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Assay Detail

CHEMBL3096274

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

Binding
Inhibition of full-length Mps1 kinase (unknown origin)
19
Total Activities
19
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

Novel Mps1 kinase inhibitors: from purine to pyrrolopyrimidine and quinazoline leads.
Bursavich MG, Dastrup D, Shenderovich M, Yager KM, Cimbora DM, Williams B, Kumar DV.
Bioorg Med Chem Lett (2013) 23 : 6829 -6833
PubMed 24183538 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.94 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2047959 1 8.70
CHEMBL3092039 1 8.70
CHEMBL3092037 1 8.30
CHEMBL2047943 1 8.30
CHEMBL3092038 1 8.10
CHEMBL3092036 1 8.05
CHEMBL3092035 1 7.92
CHEMBL3092030 1 7.70
CHEMBL3092029 1 7.66
CHEMBL3092026 1 7.55
CHEMBL3092032 1 7.50
CHEMBL3092025 1 7.46
CHEMBL3092028 1 7.34
CHEMBL3092034 1 -
CHEMBL3091469 1 -
CHEMBL3092033 1 -
CHEMBL3092031 1 -
CHEMBL3092027 1 -
CHEMBL3092024 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2047959 IC50 = 2.0 nM 8.70
CHEMBL3092039 IC50 = 2.0 nM 8.70
CHEMBL3092037 IC50 = 5.0 nM 8.30
CHEMBL2047943 IC50 = 5.0 nM 8.30
CHEMBL3092038 IC50 = 8.0 nM 8.10
CHEMBL3092036 IC50 = 9.0 nM 8.05
CHEMBL3092035 IC50 = 12.0 nM 7.92
CHEMBL3092030 IC50 = 20.0 nM 7.70
CHEMBL3092029 IC50 = 22.0 nM 7.66
CHEMBL3092026 IC50 = 28.0 nM 7.55
CHEMBL3092032 IC50 = 32.0 nM 7.50
CHEMBL3092025 IC50 = 35.0 nM 7.46
CHEMBL3092028 IC50 = 46.0 nM 7.34
CHEMBL3092034 IC50 > 100.0 nM -
CHEMBL3091469 IC50 > 100.0 nM -
CHEMBL3092033 IC50 > 100.0 nM -
CHEMBL3092031 IC50 > 100.0 nM -
CHEMBL3092027 IC50 > 100.0 nM -
CHEMBL3092024 IC50 > 100.0 nM -