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Assay Detail

CHEMBL758577

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Binding
Effect on binding affinity of mutational exchange of Lys303 in the Opioid receptor mu 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

Mu-type opioid receptor (CHEMBL270)
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 7.81 8.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL330751 1 8.39
CHEMBL485832 GUANIDINONALTRINDOLE 1 8.04
CHEMBL573214 NORBINALTORPHIMINE 1 6.99

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL330751 Ki = 4.04 nM 8.39
CHEMBL485832 GUANIDINONALTRINDOLE Ki = 9.23 nM 8.04
CHEMBL573214 NORBINALTORPHIMINE Ki = 101.9 nM 6.99