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Assay Detail

CHEMBL755873

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

Binding
In vitro radioligand binding assay, for inhibition of [3H]U-69593 binding to Opioid receptor kappa 1, in guinea pig brain membranes.
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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

Probes for narcotic receptor mediated phenomena. 26. Synthesis and biological evaluation of diarylmethylpiperazines and diarylmethylpiperidines as novel, nonpeptidic delta opioid receptor ligands.
Zhang X, Rice KC, Calderon SN, Kayakiri H, Smith L, Coop A, Jacobson AE, Rothman RB, Davis P, Dersch CM, Porreca F.
J Med Chem (1999) 42 : 5455 -5463
PubMed 10639287 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 5.14 5.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL153648 1 5.52
CHEMBL545335 1 5.12
CHEMBL346625 1 5.00
CHEMBL13470 SNC-80 1 4.93

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL153648 Ki = 3000.0 nM 5.52
CHEMBL545335 Ki = 7650.0 nM 5.12
CHEMBL346625 Ki = 10000.0 nM 5.00
CHEMBL13470 SNC-80 Ki = 11700.0 nM 4.93