Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL747872

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

Binding
Inhibition of [3H]CTOP binding to rat brain homogenate mu-opioid receptor
12
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Confidence 9 — Direct single protein target
Curated By Expert

Target

Mu-type opioid receptor (CHEMBL270)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Design of cyclic deltorphins and dermenkephalins with a disulfide bridge leads to analogues with high selectivity for delta-opioid receptors.
Misicka A, Lipkowski AW, Horvath R, Davis P, Yamamura HI, Porreca F, Hruby VJ.
J Med Chem (1994) 37 : 141 -145
PubMed 8289187 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.60 8.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL289006 1 8.29
CHEMBL284621 1 5.92
CHEMBL317956 DELTORPHIN C 2 5.78
CHEMBL32202 1 5.72
CHEMBL2372209 1 5.72
CHEMBL2372213 1 5.48
CHEMBL286629 1 5.42
CHEMBL2372208 1 5.31
CHEMBL2372214 1 4.99
CHEMBL288317 1 4.58
CHEMBL2372212 1 4.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL289006 IC50 = 5.15 nM 8.29
CHEMBL284621 IC50 = 1200.0 nM 5.92
CHEMBL317956 DELTORPHIN C IC50 = 1680.0 nM 5.78
CHEMBL32202 IC50 = 1900.0 nM 5.72
CHEMBL2372209 IC50 = 1900.0 nM 5.72
CHEMBL317956 DELTORPHIN C IC50 = 2140.0 nM 5.67
CHEMBL2372213 IC50 = 3300.0 nM 5.48
CHEMBL286629 IC50 = 3760.0 nM 5.42
CHEMBL2372208 IC50 = 4900.0 nM 5.31
CHEMBL2372214 IC50 = 10200.0 nM 4.99
CHEMBL288317 IC50 = 26000.0 nM 4.58
CHEMBL2372212 IC50 = 54600.0 nM 4.26