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Assay Detail

CHEMBL3280910

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

Binding
Displacement of [3H]-naloxone from rat opioid receptor after 30 mins by liquid scintillation counting analysis in presence of NaCl
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Opioid receptor (CHEMBL2094129)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Analgesics. 1. Synthesis and analgesic properties of N-sec-alkyl- and N-tert-alkylnormorphines.
DeGraw JI, Lawson JA, Crase JL, Johnson HL, Ellis M, Uyeno ET, Loew GH, Berkowitz DS.
J Med Chem (1978) 21 : 415 -422
PubMed 207868 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 6.98 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL415284 NALORPHINE 2.0 1 8.22
CHEMBL3275471 1 7.85
CHEMBL3275464 1 7.60
CHEMBL3275467 1 7.35
CHEMBL3275461 1 7.21
CHEMBL3275463 1 7.10
CHEMBL3272387 1 7.04
CHEMBL3275462 1 6.96
CHEMBL3275470 1 6.90
CHEMBL3275468 1 6.89
CHEMBL3275472 1 6.88
CHEMBL3275469 1 6.82
CHEMBL3275466 1 6.76
CHEMBL70 MORPHINE 4.0 1 6.60
CHEMBL3275465 1 6.47
CHEMBL3275460 1 6.00
CHEMBL3275458 1 6.00
CHEMBL3275459 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL415284 NALORPHINE IC50 = 6.0 nM 8.22
CHEMBL3275471 IC50 = 14.0 nM 7.85
CHEMBL3275464 IC50 = 25.0 nM 7.60
CHEMBL3275467 IC50 = 45.0 nM 7.35
CHEMBL3275461 IC50 = 62.0 nM 7.21
CHEMBL3275463 IC50 = 80.0 nM 7.10
CHEMBL3272387 IC50 = 92.0 nM 7.04
CHEMBL3275462 IC50 = 110.0 nM 6.96
CHEMBL3275470 IC50 = 125.0 nM 6.90
CHEMBL3275468 IC50 = 130.0 nM 6.89
CHEMBL3275472 IC50 = 133.0 nM 6.88
CHEMBL3275469 IC50 = 150.0 nM 6.82
CHEMBL3275466 IC50 = 175.0 nM 6.76
CHEMBL70 MORPHINE IC50 = 250.0 nM 6.60
CHEMBL3275465 IC50 = 340.0 nM 6.47
CHEMBL3275460 IC50 = 1000.0 nM 6.00
CHEMBL3275458 IC50 = 1000.0 nM 6.00
CHEMBL3275459 IC50 > 1000.0 nM -