Llona-Minguez S, Häggblad M, Martens U, Throup A, Loseva O, Jemth A, Lundgren B, Scobie M, Helleday T
Bioorg. Med. Chem. Lett. 27 (16) 3897-3904 [2017-08-15; online 2017-06-16]
A high-throughput screening campaign using a commercial compound library (ChemBridge DiverSET) revealed diverse chemotypes as inhibitors of the human dCTP pyrophosphatase 1 (dCTPase). Triazole, triazolopyrimidine, triazinoindole, quinoline hydrazone and arylpiperazine hits were clustered, confirmed by IC50 determinations, and their preliminary structure-activity-relationships (SAR) and ligand efficiency scores are discussed in this letter.
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Biochemical and Cellular Screening