Assay Detail

CHEMBL5707494

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Binding

Binding affinity to wild-type dog CENP-E assessed as inhibition constant

ChEMBL ↗

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Target

Centromere protein E (CHEMBL6066827) ↗

Open DB target context

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Centromere protein E (CHEMBL6066827) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Centromere protein E

CHEMBL6066827

Anchored from Assay target.

Protein identity Centromere protein E

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	Canis lupus familiaris
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Centromere protein E (CHEMBL6066827) ↗

Type	SINGLE PROTEIN
Organism	Canis lupus familiaris

Publication

Antitumor activity of an allosteric inhibitor of centromere-associated protein-E.

Wood KW, Lad L, Luo L, Qian X, Knight SD, Nevins N, Brejc K, Sutton D, Gilmartin AG, Chua PR, Desai R, Schauer SP, McNulty DE, Annan RS, Belmont LD, Garcia C, Lee Y, Diamond MA, Faucette LF, Giardiniere M, Zhang S, Sun CM, Vidal JD, Lichtsteiner S, Cornwell WD, Greshock JD, Wooster RF, Finer JT, Copeland RA, Huang PS, Morgans DJ, Dhanak D, Bergnes G, Sakowicz R, Jackson JR.
Proc Natl Acad Sci U S A (2010) 107 : 5839 -5844
PubMed 20167803 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
Ki	2	8.71	8.80

Assay Parameters

Parameter	Type	Value	Units	Text
EFO_ID	EFO_ID	-	—	MONDO:0004992
EFO_TERM	EFO_TERM	-	—	cancer

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL4303470	GSK-923295A	1.0	1	8.80
CHEMBL5712065	—	—	1	8.62

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL4303470	GSK-923295A	Ki	=	1.6	nM	8.80
CHEMBL5712065	—	Ki	=	2.4	nM	8.62