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Assay Detail

CHEMBL873196

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Binding
Evaluated for binding affinity towards human Cannabinoid receptor 1
26
Total Activities
26
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

Potent imidazole and triazole CB1 receptor antagonists related to SR141716.
Dyck B, Goodfellow VS, Phillips T, Grey J, Haddach M, Rowbottom M, Naeve GS, Brown B, Saunders J.
Bioorg Med Chem Lett (2004) 14 : 1151 -1154
PubMed 14980654 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 26 7.27 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL15528 1 8.30
CHEMBL416718 1 8.05
CHEMBL15966 1 7.96
CHEMBL111 RIMONABANT 4.0 1 7.92
CHEMBL418721 1 7.85
CHEMBL15138 1 7.85
CHEMBL280454 1 7.54
CHEMBL416535 1 7.50
CHEMBL278236 1 7.48
CHEMBL15764 1 7.39
CHEMBL15874 1 7.38
CHEMBL276312 1 7.32
CHEMBL274983 1 7.18
CHEMBL275895 1 7.18
CHEMBL15635 1 7.11
CHEMBL428693 1 7.07
CHEMBL15399 1 7.07
CHEMBL15423 1 7.04
CHEMBL15772 1 7.03
CHEMBL279787 1 7.00
CHEMBL15478 1 7.00
CHEMBL15832 1 6.86
CHEMBL15877 1 6.79
CHEMBL275416 1 6.57
CHEMBL16249 1 6.46
CHEMBL418544 1 6.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL15528 Ki = 5.0 nM 8.30
CHEMBL416718 Ki = 9.0 nM 8.05
CHEMBL15966 Ki = 11.0 nM 7.96
CHEMBL111 RIMONABANT Ki = 12.0 nM 7.92
CHEMBL418721 Ki = 14.0 nM 7.85
CHEMBL15138 Ki = 14.0 nM 7.85
CHEMBL280454 Ki = 29.0 nM 7.54
CHEMBL416535 Ki = 32.0 nM 7.50
CHEMBL278236 Ki = 33.0 nM 7.48
CHEMBL15764 Ki = 41.0 nM 7.39
CHEMBL15874 Ki = 42.0 nM 7.38
CHEMBL276312 Ki = 48.0 nM 7.32
CHEMBL274983 Ki = 66.0 nM 7.18
CHEMBL275895 Ki = 66.0 nM 7.18
CHEMBL15635 Ki = 78.0 nM 7.11
CHEMBL428693 Ki = 85.0 nM 7.07
CHEMBL15399 Ki = 85.0 nM 7.07
CHEMBL15423 Ki = 91.0 nM 7.04
CHEMBL15772 Ki = 94.0 nM 7.03
CHEMBL279787 Ki = 101.0 nM 7.00
CHEMBL15478 Ki = 100.0 nM 7.00
CHEMBL15832 Ki = 137.0 nM 6.86
CHEMBL15877 Ki = 164.0 nM 6.79
CHEMBL275416 Ki = 270.0 nM 6.57
CHEMBL16249 Ki = 350.0 nM 6.46
CHEMBL418544 Ki = 770.0 nM 6.11