{"id":"W2570397282","doi":"10.1021/acs.jmedchem.6b01583","title":"Design of a Biased Potent Small Molecule Inhibitor of the Bromodomain and PHD Finger-Containing (BRPF) Proteins Suitable for Cellular and in Vivo Studies","year":2017,"lang":"en","type":"article","venue":"Journal of Medicinal Chemistry","topic":"Protein Degradation and Inhibitors","field":"Biochemistry, Genetics and Molecular Biology","cited_by":53,"is_retracted":false,"has_abstract":true,"ca_institutions":"","funders":"Structural Genomics Consortium; Wellcome; Medical Research Council; School of Pharmacy, University College London; Cancer Research UK; Wellcome Trust","keywords":"Bromodomain; In vivo; Chemistry; PHD finger; Myeloid leukemia; BRD4; Chromatin; Drug discovery; Cell culture; Cancer research; Histone; Small molecule; Cell biology; Computational biology; Biochemistry; Biology; Genetics; Gene; Zinc finger; Transcription factor","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":[0.0002479593,0.0004341193,0.0005695709,0.0001968854,0.0001691915,0.0002965157,0.0004597087,0.0003159058,0.001117215],"category_scores_gemma":[0.0001146444,0.000230541,0.0002574501,0.0002226754,0.0001572595,0.000166628,0.0002167068,0.0004595323,0.0005690975],"about_ca_system_candidate":false,"about_ca_system_consensus":false,"about_ca_system_score_codex":0.0003456174,"about_ca_system_score_gemma":0.000406563,"about_ca_topic_candidate":false,"about_ca_topic_consensus":false,"about_ca_topic_score_codex":0.000588036,"about_ca_topic_score_gemma":0.001758087,"domain_scores_codex":[0.9998953,0.00001450891,0.000007785189,0.00002410347,0.00002382204,0.00003449793],"domain_scores_gemma":[0.9999607,0.000005686233,0.000007984824,0.000003427157,0.000006949347,0.00001534346],"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":[0.0003783192,0.0001768007,0.0001963761,0.0000990988,0.00002648262,0.0001171802,0.00002520998,0.001416301,0.9896244,0.0002980235,0.0002135129,0.007428289],"study_design_scores_gemma":[0.0003440128,0.003935293,0.00130004,0.00001142605,0.0000669682,0.0004910204,0.00001999724,0.002737961,0.9814642,0.0001032842,0.009502276,0.00002353991],"study_design_candidate":"bench_or_experimental","study_design_consensus":"bench_or_experimental","genre_codex":"empirical","genre_gemma":"empirical","genre_scores_codex":[0.9513714,0.00544519,0.03460256,0.0002232885,0.00007464287,0.000835953,0.001380845,0.0003578299,0.005708287],"genre_scores_gemma":[0.9695798,0.003723345,0.02027337,0.0002146416,0.00001813321,0.0003864437,0.001820049,0.00003796226,0.003946112],"genre_candidate":"empirical","genre_consensus":"empirical","teacher_disagreement_score":0.001117215,"threshold_uncertainty_score":0.003737509,"prediction_status":"machine_predicted_unvalidated"},"machine_scores":{"provisional":true,"baseline":true,"maturity_gate_passed":false,"score_opus":0.04299211005995594,"score_gpt":0.2732631495569711,"score_spread":0.2302710394970152,"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."}}