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Assay Detail

CHEMBL757518

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

Binding
Binding affinity against Opioid receptor mu 1 in guinea pig brain homogenate using [3H]- PL-17 as radioligand
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Mu-type opioid receptor (CHEMBL4354)
Type SINGLE PROTEIN
Organism Cavia porcellus

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 8.98 10.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL385759 1 10.57
CHEMBL410616 1 9.44
CHEMBL443068 1 9.01
CHEMBL216640 1 8.97
CHEMBL415330 1 8.89
CHEMBL265824 1 8.64
CHEMBL411557 DYNORPHIN A (1-17) 1 8.30
CHEMBL384250 1 7.99

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL385759 IC50 = 0.027 nM 10.57
CHEMBL410616 IC50 = 0.362 nM 9.44
CHEMBL443068 IC50 = 0.986 nM 9.01
CHEMBL216640 IC50 = 1.08 nM 8.97
CHEMBL415330 IC50 = 1.29 nM 8.89
CHEMBL265824 IC50 = 2.3 nM 8.64
CHEMBL411557 DYNORPHIN A (1-17) IC50 = 5.04 nM 8.30
CHEMBL384250 IC50 = 10.3 nM 7.99