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Assay Detail

CHEMBL3423895

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Binding
Inhibition of amino terminal GST-fused full length human TTK using His6-SUMO-TTK-N as substrate preincubated for 15 mins prior to ATP addition by indirect ELISA detection system
ChEMBL ↗
56
Total Activities
53
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

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 56 8.30 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3422095 — — 1 8.96
CHEMBL3422080 — — 1 8.96
CHEMBL3422086 — — 1 8.92
CHEMBL3422091 — — 2 8.92
CHEMBL3422084 — — 1 8.85
CHEMBL3422099 — — 1 8.82
CHEMBL3422097 — — 1 8.77
CHEMBL3422093 — — 2 8.74
CHEMBL3422063 — — 1 8.72
CHEMBL3422083 — — 1 8.70
CHEMBL3422085 — — 1 8.70
CHEMBL3422102 — — 1 8.66
CHEMBL3422077 — — 1 8.60
CHEMBL3422062 — — 1 8.59
CHEMBL3422098 — — 1 8.57
CHEMBL3422053 — — 1 8.57
CHEMBL3422069 — — 1 8.57
CHEMBL3422092 — — 2 8.57
CHEMBL3422075 — — 1 8.55
CHEMBL3422090 — — 1 8.55
CHEMBL3330410 — — 1 8.54
CHEMBL3422058 — — 1 8.52
CHEMBL3422078 — — 1 8.52
CHEMBL3422096 — — 1 8.41
CHEMBL3422071 — — 1 8.40
CHEMBL3422101 — — 1 8.40
CHEMBL3422074 — — 1 8.39
CHEMBL3422094 — — 1 8.39
CHEMBL3422081 — — 1 8.36
CHEMBL3422087 — — 1 8.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3422095 — IC50 = 1.1 nM 8.96
CHEMBL3422080 — IC50 = 1.1 nM 8.96
CHEMBL3422086 — IC50 = 1.2 nM 8.92
CHEMBL3422091 — IC50 = 1.2 nM 8.92
CHEMBL3422084 — IC50 = 1.4 nM 8.85
CHEMBL3422099 — IC50 = 1.5 nM 8.82
CHEMBL3422091 — IC50 = 1.6 nM 8.80
CHEMBL3422097 — IC50 = 1.7 nM 8.77
CHEMBL3422093 — IC50 = 1.8 nM 8.74
CHEMBL3422063 — IC50 = 1.9 nM 8.72
CHEMBL3422083 — IC50 = 2.0 nM 8.70
CHEMBL3422085 — IC50 = 2.0 nM 8.70
CHEMBL3422102 — IC50 = 2.2 nM 8.66
CHEMBL3422077 — IC50 = 2.5 nM 8.60
CHEMBL3422062 — IC50 = 2.6 nM 8.59
CHEMBL3422092 — IC50 = 2.7 nM 8.57
CHEMBL3422098 — IC50 = 2.7 nM 8.57
CHEMBL3422069 — IC50 = 2.7 nM 8.57
CHEMBL3422053 — IC50 = 2.7 nM 8.57
CHEMBL3422090 — IC50 = 2.8 nM 8.55
CHEMBL3422075 — IC50 = 2.8 nM 8.55
CHEMBL3330410 — IC50 = 2.9 nM 8.54
CHEMBL3422058 — IC50 = 3.0 nM 8.52
CHEMBL3422078 — IC50 = 3.0 nM 8.52
CHEMBL3422092 — IC50 = 3.1 nM 8.51
CHEMBL3422096 — IC50 = 3.9 nM 8.41
CHEMBL3422101 — IC50 = 4.0 nM 8.40
CHEMBL3422071 — IC50 = 4.0 nM 8.40
CHEMBL3422074 — IC50 = 4.1 nM 8.39
CHEMBL3422094 — IC50 = 4.1 nM 8.39
CHEMBL3422093 — IC50 = 4.3 nM 8.37
CHEMBL3422081 — IC50 = 4.4 nM 8.36
CHEMBL3422087 — IC50 = 4.6 nM 8.34
CHEMBL3422082 — IC50 = 4.8 nM 8.32
CHEMBL3422054 — IC50 = 5.9 nM 8.23
CHEMBL3422089 — IC50 = 6.0 nM 8.22
CHEMBL3422076 — IC50 = 7.3 nM 8.14
CHEMBL3422056 — IC50 = 7.4 nM 8.13
CHEMBL3422060 — IC50 = 7.6 nM 8.12
CHEMBL3422067 — IC50 = 7.7 nM 8.11
CHEMBL3422068 — IC50 = 8.0 nM 8.10
CHEMBL3422088 — IC50 = 8.3 nM 8.08
CHEMBL3422073 — IC50 = 9.4 nM 8.03
CHEMBL3422070 — IC50 = 10.0 nM 8.00
CHEMBL3422057 — IC50 = 11.0 nM 7.96
CHEMBL3422066 — IC50 = 12.0 nM 7.92
CHEMBL3422059 — IC50 = 13.0 nM 7.89
CHEMBL3422100 — IC50 = 14.0 nM 7.85
CHEMBL3330281 — IC50 = 16.0 nM 7.80
CHEMBL3422072 — IC50 = 16.0 nM 7.80