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Assay Detail

CHEMBL1050879

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

Binding
Displacement of [3H]SR141716A from CB1 receptor in rat cerebellar membrane after 90 mins by scintillation counting
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Cerebellum
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Cannabinoid receptor 1 (CHEMBL3571)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and pharmacological evaluation of sulfamide-based analogues of anandamide.
Cano C, Páez JA, Goya P, Serrano A, Pavón J, Rodríguez de Fonseca F, Suardíaz M, Martín MI.
Eur J Med Chem (2009) 44 : 4889 -4895
PubMed 19762126 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 5.47 6.88

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL15848 ANANDAMIDE 1 6.88
CHEMBL570566 1 5.72
CHEMBL583108 1 5.63
CHEMBL568489 1 5.40
CHEMBL570988 1 5.19
CHEMBL218643 1 5.18
CHEMBL569658 1 5.14
CHEMBL374746 1 5.07
CHEMBL219156 1 5.04
CHEMBL571044 1 -
CHEMBL218794 1 -
CHEMBL218795 1 -
CHEMBL219047 1 -
CHEMBL219033 1 -
CHEMBL437157 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL15848 ANANDAMIDE Ki = 132.0 nM 6.88
CHEMBL570566 Ki = 1890.0 nM 5.72
CHEMBL583108 Ki = 2339.0 nM 5.63
CHEMBL568489 Ki = 4010.0 nM 5.40
CHEMBL570988 Ki = 6406.0 nM 5.19
CHEMBL218643 Ki = 6670.0 nM 5.18
CHEMBL569658 Ki = 7190.0 nM 5.14
CHEMBL374746 Ki = 8580.0 nM 5.07
CHEMBL219156 Ki = 9102.0 nM 5.04
CHEMBL571044 Ki > 10000.0 nM -
CHEMBL218794 Ki > 10000.0 nM -
CHEMBL218795 Ki - -
CHEMBL219047 Ki - -
CHEMBL219033 Ki - -
CHEMBL437157 Ki > 10000.0 nM -