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Assay Detail

CHEMBL3257740

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

Binding
Displacement of [3H]naloxone from Sprague-Dawley rat cerebellum opioid receptor assessed as relative receptor affinity by scintillation counting
19
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Cerebellum
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Opioid receptor (CHEMBL2094129)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Conformation of 2,9-dimethyl-3'-hydroxy-5-phenyl-6,7-genzomorphan and its relation to other analgetics and enkephalin.
Clarke FH, Jaggi H, Lovell RA.
J Med Chem (1978) 21 : 600 -606
PubMed 209186 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 6.57 8.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3249801 2 8.35
CHEMBL3249802 2 7.72
CHEMBL2103744 MORPHINE SULFATE 4.0 2 7.66
CHEMBL1200825 METHADONE HYDROCHLORIDE 4.0 2 7.29
CHEMBL13786 1 7.05
CHEMBL3249804 1 6.50
CHEMBL3249418 4 6.22
CHEMBL3249805 1 6.00
CHEMBL1701 MEPERIDINE HYDROCHLORIDE 4.0 2 5.00
CHEMBL3249803 2 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3249801 IC50 = 4.5 nM 8.35
CHEMBL3249802 IC50 = 19.0 nM 7.72
CHEMBL2103744 MORPHINE SULFATE IC50 = 22.0 nM 7.66
CHEMBL1200825 METHADONE HYDROCHLORIDE IC50 = 51.0 nM 7.29
CHEMBL13786 IC50 = 90.0 nM 7.05
CHEMBL3249804 IC50 = 320.0 nM 6.50
CHEMBL3249418 IC50 = 600.0 nM 6.22
CHEMBL3249805 IC50 = 1000.0 nM 6.00
CHEMBL3249418 IC50 = 3000.0 nM 5.52
CHEMBL3249803 IC50 = 10000.0 nM 5.00
CHEMBL1701 MEPERIDINE HYDROCHLORIDE IC50 = 10000.0 nM 5.00
CHEMBL3249801 IC50 = 4466835.92 nM -
CHEMBL2103744 MORPHINE SULFATE IC50 = 21877616.24 nM -
CHEMBL1200825 METHADONE HYDROCHLORIDE IC50 = 51286138.4 nM -
CHEMBL1701 MEPERIDINE HYDROCHLORIDE IC50 = 100000000.0 nM -
CHEMBL3249802 IC50 = 19054607.18 nM -
CHEMBL3249803 IC50 = 100000000.0 nM -
CHEMBL3249418 IC50 = 602559586.07 nM -
CHEMBL3249418 IC50 = 331131121.48 nM -