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Assay Detail

CHEMBL1059680

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

Binding
Displacement of [3H]rimonabant from human CB1 receptor expressed in HEK293 cells by liquid scintillation counting
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

Discovery and functional evaluation of diverse novel human CB(1) receptor ligands.
Foloppe N, Benwell K, Brooks TD, Kennett G, Knight AR, Misra A, Monck NJ.
Bioorg Med Chem Lett (2009) 19 : 4183 -4190
PubMed 19520572 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 33 6.32 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL220360 TARANABANT 3.0 1 9.52
CHEMBL111 RIMONABANT 4.0 1 8.72
CHEMBL230356 1 8.66
CHEMBL412262 IBIPINABANT 2.0 1 8.11
CHEMBL554943 1 6.64
CHEMBL560462 1 6.59
CHEMBL560463 1 6.58
CHEMBL555341 1 6.56
CHEMBL557921 1 6.54
CHEMBL565190 1 6.51
CHEMBL560383 1 6.49
CHEMBL550309 1 6.28
CHEMBL563400 1 6.28
CHEMBL559035 1 6.21
CHEMBL562123 1 6.06
CHEMBL549501 1 6.00
CHEMBL550514 1 5.99
CHEMBL563830 1 5.98
CHEMBL561663 1 5.96
CHEMBL551122 1 5.93
CHEMBL562519 1 5.83
CHEMBL555873 1 5.79
CHEMBL564177 1 5.75
CHEMBL556422 1 5.71
CHEMBL549366 1 5.64
CHEMBL564929 1 5.64
CHEMBL552122 1 5.64
CHEMBL551462 1 5.62
CHEMBL564343 1 5.59
CHEMBL562654 1 5.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL220360 TARANABANT Ki = 0.3 nM 9.52
CHEMBL111 RIMONABANT Ki = 1.9 nM 8.72
CHEMBL230356 Ki = 2.2 nM 8.66
CHEMBL412262 IBIPINABANT Ki = 7.8 nM 8.11
CHEMBL554943 Ki = 227.0 nM 6.64
CHEMBL560462 Ki = 256.0 nM 6.59
CHEMBL560463 Ki = 264.0 nM 6.58
CHEMBL555341 Ki = 273.0 nM 6.56
CHEMBL557921 Ki = 287.0 nM 6.54
CHEMBL565190 Ki = 308.0 nM 6.51
CHEMBL560383 Ki = 325.0 nM 6.49
CHEMBL550309 Ki = 520.0 nM 6.28
CHEMBL563400 Ki = 520.0 nM 6.28
CHEMBL559035 Ki = 611.0 nM 6.21
CHEMBL562123 Ki = 875.0 nM 6.06
CHEMBL549501 Ki = 1000.0 nM 6.00
CHEMBL550514 Ki = 1030.0 nM 5.99
CHEMBL563830 Ki = 1049.0 nM 5.98
CHEMBL561663 Ki = 1086.0 nM 5.96
CHEMBL551122 Ki = 1177.0 nM 5.93
CHEMBL562519 Ki = 1473.0 nM 5.83
CHEMBL555873 Ki = 1606.0 nM 5.79
CHEMBL564177 Ki = 1764.0 nM 5.75
CHEMBL556422 Ki = 1943.0 nM 5.71
CHEMBL549366 Ki = 2269.0 nM 5.64
CHEMBL564929 Ki = 2299.0 nM 5.64
CHEMBL552122 Ki = 2314.0 nM 5.64
CHEMBL551462 Ki = 2396.0 nM 5.62
CHEMBL564343 Ki = 2593.0 nM 5.59
CHEMBL562654 Ki = 2716.0 nM 5.57
CHEMBL557442 Ki = 2785.0 nM 5.55
CHEMBL559476 Ki = 3949.0 nM 5.40
CHEMBL555869 Ki = 7490.0 nM 5.13