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Assay Detail

CHEMBL935778

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

Binding
Displacement of [3H]SR-141716 from human wild type CB1R expressed in CHO cells
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Conformational analysis and receptor docking of N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-{[5-(trifluoromethyl)pyridin-2-yl]oxy}propanamide (taranabant, MK-0364), a novel, acyclic cannabinoid-1 receptor inverse agonist.
Lin LS, Ha S, Ball RG, Tsou NN, Castonguay LA, Doss GA, Fong TM, Shen CP, Xiao JC, Goulet MT, Hagmann WK.
J Med Chem (2008) 51 : 2108 -2114
PubMed 18333607 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 9.76 10.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL220360 TARANABANT 3.0 1 10.03
CHEMBL285932 1 9.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL220360 TARANABANT IC50 = 0.094 nM 10.03
CHEMBL285932 IC50 = 0.32 nM 9.49