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Assay Detail

CHEMBL1768779

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Binding
Inhibition of aurora A
ChEMBL ↗
46
Total Activities
44
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

Structure-based design of potent and selective 3-phosphoinositide-dependent kinase-1 (PDK1) inhibitors.
Medina JR, Becker CJ, Blackledge CW, Duquenne C, Feng Y, Grant SW, Heerding D, Li WH, Miller WH, Romeril SP, Scherzer D, Shu A, Bobko MA, Chadderton AR, Dumble M, Gardiner CM, Gilbert S, Liu Q, Rabindran SK, Sudakin V, Xiang H, Brady PG, Campobasso N, Ward P, Axten JM.
J Med Chem (2011) 54 : 1871 -1895
PubMed 21341675 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 46 5.72 7.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1765751 — — 1 7.20
CHEMBL1765750 — — 1 6.90
CHEMBL1765876 — — 1 6.70
CHEMBL1765741 — — 1 6.70
CHEMBL1688215 — — 1 6.40
CHEMBL1614777 — — 1 6.40
CHEMBL1614776 — — 2 6.30
CHEMBL1614774 — — 1 5.90
CHEMBL1765746 — — 1 5.90
CHEMBL1765745 — — 1 5.90
CHEMBL1614775 — — 1 5.90
CHEMBL1765758 — — 1 5.80
CHEMBL1765748 — — 1 5.80
CHEMBL1765749 — — 1 5.70
CHEMBL1765761 — — 1 5.70
CHEMBL1614771 — — 1 5.60
CHEMBL1765762 — — 1 5.60
CHEMBL1765757 — — 1 5.50
CHEMBL1765760 — — 1 5.50
CHEMBL1765756 — — 1 5.40
CHEMBL1765739 — — 1 5.30
CHEMBL1765728 — — 1 5.30
CHEMBL1765747 — — 1 5.20
CHEMBL1765759 — — 1 5.20
CHEMBL1765733 — — 1 5.10
CHEMBL1765732 — — 1 5.10
CHEMBL1765742 — — 1 5.10
CHEMBL1765729 — — 1 4.90
CHEMBL1614773 — — 1 4.90
CHEMBL1765740 — — 2 4.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1765751 — IC50 = 63.1 nM 7.20
CHEMBL1765750 — IC50 = 125.89 nM 6.90
CHEMBL1765741 — IC50 = 199.53 nM 6.70
CHEMBL1765876 — IC50 = 199.53 nM 6.70
CHEMBL1614777 — IC50 = 398.11 nM 6.40
CHEMBL1688215 — IC50 = 398.11 nM 6.40
CHEMBL1614776 — IC50 = 501.19 nM 6.30
CHEMBL1614776 — IC50 = 794.33 nM 6.10
CHEMBL1765745 — IC50 = 1258.93 nM 5.90
CHEMBL1765746 — IC50 = 1258.93 nM 5.90
CHEMBL1614775 — IC50 = 1258.93 nM 5.90
CHEMBL1614774 — IC50 = 1258.93 nM 5.90
CHEMBL1765748 — IC50 = 1584.89 nM 5.80
CHEMBL1765758 — IC50 = 1584.89 nM 5.80
CHEMBL1765761 — IC50 = 1995.26 nM 5.70
CHEMBL1765749 — IC50 = 1995.26 nM 5.70
CHEMBL1614771 — IC50 = 2511.89 nM 5.60
CHEMBL1765762 — IC50 = 2511.89 nM 5.60
CHEMBL1765760 — IC50 = 3162.28 nM 5.50
CHEMBL1765757 — IC50 = 3162.28 nM 5.50
CHEMBL1765756 — IC50 = 3981.07 nM 5.40
CHEMBL1765739 — IC50 = 5011.87 nM 5.30
CHEMBL1765728 — IC50 = 5011.87 nM 5.30
CHEMBL1765747 — IC50 = 6309.57 nM 5.20
CHEMBL1765759 — IC50 = 6309.57 nM 5.20
CHEMBL1765742 — IC50 = 7943.28 nM 5.10
CHEMBL1765733 — IC50 = 7943.28 nM 5.10
CHEMBL1765732 — IC50 = 7943.28 nM 5.10
CHEMBL1765729 — IC50 = 12589.25 nM 4.90
CHEMBL1614773 — IC50 = 12589.25 nM 4.90
CHEMBL1765740 — IC50 = 39810.0 nM 4.40
CHEMBL1765727 — IC50 > 10000.0 nM -
CHEMBL1765879 — IC50 > 10000.0 nM -
CHEMBL1765878 — IC50 > 10000.0 nM -
CHEMBL1614772 — IC50 > 10000.0 nM -
CHEMBL1765877 — IC50 > 10000.0 nM -
CHEMBL1765730 — IC50 > 10000.0 nM -
CHEMBL1765731 — IC50 > 10000.0 nM -
CHEMBL1765734 — IC50 > 10000.0 nM -
CHEMBL1765735 — IC50 > 10000.0 nM -
CHEMBL1765736 — IC50 > 10000.0 nM -
CHEMBL1765737 — IC50 > 10000.0 nM -
CHEMBL1765738 — IC50 > 10000.0 nM -
CHEMBL1765740 — IC50 > 10000.0 nM -
CHEMBL1765743 — IC50 > 10000.0 nM -
CHEMBL1765744 — IC50 > 10000.0 nM -