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Assay Detail

CHEMBL933206

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

Binding
Displacement of [3H]CP-55940 from human recombinant CB1 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 1 (CHEMBL218) ↗
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 6.86 8.64
IC50 34 6.51 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL285932 — — 1 8.64
CHEMBL272203 — — 2 8.25
CHEMBL111 RIMONABANT 4.0 1 7.92
CHEMBL271824 — — 2 7.85
CHEMBL410727 — — 2 7.55
CHEMBL271782 — — 2 7.55
CHEMBL259255 — — 2 7.55
CHEMBL261381 — — 2 7.52
CHEMBL409150 — — 2 7.46
CHEMBL269919 — — 2 7.46
CHEMBL272035 — — 2 7.46
CHEMBL259684 — — 2 7.43
CHEMBL259476 — — 2 7.42
CHEMBL261382 — — 2 7.38
CHEMBL406924 — — 2 7.25
CHEMBL271611 — — 2 6.96
CHEMBL271783 — — 2 6.96
CHEMBL271988 — — 2 6.96
CHEMBL259042 — — 2 6.55
CHEMBL411041 — — 2 6.55
CHEMBL411112 — — 2 6.55
CHEMBL410496 — — 2 6.55
CHEMBL272616 — — 2 5.80
CHEMBL410912 — — 2 5.80
CHEMBL260095 — — 2 5.75
CHEMBL410728 — — 2 5.73
CHEMBL271610 — — 2 5.55
CHEMBL270749 — — 2 5.55
CHEMBL428610 — — 2 5.55
CHEMBL408968 — — 2 5.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL285932 — Ki = 2.3 nM 8.64
CHEMBL272203 — Ki = 5.6 nM 8.25
CHEMBL272203 — IC50 = 10.0 nM 8.00
CHEMBL111 RIMONABANT Ki = 12.0 nM 7.92
CHEMBL271824 — Ki = 14.0 nM 7.85
CHEMBL271824 — IC50 = 25.0 nM 7.60
CHEMBL271782 — Ki = 28.0 nM 7.55
CHEMBL259255 — Ki = 28.0 nM 7.55
CHEMBL410727 — Ki = 28.0 nM 7.55
CHEMBL261381 — Ki = 30.0 nM 7.52
CHEMBL269919 — Ki = 35.0 nM 7.46
CHEMBL409150 — Ki = 35.0 nM 7.46
CHEMBL272035 — Ki = 35.0 nM 7.46
CHEMBL259684 — Ki = 37.0 nM 7.43
CHEMBL259476 — Ki = 38.0 nM 7.42
CHEMBL261382 — Ki = 42.0 nM 7.38
CHEMBL410727 — IC50 = 50.0 nM 7.30
CHEMBL259255 — IC50 = 50.0 nM 7.30
CHEMBL271782 — IC50 = 50.0 nM 7.30
CHEMBL261381 — IC50 = 54.0 nM 7.27
CHEMBL406924 — Ki = 56.0 nM 7.25
CHEMBL409150 — IC50 = 62.0 nM 7.21
CHEMBL272035 — IC50 = 62.0 nM 7.21
CHEMBL269919 — IC50 = 62.0 nM 7.21
CHEMBL259684 — IC50 = 66.0 nM 7.18
CHEMBL259476 — IC50 = 67.0 nM 7.17
CHEMBL261382 — IC50 = 74.0 nM 7.13
CHEMBL406924 — IC50 = 100.0 nM 7.00
CHEMBL271783 — Ki = 110.0 nM 6.96
CHEMBL271988 — Ki = 110.0 nM 6.96
CHEMBL271611 — Ki = 110.0 nM 6.96
CHEMBL271611 — IC50 = 200.0 nM 6.70
CHEMBL271988 — IC50 = 200.0 nM 6.70
CHEMBL271783 — IC50 = 200.0 nM 6.70
CHEMBL411112 — Ki = 280.0 nM 6.55
CHEMBL411041 — Ki = 280.0 nM 6.55
CHEMBL259042 — Ki = 280.0 nM 6.55
CHEMBL410496 — Ki = 280.0 nM 6.55
CHEMBL259042 — IC50 = 500.0 nM 6.30
CHEMBL411041 — IC50 = 500.0 nM 6.30
CHEMBL410496 — IC50 = 500.0 nM 6.30
CHEMBL411112 — IC50 = 500.0 nM 6.30
CHEMBL272616 — Ki = 1600.0 nM 5.80
CHEMBL410912 — Ki = 1600.0 nM 5.80
CHEMBL260095 — Ki = 1800.0 nM 5.75
CHEMBL410728 — Ki = 1850.0 nM 5.73
CHEMBL272616 — IC50 = 2800.0 nM 5.55
CHEMBL270749 — Ki = 2820.0 nM 5.55
CHEMBL271610 — Ki = 2820.0 nM 5.55
CHEMBL428610 — Ki = 2820.0 nM 5.55