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Assay Detail

CHEMBL826339

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Binding
Binding affinity for human Dopamine receptor D2
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

D(2) dopamine receptor (CHEMBL217)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and structure-activity relationship of fluoro analogues of 8-{2-[4-(4-methoxyphenyl)piperazin-1yl]ethyl}-8-azaspiro[4.5]decane-7,9-dione as selective alpha(1d)-adrenergic receptor antagonists.
Konkel MJ, Wetzel JM, Cahir M, Craig DA, Noble SA, Gluchowski C.
J Med Chem (2005) 48 : 3076 -3079
PubMed 15828846 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 6.48 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL13647 BMY-7378 1 7.85
CHEMBL556313 1 6.92
CHEMBL299691 1 6.85
CHEMBL98241 1 6.24
CHEMBL193620 1 6.16
CHEMBL57546 1 5.66
CHEMBL192099 1 5.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL13647 BMY-7378 Ki = 14.0 nM 7.85
CHEMBL556313 Ki = 120.0 nM 6.92
CHEMBL299691 Ki = 140.0 nM 6.85
CHEMBL98241 Ki = 580.0 nM 6.24
CHEMBL193620 Ki = 700.0 nM 6.16
CHEMBL57546 Ki = 2200.0 nM 5.66
CHEMBL192099 Ki = 2200.0 nM 5.66