Assay Detail

CHEMBL1104796

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Binding

Competitive inhibition of Aurora B ATP binding site

ChEMBL ↗

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Target

Aurora kinase B (CHEMBL2185) ↗

Open DB target context

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Primary target Aurora kinase B

CHEMBL2185

Anchored from Assay target.

Protein identity Aurora kinase B

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

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

Target

Aurora kinase B (CHEMBL2185) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase.

Adams ND, Adams JL, Burgess JL, Chaudhari AM, Copeland RA, Donatelli CA, Drewry DH, Fisher KE, Hamajima T, Hardwicke MA, Huffman WF, Koretke-Brown KK, Lai ZV, McDonald OB, Nakamura H, Newlander KA, Oleykowski CA, Parrish CA, Patrick DR, Plant R, Sarpong MA, Sasaki K, Schmidt SJ, Silva DJ, Sutton D, Tang J, Thompson CS, Tummino PJ, Wang JC, Xiang H, Yang J, Dhanak D.
J Med Chem (2010) 53 : 3973 -4001
PubMed 20420387 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
Ki	2	9.08	9.42
IC50	2	6.76	6.76

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL1090479	GSK-1070916	1.0	1	9.42
CHEMBL572878	TOZASERTIB	2.0	1	8.74
CHEMBL259084	MLN-8054	1.0	1	6.76
CHEMBL415049	BARASERTIB	3.0	1	-

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL1090479	GSK-1070916	Ki	=	0.38	nM	9.42
CHEMBL572878	TOZASERTIB	Ki	=	1.8	nM	8.74
CHEMBL259084	MLN-8054	IC50	=	172.0	nM	6.76
CHEMBL415049	BARASERTIB	IC50	<	1.0	nM	-