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Assay Detail

CHEMBL1062525

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

Binding
Displacement of [3H]Diprenorphine from rat kappa opioid receptor expressed in CHO cells
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Kappa-type opioid receptor (CHEMBL3614)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Design, synthesis, and pharmacological activities of dynorphin A analogues cyclized by ring-closing metathesis.
Fang WJ, Cui Y, Murray TF, Aldrich JV.
J Med Chem (2009) 52 : 5619 -5625
PubMed 19715279 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 8.40 9.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL216640 1 9.24
CHEMBL550968 1 9.08
CHEMBL538705 1 8.86
CHEMBL555959 1 8.61
CHEMBL554841 1 8.02
CHEMBL564095 1 7.96
CHEMBL553657 1 7.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL216640 Ki = 0.57 nM 9.24
CHEMBL550968 Ki = 0.84 nM 9.08
CHEMBL538705 Ki = 1.38 nM 8.86
CHEMBL555959 Ki = 2.46 nM 8.61
CHEMBL554841 Ki = 9.46 nM 8.02
CHEMBL564095 Ki = 10.9 nM 7.96
CHEMBL553657 Ki = 87.2 nM 7.06