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Assay Detail

CHEMBL754241

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

Functional
Opioid receptors antagonist activity in smooth-muscle tissue mouse vas deferens (MVD)
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Tissue Vas deferens
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Opioid receptor (CHEMBL2095192)
Type PROTEIN FAMILY
Organism Mus musculus

Publication

Design and synthesis of highly potent and selective cyclic dynorphin A analogues.
Kawasaki AM, Knapp RJ, Kramer TH, Wire WS, Vasquez OS, Yamamura HI, Burks TF, Hruby VJ.
J Med Chem (1990) 33 : 1874 -1879
PubMed 1972964 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.20 8.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL415330 1 8.11
CHEMBL410616 1 7.71
CHEMBL443068 1 7.70
CHEMBL411557 DYNORPHIN A (1-17) 1 7.65
CHEMBL384250 1 7.61
CHEMBL216640 1 6.69
CHEMBL385759 1 6.38
CHEMBL265824 1 5.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL415330 IC50 = 7.8 nM 8.11
CHEMBL410616 IC50 = 19.5 nM 7.71
CHEMBL443068 IC50 = 20.1 nM 7.70
CHEMBL411557 DYNORPHIN A (1-17) IC50 = 22.5 nM 7.65
CHEMBL384250 IC50 = 24.5 nM 7.61
CHEMBL216640 IC50 = 204.0 nM 6.69
CHEMBL385759 IC50 = 421.0 nM 6.38
CHEMBL265824 IC50 = 1660.0 nM 5.78