@article{af323d923b0a4b25b21c462047298f17,
title = "Cell penetrant inhibitors of the KDM4 and KDM5 families of histone lysine demethylases. 2. Pyrido[3,4-d]pyrimidin-4(3H)-one derivatives",
abstract = "Following the discovery of cell penetrant pyridine-4-carboxylate inhibitors of the KDM4 (JMJD2) and KDM5 (JARID1) families of histone lysine demethylases (e.g., 1), further optimization led to the identification of non-carboxylate inhibitors derived from pyrido[3,4-d]pyrimidin-4(3H)-one. A number of exemplars such as compound 41 possess interesting activity profiles in KDM4C and KDM5C biochemical and target-specific, cellular mechanistic assays.",
keywords = "molecular medicine, drugs, drug discovery, gene expression, epigenetics",
author = "Westaway, {Susan M.} and Preston, {Alex G. S.} and Barker, {Michael D.} and Fiona Brown and Brown, {Jack A.} and Matthew Campbell and Chun-Wa Chung and Gerard Drewes and Robert Eagle and Neil Garton and Laurie Gordon and Carl Haslam and Hayhow, {Thomas G.} and Humphreys, {Philip G.} and Gerard Joberty and Roy Katso and Laurens Kruidenier and Melanie Leveridge and Michelle Pemberton and Inma Rioja and Seal, {Gail A.} and Tracy Shipley and Onkar Singh and Suckling, {Colin J.} and Joanna Taylor and Pamela Thomas and Wilson, {David M.} and Kevin Lee and Prinjha, {Rab K.}",
year = "2016",
month = feb,
day = "25",
doi = "10.1021/acs.jmedchem.5b01538",
language = "English",
volume = "59",
pages = "1370--1387",
journal = "Journal of Medicinal Chemistry",
issn = "0022-2623",
publisher = "American Chemical Society",
number = "4",
}