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Assay Detail

CHEMBL980654

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Functional
Inverse agonist activity at cannabinoid CB1 receptor
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

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

Publication

Pyridopyrimidine based cannabinoid-1 receptor inverse agonists: Synthesis and biological evaluation.
Debenham JS, Madsen-Duggan CB, Wang J, Tong X, Lao J, Fong TM, Schaeffer MT, Xiao JC, Huang CC, Shen CP, Sloan Stribling D, Shearman LP, Strack AM, Euan Macintyre D, Hale JJ, Walsh TF.
Bioorg Med Chem Lett (2009) 19 : 2591 -2594
PubMed 19328684 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.69 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL220360 TARANABANT 3.0 1 9.52
CHEMBL246723 1 8.43
CHEMBL204232 NAPHTHYRIDINONE 1 8.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL220360 TARANABANT IC50 = 0.3 nM 9.52
CHEMBL246723 IC50 = 3.7 nM 8.43
CHEMBL204232 NAPHTHYRIDINONE IC50 = 7.5 nM 8.12