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Assay Detail

CHEMBL753167

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

Functional
Inhibition of [35S]GTP-gamma-S, binding from Opioid receptor kappa 1 in Guinea pig Caudate stimulated by U69,593
4
Total Activities
4
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 an opioid kappa receptor subtype-selective N-substituent for (+)-(3R,4R)-dimethyl-4-(3-hydroxyphenyl)piperidine.
Thomas JB, Fall MJ, Cooper JB, Rothman RB, Mascarella SW, Xu H, Partilla JS, Dersch CM, McCullough KB, Cantrell BE, Zimmerman DM, Carroll FI.
J Med Chem (1998) 41 : 5188 -5197
PubMed 9857089 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 9.11 10.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL573214 NORBINALTORPHIMINE 1 10.42
CHEMBL150052 1 8.98
CHEMBL19019 NALTREXONE 4.0 1 8.69
CHEMBL10986 1 8.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL573214 NORBINALTORPHIMINE Ki = 0.038 nM 10.42
CHEMBL150052 Ki = 1.04 nM 8.98
CHEMBL19019 NALTREXONE Ki = 2.05 nM 8.69
CHEMBL10986 Ki = 4.7 nM 8.33