEMBL1631295 1 6.62
CHEMBL1631165 1 6.59
CHEMBL1631292 1 6.44
CHEMBL1631164 1 6.42
CHEMBL1631167 1 6.34
CHEMBL1631290 1 6.31
CHEMBL1631168 1 6.30
CHEMBL111 RIMONABANT 4.0 1 6.10
CHEMBL1631161 1 6.10
CHEMBL1631293 1 5.95
CHEMBL1631160 1 5.83
CHEMBL1631296 1 5.75
CHEMBL1631166 1 5.71
CHEMBL1631163 1 5.63
CHEMBL1631169 1 5.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL381689 SR-144528 Ki = 5.4 nM 8.27
CHEMBL1629731 Ki = 5.7 nM 8.24
CHEMBL1631294 Ki = 14.6 nM 7.84
CHEMBL1631297 Ki = 20.2 nM 7.70
CHEMBL1631289 Ki = 52.4 nM 7.28
CHEMBL285932 Ki = 112.0 nM 6.95
CHEMBL1631298 Ki = 121.5 nM 6.92
CHEMBL1631299 Ki = 133.5 nM 6.88
CHEMBL1631300 Ki = 135.5 nM 6.87
CHEMBL1631301 Ki = 163.4 nM 6.79
CHEMBL1631291 Ki = 204.8 nM 6.69
CHEMBL1631162 Ki = 205.9 nM 6.69
CHEMBL1631295 Ki = 237.3 nM 6.62
CHEMBL1631165 Ki = 255.1 nM 6.59
CHEMBL1631292 Ki = 365.5 nM 6.44
CHEMBL1631164 Ki = 383.3 nM 6.42
CHEMBL1631167 Ki = 459.8 nM 6.34
CHEMBL1631290 Ki = 487.3 nM 6.31
CHEMBL1631168 Ki = 495.3 nM 6.30
CHEMBL111 RIMONABANT Ki = 790.0 nM 6.10
CHEMBL1631161 Ki = 795.7 nM 6.10
CHEMBL1631293 Ki = 1132.4 nM 5.95
CHEMBL1631160 Ki = 1496.2 nM 5.83
CHEMBL1631296 Ki = 1796.8 nM 5.75
CHEMBL1631166 Ki = 1953.3 nM 5.71
CHEMBL1631163 Ki = 2344.4 nM 5.63
CHEMBL1631169 Ki = 3200.5 nM 5.50