BAY1217389

Inhibitor of TTK

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(2 ratings)

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Information

Inhibitor

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Probe Availability:

In Vitro Validations

Uniprot ID: P33981

Target Class: Protein kinase

Target SubClass: Ser/Thr Kinase

Potency: IC50

Potency Value: 0.7 nM (10 uM ATP); 1 nM (2 mM ATP)

Potency Assay: HTRF-based MPS1 assay with an ATP concentration of 2 mM

PDB ID for probe-target interaction (3D structure): 6TND

Structure-activity relationship: yes

Target aliases:

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

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency end-point : IC50 PDGFRβ <10 nmol/L

Probe Selectivity in Vitro:

BAY 1217389 was tested against the DiscoveRx kinase panel (395 kinases) and was found to bind to PDGFRβ (<10 nmol/L), Kit (between 10 and 100 nmol/L), CLK1, CLK2, CLK4, JNK1, JNK2, JNK3, LATS1, MAK, MAPKAP2, MERTK, p38β, PDGFRα, PIP5K1C,

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

While this compound is highly active at nanomolar concentrations in cells, more information is needed to establish a suitable in vivo dose.

(last updated: 19 Mar 2021 )

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

I recommend to confirm/disprove biochemical off targets ie PDGFR, KIT and possibly CLK1, CLK2, CLK4, JNK1, JNK2, JNK3, LATS1, MAK, MAPKAP2.

(last updated: 14 Apr 2021 )