| Assay ID | Title | Year | Journal | Article |
|---|
| AID1853506 | Co-operativity factor, ratio of Ki for displacement of (2S,4R)-N-(4-bromobenzyl)-4-hydroxy-1-(3,3,3-trifluoropropanoyl)pyrrolidine-2-carboxamide from VBC E3 ligase (unknown origin) binary complex assessed as inhibition constant to Ki for displacement of ( | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| Estimating the cooperativity of PROTAC-induced ternary complexes using |
| AID1853517 | Co-operativity factor, ratio of Ki for displacement of (2S,4R)-N-(4-bromobenzyl)-4-hydroxy-1-(3,3,3-trifluoropropanoyl)pyrrolidine-2-carboxamide from VBC E3 ligase (unknown origin) binary complex assessed as inhibition constant to Ki for displacement of ( | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| Estimating the cooperativity of PROTAC-induced ternary complexes using |
| AID1853496 | Displacement of (2S,4R)-N-(4-bromobenzyl)-4-hydroxy-1-(3,3,3-trifluoropropanoyl)pyrrolidine-2-carboxamide from BRD2 bromodomain 1/VBC E3 ligase (unknown origin) ternary complex assessed as inhibition constant by 19F NMR assay | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| Estimating the cooperativity of PROTAC-induced ternary complexes using |
| AID1853525 | Co-operativity factor, ratio of Ki for displacement of (2S,4R)-N-(4-bromobenzyl)-4-hydroxy-1-(3,3,3-trifluoropropanoyl)pyrrolidine-2-carboxamide from VBC E3 ligase (unknown origin) binary complex assessed as inhibition constant to Ki for displacement of ( | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| Estimating the cooperativity of PROTAC-induced ternary complexes using |
| AID1853520 | Co-operativity factor, ratio of Ki for displacement of (2S,4R)-N-(4-bromobenzyl)-4-hydroxy-1-(3,3,3-trifluoropropanoyl)pyrrolidine-2-carboxamide from VBC E3 ligase (unknown origin) binary complex assessed as inhibition constant to Ki for displacement of ( | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| Estimating the cooperativity of PROTAC-induced ternary complexes using |
| AID1853504 | Co-operativity factor, ratio of Ki for displacement of (2S,4R)-N-(4-bromobenzyl)-4-hydroxy-1-(3,3,3-trifluoropropanoyl)pyrrolidine-2-carboxamide from VBC E3 ligase (unknown origin) binary complex assessed as inhibition constant to Ki for displacement of ( | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| Estimating the cooperativity of PROTAC-induced ternary complexes using |
| AID1387965 | Binding affinity to N-terminal His6-tagged recombinant human VHL (54 to 213 residues)/elongin C (17 to 112 residues)/elongin B (1 to 104 residues) expressed in Escherichia coli BL21 (DE3) assessed as compound binary complex formation by isothermal titrati | 2018 | Journal of medicinal chemistry, 01-25, Volume: 61, Issue:2
| 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. |
| AID1387962 | Proteolysis targeting chimera activity in human HL60 cells assessed as induction of VCB-mediated delivery of BRD4 for protein degradation by proteasome by measuring cellular protein depletion at 50 nM incubated for 4 hrs by Western blotting method | 2018 | Journal of medicinal chemistry, 01-25, Volume: 61, Issue:2
| 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. |
| AID1387953 | Proteolysis targeting chimera activity in human HeLa cells assessed as induction of VCB-mediated delivery of BRD2 for protein degradation by proteasome by measuring drug level causing 50% cellular protein depletion incubated for 24 hrs by Western blotting | 2018 | Journal of medicinal chemistry, 01-25, Volume: 61, Issue:2
| 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. |
| AID1853501 | Displacement of (2S,4R)-N-(4-bromobenzyl)-4-hydroxy-1-(3,3,3-trifluoropropanoyl)pyrrolidine-2-carboxamide from BRD4 bromodomain 2/VBC E3 ligase (unknown origin) ternary complex assessed as inhibition constant by 19F NMR assay | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| Estimating the cooperativity of PROTAC-induced ternary complexes using |
| AID1589950 | Protac activity at VHL/BRD4 in human HeLa cells assessed as induction of BRD4 protein degradation at 50 nM up to 36 hrs by Western blot analysis relative to control | 2019 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 29, Issue:13
| Proteolysis targeting chimeras (PROTACs) in 'beyond rule-of-five' chemical space: Recent progress and future challenges. |
| AID1853522 | Co-operativity factor, ratio of Ki for displacement of (2S,4R)-N-(4-bromobenzyl)-4-hydroxy-1-(3,3,3-trifluoropropanoyl)pyrrolidine-2-carboxamide from VBC E3 ligase (unknown origin) binary complex assessed as inhibition constant to Ki for displacement of ( | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| Estimating the cooperativity of PROTAC-induced ternary complexes using |
| AID1387844 | Solubility of the compound in PBS | 2018 | Journal of medicinal chemistry, 01-25, Volume: 61, Issue:2
| A "Click Chemistry Platform" for the Rapid Synthesis of Bispecific Molecules for Inducing Protein Degradation. |
