MSC-4381

Inhibitor of SLC16A3

Structure

SERP Rating

Probe MSC-4381 is in the process of SERP review.

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Information

SLC16A3

Inhibitor

Up to 10 µM

Additional Data

SGC image SGC Chemical Probe Collection

Probe Availability:

MCULE

In Vitro Validations

Uniprot ID: O15427

Target Class: Transporter

Target SubClass: Monocarboxylate transporter

Potency: IC 50

Potency Value: 77 nM

Potency Assay: Fluorescence Cross Correlation Spectroscopy

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

Target aliases:

Monocarboxylate transporter 4, MCT4, SLC16A3, MOT4 ...

DOI Reference: 10.1021/acs.jmedchem.1c00448.

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

MSC-4381 is selective within the target family: SLC16A1 (MCT1): SNU-398 (MCT1+/4-) cells (IC50 > 4 µM), SLC16A7 (MCT2) and SLC16A8 (MCT3): RT4 (MCT2+/3+) cells (IC50 = 638 nM) (600 fold). CEREP binding, cellular and nuclear receptor functional assays (58 targets) at 10 µM: Closest hits are human HTR6 (IC50 = 4.6. µM), human AVPR1A (IC50 = 7.1 µM) No inhibition of PTGER1 (IC50 > 30 µM) or PTGER2 (IC50 > 30 µM).

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SERP ratings and comments

No SERP comments found for MSC-4381