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Assay Detail

CHEMBL1031294

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Binding
Inhibition of Aurora-A by coupled assay
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

The discovery of the potent aurora inhibitor MK-0457 (VX-680).
Bebbington D, Binch H, Charrier JD, Everitt S, Fraysse D, Golec J, Kay D, Knegtel R, Mak C, Mazzei F, Miller A, Mortimore M, O'Donnell M, Patel S, Pierard F, Pinder J, Pollard J, Ramaya S, Robinson D, Rutherford A, Studley J, Westcott J.
Bioorg Med Chem Lett (2009) 19 : 3586 -3592
PubMed 19447622 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 43 8.23 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL572878 TOZASERTIB 2.0 1 9.22
CHEMBL564941 1 9.00
CHEMBL559900 1 9.00
CHEMBL484006 1 8.89
CHEMBL484609 1 8.80
CHEMBL484951 1 8.80
CHEMBL482778 1 8.77
CHEMBL551633 1 8.70
CHEMBL552033 1 8.70
CHEMBL552385 1 8.70
CHEMBL563682 1 8.62
CHEMBL557279 1 8.62
CHEMBL564459 1 8.52
CHEMBL482779 1 8.43
CHEMBL557682 1 8.41
CHEMBL561617 1 8.41
CHEMBL484950 1 8.40
CHEMBL562416 1 8.40
CHEMBL561834 1 8.30
CHEMBL562415 1 8.30
CHEMBL560556 1 8.29
CHEMBL562157 1 8.22
CHEMBL556460 1 8.05
CHEMBL552500 1 8.05
CHEMBL565183 1 8.00
CHEMBL564290 1 7.77
CHEMBL550825 1 7.77
CHEMBL562497 1 7.75
CHEMBL549322 1 7.70
CHEMBL560158 1 7.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL572878 TOZASERTIB Ki = 0.6 nM 9.22
CHEMBL564941 Ki = 1.0 nM 9.00
CHEMBL559900 Ki = 1.0 nM 9.00
CHEMBL484006 Ki = 1.3 nM 8.89
CHEMBL484609 Ki = 1.6 nM 8.80
CHEMBL484951 Ki = 1.6 nM 8.80
CHEMBL482778 Ki = 1.7 nM 8.77
CHEMBL551633 Ki = 2.0 nM 8.70
CHEMBL552033 Ki = 2.0 nM 8.70
CHEMBL552385 Ki = 2.0 nM 8.70
CHEMBL563682 Ki = 2.4 nM 8.62
CHEMBL557279 Ki = 2.4 nM 8.62
CHEMBL564459 Ki = 3.0 nM 8.52
CHEMBL482779 Ki = 3.7 nM 8.43
CHEMBL561617 Ki = 3.9 nM 8.41
CHEMBL557682 Ki = 3.9 nM 8.41
CHEMBL484950 Ki = 4.0 nM 8.40
CHEMBL562416 Ki = 4.0 nM 8.40
CHEMBL561834 Ki = 5.0 nM 8.30
CHEMBL562415 Ki = 5.0 nM 8.30
CHEMBL560556 Ki = 5.1 nM 8.29
CHEMBL562157 Ki = 6.0 nM 8.22
CHEMBL552500 Ki = 9.0 nM 8.05
CHEMBL556460 Ki = 9.0 nM 8.05
CHEMBL565183 Ki = 10.0 nM 8.00
CHEMBL564290 Ki = 17.0 nM 7.77
CHEMBL550825 Ki = 17.0 nM 7.77
CHEMBL562497 Ki = 18.0 nM 7.75
CHEMBL549322 Ki = 20.0 nM 7.70
CHEMBL560158 Ki = 24.0 nM 7.62
CHEMBL552038 Ki = 24.0 nM 7.62
CHEMBL551634 Ki = 24.0 nM 7.62
CHEMBL565205 Ki = 36.0 nM 7.44
CHEMBL359482 Ki = 58.0 nM 7.24
CHEMBL549536 Ki = 81.0 nM 7.09
CHEMBL549469 Ki = 86.0 nM 7.07
CHEMBL560630 Ki < 3.0 nM -
CHEMBL554941 Ki < 1.0 nM -
CHEMBL561421 Ki < 1.0 nM -
CHEMBL564449 Ki < 1.0 nM -
CHEMBL485351 Ki < 1.0 nM -
CHEMBL485186 Ki < 1.0 nM -
CHEMBL549668 Ki < 1.0 nM -