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Assay Detail

CHEMBL966895

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

Binding
Displacement of [3H]diprenorphine from human kappa opioid receptor expressed in CHO cells
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

The discovery of tropane derivatives as nociceptin receptor ligands for the management of cough and anxiety.
Ho GD, Anthes J, Bercovici A, Caldwell JP, Cheng KC, Cui X, Fawzi A, Fernandez X, Greenlee WJ, Hey J, Korfmacher W, Lu SX, McLeod RL, Ng F, Torhan AS, Tan Z, Tulshian D, Varty GB, Xu X, Zhang H.
Bioorg Med Chem Lett (2009) 19 : 2519 -2523
PubMed 19339177 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 6.59 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL466847 1 6.96
CHEMBL513136 1 6.88
CHEMBL512414 1 6.57
CHEMBL228690 1 6.44
CHEMBL466921 1 6.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL466847 Ki = 109.0 nM 6.96
CHEMBL513136 Ki = 131.0 nM 6.88
CHEMBL512414 Ki = 268.0 nM 6.57
CHEMBL228690 Ki = 364.0 nM 6.44
CHEMBL466921 Ki = 752.0 nM 6.12