| http://purl.uniprot.org/citations/32118427 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/32118427 | http://www.w3.org/2000/01/rdf-schema#comment | "A high-throughput screen designed to discover new inhibitors of histone acetyltransferase KAT6A uncovered CTX-0124143 (1), a unique aryl acylsulfonohydrazide with an IC50 of 1.0 μM. Using this acylsulfonohydrazide as a template, we herein disclose the results of our extensive structure-activity relationship investigations, which resulted in the discovery of advanced compounds such as 55 and 80. These two compounds represent significant improvements on our recently reported prototypical lead WM-8014 (3) as they are not only equivalently potent as inhibitors of KAT6A but are less lipophilic and significantly more stable to microsomal degradation. Furthermore, during this process, we discovered a distinct structural subclass that contains key 2-fluorobenzenesulfonyl and phenylpyridine motifs, culminating in the discovery of WM-1119 (4). This compound is a highly potent KAT6A inhibitor (IC50 = 6.3 nM; KD = 0.002 μM), competes with Ac-CoA by binding to the Ac-CoA binding site, and has an oral bioavailability of 56% in rats."xsd:string |
| http://purl.uniprot.org/citations/32118427 | http://purl.org/dc/terms/identifier | "doi:10.1021/acs.jmedchem.9b02071"xsd:string |
| http://purl.uniprot.org/citations/32118427 | http://purl.uniprot.org/core/author | "Chung M.C."xsd:string |
| http://purl.uniprot.org/citations/32118427 | http://purl.uniprot.org/core/author | "Sun Y."xsd:string |
| http://purl.uniprot.org/citations/32118427 | http://purl.uniprot.org/core/author | "Nguyen N."xsd:string |
| http://purl.uniprot.org/citations/32118427 | http://purl.uniprot.org/core/author | "Thomas T."xsd:string |
| http://purl.uniprot.org/citations/32118427 | http://purl.uniprot.org/core/author | "Charman S.A."xsd:string |
| http://purl.uniprot.org/citations/32118427 | http://purl.uniprot.org/core/author | "Shackleford D.M."xsd:string |
| http://purl.uniprot.org/citations/32118427 | http://purl.uniprot.org/core/author | "Mudududdla R."xsd:string |
| http://purl.uniprot.org/citations/32118427 | http://purl.uniprot.org/core/author | "Varghese S."xsd:string |
| http://purl.uniprot.org/citations/32118427 | http://purl.uniprot.org/core/author | "Parker M.W."xsd:string |
| http://purl.uniprot.org/citations/32118427 | http://purl.uniprot.org/core/author | "Voss A.K."xsd:string |
| http://purl.uniprot.org/citations/32118427 | http://purl.uniprot.org/core/author | "Huang F."xsd:string |
| http://purl.uniprot.org/citations/32118427 | http://purl.uniprot.org/core/author | "Monahan B.J."xsd:string |
| http://purl.uniprot.org/citations/32118427 | http://purl.uniprot.org/core/author | "Street I.P."xsd:string |
| http://purl.uniprot.org/citations/32118427 | http://purl.uniprot.org/core/author | "Jarman K.E."xsd:string |
| http://purl.uniprot.org/citations/32118427 | http://purl.uniprot.org/core/author | "Jousset Sabroux H."xsd:string |
| http://purl.uniprot.org/citations/32118427 | http://purl.uniprot.org/core/author | "Falk H."xsd:string |
| http://purl.uniprot.org/citations/32118427 | http://purl.uniprot.org/core/author | "White K.L."xsd:string |
| http://purl.uniprot.org/citations/32118427 | http://purl.uniprot.org/core/author | "Xue L."xsd:string |
| http://purl.uniprot.org/citations/32118427 | http://purl.uniprot.org/core/author | "Sanchez J."xsd:string |
| http://purl.uniprot.org/citations/32118427 | http://purl.uniprot.org/core/author | "Baell J.B."xsd:string |
| http://purl.uniprot.org/citations/32118427 | http://purl.uniprot.org/core/author | "Leaver D.J."xsd:string |
| http://purl.uniprot.org/citations/32118427 | http://purl.uniprot.org/core/author | "Walters M.A."xsd:string |