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Assay Detail

CHEMBL973406

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Functional
Antagonist activity against human recombinant cannabinoid-1 receptor
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Predictive models of Cannabinoid-1 receptor antagonists derived from diverse classes.
Kang NS, Lee GN, Yoo SE.
Bioorg Med Chem Lett (2009) 19 : 2990 -2996
PubMed 19406638 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 35 6.80 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL468313 1 9.52
CHEMBL511245 1 8.95
CHEMBL513814 1 8.88
CHEMBL466244 1 8.82
CHEMBL158784 RAC-IBIPINABANT 1 8.72
CHEMBL511907 1 8.21
CHEMBL181629 1 8.20
CHEMBL390146 1 8.09
CHEMBL226223 1 7.92
CHEMBL227840 1 7.79
CHEMBL2113258 1 7.77
CHEMBL468917 1 7.68
CHEMBL265787 1 7.45
CHEMBL226273 1 7.37
CHEMBL204391 1 6.95
CHEMBL181331 1 6.77
CHEMBL225243 1 6.62
CHEMBL227791 1 6.45
CHEMBL468931 1 6.40
CHEMBL360352 1 6.33
CHEMBL512643 1 6.11
CHEMBL389883 1 5.81
CHEMBL468918 1 5.77
CHEMBL368223 1 5.74
CHEMBL361182 1 5.72
CHEMBL468919 1 5.69
CHEMBL469131 1 5.66
CHEMBL179119 1 5.65
CHEMBL181088 1 5.55
CHEMBL513683 1 5.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL468313 IC50 = 0.302 nM 9.52
CHEMBL511245 IC50 = 1.122 nM 8.95
CHEMBL513814 IC50 = 1.318 nM 8.88
CHEMBL466244 IC50 = 1.514 nM 8.82
CHEMBL158784 RAC-IBIPINABANT IC50 = 1.905 nM 8.72
CHEMBL511907 IC50 = 6.166 nM 8.21
CHEMBL181629 IC50 = 6.31 nM 8.20
CHEMBL390146 IC50 = 8.128 nM 8.09
CHEMBL226223 IC50 = 12.02 nM 7.92
CHEMBL227840 IC50 = 16.22 nM 7.79
CHEMBL2113258 IC50 = 16.98 nM 7.77
CHEMBL468917 IC50 = 20.89 nM 7.68
CHEMBL265787 IC50 = 35.48 nM 7.45
CHEMBL226273 IC50 = 42.66 nM 7.37
CHEMBL204391 IC50 = 112.2 nM 6.95
CHEMBL181331 IC50 = 169.82 nM 6.77
CHEMBL225243 IC50 = 239.88 nM 6.62
CHEMBL227791 IC50 = 354.81 nM 6.45
CHEMBL468931 IC50 = 398.11 nM 6.40
CHEMBL360352 IC50 = 467.74 nM 6.33
CHEMBL512643 IC50 = 776.25 nM 6.11
CHEMBL389883 IC50 = 1548.82 nM 5.81
CHEMBL468918 IC50 = 1698.24 nM 5.77
CHEMBL368223 IC50 = 1819.7 nM 5.74
CHEMBL361182 IC50 = 1905.46 nM 5.72
CHEMBL468919 IC50 = 2041.74 nM 5.69
CHEMBL469131 IC50 = 2187.76 nM 5.66
CHEMBL179119 IC50 = 2238.72 nM 5.65
CHEMBL181088 IC50 = 2818.38 nM 5.55
CHEMBL513683 IC50 = 3467.37 nM 5.46
CHEMBL362694 IC50 = 3467.37 nM 5.46
CHEMBL225241 IC50 = 5623.41 nM 5.25
CHEMBL361181 IC50 = 6025.6 nM 5.22
CHEMBL467263 IC50 = 6606.93 nM 5.18
CHEMBL362638 IC50 = 19054.61 nM 4.72