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Assay Detail

CHEMBL755004

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

Functional
Antagonist activity of compound on U50,488H stimulated [35S]GTP-gamma-S binding to opioid receptor kappa 1
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Effect of N-alkyl and N-alkenyl substituents in noroxymorphindole, 17-substituted-6,7-dehydro-4,5alpha-epoxy-3,14-dihydroxy-6,7:2',3'-indolomorphinans, on opioid receptor affinity, selectivity, and efficacy.
McLamore S, Ullrich T, Rothman RB, Xu H, Dersch C, Coop A, Davis P, Porreca F, Jacobson AE, Rice KC.
J Med Chem (2001) 44 : 1471 -1474
PubMed 11311071 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 7.13 8.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1237164 NALTRINDOLE HYDROCHLORIDE 1 8.33
CHEMBL611702 1 6.93
CHEMBL611697 1 6.13
CHEMBL611704 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1237164 NALTRINDOLE HYDROCHLORIDE Ki = 4.7 nM 8.33
CHEMBL611702 Ki = 118.0 nM 6.93
CHEMBL611697 Ki = 740.0 nM 6.13
CHEMBL611704 Ki > 1000.0 nM -