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Assay Detail

CHEMBL670125

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

Binding
In vitro ability to displace Dopamine D2 receptor binding to rat striatal membranes in competition experiments against 3H-spiperone, expressed as Ki
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Striatum
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

The synthesis and evaluation of the major metabolites of mazapertine
Reitz AB, McDonnell ME, Baxter EW, Codd EE, Wu W
Bioorg Med Chem Lett (1997) 7 : 1927 -1930
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 8.18 8.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL10085 MAZAPERTINE 2.0 1 8.66
CHEMBL58053 1 8.06
CHEMBL58517 1 8.05
CHEMBL61096 1 7.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL10085 MAZAPERTINE Ki = 2.2 nM 8.66
CHEMBL58053 Ki = 8.8 nM 8.06
CHEMBL58517 Ki = 9.0 nM 8.05
CHEMBL61096 Ki = 11.0 nM 7.96