SR-0813

Inhibitor of MLLT1, MLLT3

Structure

SERP Rating

Probe SR-0813 is in the process of SERP review.

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Information

MLLT1
MLLT3

Inhibitor

up to 1 uM

DOI - 10.1021/acscentsci.0c01550

Probe Availability:

MedChemExpress

In Vitro Validations

Uniprot ID: Q03111

Target Class: Epigenetic

Target SubClass: YEATS

Potency: IC 50

Potency Value: 25 nM

Potency Assay: ENL-H3K27cr HTRF

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

Structure-activity relationship: yes

Target aliases:

Protein ENL, YEATS1, LTG19, ENL, MLLT1, ENL_HUMAN, ...

DOI Reference: 10.1021/acscentsci.0c01550

Uniprot ID: Q03111

Target Class: Epigenetic

Target SubClass: YEATS

Potency: Kd

Potency Value: 30 nM

Potency Assay: SPR

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

Target aliases:

Protein ENL, YEATS1, LTG19, ENL, MLLT1, ENL_HUMAN, ...

DOI Reference: 10.1021/acscentsci.0c01550

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Selective over YEATS2 and YEATS4. Outside target family: SR-0813 was profiled for off-target effects on bromodomain proteins. SR-0813 was inactive in the BRD4 BD1 HTRF assay, and not a single bromodomain off-target was identified using the BROMOscan profiling (bromoMAX; 32 bromodomains) SR-0813 was tested for kinase off-targets using the KINOMEscan profiling service (scanMAX, 468 kinases). Of the 468 kinases tested, 4 were identified as potential off-targets, but only YSK4 (also known as MAP3K19), was bound by SR-0813 with over 100-fold lower affinity (Kd = 3.5 μM) than ENL YEATS.

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SERP ratings and comments

No SERP comments found for SR-0813