Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL933207

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

Binding
Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells
ChEMBL ↗
71
Total Activities
37
Compounds Tested
2
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, cannabinoid receptor affinity, and molecular modeling studies of substituted 1-aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamides.
Silvestri R, Cascio MG, La Regina G, Piscitelli F, Lavecchia A, Brizzi A, Pasquini S, Botta M, Novellino E, Di Marzo V, Corelli F.
J Med Chem (2008) 51 : 1560 -1576
PubMed 18293908 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 37 6.52 8.89
IC50 34 6.38 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL271824 — — 2 8.89
CHEMBL272203 — — 2 8.77
CHEMBL381689 SR-144528 — 1 8.27
CHEMBL261381 — — 2 7.70
CHEMBL259255 — — 2 7.54
CHEMBL406924 — — 2 7.19
CHEMBL410912 — — 2 7.19
CHEMBL261382 — — 2 7.06
CHEMBL285932 — — 1 6.95
CHEMBL272035 — — 2 6.82
CHEMBL410728 — — 2 6.70
CHEMBL271782 — — 2 6.41
CHEMBL410913 — — 2 6.41
CHEMBL271783 — — 2 6.41
CHEMBL259684 — — 2 6.29
CHEMBL269919 — — 2 6.24
CHEMBL111 RIMONABANT 4.0 1 6.10
CHEMBL259476 — — 2 6.01
CHEMBL259042 — — 2 5.86
CHEMBL410496 — — 2 5.76
CHEMBL271988 — — 2 5.66
CHEMBL408968 — — 2 5.62
CHEMBL271611 — — 2 5.41
CHEMBL409150 — — 2 5.41
CHEMBL272616 — — 2 5.41
CHEMBL410727 — — 2 5.41
CHEMBL411112 — — 2 5.41
CHEMBL271610 — — 2 -
CHEMBL428610 — — 2 -
CHEMBL412252 — — 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL271824 — Ki = 1.3 nM 8.89
CHEMBL271824 — IC50 = 1.7 nM 8.77
CHEMBL272203 — Ki = 1.7 nM 8.77
CHEMBL272203 — IC50 = 2.2 nM 8.66
CHEMBL381689 SR-144528 Ki = 5.4 nM 8.27
CHEMBL261381 — Ki = 20.0 nM 7.70
CHEMBL261381 — IC50 = 25.0 nM 7.60
CHEMBL259255 — Ki = 29.0 nM 7.54
CHEMBL259255 — IC50 = 37.0 nM 7.43
CHEMBL410912 — Ki = 65.0 nM 7.19
CHEMBL406924 — Ki = 64.0 nM 7.19
CHEMBL406924 — IC50 = 81.0 nM 7.09
CHEMBL410912 — IC50 = 83.0 nM 7.08
CHEMBL261382 — Ki = 87.0 nM 7.06
CHEMBL261382 — IC50 = 110.0 nM 6.96
CHEMBL285932 — Ki = 112.0 nM 6.95
CHEMBL272035 — Ki = 150.0 nM 6.82
CHEMBL272035 — IC50 = 190.0 nM 6.72
CHEMBL410728 — IC50 = 200.0 nM 6.70
CHEMBL271783 — Ki = 390.0 nM 6.41
CHEMBL271782 — Ki = 390.0 nM 6.41
CHEMBL410913 — Ki = 390.0 nM 6.41
CHEMBL410913 — IC50 = 500.0 nM 6.30
CHEMBL271783 — IC50 = 500.0 nM 6.30
CHEMBL271782 — IC50 = 500.0 nM 6.30
CHEMBL259684 — Ki = 510.0 nM 6.29
CHEMBL269919 — Ki = 570.0 nM 6.24
CHEMBL259684 — IC50 = 650.0 nM 6.19
CHEMBL269919 — IC50 = 720.0 nM 6.14
CHEMBL111 RIMONABANT Ki = 790.0 nM 6.10
CHEMBL259476 — Ki = 980.0 nM 6.01
CHEMBL259476 — IC50 = 1240.0 nM 5.91
CHEMBL259042 — Ki = 1370.0 nM 5.86
CHEMBL259042 — IC50 = 1740.0 nM 5.76
CHEMBL410496 — Ki = 1750.0 nM 5.76
CHEMBL410728 — Ki = 1730.0 nM 5.76
CHEMBL271988 — Ki = 2180.0 nM 5.66
CHEMBL410496 — IC50 = 2220.0 nM 5.65
CHEMBL408968 — Ki = 2400.0 nM 5.62
CHEMBL271988 — IC50 = 2770.0 nM 5.56
CHEMBL408968 — IC50 = 3000.0 nM 5.52
CHEMBL409150 — Ki = 3940.0 nM 5.41
CHEMBL410727 — Ki = 3940.0 nM 5.41
CHEMBL271611 — Ki = 3940.0 nM 5.41
CHEMBL411112 — Ki = 3940.0 nM 5.41
CHEMBL272616 — Ki = 3940.0 nM 5.41
CHEMBL411112 — IC50 = 5000.0 nM 5.30
CHEMBL410727 — IC50 = 5000.0 nM 5.30
CHEMBL272616 — IC50 = 5000.0 nM 5.30
CHEMBL409150 — IC50 = 5000.0 nM 5.30