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Assay Detail

CHEMBL3370373

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of GST-fused full length human TTK compound pre-incubated for 15 mins prior ATP addition by MBP-based assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
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

Discovery of inhibitors of the mitotic kinase TTK based on N-(3-(3-sulfamoylphenyl)-1H-indazol-5-yl)-acetamides and carboxamides.
Laufer R, Ng G, Liu Y, Patel NK, Edwards LG, Lang Y, Li SW, Feher M, Awrey DE, Leung G, Beletskaya I, Plotnikova O, Mason JM, Hodgson R, Wei X, Mao G, Luo X, Huang P, Green E, Kiarash R, Lin DC, Harris-Brandts M, Ban F, Nadeem V, Mak TW, Pan GJ, Qiu W, Chirgadze NY, Pauls HW.
Bioorg Med Chem (2014) 22 : 4968 -4997
PubMed 25043312 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.02 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2047943 1 8.74
CHEMBL2380586 1 8.00
CHEMBL2140523 1 7.46
CHEMBL3330411 1 6.43
CHEMBL3330239 1 5.75
CHEMBL1725279 SP-600125 1 5.60
CHEMBL3330238 1 5.58
CHEMBL3330412 1 5.30
CHEMBL3330413 1 4.92
CHEMBL315708 1 4.92
CHEMBL3330241 1 4.77
CHEMBL3330240 1 4.75
CHEMBL3330242 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2047943 IC50 = 1.8 nM 8.74
CHEMBL2380586 IC50 = 10.0 nM 8.00
CHEMBL2140523 IC50 = 35.0 nM 7.46
CHEMBL3330411 IC50 = 370.0 nM 6.43
CHEMBL3330239 IC50 = 1800.0 nM 5.75
CHEMBL1725279 SP-600125 IC50 = 2500.0 nM 5.60
CHEMBL3330238 IC50 = 2600.0 nM 5.58
CHEMBL3330412 IC50 = 5000.0 nM 5.30
CHEMBL3330413 IC50 = 12000.0 nM 4.92
CHEMBL315708 IC50 = 12000.0 nM 4.92
CHEMBL3330241 IC50 = 17000.0 nM 4.77
CHEMBL3330240 IC50 = 18000.0 nM 4.75
CHEMBL3330242 IC50 > 50000.0 nM -