Assay Detail

CHEMBL3424198

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Binding

Inhibition of human His-tagged TTK (510 to 857)-mediated MBP phosphorylation after 20 mins by scintillation counting analysis in presence of gamma-[32P]ATP

ChEMBL ↗

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Target

Dual specificity protein kinase TTK (CHEMBL3983) ↗

Open DB target context

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Dual specificity protein kinase TTK (CHEMBL3983) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Dual specificity protein kinase TTK

CHEMBL3983

Anchored from Assay target.

Protein identity Dual specificity protein kinase TTK

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

Dual specificity protein kinase TTK (CHEMBL3983) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

The Discovery of Orally Bioavailable Tyrosine Threonine Kinase (TTK) Inhibitors: 3-(4-(heterocyclyl)phenyl)-1H-indazole-5-carboxamides as Anticancer Agents.

Liu Y, Lang Y, Patel NK, Ng G, Laufer R, Li SW, Edwards L, Forrest B, Sampson PB, Feher M, Ban F, Awrey DE, Beletskaya I, Mao G, Hodgson R, Plotnikova O, Qiu W, Chirgadze NY, Mason JM, Wei X, Lin DC, Che Y, Kiarash R, Madeira B, Fletcher GC, Mak TW, Bray MR, Pauls HW.
J Med Chem (2015) 58 : 3366 -3392
PubMed 25763473 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	7.46	7.46

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL2140523	—	—	1	7.46

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL2140523	—	IC50	=	35.0	nM	7.46