Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL3372149

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

Functional
Antagonist activity against human D3R expressed in CHO cells assessed as inhibition of dopamine-induced [35S]GTPgammaS binding by dopamine potency shift assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
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
IC50 4 8.70 9.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3323016 1 9.48
CHEMBL3323011 1 8.89
CHEMBL3323117 1 7.72
CHEMBL3322994 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3323016 IC50 = 0.33 nM 9.48
CHEMBL3323011 IC50 = 1.3 nM 8.89
CHEMBL3323117 IC50 = 19.0 nM 7.72
CHEMBL3322994 IC50 = 0.0038 nM -