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Assay Detail

CHEMBL992744

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

Binding
Binding affinity to human cloned dopamine D3 receptor
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

D(3) dopamine receptor (CHEMBL234)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.
Ablordeppey SY, Altundas R, Bricker B, Zhu XY, Kumar EV, Jackson T, Khan A, Roth BL.
Bioorg Med Chem (2008) 16 : 7291 -7301
PubMed 18595716 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 7.07 8.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 8.60
CHEMBL708 ZIPRASIDONE 4.0 1 8.14
CHEMBL85 RISPERIDONE 4.0 1 8.02
CHEMBL715 OLANZAPINE 4.0 1 7.35
CHEMBL476108 1 6.80
CHEMBL476934 1 6.66
CHEMBL42 CLOZAPINE 4.0 1 6.62
CHEMBL140872 1 6.61
CHEMBL716 QUETIAPINE 4.0 1 6.50
CHEMBL476109 1 6.26
CHEMBL476933 1 6.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 2.5 nM 8.60
CHEMBL708 ZIPRASIDONE Ki = 7.2 nM 8.14
CHEMBL85 RISPERIDONE Ki = 9.6 nM 8.02
CHEMBL715 OLANZAPINE Ki = 45.0 nM 7.35
CHEMBL476108 Ki = 158.8 nM 6.80
CHEMBL476934 Ki = 220.0 nM 6.66
CHEMBL42 CLOZAPINE Ki = 240.0 nM 6.62
CHEMBL140872 Ki = 244.1 nM 6.61
CHEMBL716 QUETIAPINE Ki = 320.0 nM 6.50
CHEMBL476109 Ki = 548.1 nM 6.26
CHEMBL476933 Ki = 600.0 nM 6.22