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Assay Detail

CHEMBL676050

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

Binding
Inhibitory concentration required for displacing radioligand [3H]SPI from DA D-2 receptor
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

D(2) dopamine receptor (CHEMBL339)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Conformational analysis of dopamine D-2 receptor antagonists of the benzamide series in relation to a recently proposed D-2 receptor-interaction model.
Pettersson I, Liljefors T.
J Med Chem (1992) 35 : 2355 -2363
PubMed 1535660 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.49 9.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL274491 1 9.31
CHEMBL325109 CLEBOPRIDE 2.0 1 7.77
CHEMBL8809 RACLOPRIDE 2.0 1 7.50
CHEMBL267044 LEVOSULPIRIDE 2.0 1 6.77
CHEMBL86 METOCLOPRAMIDE 4.0 1 6.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL274491 IC50 = 0.49 nM 9.31
CHEMBL325109 CLEBOPRIDE IC50 = 17.0 nM 7.77
CHEMBL8809 RACLOPRIDE IC50 = 32.0 nM 7.50
CHEMBL267044 LEVOSULPIRIDE IC50 = 170.0 nM 6.77
CHEMBL86 METOCLOPRAMIDE IC50 = 820.0 nM 6.09