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Assay Detail

CHEMBL5708592

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

Binding
Time-dependent inhibition of full length N-terminal GST-tagged human recombinant MPS1 (2 to 857 residues) assessed as inhibition constant in presence of ATP
1
Total Activities
1
Compounds Tested
1
Activity Types
2
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

Targeting the mitotic checkpoint for cancer therapy with NMS-P715, an inhibitor of MPS1 kinase.
Colombo R, Caldarelli M, Mennecozzi M, Giorgini ML, Sola F, Cappella P, Cappella P, Perrera C, Depaolini SR, Rusconi L, Cucchi U, Avanzi N, Bertrand JA, Bossi RT, Pesenti E, Galvani A, Isacchi A, Colotta F, Donati D, Moll J.
Cancer Res (2010) 70 : 10255 -10264
PubMed 21159646 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 9.00 9.00

Assay Parameters

Parameter Type Value Units Text
EFO_ID EFO_ID - MONDO:0004992
EFO_TERM EFO_TERM - cancer

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1236095 1 9.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1236095 Ki = 0.99 nM 9.00