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Assay Detail

CHEMBL3379904

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

Binding
Antagonist activity against human D2R expressed in CHO cells assessed as inhibition of quinpirole-induced mitogenesis after 24 hrs by [3H]thymidine uptake assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

D(2) dopamine receptor (CHEMBL217)
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 9 6.54 7.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3322993 1 7.58
CHEMBL3322994 1 7.26
CHEMBL3323015 1 6.69
CHEMBL3323016 1 6.38
CHEMBL3323013 1 6.31
CHEMBL3323017 1 5.94
CHEMBL3323011 1 5.64
CHEMBL3322998 1 -
CHEMBL3323003 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3322993 IC50 = 26.0 nM 7.58
CHEMBL3322994 IC50 = 55.0 nM 7.26
CHEMBL3323015 IC50 = 205.0 nM 6.69
CHEMBL3323016 IC50 = 420.0 nM 6.38
CHEMBL3323013 IC50 = 490.0 nM 6.31
CHEMBL3323017 IC50 = 1160.0 nM 5.94
CHEMBL3323011 IC50 = 2300.0 nM 5.64
CHEMBL3322998 IC50 - -
CHEMBL3323003 IC50 - -