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Assay Detail

CHEMBL3379900

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

Binding
Displacement of [125I]IABN from human D3R E90Q mutant expressed in HEK293 cell membranes by gamma counting method
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Design, synthesis, and structure-activity relationship studies of a series of [4-(4-carboxamidobutyl)]-1-arylpiperazines: insights into structural features contributing to dopamine D3 versus D2 receptor subtype selectivity.
Ananthan S, Saini SK, Zhou G, Hobrath JV, Padmalayam I, Zhai L, Bostwick JR, Antonio T, Reith ME, McDowell S, Cho E, McAleer L, Taylor M, Luedtke RR.
J Med Chem (2014) 57 : 7042 -7060
PubMed 25126833 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 7.78 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3323114 1 7.92
CHEMBL3323112 1 7.72
CHEMBL3323011 1 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3323114 Ki = 12.0 nM 7.92
CHEMBL3323112 Ki = 19.0 nM 7.72
CHEMBL3323011 Ki = 20.0 nM 7.70