| http://purl.uniprot.org/citations/26652588 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/26652588 | http://www.w3.org/2000/01/rdf-schema#comment | "Lead optimization efforts resulted in the discovery of two potent, selective, and orally bioavailable PI3Kδ inhibitors, 1 (AM-8508) and 2 (AM-9635), with good pharmacokinetic properties. The compounds inhibit B cell receptor (BCR)-mediated AKT phosphorylation (pAKT) in PI3Kδ-dependent in vitro cell based assays. These compounds which share a benzimidazole bicycle are effective when administered in vivo at unbound concentrations consistent with their in vitro cell potency as a consequence of improved unbound drug concentration with lower unbound clearance. Furthermore, the compounds demonstrated efficacy in a Keyhole Limpet Hemocyanin (KLH) study in rats, where the blockade of PI3Kδ activity by inhibitors 1 and 2 led to effective inhibition of antigen-specific IgG and IgM formation after immunization with KLH."xsd:string |
| http://purl.uniprot.org/citations/26652588 | http://purl.org/dc/terms/identifier | "doi:10.1021/acs.jmedchem.5b01651"xsd:string |
| http://purl.uniprot.org/citations/26652588 | http://purl.uniprot.org/core/author | "He X."xsd:string |
| http://purl.uniprot.org/citations/26652588 | http://purl.uniprot.org/core/author | "Zhang X."xsd:string |
| http://purl.uniprot.org/citations/26652588 | http://purl.uniprot.org/core/author | "Yu G."xsd:string |
| http://purl.uniprot.org/citations/26652588 | http://purl.uniprot.org/core/author | "Wong S."xsd:string |
| http://purl.uniprot.org/citations/26652588 | http://purl.uniprot.org/core/author | "Whittington D.A."xsd:string |
| http://purl.uniprot.org/citations/26652588 | http://purl.uniprot.org/core/author | "Shin Y."xsd:string |
| http://purl.uniprot.org/citations/26652588 | http://purl.uniprot.org/core/author | "Tran T."xsd:string |
| http://purl.uniprot.org/citations/26652588 | http://purl.uniprot.org/core/author | "McCarter J."xsd:string |
| http://purl.uniprot.org/citations/26652588 | http://purl.uniprot.org/core/author | "Hu Y.L."xsd:string |
| http://purl.uniprot.org/citations/26652588 | http://purl.uniprot.org/core/author | "Cardozo M."xsd:string |
| http://purl.uniprot.org/citations/26652588 | http://purl.uniprot.org/core/author | "Mohn D."xsd:string |
| http://purl.uniprot.org/citations/26652588 | http://purl.uniprot.org/core/author | "Vissinga C."xsd:string |
| http://purl.uniprot.org/citations/26652588 | http://purl.uniprot.org/core/author | "San Miguel T."xsd:string |
| http://purl.uniprot.org/citations/26652588 | http://purl.uniprot.org/core/author | "Henne K."xsd:string |
| http://purl.uniprot.org/citations/26652588 | http://purl.uniprot.org/core/author | "Medina J.C."xsd:string |
| http://purl.uniprot.org/citations/26652588 | http://purl.uniprot.org/core/author | "Duquette J."xsd:string |
| http://purl.uniprot.org/citations/26652588 | http://purl.uniprot.org/core/author | "Suchomel J."xsd:string |
| http://purl.uniprot.org/citations/26652588 | http://purl.uniprot.org/core/author | "Metz D."xsd:string |
| http://purl.uniprot.org/citations/26652588 | http://purl.uniprot.org/core/author | "Kelly R.C."xsd:string |
| http://purl.uniprot.org/citations/26652588 | http://purl.uniprot.org/core/author | "McGee L.R."xsd:string |
| http://purl.uniprot.org/citations/26652588 | http://purl.uniprot.org/core/author | "Zalameda L."xsd:string |
| http://purl.uniprot.org/citations/26652588 | http://purl.uniprot.org/core/author | "Cushing T.D."xsd:string |