Details | DC50 | Dmax | Source | |
DRUG DEVELOPMENT. Phthalimide conjugation as a strategy for in vivo target protein degradation. Science. 2015 Jun 19;348(6241):1376-81. PMID:25999370 DOI:10.1126/science.aab1433 | ||||
Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4. Chem Biol. 2015 Jun 18;22(6):755-63. PMID:26051217 DOI:10.1016/j.chembiol.2015.05.009 | ||||
Structural basis of PROTAC cooperative recognition for selective protein degradation. Nat Chem Biol. 2017 Mar 13. PMID:28288108 DOI:10.1038/nchembio.2329 | ||||
Structural basis of PROTAC cooperative recognition for selective protein degradation. Nat Chem Biol. 2017 Mar 13. PMID:28288108 DOI:10.1038/nchembio.2329 | ||||
Structural basis of PROTAC cooperative recognition for selective protein degradation. Nat Chem Biol. 2017 Mar 13. PMID:28288108 DOI:10.1038/nchembio.2329 | ||||
Structural basis of PROTAC cooperative recognition for selective protein degradation. Nat Chem Biol. 2017 Mar 13. PMID:28288108 DOI:10.1038/nchembio.2329 | ||||
Structural basis of PROTAC cooperative recognition for selective protein degradation. Nat Chem Biol. 2017 Mar 13. PMID:28288108 DOI:10.1038/nchembio.2329 | ||||
Structural basis of PROTAC cooperative recognition for selective protein degradation. Nat Chem Biol. 2017 Mar 13. PMID:28288108 DOI:10.1038/nchembio.2329 | ||||
Structural basis of PROTAC cooperative recognition for selective protein degradation. Nat Chem Biol. 2017 Mar 13. PMID:28288108 DOI:10.1038/nchembio.2329 | ||||
Structural basis of PROTAC cooperative recognition for selective protein degradation. Nat Chem Biol. 2017 Mar 13. PMID:28288108 DOI:10.1038/nchembio.2329 | ||||
Structural basis of PROTAC cooperative recognition for selective protein degradation. Nat Chem Biol. 2017 Mar 13. PMID:28288108 DOI:10.1038/nchembio.2329 | ||||
Structural basis of PROTAC cooperative recognition for selective protein degradation. Nat Chem Biol. 2017 Mar 13. PMID:28288108 DOI:10.1038/nchembio.2329 | ||||
Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression. J Med Chem. 2018 Jan 25;61(2):462-481. PMID:28339196 DOI:10.1021/acs.jmedchem.6b01816 | ||||
Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression. J Med Chem. 2018 Jan 25;61(2):462-481. PMID:28339196 DOI:10.1021/acs.jmedchem.6b01816 | ||||
Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression. J Med Chem. 2018 Jan 25;61(2):462-481. PMID:28339196 DOI:10.1021/acs.jmedchem.6b01816 | ||||
Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression. J Med Chem. 2018 Jan 25;61(2):462-481. PMID:28339196 DOI:10.1021/acs.jmedchem.6b01816 | ||||
Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression. J Med Chem. 2018 Jan 25;61(2):462-481. PMID:28339196 DOI:10.1021/acs.jmedchem.6b01816 | ||||
A "Click Chemistry Platform" for the Rapid Synthesis of Bispecific Molecules for Inducing Protein Degradation. J Med Chem. 2018 Jan 25;61(2):453-461. PMID:28378579 DOI:10.1021/acs.jmedchem.6b01781 | ||||
A "Click Chemistry Platform" for the Rapid Synthesis of Bispecific Molecules for Inducing Protein Degradation. J Med Chem. 2018 Jan 25;61(2):453-461. PMID:28378579 DOI:10.1021/acs.jmedchem.6b01781 | ||||
A "Click Chemistry Platform" for the Rapid Synthesis of Bispecific Molecules for Inducing Protein Degradation. J Med Chem. 2018 Jan 25;61(2):453-461. PMID:28378579 DOI:10.1021/acs.jmedchem.6b01781 | ||||
