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Assay Detail

CHEMBL823997

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Functional
Agonistic activity at kappa opioid receptor of rabbit vas deferens
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Tissue Vas deferens
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Kappa-type opioid receptor (CHEMBL237)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Preparation and evaluation of some hydrophilic phenylacetyl-piperazines as peripherally selective -opioid receptor agonists
Birch P, Hayes A, Johnson M, Lea T, Murray P, Rogers H, Scopes D
Bioorg Med Chem Lett (1992) 2 : 1275 -1278
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 8.11 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL277863 1 10.70
CHEMBL423653 1 9.66
CHEMBL279298 1 9.05
CHEMBL23607 1 8.82
CHEMBL22544 1 8.34
CHEMBL276970 1 8.20
CHEMBL23472 ICI-204448 1 8.13
CHEMBL23499 1 7.85
CHEMBL277636 1 7.43
CHEMBL25604 1 7.31
CHEMBL23631 1 6.85
CHEMBL23352 1 6.64
CHEMBL23535 1 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL277863 IC50 = 0.02 nM 10.70
CHEMBL423653 IC50 = 0.22 nM 9.66
CHEMBL279298 IC50 = 0.9 nM 9.05
CHEMBL23607 IC50 = 1.5 nM 8.82
CHEMBL22544 IC50 = 4.6 nM 8.34
CHEMBL276970 IC50 = 6.3 nM 8.20
CHEMBL23472 ICI-204448 IC50 = 7.4 nM 8.13
CHEMBL23499 IC50 = 14.0 nM 7.85
CHEMBL277636 IC50 = 37.0 nM 7.43
CHEMBL25604 IC50 = 49.0 nM 7.31
CHEMBL23631 IC50 = 140.0 nM 6.85
CHEMBL23352 IC50 = 230.0 nM 6.64
CHEMBL23535 IC50 = 400.0 nM 6.40