Title : Modulating the strength of hydrogen bond acceptors to achieve low Caco2 efflux for oral bioavailability of PARP inhibitors blocking centrosome clustering.

Pub. Date : 2016 Oct 1

PMID : 27578247






2 Functional Relationships(s)
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1 Modulating the strength of hydrogen bond acceptors to achieve low Caco2 efflux for oral bioavailability of PARP inhibitors blocking centrosome clustering. caco2 collagen type XI alpha 2 chain Homo sapiens
2 During the lead generation and optimization of PARP inhibitors blocking centrosome clustering, it was discovered that increasing hydrogen bond acceptor (HBA) strength improved cellular potency but led to elevated Caco2 and MDR1 efflux and thus poor oral bioavailability. caco2 collagen type XI alpha 2 chain Homo sapiens