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Assay Detail

CHEMBL672295

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

Binding
Binding affinity towards dopamine D2 receptors in rat brain synaptosomal preparations
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

A new arylpiperazine antipsychotic with high D2/D3/5-HT1A/alpha 1A-adrenergic affinity and a low potential for extrapyramidal effects.
Reitz AB, Bennett DJ, Blum PS, Codd EE, Maryanoff CA, Ortegon ME, Renzi MJ, Scott MK, Shank RP, Vaught JL.
J Med Chem (1994) 37 : 1060 -1062
PubMed 7909336 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 7.61 8.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL10085 MAZAPERTINE 2.0 1 8.66
CHEMBL275045 1 7.64
CHEMBL10327 1 7.43
CHEMBL10105 1 7.34
CHEMBL10417 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL10085 MAZAPERTINE Ki = 2.2 nM 8.66
CHEMBL275045 Ki = 23.0 nM 7.64
CHEMBL10327 Ki = 37.0 nM 7.43
CHEMBL10105 Ki = 46.0 nM 7.34
CHEMBL10417 Ki = 100.0 nM 7.00