Assay Detail

CHEMBL1031310

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Binding

Inhibition of Aurora-B by time dependent kinetic study

ChEMBL ↗

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Target

Aurora kinase B (CHEMBL2185) ↗

Open DB target context

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Aurora kinase B (CHEMBL2185) is the working anchor for this assay review. Loading the live Open DB target snapshot…

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	Intermediate

Target

Aurora kinase B (CHEMBL2185) ↗

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	2	8.92	9.10

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL484006	—	—	1	9.10
CHEMBL572878	TOZASERTIB	2.0	1	8.74

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL484006	—	Ki	=	0.8	nM	9.10
CHEMBL572878	TOZASERTIB	Ki	=	1.8	nM	8.74