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Assay Detail

CHEMBL755420

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

Binding
Affinity against Opioid receptor kappa 1 was determined by measuring the inhibition of [3H]bremazocine binding to guinea pig cerebellar membranes
7
Total Activities
7
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

Synthesis and opioid activity of [D-Pro10]dynorphin A-(1-11) analogues with N-terminal alkyl substitution.
Choi H, Murray TF, DeLander GE, Schmidt WK, Aldrich JV.
J Med Chem (1997) 40 : 2733 -2739
PubMed 9276018 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 9.81 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL442323 1 10.70
CHEMBL268818 1 10.54
CHEMBL384584 1 10.52
CHEMBL406338 1 10.31
CHEMBL406893 1 9.72
CHEMBL266782 1 8.44
CHEMBL267215 1 8.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL442323 Ki = 0.02 nM 10.70
CHEMBL268818 Ki = 0.029 nM 10.54
CHEMBL384584 Ki = 0.03 nM 10.52
CHEMBL406338 Ki = 0.049 nM 10.31
CHEMBL406893 Ki = 0.19 nM 9.72
CHEMBL266782 Ki = 3.6 nM 8.44
CHEMBL267215 Ki = 3.66 nM 8.44