{"id":"W2222665439","doi":"10.1021/acs.jmedchem.5b01635","title":"8-Substituted Pyrido[3,4-<i>d</i>]pyrimidin-4(3<i>H</i>)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors","year":2016,"lang":"en","type":"article","venue":"Journal of Medicinal Chemistry","topic":"Epigenetics and DNA Methylation","field":"Biochemistry, Genetics and Molecular Biology","cited_by":98,"is_retracted":false,"has_abstract":true,"ca_institutions":"","funders":"Biotechnology and Biological Sciences Research Council; Engineering and Physical Sciences Research Council; Novartis Pharma; Ministero dello Sviluppo Economico; Genome Canada; Fundação de Amparo à Pesquisa do Estado de São Paulo; Cancer Research UK; Ontario Ministry of Economic Development and Innovation; National Institute for Health and Care Research; Wellcome Trust; European Federation of Pharmaceutical Industries and Associations; Wellcome; Royal Marsden NHS Foundation Trust; Pfizer; Avon Foundation for Women","keywords":"Chemistry; Demethylase; H3K4me3; Stereochemistry; Demethylation; Moiety; Linker; HeLa; Lysine; Pyrazole; Histone; Biochemistry; Cell; Amino acid","routes":{"ca_aff":false,"ca_fund":true,"ca_venue":false,"about_ca":false,"invisible_to_affiliation_only":true},"retraction":null,"screen":null,"direct_labels":[],"prediction":{"model_version":"metacan-v3-hybrid-931329e0061c","candidate_categories":[],"consensus_categories":[],"category_scores_codex":[0.0000993584,0.0002513082,0.0002588873,0.0001094979,0.0001008193,0.0001211644,0.0003485119,0.0001968105,0.000901698],"category_scores_gemma":[0.00009779127,0.0001167579,0.0001290099,0.0001305396,0.0001420981,0.0001331201,0.0001113106,0.0003582792,0.0003272603],"about_ca_system_candidate":false,"about_ca_system_consensus":false,"about_ca_system_score_codex":0.0002830988,"about_ca_system_score_gemma":0.0001654555,"about_ca_topic_candidate":false,"about_ca_topic_consensus":false,"about_ca_topic_score_codex":0.0005266108,"about_ca_topic_score_gemma":0.001846482,"domain_scores_codex":[0.9999421,0.000009826453,0.00000450032,0.00001005744,0.00001621097,0.00001732319],"domain_scores_gemma":[0.9999644,0.000004489095,0.00001303625,0.000004419663,0.000006119082,0.000007653442],"domain_codex":null,"domain_gemma":null,"domain_candidate":null,"domain_consensus":null,"study_design_codex":"bench_or_experimental","study_design_gemma":"bench_or_experimental","study_design_scores_codex":[0.0002238754,0.0000821194,0.0001591918,0.0001314079,0.00001113206,0.0001095419,0.00003347647,0.0008029184,0.9907315,0.0003662865,0.000279254,0.007069231],"study_design_scores_gemma":[0.000129632,0.001340069,0.001759398,0.000008475718,0.00002840712,0.0003921165,0.0000148725,0.001176466,0.9847685,0.00008054587,0.01028577,0.00001583729],"study_design_candidate":"bench_or_experimental","study_design_consensus":"bench_or_experimental","genre_codex":"empirical","genre_gemma":"empirical","genre_scores_codex":[0.9732096,0.008295494,0.008918789,0.0002551919,0.00008857708,0.0001311534,0.0006737465,0.0002494559,0.008178034],"genre_scores_gemma":[0.9851478,0.003823365,0.006513773,0.00007112648,0.00001573494,0.00006459159,0.0005421388,0.00001778222,0.003803705],"genre_candidate":"empirical","genre_consensus":"empirical","teacher_disagreement_score":0.000901698,"threshold_uncertainty_score":0.003016472,"prediction_status":"machine_predicted_unvalidated"},"machine_scores":{"provisional":true,"baseline":true,"maturity_gate_passed":false,"score_opus":0.00876069058603376,"score_gpt":0.2505145353264289,"score_spread":0.2417538447403951,"validation_status":"score_only:v0-immature-baseline","note":"Baseline scores from an immature model (maturity gate not passed). Scores rank; they never assert a category."}}