Assay Detail

CHEMBL3395867

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Binding

Inhibition of aurora A (unknown origin)

ChEMBL ↗

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Target

Aurora kinase A (CHEMBL4722) ↗

Open DB target context

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Aurora kinase A (CHEMBL4722) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Aurora kinase A

CHEMBL4722

Anchored from Assay target.

Protein identity Aurora kinase A

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
Organism	Homo sapiens
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Aurora kinase A (CHEMBL4722) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

SAR156497, an exquisitely selective inhibitor of aurora kinases.

Carry JC, Clerc F, Minoux H, Schio L, Mauger J, Nair A, Parmantier E, Le Moigne R, Delorme C, Nicolas JP, Krick A, Abécassis PY, Crocq-Stuerga V, Pouzieux S, Delarbre L, Maignan S, Bertrand T, Bjergarde K, Ma N, Lachaud S, Guizani H, Lebel R, Doerflinger G, Monget S, Perron S, Gasse F, Angouillant-Boniface O, Filoche-Rommé B, Murer M, Gontier S, Prévost C, Monteiro ML, Combeau C.
J Med Chem (2015) 58 : 362 -375
PubMed 25369539 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	4	8.47	9.15

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL572878	TOZASERTIB	2.0	1	9.15
CHEMBL483158	ALISERTIB	3.0	1	9.00
CHEMBL402548	DANUSERTIB	2.0	1	7.89
CHEMBL482968	ENMD-2076	2.0	1	7.85

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL572878	TOZASERTIB	IC50	=	0.7	nM	9.15
CHEMBL483158	ALISERTIB	IC50	=	1.0	nM	9.00
CHEMBL402548	DANUSERTIB	IC50	=	13.0	nM	7.89
CHEMBL482968	ENMD-2076	IC50	=	14.0	nM	7.85