{"id":"W4205341592","doi":"10.1021/acs.jmedchem.1c01708","title":"Size-Reduced Macrocyclic Analogues of [Pyr<sup>1</sup>]-apelin-13 Showing Negative Gα<sub>12</sub> Bias Still Produce Prolonged Cardiac Effects","year":2022,"lang":"en","type":"article","venue":"Journal of Medicinal Chemistry","topic":"Apelin-related biomedical research","field":"Medicine","cited_by":11,"is_retracted":false,"has_abstract":true,"ca_institutions":"Institute for Research in Immunology and Cancer; Université de Montréal; Université de Sherbrooke","funders":"Fonds de Recherche du Québec - Santé; Canada Foundation for Innovation; Université de Sherbrooke; Canadian Institutes of Health Research; Mitacs; Canada Research Chairs; Heart and Stroke Foundation of Canada","keywords":"Chemistry; Potency; Agonist; EC50; Apelin; Stereochemistry; In vivo; Metabolic stability; Intrinsic activity; Pharmacology; Receptor; In vitro; Biochemistry","routes":{"ca_aff":true,"ca_fund":true,"ca_venue":false,"about_ca":false,"invisible_to_affiliation_only":false},"retraction":null,"screen":null,"direct_labels":[],"prediction":{"model_version":"metacan-v3-hybrid-931329e0061c","candidate_categories":[],"consensus_categories":[],"category_scores_codex":[0.00007867281,0.0002126186,0.0002675109,0.00009013269,0.00009541355,0.0001389797,0.0001945614,0.000232049,0.003343449],"category_scores_gemma":[0.0001707249,0.00007573015,0.0001327464,0.0001039361,0.0002013648,0.0001485376,0.0001123542,0.0004794626,0.0007280785],"about_ca_system_candidate":false,"about_ca_system_consensus":false,"about_ca_system_score_codex":0.000117483,"about_ca_system_score_gemma":0.00010252,"about_ca_topic_candidate":false,"about_ca_topic_consensus":false,"about_ca_topic_score_codex":0.0002495816,"about_ca_topic_score_gemma":0.0003247958,"domain_scores_codex":[0.9999446,0.000009087849,0.00000407129,0.00001258156,0.00001212172,0.00001756976],"domain_scores_gemma":[0.9998864,0.00002578175,0.00003035414,0.00001272646,0.000009941465,0.00003473905],"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":[0.000912057,0.00005356202,0.00007090944,0.00004688348,0.00001200321,0.0000604737,0.0000125234,0.00009043863,0.9950027,0.00009477301,0.0000934099,0.003550306],"study_design_scores_gemma":[0.0001284463,0.003227747,0.002780339,0.000005947964,0.00002769163,0.0003434446,0.00002527568,0.0003364368,0.98985,0.00007088705,0.003193579,0.00001001463],"study_design_candidate":"bench_or_experimental","study_design_consensus":"bench_or_experimental","genre_codex":"empirical","genre_gemma":"empirical","genre_scores_codex":[0.9928975,0.001101459,0.001178396,0.00006037955,0.00007597475,0.00003738964,0.0002750607,0.00006031791,0.004313476],"genre_scores_gemma":[0.994511,0.0006880801,0.001529071,0.000108732,0.0000270471,0.00004184314,0.0004313931,0.00002046383,0.002642313],"genre_candidate":"empirical","genre_consensus":"empirical","teacher_disagreement_score":0.003343449,"threshold_uncertainty_score":0.01118499,"prediction_status":"machine_predicted_unvalidated"},"machine_scores":{"provisional":true,"baseline":true,"maturity_gate_passed":false,"score_opus":0.02333881699511839,"score_gpt":0.2884313110138776,"score_spread":0.2650924940187593,"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."}}