Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL889632

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

Binding
Displacement of [3H]CP-55940 from human recombinant CB1R expressed in CHO cells
13
Total Activities
13
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 Expert

Target

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

Publication

Discovery of N-{(1S,2S)-2-(3-cyanophenyl)- 3-[4-(2-[18F]fluoroethoxy)phenyl]-1-methylpropyl}- 2-methyl-2-[(5-methylpyridin-2-yl)oxy]propanamide, a cannabinoid-1 receptor positron emission tomography tracer suitable for clinical use.
Liu P, Lin LS, Hamill TG, Jewell JP, Lanza TJ, Gibson RE, Krause SM, Ryan C, Eng W, Sanabria S, Tong X, Wang J, Levorse DA, Owens KA, Fong TM, Shen CP, Lao J, Kumar S, Yin W, Payack JF, Springfield SA, Hargreaves R, Burns HD, Goulet MT, Hagmann WK.
J Med Chem (2007) 50 : 3427 -3430
PubMed 17608398 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 9.04 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL220360 TARANABANT 3.0 1 9.52
CHEMBL226590 1 9.33
CHEMBL226591 1 9.15
CHEMBL226642 1 9.14
CHEMBL376794 1 9.11
CHEMBL226589 1 9.10
CHEMBL226534 1 9.05
CHEMBL376767 1 9.05
CHEMBL226684 1 9.05
CHEMBL227329 1 8.89
CHEMBL226640 1 8.74
CHEMBL387526 1 8.74
CHEMBL226685 1 8.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL220360 TARANABANT IC50 = 0.3 nM 9.52
CHEMBL226590 IC50 = 0.47 nM 9.33
CHEMBL226591 IC50 = 0.7 nM 9.15
CHEMBL226642 IC50 = 0.73 nM 9.14
CHEMBL376794 IC50 = 0.77 nM 9.11
CHEMBL226589 IC50 = 0.8 nM 9.10
CHEMBL226534 IC50 = 0.9 nM 9.05
CHEMBL376767 IC50 = 0.9 nM 9.05
CHEMBL226684 IC50 = 0.9 nM 9.05
CHEMBL227329 IC50 = 1.3 nM 8.89
CHEMBL226640 IC50 = 1.8 nM 8.74
CHEMBL387526 IC50 = 1.8 nM 8.74
CHEMBL226685 IC50 = 2.0 nM 8.70