Assay Detail

CHEMBL3424199

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Binding

Inhibition of human TTK-mediated MAD1/MAD2 complex phosphorylation after 1 hr by scintillation counting analysis in presence of gamma-[32P]ATP

ChEMBL ↗

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Target

Dual specificity protein kinase TTK (CHEMBL3983) ↗

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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	8.55	8.55

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL188343	REVERSINE	—	1	8.55

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL188343	REVERSINE	IC50	=	2.8	nM	8.55