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Assay Detail

CHEMBL756245

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Binding
Compound was evaluated for the Opioid receptor kappa 1 affinity using guinea pig brain membranes.
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

2-(3,4-Dichlorophenyl)-N-methyl-N-[2-(1-pyrrolidinyl)-1-substituted- ethyl]-acetamides: the use of conformational analysis in the development of a novel series of potent opioid kappa agonists.
Costello GF, James R, Shaw JS, Slater AM, Stutchbury NC.
J Med Chem (1991) 34 : 181 -189
PubMed 1846918 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.88 8.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL56653 1 8.20
CHEMBL38576 ICI-199,441 1 8.16
CHEMBL56651 1 7.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL56653 IC50 = 6.3 nM 8.20
CHEMBL38576 ICI-199,441 IC50 = 6.9 nM 8.16
CHEMBL56651 IC50 = 53.2 nM 7.27