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Assay Detail

CHEMBL1044345

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

Binding
Displacement of [3H]CP-55940 from recombinant human CB1 receptor expressed in CHO cells
20
Total Activities
20
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 Intermediate

Target

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

Publication

Synthesis and evaluation of N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-aminopropanamide as human cannabinoid-1 receptor (CB1R) inverse agonists.
Du W, Jewell JP, Lin LS, Colandrea VJ, Xiao JC, Lao J, Shen CP, Bateman TJ, Reddy VB, Ha SN, Shah SK, Fong TM, Hale JJ, Hagmann WK.
Bioorg Med Chem Lett (2009) 19 : 5195 -5199
PubMed 19632830 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 7.44 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL220360 TARANABANT 3.0 1 9.52
CHEMBL567679 1 8.80
CHEMBL582806 1 8.12
CHEMBL582820 1 8.07
CHEMBL572097 1 8.00
CHEMBL569292 1 7.91
CHEMBL567874 1 7.75
CHEMBL572271 1 7.71
CHEMBL567876 1 7.42
CHEMBL568849 1 7.34
CHEMBL584309 1 7.32
CHEMBL567461 1 7.31
CHEMBL568094 1 7.31
CHEMBL567513 1 7.01
CHEMBL571204 1 6.88
CHEMBL572080 1 6.87
CHEMBL571831 1 6.73
CHEMBL567297 1 6.69
CHEMBL584332 1 6.52
CHEMBL569614 1 5.53

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL220360 TARANABANT IC50 = 0.3 nM 9.52
CHEMBL567679 IC50 = 1.6 nM 8.80
CHEMBL582806 IC50 = 7.5 nM 8.12
CHEMBL582820 IC50 = 8.6 nM 8.07
CHEMBL572097 IC50 = 10.1 nM 8.00
CHEMBL569292 IC50 = 12.2 nM 7.91
CHEMBL567874 IC50 = 17.9 nM 7.75
CHEMBL572271 IC50 = 19.5 nM 7.71
CHEMBL567876 IC50 = 37.7 nM 7.42
CHEMBL568849 IC50 = 46.1 nM 7.34
CHEMBL584309 IC50 = 47.7 nM 7.32
CHEMBL567461 IC50 = 49.2 nM 7.31
CHEMBL568094 IC50 = 49.0 nM 7.31
CHEMBL567513 IC50 = 97.0 nM 7.01
CHEMBL571204 IC50 = 132.0 nM 6.88
CHEMBL572080 IC50 = 136.0 nM 6.87
CHEMBL571831 IC50 = 186.0 nM 6.73
CHEMBL567297 IC50 = 203.0 nM 6.69
CHEMBL584332 IC50 = 301.0 nM 6.52
CHEMBL569614 IC50 = 2982.0 nM 5.53