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Assay Detail

CHEMBL754077

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

Binding
In vitro inhibitory activity against opioid receptor in Guinea pig ileum
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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

Synthesis, antinociceptive activity, and opioid receptor profiles of substituted trans-3-(decahydro- and octahydro-4a-isoquinolinyl)phenols.
Judd DB, Brown DS, Lloyd JE, McElroy AB, Scopes DI, Birch PJ, Hayes AG, Sheehan MJ.
J Med Chem (1992) 35 : 48 -56
PubMed 1310115 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.31 8.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL279968 ETHYLKETOCYCLAZOCINE 1 8.23
CHEMBL38874 DAMGO 1 7.85
CHEMBL152663 1 7.82
CHEMBL70 MORPHINE 4.0 1 7.55
CHEMBL150615 1 7.22
CHEMBL152720 1 7.22
CHEMBL153459 1 7.05
CHEMBL153616 1 6.92
CHEMBL347719 1 6.89
CHEMBL357705 1 6.85
CHEMBL153538 1 6.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL279968 ETHYLKETOCYCLAZOCINE IC50 = 5.9 nM 8.23
CHEMBL38874 DAMGO IC50 = 14.0 nM 7.85
CHEMBL152663 IC50 = 15.0 nM 7.82
CHEMBL70 MORPHINE IC50 = 28.0 nM 7.55
CHEMBL150615 IC50 = 60.0 nM 7.22
CHEMBL152720 IC50 = 60.0 nM 7.22
CHEMBL153459 IC50 = 90.0 nM 7.05
CHEMBL153616 IC50 = 120.0 nM 6.92
CHEMBL347719 IC50 = 130.0 nM 6.89
CHEMBL357705 IC50 = 140.0 nM 6.85
CHEMBL153538 IC50 = 150.0 nM 6.82