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Assay Detail

CHEMBL827144

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Binding
Binding affinity for rat Dopamine receptor D3
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

D(3) dopamine receptor (CHEMBL3138)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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 7.61 8.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL13647 BMY-7378 1 8.51
CHEMBL299691 1 8.28
CHEMBL556313 1 8.09
CHEMBL193620 1 7.64
CHEMBL57546 1 7.04
CHEMBL98241 1 6.92
CHEMBL192099 1 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL13647 BMY-7378 Ki = 3.1 nM 8.51
CHEMBL299691 Ki = 5.2 nM 8.28
CHEMBL556313 Ki = 8.1 nM 8.09
CHEMBL193620 Ki = 23.0 nM 7.64
CHEMBL57546 Ki = 91.0 nM 7.04
CHEMBL98241 Ki = 120.0 nM 6.92
CHEMBL192099 Ki = 160.0 nM 6.80