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Assay Detail

CHEMBL859083

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

Functional
Functional activity at human CB1 receptor transfected in CHOK1 cells by [35SGTP]gammaS assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

New bicyclic cannabinoid receptor-1 (CB1-R) antagonists.
Carpino PA, Griffith DA, Sakya S, Dow RL, Black SC, Hadcock JR, Iredale PA, Scott DO, Fichtner MW, Rose CR, Day R, Dibrino J, Butler M, Debartolo DB, Dutcher D, Gautreau D, Lizano JS, O'connor RE, Sands MA, Kelly-Sullivan D, Ward KM.
Bioorg Med Chem Lett (2006) 16 : 731 -736
PubMed 16263283 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 8.73 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL425047 1 10.00
CHEMBL204188 1 10.00
CHEMBL201520 1 9.00
CHEMBL201565 1 9.00
CHEMBL201602 1 9.00
CHEMBL379246 1 9.00
CHEMBL111 RIMONABANT 4.0 1 9.00
CHEMBL203925 1 8.70
CHEMBL425762 1 8.52
CHEMBL381858 1 8.40
CHEMBL202419 1 8.40
CHEMBL379667 1 8.40
CHEMBL204339 1 8.40
CHEMBL202583 1 8.30
CHEMBL201582 1 7.89
CHEMBL201923 1 7.70
CHEMBL380937 1 -
CHEMBL201929 1 -
CHEMBL201862 1 -
CHEMBL201924 1 -
CHEMBL370560 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL425047 Ki = 0.1 nM 10.00
CHEMBL204188 Ki = 0.1 nM 10.00
CHEMBL201520 Ki = 1.0 nM 9.00
CHEMBL201565 Ki = 1.0 nM 9.00
CHEMBL201602 Ki = 1.0 nM 9.00
CHEMBL379246 Ki = 1.0 nM 9.00
CHEMBL111 RIMONABANT Ki = 1.0 nM 9.00
CHEMBL203925 Ki = 2.0 nM 8.70
CHEMBL425762 Ki = 3.0 nM 8.52
CHEMBL381858 Ki = 4.0 nM 8.40
CHEMBL202419 Ki = 4.0 nM 8.40
CHEMBL379667 Ki = 4.0 nM 8.40
CHEMBL204339 Ki = 4.0 nM 8.40
CHEMBL202583 Ki = 5.0 nM 8.30
CHEMBL201582 Ki = 13.0 nM 7.89
CHEMBL201923 Ki = 20.0 nM 7.70
CHEMBL380937 Ki - -
CHEMBL201929 Ki - -
CHEMBL201862 Ki - -
CHEMBL201924 Ki - -
CHEMBL370560 Ki - -