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Assay Detail

CHEMBL755154

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

Binding
Inhibition of Opioid receptors binding by inhibiting specific [3H]naloxone binding by 50% in the presence of 100 mM NaCl
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Opioid receptors; mu/kappa/delta (CHEMBL2095181)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Synthesis and biological activity of fluoroalkylamine derivatives of narcotic analgesics.
Reifenrath WG, Roche EB, Al-Turk WA, Johnson HL.
J Med Chem (1980) 23 : 985 -990
PubMed 6106064 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.58 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL177893 1 7.00
CHEMBL177389 1 6.70
CHEMBL70 MORPHINE 4.0 1 6.60
CHEMBL178062 1 5.94
CHEMBL174811 1 5.60
CHEMBL607 MEPERIDINE 4.0 1 4.40
CHEMBL368974 1 4.22
CHEMBL176525 1 4.19
CHEMBL366585 1 -
CHEMBL175071 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL177893 IC50 = 100.0 nM 7.00
CHEMBL177389 IC50 = 200.0 nM 6.70
CHEMBL70 MORPHINE IC50 = 250.0 nM 6.60
CHEMBL178062 IC50 = 1150.0 nM 5.94
CHEMBL174811 IC50 = 2500.0 nM 5.60
CHEMBL607 MEPERIDINE IC50 = 40000.0 nM 4.40
CHEMBL368974 IC50 = 60000.0 nM 4.22
CHEMBL176525 IC50 = 64000.0 nM 4.19
CHEMBL366585 IC50 = 120000.0 nM -
CHEMBL175071 IC50 = 110000.0 nM -