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Assay Detail

CHEMBL670519

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

Binding
The affinity for the Dopamine receptor D2 was assessed by the inhibition of [3H]-spiperone binding in rat striatal membranes in vitro.
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Potential antipsychotic agents. 7. Synthesis and antidopaminergic properties of the atypical highly potent (S)-5-bromo-2,3-dimethoxy-N-[(1-ethyl-2-pyrrolidinyl)methyl]benzamide and related compounds. A comparative study.
Högberg T, de Paulis T, Johansson L, Kumar Y, Hall H, Ogren SO.
J Med Chem (1990) 33 : 2305 -2309
PubMed 1973734 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 7.78 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL289330 1 8.92
CHEMBL76402 1 8.85
CHEMBL75876 1 8.77
CHEMBL77492 1 8.72
CHEMBL75842 1 8.30
CHEMBL301532 1 8.14
CHEMBL305916 1 8.06
CHEMBL76266 1 8.00
CHEMBL283099 1 7.92
CHEMBL8809 RACLOPRIDE 2.0 1 7.50
CHEMBL74970 1 7.36
CHEMBL75447 1 7.34
CHEMBL419832 1 7.34
CHEMBL75887 1 7.28
CHEMBL2114141 1 6.84
CHEMBL307491 1 5.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL289330 IC50 = 1.2 nM 8.92
CHEMBL76402 IC50 = 1.4 nM 8.85
CHEMBL75876 IC50 = 1.7 nM 8.77
CHEMBL77492 IC50 = 1.9 nM 8.72
CHEMBL75842 IC50 = 5.0 nM 8.30
CHEMBL301532 IC50 = 7.2 nM 8.14
CHEMBL305916 IC50 = 8.8 nM 8.06
CHEMBL76266 IC50 = 10.0 nM 8.00
CHEMBL283099 IC50 = 12.0 nM 7.92
CHEMBL8809 RACLOPRIDE IC50 = 32.0 nM 7.50
CHEMBL74970 IC50 = 44.0 nM 7.36
CHEMBL75447 IC50 = 46.0 nM 7.34
CHEMBL419832 IC50 = 46.0 nM 7.34
CHEMBL75887 IC50 = 52.0 nM 7.28
CHEMBL2114141 IC50 = 145.0 nM 6.84
CHEMBL307491 IC50 = 8210.0 nM 5.09