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Assay Detail

CHEMBL5037539

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

Binding
Displacement of kinase tracer 236 from TTK (unknown origin) by LanthaScreen Eu kinase binding assay
17
Total Activities
17
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

Structure-Guided Optimization Provides a Series of TTK Protein Inhibitors with Potent Antitumor Activity.
Elsner J, Cashion D, Robinson D, Bahmanyar S, Tehrani L, Fultz KE, Narla RK, Peng X, Tran T, Apuy J, LeBrun L, Leftheris K, Boylan JF, Zhu D, Riggs JR.
J Med Chem (2021) 64 : 12670 -12679
PubMed 34459599 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 8.51 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5093015 1 9.00
CHEMBL5092826 1 9.00
CHEMBL5081270 1 8.70
CHEMBL5075313 1 8.70
CHEMBL5073101 1 8.70
CHEMBL5077668 1 8.70
CHEMBL5081668 1 8.55
CHEMBL5084062 1 8.52
CHEMBL5091689 1 8.52
CHEMBL5085753 1 8.52
CHEMBL5085278 1 8.40
CHEMBL5086022 1 8.40
CHEMBL5079606 1 8.28
CHEMBL5085182 1 8.25
CHEMBL5086435 1 8.22
CHEMBL5077627 1 8.12
CHEMBL5087340 1 8.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5093015 IC50 = 1.0 nM 9.00
CHEMBL5092826 IC50 = 1.0 nM 9.00
CHEMBL5081270 IC50 = 2.0 nM 8.70
CHEMBL5075313 IC50 = 2.0 nM 8.70
CHEMBL5073101 IC50 = 2.0 nM 8.70
CHEMBL5077668 IC50 = 2.0 nM 8.70
CHEMBL5081668 IC50 = 2.8 nM 8.55
CHEMBL5084062 IC50 = 3.0 nM 8.52
CHEMBL5091689 IC50 = 3.0 nM 8.52
CHEMBL5085753 IC50 = 3.0 nM 8.52
CHEMBL5085278 IC50 = 4.0 nM 8.40
CHEMBL5086022 IC50 = 4.0 nM 8.40
CHEMBL5079606 IC50 = 5.3 nM 8.28
CHEMBL5085182 IC50 = 5.6 nM 8.25
CHEMBL5086435 IC50 = 6.0 nM 8.22
CHEMBL5077627 IC50 = 7.5 nM 8.12
CHEMBL5087340 IC50 = 9.0 nM 8.05