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Assay Detail

CHEMBL749840

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

Binding
50% Inhibition of stereospecific [3H]-naltrexone (10e-9 M) binding towards opiate receptor in rat brain homogenate
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Opioid receptor (CHEMBL2094129)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Acylmorphinans. A novel class of potent analgesic agents.
Mohacsi E, O'Brien J, Blount J, Sepinwall J.
J Med Chem (1985) 28 : 1177 -1180
PubMed 2863378 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.92 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6067642 CODEINE PHOSPHATE 4.0 1 8.00
CHEMBL1202420 1 7.85
CHEMBL1202422 1 7.16
CHEMBL17884 1 6.68
CHEMBL17681 1 4.89
CHEMBL70 MORPHINE 4.0 1 -
CHEMBL592 LEVORPHANOL 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6067642 CODEINE PHOSPHATE IC50 = 10.0 nM 8.00
CHEMBL1202420 IC50 = 14.0 nM 7.85
CHEMBL1202422 IC50 = 70.0 nM 7.16
CHEMBL17884 IC50 = 210.0 nM 6.68
CHEMBL17681 IC50 = 13000.0 nM 4.89
CHEMBL70 MORPHINE IC50 = 0.027 nM -
CHEMBL592 LEVORPHANOL IC50 = 0.004 nM -