AR-C141990

AR-C141990 : Inhibitor of SLC16A1

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(1 ratings)

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Probe AR-C141990 is in the process of SERP review.

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Information

SLC16A1

Inhibitor

up to 1 uM

Probe Availability:

In Vitro Validations

Uniprot ID: P53985

Target Class: Solute carrier

Target SubClass: Monocarboxylate porter

Potency: Ki

Potency Value: 4.8 nM

Potency Assay: Scintillation Proximity Assay

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

Target aliases:

Monocarboxylate transporter 1, MCT1, SLC16A1, MOT1 ...

DOI Reference: 10.1016/j.bmcl.2006.01.024

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Selectivity within target family: Exhibits approximately 10-fold selectivity for MCT1 over MCT2 and no significant activity against MCT3 or 4 ( DOI: 10.1111/j.1432-2277.2012.01579.x).

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

This is a potent inhibitor of MCT1 with weaker (by approximately 10-fold) activity against MCT2. The specific on-target activity and possible off-targets have not been exhaustively characterized, but based on the current literature this seems like a good probe for MCT1 in in vitro and in vivo applications in rat models.

(last updated: 17 Oct 2023 )