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Assay Detail

CHEMBL953974

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Functional
Agonist activity at cloned human CB2 receptor in Sf9 cells assessed as stimulation of [35S]GTPgammaS binding assay
53
Total Activities
53
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cannabinoid receptor 2 (CHEMBL253)
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
EC50 53 8.24 9.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL470965 1 9.28
CHEMBL471129 1 9.15
CHEMBL471374 1 9.00
CHEMBL471992 1 8.96
CHEMBL472506 1 8.89
CHEMBL511134 1 8.89
CHEMBL465 DRONABINOL 4.0 1 8.82
CHEMBL507572 1 8.70
CHEMBL462330 1 8.70
CHEMBL510854 1 8.70
CHEMBL472157 1 8.68
CHEMBL488310 1 8.64
CHEMBL453846 1 8.62
CHEMBL518206 1 8.59
CHEMBL517283 1 8.57
CHEMBL471980 1 8.54
CHEMBL453844 1 8.52
CHEMBL454607 1 8.49
CHEMBL510072 1 8.49
CHEMBL472121 1 8.48
CHEMBL458142 1 8.48
CHEMBL519592 1 8.47
CHEMBL453842 1 8.38
CHEMBL471558 1 8.32
CHEMBL512906 1 8.30
CHEMBL454864 1 8.21
CHEMBL462533 1 8.19
CHEMBL487629 1 8.14
CHEMBL512886 1 8.08
CHEMBL451779 1 7.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL470965 EC50 = 0.52 nM 9.28
CHEMBL471129 EC50 = 0.7 nM 9.15
CHEMBL471374 EC50 = 1.0 nM 9.00
CHEMBL471992 EC50 = 1.1 nM 8.96
CHEMBL472506 EC50 = 1.3 nM 8.89
CHEMBL511134 EC50 = 1.3 nM 8.89
CHEMBL465 DRONABINOL EC50 = 1.5 nM 8.82
CHEMBL507572 EC50 = 2.0 nM 8.70
CHEMBL462330 EC50 = 2.0 nM 8.70
CHEMBL510854 EC50 = 2.0 nM 8.70
CHEMBL472157 EC50 = 2.1 nM 8.68
CHEMBL488310 EC50 = 2.3 nM 8.64
CHEMBL453846 EC50 = 2.4 nM 8.62
CHEMBL518206 EC50 = 2.6 nM 8.59
CHEMBL517283 EC50 = 2.7 nM 8.57
CHEMBL471980 EC50 = 2.9 nM 8.54
CHEMBL453844 EC50 = 3.0 nM 8.52
CHEMBL454607 EC50 = 3.2 nM 8.49
CHEMBL510072 EC50 = 3.2 nM 8.49
CHEMBL472121 EC50 = 3.3 nM 8.48
CHEMBL458142 EC50 = 3.3 nM 8.48
CHEMBL519592 EC50 = 3.4 nM 8.47
CHEMBL453842 EC50 = 4.2 nM 8.38
CHEMBL471558 EC50 = 4.8 nM 8.32
CHEMBL512906 EC50 = 5.0 nM 8.30
CHEMBL454864 EC50 = 6.2 nM 8.21
CHEMBL462533 EC50 = 6.4 nM 8.19
CHEMBL487629 EC50 = 7.3 nM 8.14
CHEMBL512886 EC50 = 8.3 nM 8.08
CHEMBL451779 EC50 = 11.0 nM 7.96
CHEMBL487456 EC50 = 13.0 nM 7.89
CHEMBL188 WIN-552122 EC50 = 14.0 nM 7.85
CHEMBL452803 EC50 = 18.0 nM 7.75
CHEMBL453843 EC50 = 22.0 nM 7.66
CHEMBL453847 EC50 = 24.0 nM 7.62
CHEMBL472165 EC50 = 25.0 nM 7.60
CHEMBL527208 EC50 = 25.0 nM 7.60
CHEMBL486440 EC50 = 25.0 nM 7.60
CHEMBL462329 EC50 = 36.0 nM 7.44
CHEMBL458143 EC50 = 38.0 nM 7.42
CHEMBL511021 EC50 = 43.0 nM 7.37
CHEMBL454096 EC50 = 52.0 nM 7.28
CHEMBL452039 EC50 = 65.0 nM 7.19
CHEMBL488816 EC50 = 69.0 nM 7.16
CHEMBL471984 EC50 - -
CHEMBL469693 EC50 - -
CHEMBL486438 EC50 - -
CHEMBL452804 EC50 - -
CHEMBL510141 EC50 - -
CHEMBL461920 EC50 - -