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Assay Detail

CHEMBL753176

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

Functional
Inhibition of stimulation of [35S]GTP-gamma-S, binding produced by the selective agonist (U69593, kappa-receptor), in guinea pig caudate membranes.
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Kappa-type opioid receptor (CHEMBL3952)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Identification of the first trans-(3R,4R)- dimethyl-4-(3-hydroxyphenyl)piperidine derivative to possess highly potent and selective opioid kappa receptor antagonist activity.
Thomas JB, Atkinson RN, Rothman RB, Fix SE, Mascarella SW, Vinson NA, Xu H, Dersch CM, Lu Y, Cantrell BE, Zimmerman DM, Carroll FI.
J Med Chem (2001) 44 : 2687 -2690
PubMed 11495579 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 10.70 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL51204 1 10.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL51204 Ki = 0.02 nM 10.70