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Assay Detail

CHEMBL839538

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

Binding
Binding affinity for cannabinoid receptor 1
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Triaryl bis-sulfones as a new class of cannabinoid CB2 receptor inhibitors: identification of a lead and initial SAR studies.
Lavey BJ, Kozlowski JA, Hipkin RW, Gonsiorek W, Lundell DJ, Piwinski JJ, Narula S, Lunn CA.
Bioorg Med Chem Lett (2005) 15 : 783 -786
PubMed 15664857 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 5.86 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL181675 1 7.10
CHEMBL362822 1 7.08
CHEMBL362480 1 6.93
CHEMBL181843 1 6.63
CHEMBL361957 1 6.32
CHEMBL180963 1 6.07
CHEMBL360697 1 6.05
CHEMBL180465 1 6.04
CHEMBL360306 1 5.95
CHEMBL181868 1 5.93
CHEMBL180748 1 5.93
CHEMBL179888 1 5.75
CHEMBL359712 1 5.75
CHEMBL180196 1 5.72
CHEMBL181288 1 5.71
CHEMBL180788 1 5.64
CHEMBL181677 1 5.45
CHEMBL180450 1 4.97
CHEMBL361218 1 4.14
CHEMBL426962 1 4.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL181675 Ki = 79.0 nM 7.10
CHEMBL362822 Ki = 84.0 nM 7.08
CHEMBL362480 Ki = 117.0 nM 6.93
CHEMBL181843 Ki = 235.0 nM 6.63
CHEMBL361957 Ki = 478.0 nM 6.32
CHEMBL180963 Ki = 855.0 nM 6.07
CHEMBL360697 Ki = 884.0 nM 6.05
CHEMBL180465 Ki = 905.0 nM 6.04
CHEMBL360306 Ki = 1129.0 nM 5.95
CHEMBL181868 Ki = 1172.0 nM 5.93
CHEMBL180748 Ki = 1173.0 nM 5.93
CHEMBL179888 Ki = 1758.0 nM 5.75
CHEMBL359712 Ki = 1779.0 nM 5.75
CHEMBL180196 Ki = 1923.0 nM 5.72
CHEMBL181288 Ki = 1968.0 nM 5.71
CHEMBL180788 Ki = 2309.0 nM 5.64
CHEMBL181677 Ki = 3559.0 nM 5.45
CHEMBL180450 Ki = 10625.0 nM 4.97
CHEMBL361218 Ki = 72089.0 nM 4.14
CHEMBL426962 Ki = 100000.0 nM 4.00