A "Click Chemistry Platform" for the Rapid Synthesis of Bispecific Molecules for Inducing Protein Degradation. J Med Chem. 2018 Jan 25;61(2):453-461. PMID:28378579 DOI:10.1021/acs.jmedchem.6b01781 | ||||
A "Click Chemistry Platform" for the Rapid Synthesis of Bispecific Molecules for Inducing Protein Degradation. J Med Chem. 2018 Jan 25;61(2):453-461. PMID:28378579 DOI:10.1021/acs.jmedchem.6b01781 | ||||
A "Click Chemistry Platform" for the Rapid Synthesis of Bispecific Molecules for Inducing Protein Degradation. J Med Chem. 2018 Jan 25;61(2):453-461. PMID:28378579 DOI:10.1021/acs.jmedchem.6b01781 | ||||
A "Click Chemistry Platform" for the Rapid Synthesis of Bispecific Molecules for Inducing Protein Degradation. J Med Chem. 2018 Jan 25;61(2):453-461. PMID:28378579 DOI:10.1021/acs.jmedchem.6b01781 | ||||
A "Click Chemistry Platform" for the Rapid Synthesis of Bispecific Molecules for Inducing Protein Degradation. J Med Chem. 2018 Jan 25;61(2):453-461. PMID:28378579 DOI:10.1021/acs.jmedchem.6b01781 | ||||
A "Click Chemistry Platform" for the Rapid Synthesis of Bispecific Molecules for Inducing Protein Degradation. J Med Chem. 2018 Jan 25;61(2):453-461. PMID:28378579 DOI:10.1021/acs.jmedchem.6b01781 | ||||
A "Click Chemistry Platform" for the Rapid Synthesis of Bispecific Molecules for Inducing Protein Degradation. J Med Chem. 2018 Jan 25;61(2):453-461. PMID:28378579 DOI:10.1021/acs.jmedchem.6b01781 | ||||
Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds. J Med Chem. 2018 Jan 25;61(2):504-513. PMID:28595007 DOI:10.1021/acs.jmedchem.6b01912 | ||||
Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds. J Med Chem. 2018 Jan 25;61(2):504-513. PMID:28595007 DOI:10.1021/acs.jmedchem.6b01912 | ||||
Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds. J Med Chem. 2018 Jan 25;61(2):504-513. PMID:28595007 DOI:10.1021/acs.jmedchem.6b01912 | ||||
Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds. J Med Chem. 2018 Jan 25;61(2):504-513. PMID:28595007 DOI:10.1021/acs.jmedchem.6b01912 | ||||
Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds. J Med Chem. 2018 Jan 25;61(2):504-513. PMID:28595007 DOI:10.1021/acs.jmedchem.6b01912 | ||||
Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds. J Med Chem. 2018 Jan 25;61(2):504-513. PMID:28595007 DOI:10.1021/acs.jmedchem.6b01912 | ||||
Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds. J Med Chem. 2018 Jan 25;61(2):504-513. PMID:28595007 DOI:10.1021/acs.jmedchem.6b01912 | ||||
3-Fluoro-4-hydroxyprolines: Synthesis, conformational analysis and stereoselective recognition by the VHL E3 ubiquitin ligase for targeted protein degradation. J Am Chem Soc. 2018 Jun 27. PMID:29949369 DOI:10.1021/jacs.8b05807 | ||||
3-Fluoro-4-hydroxyprolines: Synthesis, conformational analysis and stereoselective recognition by the VHL E3 ubiquitin ligase for targeted protein degradation. J Am Chem Soc. 2018 Jun 27. PMID:29949369 DOI:10.1021/jacs.8b05807 | ||||
Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression. J Med Chem. 2018 Aug 9;61(15):6685-6704. PMID:30019901 DOI:10.1021/acs.jmedchem.8b00506 | ||||
Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression. J Med Chem. 2018 Aug 9;61(15):6685-6704. PMID:30019901 DOI:10.1021/acs.jmedchem.8b00506 | ||||
Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression. J Med Chem. 2018 Aug 9;61(15):6685-6704. PMID:30019901 DOI:10.1021/acs.jmedchem.8b00506 | ||||
Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression. J Med Chem. 2018 Aug 9;61(15):6685-6704. PMID:30019901 DOI:10.1021/acs.jmedchem.8b00506 | ||||
Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression. J Med Chem. 2018 Aug 9;61(15):6685-6704. PMID:30019901 DOI:10.1021/acs.jmedchem.8b00506 | ||||
Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression. J Med Chem. 2018 Aug 9;61(15):6685-6704. PMID:30019901 DOI:10.1021/acs.jmedchem.8b00506 | ||||
Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression. J Med Chem. 2018 Aug 9;61(15):6685-6704. PMID:30019901 DOI:10.1021/acs.jmedchem.8b00506 | ||||
MDM2-Recruiting PROTAC Offers Superior, Synergistic Antiproliferative Activity via Simultaneous Degradation of BRD4 and Stabilization of p53. Cancer Res. 2019 Jan 1;79(1):251-262. PMID:30385614 DOI:10.1158/0008-5472.CAN-18-2918 | ||||
A novel cereblon modulator for targeted protein degradation. Eur J Med Chem. 2019 Mar 15;166:65-74. PMID:30684871 DOI:10.1016/j.ejmech.2019.01.023 | ||||
A novel cereblon modulator for targeted protein degradation. Eur J Med Chem. 2019 Mar 15;166:65-74. PMID:30684871 DOI:10.1016/j.ejmech.2019.01.023 | ||||
A novel cereblon modulator for targeted protein degradation. Eur J Med Chem. 2019 Mar 15;166:65-74. PMID:30684871 DOI:10.1016/j.ejmech.2019.01.023 | ||||
A novel cereblon modulator for targeted protein degradation. Eur J Med Chem. 2019 Mar 15;166:65-74. PMID:30684871 DOI:10.1016/j.ejmech.2019.01.023 | ||||
Covalent Ligand Screening Uncovers a RNF4 E3 Ligase Recruiter for Targeted Protein Degradation Applications. ACS Chem Biol. 2019 Nov 15;14(11):2430-2440. PMID:31059647 DOI:10.1021/acschembio.8b01083 | ||||
Harnessing the anti-cancer natural product nimbolide for targeted protein degradation. Nat Chem Biol. 2019 Jul;15(7):747-755. PMID:31209351 DOI:10.1038/s41589-019-0304-8 | ||||
Protein targeting chimeric molecules specific for dual bromodomain 4 (BRD4) and Polo-like kinase 1 (PLK1) proteins in acute myeloid leukemia cells. Biochem Biophys Res Commun. 2020 Jan 22;521(4):833-839. PMID:31708096 DOI:10.1016/j.bbrc.2019.11.007 | ||||
Structure-Based Design of a Macrocyclic PROTAC. Angew Chem Int Ed Engl. 2019 Nov 19. PMID:31746102 DOI:10.1002/anie.201914396 | ||||
Discovery of novel small molecule induced selective degradation of the bromodomain and extra-terminal (BET) bromodomain protein BRD4 and BRD2 with cellular potencies. Bioorg Med Chem. 2020 Jan 1;28(1):115181. PMID:31767403 DOI:10.1016/j.bmc.2019.115181 | ||||
Discovery of novel small molecule induced selective degradation of the bromodomain and extra-terminal (BET) bromodomain protein BRD4 and BRD2 with cellular potencies. Bioorg Med Chem. 2020 Jan 1;28(1):115181. PMID:31767403 DOI:10.1016/j.bmc.2019.115181 | ||||
Discovery of novel small molecule induced selective degradation of the bromodomain and extra-terminal (BET) bromodomain protein BRD4 and BRD2 with cellular potencies. Bioorg Med Chem. 2020 Jan 1;28(1):115181. PMID:31767403 DOI:10.1016/j.bmc.2019.115181 | ||||
