SIMUROSERTIB

SIMUROSERTIB : ATP competitive inhibitor of CDC7

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(0 ratings)

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Probe SIMUROSERTIB is in the process of SERP review.

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Information

CDC7

ATP competitive

300 nM, up to 1 uM, time dependent

In Vitro Validations

Uniprot ID: O00311

Target Class: Kinase

Target SubClass: Ser/Thr Kinase

Potency: IC50

Potency Value: <0.3 nM

Potency Assay: Biochemical assay

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

Target aliases:

Cell division cycle 7-related protein kinase, CDC7 ...

DOI Reference: 10.1126/sciadv.aav3660

Uniprot ID: O00311

Target Class: Kinase

Target SubClass: Ser/Thr Kinase

Potency: Kd

Potency Value: 0.42 nM

Potency Assay: SPR

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

Target aliases:

Cell division cycle 7-related protein kinase, CDC7 ...

DOI Reference: 10.1126/sciadv.aav3660

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay (off target): Kinase selectivity assays demonstrated high selectivity of TAK-931 against CDC7 @ 1 uM, which was >120 times higher than that of the other 317 tested kinases.

Potency assay, off target (cells): phosphorylation of Pol II at Ser 2 indicating inhibition of CDK9; no inhibition was observed up to 1 µM

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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

Given the selectivity profile of SIMUROSERTIB in all assays (biological, cell-based, and cell proliferation), this compound is highly recommended. Moreover, SIMUROSERTIB has a great profile in inhibiting cell proliferation of related cancer cells.

(last updated: 20 Feb 2025 )