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Assay Detail

CHEMBL4349113

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

Binding
Inhibition of recombinant human GST-tagged LTK cytoplasmic domain (450 to 864 residues) expressed in baculovirus expression system by Z'-LYTE assay
1
Total Activities
1
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

Leukocyte tyrosine kinase receptor (CHEMBL5627)
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 1 9.25 9.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4546504 1 9.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4546504 IC50 = 0.567 nM 9.25