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Assay Detail

CHEMBL3583992

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

Binding
Displacement of [3H]CP55940 from human CB2 receptor expressed in CHO-K1 cell membrane by competitive displacement assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cannabinoid receptor 2 (CHEMBL253)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel azoles as potent and selective cannabinoid CB2 receptor agonists.
Harnett JJ, Dolo C, Viossat I, Auger F, Ferrandis E, Bigg D, Auguet M, Auvin S, Chabrier PE.
Bioorg Med Chem Lett (2014) 25 : 88 -91
PubMed 25466197 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 6.84 7.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL408430 1 7.66
CHEMBL3581222 1 7.53
CHEMBL3581226 1 7.30
CHEMBL3581228 1 7.29
CHEMBL3581225 1 7.11
CHEMBL3581220 1 7.09
CHEMBL3581229 1 6.90
CHEMBL3581224 1 6.84
CHEMBL3581227 1 6.75
CHEMBL3581223 1 5.57
CHEMBL3581221 1 5.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL408430 Ki = 21.8 nM 7.66
CHEMBL3581222 Ki = 29.4 nM 7.53
CHEMBL3581226 Ki = 49.7 nM 7.30
CHEMBL3581228 Ki = 51.6 nM 7.29
CHEMBL3581225 Ki = 77.4 nM 7.11
CHEMBL3581220 Ki = 81.7 nM 7.09
CHEMBL3581229 Ki = 127.0 nM 6.90
CHEMBL3581224 Ki = 144.0 nM 6.84
CHEMBL3581227 Ki = 177.0 nM 6.75
CHEMBL3581223 Ki = 2700.0 nM 5.57
CHEMBL3581221 Ki = 6237.0 nM 5.21