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Assay Detail

CHEMBL756021

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

Functional
Opioid receptors antagonist activity in smooth-muscle tissue of guinea pig ileum (GPI)
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Tissue Ileum
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Opioid receptors; mu/kappa/delta (CHEMBL2095181)
Type PROTEIN FAMILY
Organism Homo sapiens

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 7.89 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL443068 1 8.89
CHEMBL415330 1 8.77
CHEMBL410616 1 8.76
CHEMBL384250 1 8.64
CHEMBL411557 DYNORPHIN A (1-17) 1 8.60
CHEMBL216640 1 8.12
CHEMBL385759 1 5.97
CHEMBL265824 1 5.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL443068 IC50 = 1.3 nM 8.89
CHEMBL415330 IC50 = 1.7 nM 8.77
CHEMBL410616 IC50 = 1.75 nM 8.76
CHEMBL384250 IC50 = 2.27 nM 8.64
CHEMBL411557 DYNORPHIN A (1-17) IC50 = 2.5 nM 8.60
CHEMBL216640 IC50 = 7.5 nM 8.12
CHEMBL385759 IC50 = 1080.0 nM 5.97
CHEMBL265824 IC50 = 4406.0 nM 5.36