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Assay Detail

CHEMBL751016

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

Binding
Inhibitory activity against Opioid receptor kappa 1 in electrically stimulated mouse vas deferens (MVD) preparation.
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Kappa-type opioid receptor (CHEMBL4329)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Arylacetamide-derived fluorescent probes: synthesis, biological evaluation, and direct fluorescent labeling of kappa opioid receptors in mouse microglial cells.
Chang AC, Chao CC, Takemori AE, Gekker G, Hu S, Peterson PK, Portoghese PS.
J Med Chem (1996) 39 : 1729 -1735
PubMed 8648612 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 8.16 9.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL413530 1 9.92
CHEMBL1907788 1 8.92
CHEMBL1907786 1 8.92
CHEMBL1907789 1 8.82
CHEMBL38576 ICI-199,441 1 8.60
CHEMBL48344 1 8.35
CHEMBL1907787 1 8.19
CHEMBL430971 1 7.90
CHEMBL49591 1 6.99
CHEMBL47318 1 6.77
CHEMBL412689 1 6.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL413530 IC50 = 0.12 nM 9.92
CHEMBL1907788 IC50 = 1.2 nM 8.92
CHEMBL1907786 IC50 = 1.2 nM 8.92
CHEMBL1907789 IC50 = 1.5 nM 8.82
CHEMBL38576 ICI-199,441 IC50 = 2.5 nM 8.60
CHEMBL48344 IC50 = 4.5 nM 8.35
CHEMBL1907787 IC50 = 6.5 nM 8.19
CHEMBL430971 IC50 = 12.6 nM 7.90
CHEMBL49591 IC50 = 102.0 nM 6.99
CHEMBL47318 IC50 = 170.0 nM 6.77
CHEMBL412689 IC50 = 421.0 nM 6.38