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Assay Detail

CHEMBL1073807

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Binding
Binding affinity to dopamine D1 receptor
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

D(1A) dopamine receptor (CHEMBL2056)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of new SCH 39166 analogs as potent and selective dopamine D1 receptor antagonists.
Qiang L, Sasikumar TK, Burnett DA, Su J, Tang H, Ye Y, Mazzola RD, Zhu Z, McKittrick BA, Greenlee WJ, Fawzi A, Smith M, Zhang H, Lachowicz JE.
Bioorg Med Chem Lett (2010) 20 : 836 -840
PubMed 20061148 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 8.66 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL596824 1 9.70
CHEMBL599282 1 9.30
CHEMBL603901 1 9.30
CHEMBL597909 1 9.30
CHEMBL599487 1 9.22
CHEMBL599977 1 9.15
CHEMBL600986 1 9.15
CHEMBL597702 1 9.15
CHEMBL596622 1 9.05
CHEMBL298406 ECOPIPAM 3.0 1 8.92
CHEMBL62 SCH-23390 1 8.85
CHEMBL603485 1 8.85
CHEMBL600987 1 8.82
CHEMBL604108 1 8.70
CHEMBL598516 1 8.64
CHEMBL601634 1 8.64
CHEMBL604132 1 8.62
CHEMBL591685 1 8.55
CHEMBL604135 1 8.33
CHEMBL602659 1 8.24
CHEMBL602052 1 8.24
CHEMBL598515 1 8.15
CHEMBL604129 1 8.15
CHEMBL601635 1 6.82
CHEMBL600998 1 6.65

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL596824 Ki = 0.2 nM 9.70
CHEMBL599282 Ki = 0.5 nM 9.30
CHEMBL603901 Ki = 0.5 nM 9.30
CHEMBL597909 Ki = 0.5 nM 9.30
CHEMBL599487 Ki = 0.6 nM 9.22
CHEMBL599977 Ki = 0.7 nM 9.15
CHEMBL600986 Ki = 0.7 nM 9.15
CHEMBL597702 Ki = 0.7 nM 9.15
CHEMBL596622 Ki = 0.9 nM 9.05
CHEMBL298406 ECOPIPAM Ki = 1.2 nM 8.92
CHEMBL62 SCH-23390 Ki = 1.4 nM 8.85
CHEMBL603485 Ki = 1.4 nM 8.85
CHEMBL600987 Ki = 1.5 nM 8.82
CHEMBL604108 Ki = 2.0 nM 8.70
CHEMBL598516 Ki = 2.3 nM 8.64
CHEMBL601634 Ki = 2.3 nM 8.64
CHEMBL604132 Ki = 2.4 nM 8.62
CHEMBL591685 Ki = 2.8 nM 8.55
CHEMBL604135 Ki = 4.7 nM 8.33
CHEMBL602659 Ki = 5.7 nM 8.24
CHEMBL602052 Ki = 5.8 nM 8.24
CHEMBL598515 Ki = 7.0 nM 8.15
CHEMBL604129 Ki = 7.1 nM 8.15
CHEMBL601635 Ki = 152.0 nM 6.82
CHEMBL600998 Ki = 225.0 nM 6.65