Discovery of novel small molecule induced selective degradation of the bromodomain and extra-terminal (BET) bromodomain protein BRD4 and BRD2 with cellular potencies. Bioorg Med Chem. 2020 Jan 1;28(1):115181. PMID:31767403 DOI:10.1016/j.bmc.2019.115181 | ||||
Discovery of novel small molecule induced selective degradation of the bromodomain and extra-terminal (BET) bromodomain protein BRD4 and BRD2 with cellular potencies. Bioorg Med Chem. 2020 Jan 1;28(1):115181. PMID:31767403 DOI:10.1016/j.bmc.2019.115181 | ||||
Discovery of a new class of PROTAC BRD4 degraders based on a dihydroquinazolinone derivative and lenalidomide/pomalidomide. Bioorg Med Chem. 2020 Jan 1;28(1):115228. PMID:31813613 DOI:10.1016/j.bmc.2019.115228 | ||||
Discovery of a new class of PROTAC BRD4 degraders based on a dihydroquinazolinone derivative and lenalidomide/pomalidomide. Bioorg Med Chem. 2020 Jan 1;28(1):115228. PMID:31813613 DOI:10.1016/j.bmc.2019.115228 | ||||
Discovery of a new class of PROTAC BRD4 degraders based on a dihydroquinazolinone derivative and lenalidomide/pomalidomide. Bioorg Med Chem. 2020 Jan 1;28(1):115228. PMID:31813613 DOI:10.1016/j.bmc.2019.115228 | ||||
Discovery of a new class of PROTAC BRD4 degraders based on a dihydroquinazolinone derivative and lenalidomide/pomalidomide. Bioorg Med Chem. 2020 Jan 1;28(1):115228. PMID:31813613 DOI:10.1016/j.bmc.2019.115228 | ||||
Discovery of a new class of PROTAC BRD4 degraders based on a dihydroquinazolinone derivative and lenalidomide/pomalidomide. Bioorg Med Chem. 2020 Jan 1;28(1):115228. PMID:31813613 DOI:10.1016/j.bmc.2019.115228 | ||||
Discovery of a new class of PROTAC BRD4 degraders based on a dihydroquinazolinone derivative and lenalidomide/pomalidomide. Bioorg Med Chem. 2020 Jan 1;28(1):115228. PMID:31813613 DOI:10.1016/j.bmc.2019.115228 | ||||
Discovery of a new class of PROTAC BRD4 degraders based on a dihydroquinazolinone derivative and lenalidomide/pomalidomide. Bioorg Med Chem. 2020 Jan 1;28(1):115228. PMID:31813613 DOI:10.1016/j.bmc.2019.115228 | ||||
Discovery of a new class of PROTAC BRD4 degraders based on a dihydroquinazolinone derivative and lenalidomide/pomalidomide. Bioorg Med Chem. 2020 Jan 1;28(1):115228. PMID:31813613 DOI:10.1016/j.bmc.2019.115228 | ||||
Discovery of a new class of PROTAC BRD4 degraders based on a dihydroquinazolinone derivative and lenalidomide/pomalidomide. Bioorg Med Chem. 2020 Jan 1;28(1):115228. PMID:31813613 DOI:10.1016/j.bmc.2019.115228 | ||||
Discovery of a new class of PROTAC BRD4 degraders based on a dihydroquinazolinone derivative and lenalidomide/pomalidomide. Bioorg Med Chem. 2020 Jan 1;28(1):115228. PMID:31813613 DOI:10.1016/j.bmc.2019.115228 | ||||
Discovery of a new class of PROTAC BRD4 degraders based on a dihydroquinazolinone derivative and lenalidomide/pomalidomide. Bioorg Med Chem. 2020 Jan 1;28(1):115228. PMID:31813613 DOI:10.1016/j.bmc.2019.115228 | ||||
Discovery of a new class of PROTAC BRD4 degraders based on a dihydroquinazolinone derivative and lenalidomide/pomalidomide. Bioorg Med Chem. 2020 Jan 1;28(1):115228. PMID:31813613 DOI:10.1016/j.bmc.2019.115228 | ||||
Discovery of a new class of PROTAC BRD4 degraders based on a dihydroquinazolinone derivative and lenalidomide/pomalidomide. Bioorg Med Chem. 2020 Jan 1;28(1):115228. PMID:31813613 DOI:10.1016/j.bmc.2019.115228 | ||||
