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Assay Detail

CHEMBL953973

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

Binding
Displacement of [3H]CP-55940 from human CB1 receptor
52
Total Activities
52
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cannabinoid receptor 1 (CHEMBL218)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel benzimidazole derivatives as selective CB2 agonists.
Pagé D, Balaux E, Boisvert L, Liu Z, Milburn C, Tremblay M, Wei Z, Woo S, Luo X, Cheng YX, Yang H, Srivastava S, Zhou F, Brown W, Tomaszewski M, Walpole C, Hodzic L, St-Onge S, Godbout C, Salois D, Payza K.
Bioorg Med Chem Lett (2008) 18 : 3695 -3700
PubMed 18522867 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 52 5.97 8.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL465 DRONABINOL 4.0 1 8.54
CHEMBL470965 1 6.96
CHEMBL188 WIN-552122 1 6.85
CHEMBL511134 1 6.39
CHEMBL471129 1 6.31
CHEMBL471374 1 5.92
CHEMBL510072 1 5.62
CHEMBL518206 1 5.61
CHEMBL507572 1 5.58
CHEMBL472506 1 5.51
CHEMBL458142 1 5.46
CHEMBL511021 1 5.38
CHEMBL488310 1 5.37
CHEMBL510854 1 5.34
CHEMBL453846 1 5.33
CHEMBL471992 1 5.32
CHEMBL486440 1 -
CHEMBL469693 1 -
CHEMBL512886 1 -
CHEMBL471558 1 -
CHEMBL472121 1 -
CHEMBL471984 1 -
CHEMBL512906 1 -
CHEMBL472165 1 -
CHEMBL472157 1 -
CHEMBL487456 1 -
CHEMBL454607 1 -
CHEMBL462533 1 -
CHEMBL462330 1 -
CHEMBL462329 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL465 DRONABINOL Ki = 2.9 nM 8.54
CHEMBL470965 Ki = 110.0 nM 6.96
CHEMBL188 WIN-552122 Ki = 140.0 nM 6.85
CHEMBL511134 Ki = 406.0 nM 6.39
CHEMBL471129 Ki = 491.0 nM 6.31
CHEMBL471374 Ki = 1209.0 nM 5.92
CHEMBL510072 Ki = 2396.0 nM 5.62
CHEMBL518206 Ki = 2483.0 nM 5.61
CHEMBL507572 Ki = 2608.0 nM 5.58
CHEMBL472506 Ki = 3115.0 nM 5.51
CHEMBL458142 Ki = 3475.0 nM 5.46
CHEMBL511021 Ki = 4190.0 nM 5.38
CHEMBL488310 Ki = 4315.0 nM 5.37
CHEMBL510854 Ki = 4534.0 nM 5.34
CHEMBL453846 Ki = 4679.0 nM 5.33
CHEMBL471992 Ki = 4766.0 nM 5.32
CHEMBL518814 Ki > 5000.0 nM -
CHEMBL461920 Ki > 5000.0 nM -
CHEMBL453843 Ki > 5000.0 nM -
CHEMBL453842 Ki > 5000.0 nM -
CHEMBL453844 Ki > 5000.0 nM -
CHEMBL454864 Ki > 5000.0 nM -
CHEMBL471980 Ki > 5000.0 nM -
CHEMBL510141 Ki > 5000.0 nM -
CHEMBL454096 Ki > 5000.0 nM -
CHEMBL452039 Ki > 5000.0 nM -
CHEMBL451779 Ki > 5000.0 nM -
CHEMBL452804 Ki > 5000.0 nM -
CHEMBL452803 Ki > 5000.0 nM -
CHEMBL453847 Ki > 5000.0 nM -
CHEMBL487629 Ki > 5000.0 nM -
CHEMBL486438 Ki > 5000.0 nM -
CHEMBL488816 Ki > 5000.0 nM -
CHEMBL472157 Ki > 5000.0 nM -
CHEMBL486440 Ki > 5000.0 nM -
CHEMBL469693 Ki > 5000.0 nM -
CHEMBL512886 Ki > 5000.0 nM -
CHEMBL471558 Ki > 5000.0 nM -
CHEMBL472121 Ki > 5000.0 nM -
CHEMBL471984 Ki > 5000.0 nM -
CHEMBL512906 Ki > 5000.0 nM -
CHEMBL472165 Ki > 5000.0 nM -
CHEMBL461921 Ki > 5000.0 nM -
CHEMBL487456 Ki > 5000.0 nM -
CHEMBL454607 Ki > 5000.0 nM -
CHEMBL462533 Ki > 5000.0 nM -
CHEMBL462330 Ki > 5000.0 nM -
CHEMBL462329 Ki > 5000.0 nM -
CHEMBL517283 Ki > 5000.0 nM -
CHEMBL462119 Ki > 5000.0 nM -