AZD3965

AZD3965 : Inhibitor of SLC16A1

Structure

SERP Rating

In Cells

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In Model Organisms

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Probe AZD3965 is in the process of SERP review.

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Information

SLC16A1

Inhibitor

up to 100 nM

Probe Availability:

MCULE

In Vitro Validations

Uniprot ID: P53985

Target Class: Transporter

Target SubClass: Solute carrier

Potency: Ki

Potency Value: 1.6 nM

Potency Assay: Scintillation proximity assay on cell membranes

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

Target aliases:

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

DOI Reference: 10.18632/oncotarget.18215

Uniprot ID: P53985

Target Class: Transporter

Target SubClass: Solute carrier

Potency: Ki

Potency Value: 3.2 nM

Potency Assay: AZD3965 binding affinity to yeast membranes expressing recombinant human MCT1 by displacement of [3H]-MCT1

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

Target aliases:

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

DOI Reference: 10.18632/oncotarget.18215

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Off Target: SLC16A7

Potency end-point : Ki 20 nM

Probe Selectivity in Vitro:

No inhibition of lactate transport mediated by MCT3 or MCT4 w in the MCT1, MCT2, MCT3 and MCT4 null rat pancreatic cell line, INS1, selectively expressing MCT3 or MCT4; cells were pre-incubated for 1 hr with 10 μM AZD3965 and lactate transport was assessed using a pH- sensitive fluorescent dye

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(last updated: 6 Feb 2023 )