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Assay Detail

CHEMBL755492

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Binding
Effect on binding affinity of mutational exchange of Glu297 in the Opioid receptor kappa 1 in transiently expressed rat cos-7 cells activity expressed as binding affinity.
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type cos-7
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Mutational evidence for a common kappa antagonist binding pocket in the wild-type kappa and mutant mu[K303E] opioid receptors.
Jones RM, Hjorth SA, Schwartz TW, Portoghese PS.
J Med Chem (1998) 41 : 4911 -4914
PubMed 9836606 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 9.85 10.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL485832 GUANIDINONALTRINDOLE 1 10.05
CHEMBL573214 NORBINALTORPHIMINE 1 9.92
CHEMBL330751 1 9.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL485832 GUANIDINONALTRINDOLE Ki = 0.09 nM 10.05
CHEMBL573214 NORBINALTORPHIMINE Ki = 0.12 nM 9.92
CHEMBL330751 Ki = 0.27 nM 9.57