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Assay Detail

CHEMBL753918

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

Binding
Ability to inhibit the specific binding of [3H]- dihydromorphine to opiate receptors in rat brain membrane preparation by 50%
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Opioid receptor (CHEMBL2094129)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Combined analgesic/neuroleptic activity in N-butyrophenone prodine-like compounds.
Iorio MA, Reymer TP, Frigeni V.
J Med Chem (1987) 30 : 1906 -1910
PubMed 2888899 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.87 8.53

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL299471 1 8.53
CHEMBL292006 1 8.48
CHEMBL56547 1 8.06
CHEMBL1160253 1 7.63
CHEMBL57306 1 6.22
CHEMBL54206 1 5.49
CHEMBL59213 1 5.26
CHEMBL54 HALOPERIDOL 4.0 1 5.25
CHEMBL56843 1 -
CHEMBL57029 1 -
CHEMBL57140 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL299471 IC50 = 2.96 nM 8.53
CHEMBL292006 IC50 = 3.33 nM 8.48
CHEMBL56547 IC50 = 8.67 nM 8.06
CHEMBL1160253 IC50 = 23.5 nM 7.63
CHEMBL57306 IC50 = 598.0 nM 6.22
CHEMBL54206 IC50 = 3215.0 nM 5.49
CHEMBL59213 IC50 = 5500.0 nM 5.26
CHEMBL54 HALOPERIDOL IC50 = 5687.0 nM 5.25
CHEMBL56843 IC50 > 10000.0 nM -
CHEMBL57029 IC50 > 10000.0 nM -
CHEMBL57140 IC50 > 10000.0 nM -