Title : Development of a Selective, Allosteric PLD2 Inhibitor

Pub. Date : 2010

PMID : 23762931






2 Functional Relationships(s)
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Compound Name
Protein Name
Organism
1 ML298 displays no inhibition of PLD1, and therefore is an improvement over our first generation PLD2 selective inhibitor, VU0364739 (cellular PLD1, IC50 = 1,500 nM, cellular PLD2, IC50 = 20 nM), as at standard in vitro doses, and in vivo exposure levels, both PLD1 and PLD2 are inhibited. VU0364739 phospholipase D1 Homo sapiens
2 ML298 displays no inhibition of PLD1, and therefore is an improvement over our first generation PLD2 selective inhibitor, VU0364739 (cellular PLD1, IC50 = 1,500 nM, cellular PLD2, IC50 = 20 nM), as at standard in vitro doses, and in vivo exposure levels, both PLD1 and PLD2 are inhibited. VU0364739 phospholipase D1 Homo sapiens