NMS-P715

Inhibitor of TTK

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(1 ratings)

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Probe NMS-P715 is in the process of SERP review.

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Information

Inhibitor

up to 1 uM

Probe Availability:

In Vitro Validations

Uniprot ID: P33981

Target Class: Kinase

Target SubClass: Ser/Thr Kinase

Potency: IC50

Potency Value: 7 nM

Potency Assay: Biochemical assay

PDB ID for probe-target interaction (3D structure): 2X9E, 5AP7, 5NTT

Target aliases:

Dual specificity protein kinase TTK, MPS1L1, MPS1, ...

DOI Reference: 10.1016/j.bmcl.2011.05.122

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Selective against Aur-A, CDK2/A, PLK1

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

This compound inhibits recombinant MPS1 (TTK) with an IC50 of 182 nM. Selectivity (>20-fold) has been demonstrated for 60 kinases in vitro. Growth inhibition of A2780 cells was observed with 1 uM compound. Mouse xenograft data (90-100 mg/kg) afforded tumor cell growth inhibition. On target activity is supported by mutations in TTK that were observed in NMS-P715 resistant cell lines. NMS-P715 is an intriguing MPS1 that merits further investigation to more fully assess the scope of off target activity in cells and in vivo

(last updated: 3 Aug 2022 )