VU0364739

VU0364739 : Inhibitor of PLD2

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(1 ratings)

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Probe VU0364739 is in the process of SERP review.

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Information

PLD2

Inhibitor

1 µM up to 5- 10 µM

Probe Availability:

In Vitro Validations

Uniprot ID: O14939

Target Class: Enzyme

Target SubClass: Phospholipase

Potency: IC50

Potency Value: 100 nM

Potency Assay: Biochemical assay using purified PLD2

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

Target aliases:

Phospholipase D2, PLD2, PLD2_HUMAN, hPLD2, PLD 2, ...

DOI Reference: 10.1021/jm100814g

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Selective against PLD1 in biochemical assay (PLD1: IC50 of 7500 nM).

Probe Selectivity in Cell:

Selective against PLD1 (IC50 1500 nM) in cellular assay.

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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

While it remains an important in vitro tool to probe and describe the differential roles and pharmacology of PLD2, additional optimization will be required to develop robust in vivo proof-of-concept compounds.

(last updated: 9 Aug 2022 )

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 13 Sept 2022 )