Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL3370374

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

Binding
Inhibition of SUMO-tagged human TTK (1-275 residues) compound pre-incubated for 15 mins prior ATP addition by MBP-based assay
56
Total Activities
56
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 56 6.92 8.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3330410 1 8.54
CHEMBL3330260 1 8.46
CHEMBL3330409 1 8.44
CHEMBL3330282 1 8.40
CHEMBL3330407 1 8.05
CHEMBL3330408 1 8.00
CHEMBL3330405 1 7.96
CHEMBL3329232 1 7.92
CHEMBL3330404 1 7.85
CHEMBL3330406 1 7.82
CHEMBL3330281 1 7.80
CHEMBL3330256 1 7.80
CHEMBL3330274 1 7.77
CHEMBL3330272 1 7.75
CHEMBL3330279 1 7.62
CHEMBL3330273 1 7.60
CHEMBL3330401 1 7.58
CHEMBL3330402 1 7.58
CHEMBL3330403 1 7.52
CHEMBL3330265 1 7.48
CHEMBL3330278 1 7.46
CHEMBL3330255 1 7.41
CHEMBL3330280 1 7.34
CHEMBL3330285 1 7.33
CHEMBL3330283 1 7.28
CHEMBL3330276 1 7.24
CHEMBL3330284 1 7.21
CHEMBL3330275 1 7.10
CHEMBL3330270 1 7.05
CHEMBL3330264 1 7.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3330410 IC50 = 2.9 nM 8.54
CHEMBL3330260 IC50 = 3.5 nM 8.46
CHEMBL3330409 IC50 = 3.6 nM 8.44
CHEMBL3330282 IC50 = 4.0 nM 8.40
CHEMBL3330407 IC50 = 8.9 nM 8.05
CHEMBL3330408 IC50 = 10.0 nM 8.00
CHEMBL3330405 IC50 = 11.0 nM 7.96
CHEMBL3329232 IC50 = 12.0 nM 7.92
CHEMBL3330404 IC50 = 14.0 nM 7.85
CHEMBL3330406 IC50 = 15.0 nM 7.82
CHEMBL3330281 IC50 = 16.0 nM 7.80
CHEMBL3330256 IC50 = 16.0 nM 7.80
CHEMBL3330274 IC50 = 17.0 nM 7.77
CHEMBL3330272 IC50 = 18.0 nM 7.75
CHEMBL3330279 IC50 = 24.0 nM 7.62
CHEMBL3330273 IC50 = 25.0 nM 7.60
CHEMBL3330401 IC50 = 26.0 nM 7.58
CHEMBL3330402 IC50 = 26.0 nM 7.58
CHEMBL3330403 IC50 = 30.0 nM 7.52
CHEMBL3330265 IC50 = 33.0 nM 7.48
CHEMBL3330278 IC50 = 35.0 nM 7.46
CHEMBL3330255 IC50 = 39.0 nM 7.41
CHEMBL3330280 IC50 = 46.0 nM 7.34
CHEMBL3330285 IC50 = 47.0 nM 7.33
CHEMBL3330283 IC50 = 53.0 nM 7.28
CHEMBL3330276 IC50 = 58.0 nM 7.24
CHEMBL3330284 IC50 = 61.0 nM 7.21
CHEMBL3330275 IC50 = 80.0 nM 7.10
CHEMBL3330270 IC50 = 90.0 nM 7.05
CHEMBL3330264 IC50 = 90.0 nM 7.05
CHEMBL3330266 IC50 = 250.0 nM 6.60
CHEMBL3330250 IC50 = 280.0 nM 6.55
CHEMBL3330277 IC50 = 310.0 nM 6.51
CHEMBL3330258 IC50 = 330.0 nM 6.48
CHEMBL3330257 IC50 = 340.0 nM 6.47
CHEMBL3330271 IC50 = 340.0 nM 6.47
CHEMBL3330254 IC50 = 380.0 nM 6.42
CHEMBL3330259 IC50 = 390.0 nM 6.41
CHEMBL3330267 IC50 = 550.0 nM 6.26
CHEMBL3330253 IC50 = 580.0 nM 6.24
CHEMBL3330247 IC50 = 600.0 nM 6.22
CHEMBL3330248 IC50 = 640.0 nM 6.19
CHEMBL3330262 IC50 = 710.0 nM 6.15
CHEMBL3330269 IC50 = 980.0 nM 6.01
CHEMBL3330243 IC50 = 1400.0 nM 5.85
CHEMBL3330238 IC50 = 1600.0 nM 5.80
CHEMBL3330239 IC50 = 1900.0 nM 5.72
CHEMBL3330246 IC50 = 2300.0 nM 5.64
CHEMBL3330263 IC50 = 2600.0 nM 5.58
CHEMBL3330251 IC50 = 4300.0 nM 5.37