| http://purl.uniprot.org/citations/28190634 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/28190634 | http://www.w3.org/2000/01/rdf-schema#comment | "We describe a novel class of acidic mPGES-1 inhibitors with nanomolar enzymatic and human whole blood (HWB) potency. Rational design in conjunction with structure-based design led initially to the identification of anthranilic acid 5, an mPGES-1 inhibitor with micromolar HWB potency. Structural modifications of 5 improved HWB potency by over 1000×, reduced CYP2C9 single point inhibition, and improved rat clearance, which led to the selection of [(cyclopentyl)ethyl]benzoic acid compound 16 for clinical studies. Compound 16 showed an IC80 of 24nM for inhibition of PGE2 formation in vitro in LPS-stimulated HWB. A single oral dose resulted in plasma concentrations of 16 that exceeded its HWB IC80 in both rat (5mg/kg) and dog (3mg/kg) for over twelve hours."xsd:string |
| http://purl.uniprot.org/citations/28190634 | http://purl.org/dc/terms/identifier | "doi:10.1016/j.bmcl.2016.11.011"xsd:string |
| http://purl.uniprot.org/citations/28190634 | http://purl.uniprot.org/core/author | "Harvey A."xsd:string |
| http://purl.uniprot.org/citations/28190634 | http://purl.uniprot.org/core/author | "Antonysamy S."xsd:string |
| http://purl.uniprot.org/citations/28190634 | http://purl.uniprot.org/core/author | "Navarro A."xsd:string |
| http://purl.uniprot.org/citations/28190634 | http://purl.uniprot.org/core/author | "Chandrasekhar S."xsd:string |
| http://purl.uniprot.org/citations/28190634 | http://purl.uniprot.org/core/author | "Luz J.G."xsd:string |
| http://purl.uniprot.org/citations/28190634 | http://purl.uniprot.org/core/author | "Hughes N.E."xsd:string |
| http://purl.uniprot.org/citations/28190634 | http://purl.uniprot.org/core/author | "Mudra D.R."xsd:string |
| http://purl.uniprot.org/citations/28190634 | http://purl.uniprot.org/core/author | "Norman B.H."xsd:string |
| http://purl.uniprot.org/citations/28190634 | http://purl.uniprot.org/core/author | "Fisher M.J."xsd:string |
| http://purl.uniprot.org/citations/28190634 | http://purl.uniprot.org/core/author | "McGee J.E."xsd:string |
| http://purl.uniprot.org/citations/28190634 | http://purl.uniprot.org/core/author | "Yu X.P."xsd:string |
| http://purl.uniprot.org/citations/28190634 | http://purl.uniprot.org/core/author | "Fretland A."xsd:string |
| http://purl.uniprot.org/citations/28190634 | http://purl.uniprot.org/core/author | "Gooding K."xsd:string |
| http://purl.uniprot.org/citations/28190634 | http://purl.uniprot.org/core/author | "Warshawsky A.M."xsd:string |
| http://purl.uniprot.org/citations/28190634 | http://purl.uniprot.org/core/author | "Schiffler M.A."xsd:string |
| http://purl.uniprot.org/citations/28190634 | http://purl.uniprot.org/core/author | "Kuklish S.L."xsd:string |
| http://purl.uniprot.org/citations/28190634 | http://purl.uniprot.org/core/author | "Sloan A.V."xsd:string |
| http://purl.uniprot.org/citations/28190634 | http://purl.uniprot.org/core/author | "Bhattachar S.N."xsd:string |
| http://purl.uniprot.org/citations/28190634 | http://purl.uniprot.org/core/author | "York J.S."xsd:string |
| http://purl.uniprot.org/citations/28190634 | http://purl.uniprot.org/core/author | "Manninen P.R."xsd:string |
| http://purl.uniprot.org/citations/28190634 | http://purl.uniprot.org/core/author | "Partridge K.M."xsd:string |
| http://purl.uniprot.org/citations/28190634 | http://purl.uniprot.org/core/author | "Quimby S.J."xsd:string |