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Assay Detail

CHEMBL753915

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Binding
Binding affinity against Opioid receptor kappa 1 isolated from rat brain membrane was determined using [3H]U-69593 as radioligand
8
Total Activities
8
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 (CHEMBL3614)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and biological evaluation of 14-alkoxymorphinans. 20. 14-phenylpropoxymetopon: an extremely powerful analgesic.
Schütz J, Spetea M, Koch M, Aceto MD, Harris LS, Coop A, Schmidhammer H.
J Med Chem (2003) 46 : 4182 -4187
PubMed 12954070 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 8.43 9.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL133836 DIHYDROETORPHINE 1 9.89
CHEMBL140050 ETORPHINE 2.0 1 9.74
CHEMBL335969 1 9.40
CHEMBL337272 1 8.65
CHEMBL334511 1 7.62
CHEMBL134067 1 7.60
CHEMBL133454 1 7.57
CHEMBL70 MORPHINE 4.0 1 6.95

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL133836 DIHYDROETORPHINE Ki = 0.13 nM 9.89
CHEMBL140050 ETORPHINE Ki = 0.18 nM 9.74
CHEMBL335969 Ki = 0.4 nM 9.40
CHEMBL337272 Ki = 2.26 nM 8.65
CHEMBL334511 Ki = 24.1 nM 7.62
CHEMBL134067 Ki = 25.0 nM 7.60
CHEMBL133454 Ki = 26.9 nM 7.57
CHEMBL70 MORPHINE Ki = 113.0 nM 6.95