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Assay Detail

CHEMBL881350

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

Binding
In vitro binding affinity against rat cannabinoid receptor 1 using 0.5 nM [3H]CP-55940
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Synthesis and structure-activity relationship of a novel series of aminoalkylindoles with potential for imaging the neuronal cannabinoid receptor by positron emission tomography.
Willis PG, Pavlova OA, Chefer SI, Vaupel DB, Mukhin AG, Horti AG.
J Med Chem (2005) 48 : 5813 -5822
PubMed 16134948 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 8.55 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL193331 1 9.15
CHEMBL68641 1 9.05
CHEMBL370009 1 8.96
CHEMBL194998 1 8.96
CHEMBL364266 1 8.92
CHEMBL364223 1 8.89
CHEMBL194313 1 8.85
CHEMBL195297 1 8.77
CHEMBL371328 1 8.66
CHEMBL195838 1 8.64
CHEMBL194314 1 8.40
CHEMBL445392 1 8.11
CHEMBL196834 1 7.92
CHEMBL196364 1 7.91
CHEMBL196648 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL193331 Ki = 0.7 nM 9.15
CHEMBL68641 Ki = 0.9 nM 9.05
CHEMBL370009 Ki = 1.1 nM 8.96
CHEMBL194998 Ki = 1.1 nM 8.96
CHEMBL364266 Ki = 1.2 nM 8.92
CHEMBL364223 Ki = 1.3 nM 8.89
CHEMBL194313 Ki = 1.4 nM 8.85
CHEMBL195297 Ki = 1.7 nM 8.77
CHEMBL371328 Ki = 2.2 nM 8.66
CHEMBL195838 Ki = 2.3 nM 8.64
CHEMBL194314 Ki = 4.0 nM 8.40
CHEMBL445392 Ki = 7.8 nM 8.11
CHEMBL196834 Ki = 12.0 nM 7.92
CHEMBL196364 Ki = 12.4 nM 7.91
CHEMBL196648 Ki = 100.0 nM 7.00