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Assay Detail

CHEMBL1105741

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

Binding
Inhibition of cannabinoid CB1 receptor
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Discovery of N-[(4R)-6-(4-chlorophenyl)-7-(2,4-dichlorophenyl)-2,2-dimethyl-3,4-dihydro-2H-pyrano[2,3-b]pyridin-4-yl]-5-methyl-1H-pyrazole-3-carboxamide (MK-5596) as a novel cannabinoid-1 receptor (CB1R) inverse agonist for the treatment of obesity.
Yan L, Huo P, Debenham JS, Madsen-Duggan CB, Lao J, Chen RZ, Xiao JC, Shen CP, Stribling DS, Shearman LP, Strack AM, Tsou N, Ball RG, Wang J, Tong X, Bateman TJ, Reddy VB, Fong TM, Hale JJ.
J Med Chem (2010) 53 : 4028 -4037
PubMed 20423086 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.74 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL220360 TARANABANT 3.0 1 9.52
CHEMBL1092169 1 8.37
CHEMBL1094521 1 8.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL220360 TARANABANT IC50 = 0.3 nM 9.52
CHEMBL1092169 IC50 = 4.3 nM 8.37
CHEMBL1094521 IC50 = 4.8 nM 8.32