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Assay Detail

CHEMBL675732

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

Binding
Compound was evaluated for binding affinity towards DA D-2 receptor using radioligand [3H]SPI
6
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
Ki 6 7.94 9.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL274491 1 9.92
CHEMBL325109 CLEBOPRIDE 2.0 1 8.66
CHEMBL8809 RACLOPRIDE 2.0 1 8.02
CHEMBL267044 LEVOSULPIRIDE 2.0 1 7.41
CHEMBL86 METOCLOPRAMIDE 4.0 2 6.98

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL274491 Ki = 0.12 nM 9.92
CHEMBL325109 CLEBOPRIDE Ki = 2.2 nM 8.66
CHEMBL8809 RACLOPRIDE Ki = 9.5 nM 8.02
CHEMBL267044 LEVOSULPIRIDE Ki = 39.0 nM 7.41
CHEMBL86 METOCLOPRAMIDE Ki = 104.0 nM 6.98
CHEMBL86 METOCLOPRAMIDE Ki = 235.0 nM 6.63