Discovery of a new class of PROTAC BRD4 degraders based on a dihydroquinazolinone derivative and lenalidomide/pomalidomide. Bioorg Med Chem. 2020 Jan 1;28(1):115228. PMID:31813613 DOI:10.1016/j.bmc.2019.115228 | ||||
Discovery of a new class of PROTAC BRD4 degraders based on a dihydroquinazolinone derivative and lenalidomide/pomalidomide. Bioorg Med Chem. 2020 Jan 1;28(1):115228. PMID:31813613 DOI:10.1016/j.bmc.2019.115228 | ||||
Discovery of a new class of PROTAC BRD4 degraders based on a dihydroquinazolinone derivative and lenalidomide/pomalidomide. Bioorg Med Chem. 2020 Jan 1;28(1):115228. PMID:31813613 DOI:10.1016/j.bmc.2019.115228 | ||||
Discovery of a new class of PROTAC BRD4 degraders based on a dihydroquinazolinone derivative and lenalidomide/pomalidomide. Bioorg Med Chem. 2020 Jan 1;28(1):115228. PMID:31813613 DOI:10.1016/j.bmc.2019.115228 | ||||
PHOTACs enable optical control of protein degradation. Sci Adv. 2020 Feb 21;6(8):eaay5064. PMID:32128406 DOI:10.1126/sciadv.aay5064 | ||||
PHOTACs enable optical control of protein degradation. Sci Adv. 2020 Feb 21;6(8):eaay5064. PMID:32128406 DOI:10.1126/sciadv.aay5064 | ||||
PHOTACs enable optical control of protein degradation. Sci Adv. 2020 Feb 21;6(8):eaay5064. PMID:32128406 DOI:10.1126/sciadv.aay5064 | ||||
PHOTACs enable optical control of protein degradation. Sci Adv. 2020 Feb 21;6(8):eaay5064. PMID:32128406 DOI:10.1126/sciadv.aay5064 | ||||
PHOTACs enable optical control of protein degradation. Sci Adv. 2020 Feb 21;6(8):eaay5064. PMID:32128406 DOI:10.1126/sciadv.aay5064 | ||||
PHOTACs enable optical control of protein degradation. Sci Adv. 2020 Feb 21;6(8):eaay5064. PMID:32128406 DOI:10.1126/sciadv.aay5064 | ||||
PHOTACs enable optical control of protein degradation. Sci Adv. 2020 Feb 21;6(8):eaay5064. PMID:32128406 DOI:10.1126/sciadv.aay5064 | ||||
PHOTACs enable optical control of protein degradation. Sci Adv. 2020 Feb 21;6(8):eaay5064. PMID:32128406 DOI:10.1126/sciadv.aay5064 | ||||
PHOTACs enable optical control of protein degradation. Sci Adv. 2020 Feb 21;6(8):eaay5064. PMID:32128406 DOI:10.1126/sciadv.aay5064 | ||||
PHOTACs enable optical control of protein degradation. Sci Adv. 2020 Feb 21;6(8):eaay5064. PMID:32128406 DOI:10.1126/sciadv.aay5064 | ||||
PHOTACs enable optical control of protein degradation. Sci Adv. 2020 Feb 21;6(8):eaay5064. PMID:32128406 DOI:10.1126/sciadv.aay5064 | ||||
PHOTACs enable optical control of protein degradation. Sci Adv. 2020 Feb 21;6(8):eaay5064. PMID:32128406 DOI:10.1126/sciadv.aay5064 | ||||
PHOTACs enable optical control of protein degradation. Sci Adv. 2020 Feb 21;6(8):eaay5064. PMID:32128406 DOI:10.1126/sciadv.aay5064 | ||||
Development of small-molecule BRD4 degraders based on pyrrolopyridone derivative. Bioorg Chem. 2020 Jun;99:103817. PMID:32361153 DOI:10.1016/j.bioorg.2020.103817 | ||||
Development of small-molecule BRD4 degraders based on pyrrolopyridone derivative. Bioorg Chem. 2020 Jun;99:103817. PMID:32361153 DOI:10.1016/j.bioorg.2020.103817 | ||||
Development of small-molecule BRD4 degraders based on pyrrolopyridone derivative. Bioorg Chem. 2020 Jun;99:103817. PMID:32361153 DOI:10.1016/j.bioorg.2020.103817 | ||||
Development of small-molecule BRD4 degraders based on pyrrolopyridone derivative. Bioorg Chem. 2020 Jun;99:103817. PMID:32361153 DOI:10.1016/j.bioorg.2020.103817 |