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Assay Detail

CHEMBL754918

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

Binding
Agonist potency using GTP-gamma [35S]- binding assay for opioid receptor kappa 1
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Kappa-type opioid receptor (CHEMBL237)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel C-terminus modifications of the Dmt-Tic motif: a new class of dipeptide analogues showing altered pharmacological profiles toward the opioid receptors.
Pagé D, Naismith A, Schmidt R, Coupal M, Labarre M, Gosselin M, Bellemare D, Payza K, Brown W.
J Med Chem (2001) 44 : 2387 -2390
PubMed 11448220 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 7.92 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL76573 1 8.85
CHEMBL77001 1 8.17
CHEMBL310842 1 8.16
CHEMBL77804 1 7.94
CHEMBL421520 1 7.61
CHEMBL80463 1 6.79

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL76573 EC50 = 1.4 nM 8.85
CHEMBL77001 EC50 = 6.8 nM 8.17
CHEMBL310842 EC50 = 6.9 nM 8.16
CHEMBL77804 EC50 = 11.5 nM 7.94
CHEMBL421520 EC50 = 24.3 nM 7.61
CHEMBL80463 EC50 = 161.0 nM 6.79