{"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":"codex-gemma-dda1882f352a","candidate_categories":[],"consensus_categories":[],"category_scores_codex":[0.0007019275,0.000313166,0.0004333498,0.00008012349,0.0001226266,0.00002650448,0.0002661166,0.0002970317,0.00009620539],"category_scores_gemma":[0.0007073449,0.0002303479,0.0001655768,0.0001451457,0.0003499298,0.00002436823,0.0001167214,0.0002841448,0.000004831964],"about_ca_system_candidate":false,"about_ca_system_consensus":false,"about_ca_system_score_codex":0.00007553938,"about_ca_system_score_gemma":0.0002935682,"about_ca_topic_candidate":false,"about_ca_topic_consensus":false,"about_ca_topic_score_codex":0.00001464759,"about_ca_topic_score_gemma":0.000001894632,"domain_scores_codex":[0.9978795,0.0000754482,0.0007687092,0.000379029,0.0005449966,0.0003523378],"domain_scores_gemma":[0.9980139,0.00007935634,0.0007226531,0.0003153071,0.0004538888,0.0004149266],"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":[0.0003251899,0.0001586552,0.001869233,0.0001050626,0.00009958884,0.00005163534,0.00007281992,0.00001837665,0.9911264,0.000004836635,0.0008246486,0.005343575],"study_design_scores_gemma":[0.002403065,0.0004358695,0.001876263,0.0002126793,0.0001563014,0.0001732075,0.000138339,0.00001165991,0.9768607,0.0002068727,0.0172335,0.0002915313],"study_design_candidate":"bench_or_experimental","study_design_consensus":"bench_or_experimental","genre_codex":"empirical","genre_gemma":"empirical","genre_scores_codex":[0.9774237,0.01615447,0.002954303,0.00136812,0.0002657385,0.00009247013,0.00001204175,0.000009330529,0.001719793],"genre_scores_gemma":[0.9886551,0.00704586,0.001459693,0.0001673306,0.00132818,0.0000040787,0.00002241383,0.00003892917,0.001278383],"genre_candidate":"empirical","genre_consensus":"empirical","teacher_disagreement_score":0.01640885,"threshold_uncertainty_score":0.9393314,"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."}}