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Assay Detail

CHEMBL5386424

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

Binding
Inhibition of Mps1 (unknown origin) incubated for 120 mins in presence of substrate/ATP by ADP-Glo assay
26
Total Activities
26
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, synthesis and biological evaluation of a new class of 7H-pyrrolo[2,3-d]pyrimidine derivatives as Mps1 inhibitors for the treatment of breast cancer.
Li X, Wei W, Tao L, Zeng J, Zhu Y, Yang T, Wang Q, Tang M, Liu Z, Yu L.
Eur J Med Chem (2023) 245 : 114887 -114887
PubMed 36370549 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 7.14 7.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5423969 1 7.54
CHEMBL5438644 1 7.50
CHEMBL5432497 1 7.48
CHEMBL5436903 1 7.47
CHEMBL5419486 1 7.46
CHEMBL2047943 1 7.44
CHEMBL5412569 1 7.40
CHEMBL5405238 1 7.39
CHEMBL5404777 1 7.33
CHEMBL5433818 1 7.31
CHEMBL5415111 1 7.31
CHEMBL5406160 1 7.30
CHEMBL5406816 1 7.29
CHEMBL5428607 1 7.27
CHEMBL5440033 1 7.17
CHEMBL5416115 1 7.17
CHEMBL5410795 1 7.08
CHEMBL5405237 1 6.97
CHEMBL5432900 1 6.88
CHEMBL5421792 1 6.86
CHEMBL5428995 1 6.84
CHEMBL5440244 1 6.83
CHEMBL5432239 1 6.81
CHEMBL5403223 1 6.81
CHEMBL5414691 1 6.47
CHEMBL5422356 1 6.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5423969 IC50 = 29.0 nM 7.54
CHEMBL5438644 IC50 = 32.0 nM 7.50
CHEMBL5432497 IC50 = 33.0 nM 7.48
CHEMBL5436903 IC50 = 34.0 nM 7.47
CHEMBL5419486 IC50 = 35.0 nM 7.46
CHEMBL2047943 IC50 = 36.0 nM 7.44
CHEMBL5412569 IC50 = 40.0 nM 7.40
CHEMBL5405238 IC50 = 41.0 nM 7.39
CHEMBL5404777 IC50 = 47.0 nM 7.33
CHEMBL5433818 IC50 = 49.0 nM 7.31
CHEMBL5415111 IC50 = 49.0 nM 7.31
CHEMBL5406160 IC50 = 50.0 nM 7.30
CHEMBL5406816 IC50 = 51.0 nM 7.29
CHEMBL5428607 IC50 = 54.0 nM 7.27
CHEMBL5440033 IC50 = 67.0 nM 7.17
CHEMBL5416115 IC50 = 68.0 nM 7.17
CHEMBL5410795 IC50 = 83.0 nM 7.08
CHEMBL5405237 IC50 = 106.0 nM 6.97
CHEMBL5432900 IC50 = 132.0 nM 6.88
CHEMBL5421792 IC50 = 137.0 nM 6.86
CHEMBL5428995 IC50 = 144.0 nM 6.84
CHEMBL5440244 IC50 = 149.0 nM 6.83
CHEMBL5432239 IC50 = 154.0 nM 6.81
CHEMBL5403223 IC50 = 154.0 nM 6.81
CHEMBL5414691 IC50 = 338.0 nM 6.47
CHEMBL5422356 IC50 = 464.0 nM 6.33