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Assay Detail

CHEMBL3379351

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

Binding
Displacement of [125I]IABN from human D2LR expressed in HEK293 cell membranes by gamma counting method
34
Total Activities
34
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(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
Ki 34 6.19 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3322994 1 7.92
CHEMBL3322993 1 7.72
CHEMBL3322995 1 6.79
CHEMBL3322992 1 6.75
CHEMBL3323010 1 6.72
CHEMBL3322996 1 6.72
CHEMBL3323114 1 6.53
CHEMBL3323112 1 6.52
CHEMBL3323013 1 6.47
CHEMBL3323116 1 6.47
CHEMBL3323009 1 6.44
CHEMBL3323008 1 6.44
CHEMBL3323015 1 6.36
CHEMBL3323016 1 6.35
CHEMBL3323018 1 6.32
CHEMBL3323011 1 6.29
CHEMBL3323019 1 6.28
CHEMBL3322998 1 6.24
CHEMBL3323017 1 6.18
CHEMBL3323014 1 6.17
CHEMBL3323115 1 6.09
CHEMBL3323012 1 6.04
CHEMBL3323113 1 6.03
CHEMBL3323003 1 5.95
CHEMBL3322997 1 5.88
CHEMBL3323004 1 5.84
CHEMBL3323117 1 5.82
CHEMBL3323002 1 5.81
CHEMBL3323001 1 5.72
CHEMBL3323006 1 5.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3322994 Ki = 12.0 nM 7.92
CHEMBL3322993 Ki = 19.0 nM 7.72
CHEMBL3322995 Ki = 162.0 nM 6.79
CHEMBL3322992 Ki = 178.0 nM 6.75
CHEMBL3323010 Ki = 191.0 nM 6.72
CHEMBL3322996 Ki = 191.0 nM 6.72
CHEMBL3323114 Ki = 298.0 nM 6.53
CHEMBL3323112 Ki = 301.0 nM 6.52
CHEMBL3323013 Ki = 336.0 nM 6.47
CHEMBL3323116 Ki = 337.0 nM 6.47
CHEMBL3323009 Ki = 361.0 nM 6.44
CHEMBL3323008 Ki = 366.0 nM 6.44
CHEMBL3323015 Ki = 436.0 nM 6.36
CHEMBL3323016 Ki = 450.0 nM 6.35
CHEMBL3323018 Ki = 481.0 nM 6.32
CHEMBL3323011 Ki = 511.0 nM 6.29
CHEMBL3323019 Ki = 527.0 nM 6.28
CHEMBL3322998 Ki = 572.0 nM 6.24
CHEMBL3323017 Ki = 655.0 nM 6.18
CHEMBL3323014 Ki = 683.0 nM 6.17
CHEMBL3323115 Ki = 809.0 nM 6.09
CHEMBL3323012 Ki = 913.0 nM 6.04
CHEMBL3323113 Ki = 934.0 nM 6.03
CHEMBL3323003 Ki = 1133.0 nM 5.95
CHEMBL3322997 Ki = 1303.0 nM 5.88
CHEMBL3323004 Ki = 1452.0 nM 5.84
CHEMBL3323117 Ki = 1510.0 nM 5.82
CHEMBL3323002 Ki = 1563.0 nM 5.81
CHEMBL3323001 Ki = 1883.0 nM 5.72
CHEMBL3323006 Ki = 3646.0 nM 5.44
CHEMBL3323007 Ki = 4604.0 nM 5.34
CHEMBL3323000 Ki = 4983.0 nM 5.30
CHEMBL3322999 Ki = 13567.0 nM 4.87
CHEMBL3323005 Ki = 24938.0 nM 4.60