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Assay Detail

CHEMBL4349093

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Binding
Inhibition of TTK autophosphorylation in human CAL51 cells by radioimmuno-precipitation assay
3
Total Activities
3
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

Design and Optimization Leading to an Orally Active TTK Protein Kinase Inhibitor with Robust Single Agent Efficacy.
Riggs JR, Elsner J, Cashion D, Robinson D, Tehrani L, Nagy M, Fultz KE, Krishna Narla R, Peng X, Tran T, Kulkarni A, Bahmanyar S, Condroski K, Pagarigan B, Fenalti G, LeBrun L, Leftheris K, Zhu D, Boylan JF.
J Med Chem (2019) 62 : 4401 -4410
PubMed 30998356 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.74 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4546504 1 8.05
CHEMBL4521278 1 7.80
CHEMBL4569626 1 7.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4546504 IC50 = 9.0 nM 8.05
CHEMBL4521278 IC50 = 16.0 nM 7.80
CHEMBL4569626 IC50 = 44.0 nM 7.36