RP-6306

RP-6306 : Inhibitor of PKMYT1

Structure

SERP Rating

Probe RP-6306 is in the process of SERP review.

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Information

PKMYT1

Inhibitor

up to 1 uM

Probe Availability:

MedChemExpress

In Vitro Validations

Uniprot ID: Q99640

Target Class: Kinase

Target SubClass: Ser/Thr kinase

Potency: IC50

Potency Value: < 10 nM

Potency Assay: ADP-GLO assay

PDB ID for probe-target interaction (3D structure): 8D6E

Target aliases:

Membrane-associated tyrosine- and threonine-specif ...

DOI Reference: 10.1021/acs.jmedchem.2c00552

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

RP-6306 was tested in a Kinativ Colo-205 cell lysate kinase binding assay at 1.2 μM binding to only 6 of the 274 kinases detected. NanoBRET cell-based assays was expanded to include five ephrins (A1, A2, B2, B3, and B4), FRK, c-SRC, and WEE1. RP-6306 showed a high degree of selectivity (29–4000×) over these kinases in these cellular binding assays.

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