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Assay Detail

CHEMBL2340177

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

Binding
Displacement of [3H]U69593 from KOR in Hartley guinea pig membrane
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Kappa-type opioid receptor (CHEMBL3952)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Orvinols with mixed kappa/mu opioid receptor agonist activity.
Greedy BM, Bradbury F, Thomas MP, Grivas K, Cami-Kobeci G, Archambeau A, Bosse K, Clark MJ, Aceto M, Lewis JW, Traynor JR, Husbands SM.
J Med Chem (2013) 56 : 3207 -3216
PubMed 23438330 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 8.82 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2338743 1 9.40
CHEMBL511142 BUPRENORPHINE 4.0 1 9.30
CHEMBL2338754 1 8.92
CHEMBL2338735 1 8.70
CHEMBL2338755 1 8.33
CHEMBL2338736 1 8.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2338743 Ki = 0.4 nM 9.40
CHEMBL511142 BUPRENORPHINE Ki = 0.5 nM 9.30
CHEMBL2338754 Ki = 1.2 nM 8.92
CHEMBL2338735 Ki = 2.0 nM 8.70
CHEMBL2338755 Ki = 4.7 nM 8.33
CHEMBL2338736 Ki = 5.5 nM 8.26