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Assay Detail

CHEMBL1803287

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

Binding
Displacement of [3H]-CP55940 from human CB1 receptor expressed in HEK-293-EBNA cell membranes after 90 mins by scintillation counting
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Development of endocannabinoid-based chemical probes for the study of cannabinoid receptors.
Martín-Couce L, Martín-Fontecha M, Capolicchio S, López-Rodríguez ML, Ortega-Gutiérrez S.
J Med Chem (2011) 54 : 5265 -5269
PubMed 21675776 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 6.31 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL146346 1 7.60
CHEMBL1800732 1 7.07
CHEMBL1800731 1 6.66
CHEMBL122972 2-ARACHIDONOYLGLYCEROL 1 6.32
CHEMBL1800182 1 5.70
CHEMBL1800727 1 5.70
CHEMBL1800728 1 5.70
CHEMBL1800729 1 5.70
CHEMBL1800181 1 -
CHEMBL1800730 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL146346 Ki = 25.0 nM 7.60
CHEMBL1800732 Ki = 84.7 nM 7.07
CHEMBL1800731 Ki = 221.0 nM 6.66
CHEMBL122972 2-ARACHIDONOYLGLYCEROL Ki = 480.0 nM 6.32
CHEMBL1800182 Ki = 2000.0 nM 5.70
CHEMBL1800727 Ki = 2000.0 nM 5.70
CHEMBL1800728 Ki = 2000.0 nM 5.70
CHEMBL1800729 Ki = 2000.0 nM 5.70
CHEMBL1800181 Ki > 2000.0 nM -
CHEMBL1800730 Ki > 5000.0 nM -