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Assay Detail

CHEMBL993739

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Binding
Inhibition of aurora B kinase
40
Total Activities
40
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Aurora kinase B (CHEMBL2185)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and development of aurora kinase inhibitors as anticancer agents.
Pollard JR, Mortimore M.
J Med Chem (2009) 52 : 2629 -2651
PubMed 19320489 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 37 7.46 9.00
Ki 3 7.66 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL215275 1 9.00
CHEMBL381724 1 9.00
CHEMBL216769 1 8.70
CHEMBL217804 1 8.70
CHEMBL495727 AT-9283 2.0 1 8.52
CHEMBL201307 1 8.15
CHEMBL215322 1 8.12
CHEMBL484951 1 8.10
CHEMBL485186 1 8.02
CHEMBL484006 1 7.96
CHEMBL472193 1 7.85
CHEMBL482778 1 7.85
CHEMBL482779 1 7.75
CHEMBL572878 TOZASERTIB 2.0 1 7.75
CHEMBL482967 CYC-116 1.0 1 7.72
CHEMBL484609 1 7.70
CHEMBL485351 1 7.60
CHEMBL484950 1 7.57
CHEMBL482774 1 7.38
CHEMBL385872 1 7.32
CHEMBL485337 1 7.24
CHEMBL402548 DANUSERTIB 2.0 1 7.10
CHEMBL427787 1 7.00
CHEMBL472202 1 6.92
CHEMBL202721 1 6.89
CHEMBL259084 MLN-8054 1.0 1 6.76
CHEMBL514409 HESPERADIN 1 6.60
CHEMBL482968 ENMD-2076 2.0 1 6.54
CHEMBL385266 1 6.52
CHEMBL484601 1 6.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL215275 IC50 = 1.0 nM 9.00
CHEMBL381724 IC50 = 1.0 nM 9.00
CHEMBL217804 IC50 = 2.0 nM 8.70
CHEMBL216769 IC50 = 2.0 nM 8.70
CHEMBL495727 AT-9283 IC50 = 3.0 nM 8.52
CHEMBL201307 IC50 = 7.0 nM 8.15
CHEMBL215322 IC50 = 7.5 nM 8.12
CHEMBL484951 IC50 = 8.0 nM 8.10
CHEMBL485186 IC50 = 9.5 nM 8.02
CHEMBL484006 IC50 = 11.0 nM 7.96
CHEMBL482778 IC50 = 14.0 nM 7.85
CHEMBL472193 IC50 = 14.0 nM 7.85
CHEMBL482779 IC50 = 18.0 nM 7.75
CHEMBL572878 TOZASERTIB Ki = 18.0 nM 7.75
CHEMBL482967 CYC-116 IC50 = 19.0 nM 7.72
CHEMBL484609 IC50 = 20.0 nM 7.70
CHEMBL485351 IC50 = 25.0 nM 7.60
CHEMBL484950 Ki = 27.0 nM 7.57
CHEMBL482774 IC50 = 42.0 nM 7.38
CHEMBL385872 IC50 = 48.0 nM 7.32
CHEMBL485337 IC50 = 57.0 nM 7.24
CHEMBL402548 DANUSERTIB IC50 = 79.0 nM 7.10
CHEMBL427787 IC50 = 99.0 nM 7.00
CHEMBL472202 IC50 = 120.0 nM 6.92
CHEMBL202721 IC50 = 130.0 nM 6.89
CHEMBL259084 MLN-8054 IC50 = 172.0 nM 6.76
CHEMBL514409 HESPERADIN IC50 = 250.0 nM 6.60
CHEMBL482968 ENMD-2076 IC50 = 290.0 nM 6.54
CHEMBL385266 IC50 = 300.0 nM 6.52
CHEMBL484601 IC50 = 530.0 nM 6.28
CHEMBL384575 IC50 = 630.0 nM 6.20
CHEMBL483158 ALISERTIB IC50 = 1100.0 nM 5.96
CHEMBL217748 IC50 = 1210.0 nM 5.92
CHEMBL518981 IC50 < 1.0 nM -
CHEMBL190252 IC50 - -
CHEMBL359482 Ki - -
CHEMBL214848 IC50 < 1.0 nM -
CHEMBL214849 IC50 < 1.0 nM -
CHEMBL216053 IC50 < 1.0 nM -
CHEMBL215152 DEFOSBARASERTIB IC50 < 1.0 nM -