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Assay Detail

CHEMBL1073376

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Binding
Inhibition of Aurora-A by microplate scintillation counting
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Aurora kinase A (CHEMBL4722)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Substituted 2-arylbenzothiazoles as kinase inhibitors: hit-to-lead optimization.
Tasler S, Müller O, Wieber T, Herz T, Pegoraro S, Saeb W, Lang M, Krauss R, Totzke F, Zirrgiebel U, Ehlert JE, Kubbutat MH, Schächtele C.
Bioorg Med Chem (2009) 17 : 6728 -6737
PubMed 19692247 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 36 6.71 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL593987 1 8.05
CHEMBL595615 1 7.85
CHEMBL596292 1 7.62
CHEMBL594228 1 7.58
CHEMBL604992 1 7.58
CHEMBL593274 1 7.57
CHEMBL593275 1 7.27
CHEMBL593908 1 7.22
CHEMBL593306 1 7.21
CHEMBL593221 1 7.19
CHEMBL595143 1 7.09
CHEMBL593909 1 7.07
CHEMBL606466 1 7.04
CHEMBL593292 1 6.96
CHEMBL593860 1 6.92
CHEMBL595373 1 6.77
CHEMBL593760 1 6.70
CHEMBL604483 1 6.66
CHEMBL596087 1 6.64
CHEMBL595142 1 6.64
CHEMBL593245 1 6.54
CHEMBL604485 1 6.52
CHEMBL595406 1 6.47
CHEMBL473556 1 6.46
CHEMBL594661 1 6.41
CHEMBL593971 1 6.40
CHEMBL604893 1 6.16
CHEMBL593294 1 6.10
CHEMBL593905 1 5.92
CHEMBL593910 1 5.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL593987 IC50 = 9.0 nM 8.05
CHEMBL595615 IC50 = 14.0 nM 7.85
CHEMBL596292 IC50 = 24.0 nM 7.62
CHEMBL594228 IC50 = 26.0 nM 7.58
CHEMBL604992 IC50 = 26.0 nM 7.58
CHEMBL593274 IC50 = 27.0 nM 7.57
CHEMBL593275 IC50 = 54.0 nM 7.27
CHEMBL593908 IC50 = 60.0 nM 7.22
CHEMBL593306 IC50 = 62.0 nM 7.21
CHEMBL593221 IC50 = 65.0 nM 7.19
CHEMBL595143 IC50 = 82.0 nM 7.09
CHEMBL593909 IC50 = 85.0 nM 7.07
CHEMBL606466 IC50 = 91.0 nM 7.04
CHEMBL593292 IC50 = 110.0 nM 6.96
CHEMBL593860 IC50 = 120.0 nM 6.92
CHEMBL595373 IC50 = 170.0 nM 6.77
CHEMBL593760 IC50 = 200.0 nM 6.70
CHEMBL604483 IC50 = 220.0 nM 6.66
CHEMBL596087 IC50 = 230.0 nM 6.64
CHEMBL595142 IC50 = 230.0 nM 6.64
CHEMBL593245 IC50 = 290.0 nM 6.54
CHEMBL604485 IC50 = 300.0 nM 6.52
CHEMBL595406 IC50 = 340.0 nM 6.47
CHEMBL473556 IC50 = 350.0 nM 6.46
CHEMBL594661 IC50 = 390.0 nM 6.41
CHEMBL593971 IC50 = 400.0 nM 6.40
CHEMBL604893 IC50 = 690.0 nM 6.16
CHEMBL593294 IC50 = 800.0 nM 6.10
CHEMBL593905 IC50 = 1200.0 nM 5.92
CHEMBL593910 IC50 = 1300.0 nM 5.89
CHEMBL593911 IC50 = 1600.0 nM 5.80
CHEMBL593770 IC50 = 3300.0 nM 5.48
CHEMBL514942 IC50 = 4400.0 nM 5.36
CHEMBL595374 IC50 = 9400.0 nM 5.03
CHEMBL596059 IC50 > 10000.0 nM -
CHEMBL593293 IC50 > 10000.0 nM -