| AID1409607 | IC50 for antiviral activity against SARS-CoV-2 in the Vero E6 cell line at 48 h by immunofluorescence-based assay (detecting the viral NP protein in the nucleus of the Vero E6 cells). | 2020 | Nature, 07, Volume: 583, Issue:7816
| A SARS-CoV-2 protein interaction map reveals targets for drug repurposing. |
| AID1850524 | Thermodynamic solubility of the compound in phosphate buffer at pH 7 incubated for 1 hr by shake flask based HPLC-UV analysis | | | |
| AID1853507 | Co-operativity factor, ratio of Ki for displacement of (2S,4R)-N-(4-bromobenzyl)-4-hydroxy-1-(3,3,3-trifluoropropanoyl)pyrrolidine-2-carboxamide from VBC E3 ligase (unknown origin) binary complex assessed as inhibition constant to Ki for displacement of ( | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| Estimating the cooperativity of PROTAC-induced ternary complexes using |
| AID1830813 | AUC (0 to infinity) in C57BL/6 mouse at 5 mg/kg, sc measured up to 8 hrs by LC-MS analysis | 2021 | Journal of medicinal chemistry, 10-28, Volume: 64, Issue:20
| Development of BromoTag: A "Bump-and-Hole"-PROTAC System to Induce Potent, Rapid, and Selective Degradation of Tagged Target Proteins. |
| AID1387964 | Binding affinity to N-terminal His6-tagged recombinant human Brd4 BD2 expressed in Escherichia coli BL21 (DE3) assessed as compound binary complex formation by isothermal titration calorimetry-based assay | 2018 | Journal of medicinal chemistry, 01-25, Volume: 61, Issue:2
| 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. |
| AID1830816 | Cmax in C57BL/6 mouse at 5 mg/kg, sc measured up to 8 hrs by LC-MS analysis | 2021 | Journal of medicinal chemistry, 10-28, Volume: 64, Issue:20
| Development of BromoTag: A "Bump-and-Hole"-PROTAC System to Induce Potent, Rapid, and Selective Degradation of Tagged Target Proteins. |
| AID1830815 | Tmax in C57BL/6 mouse at 5 mg/kg, sc measured up to 8 hrs by LC-MS analysis | 2021 | Journal of medicinal chemistry, 10-28, Volume: 64, Issue:20
| Development of BromoTag: A "Bump-and-Hole"-PROTAC System to Induce Potent, Rapid, and Selective Degradation of Tagged Target Proteins. |
| AID1853526 | Displacement of (2S,4R)-N-(4-bromobenzyl)-4-hydroxy-1-(3,3,3-trifluoropropanoyl)pyrrolidine-2-carboxamide from VBC E3 ligase (unknown origin) binary complex by 19F NMR assay | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| Estimating the cooperativity of PROTAC-induced ternary complexes using |
| AID1853502 | Co-operativity factor, ratio of Ki for displacement of (2S,4R)-N-(4-bromobenzyl)-4-hydroxy-1-(3,3,3-trifluoropropanoyl)pyrrolidine-2-carboxamide from VBC E3 ligase (unknown origin) binary complex assessed as inhibition constant to Ki for displacement of ( | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| Estimating the cooperativity of PROTAC-induced ternary complexes using |
| AID1853510 | Co-operativity factor, ratio of Ki for displacement of (2S,4R)-N-(4-bromobenzyl)-4-hydroxy-1-(3,3,3-trifluoropropanoyl)pyrrolidine-2-carboxamide from VBC E3 ligase (unknown origin) binary complex assessed as inhibition constant to Ki for displacement of ( | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| Estimating the cooperativity of PROTAC-induced ternary complexes using |
| AID1853513 | Co-operativity factor, ratio of Ki for displacement of (2S,4R)-N-(4-bromobenzyl)-4-hydroxy-1-(3,3,3-trifluoropropanoyl)pyrrolidine-2-carboxamide from VBC E3 ligase (unknown origin) binary complex assessed as inhibition constant to Ki for displacement of ( | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| Estimating the cooperativity of PROTAC-induced ternary complexes using |
| AID1853490 | Displacement of (2S,4R)-N-(4-bromobenzyl)-4-hydroxy-1-(3,3,3-trifluoropropanoyl)pyrrolidine-2-carboxamide from BRD2 bromodomain 1/VBC E3 ligase (unknown origin) ternary complex by 19F NMR assay | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| Estimating the cooperativity of PROTAC-induced ternary complexes using |
| AID1387963 | Proteolysis targeting chimera activity in human HL60 cells assessed as induction of VCB-mediated delivery of BRD4 for protein degradation by proteasome by measuring cellular cMyc protein depletion at 50 nM incubated for 4 hrs by Western blotting method | 2018 | Journal of medicinal chemistry, 01-25, Volume: 61, Issue:2
| 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. |
| AID1409609 | Cytotoxicity of compound against Vero E6 cells by MTT assay. | 2020 | Nature, 07, Volume: 583, Issue:7816
| A SARS-CoV-2 protein interaction map reveals targets for drug repurposing. |
| AID1387960 | Antiproliferative activity against human MV4-11 cells after 48 hrs by CellTiter-Glo luminescent cell viability assay | 2018 | Journal of medicinal chemistry, 01-25, Volume: 61, Issue:2
| 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. |
| AID1853519 | Co-operativity factor, ratio of Ki for displacement of (2S,4R)-N-(4-bromobenzyl)-4-hydroxy-1-(3,3,3-trifluoropropanoyl)pyrrolidine-2-carboxamide from VBC E3 ligase (unknown origin) binary complex assessed as inhibition constant to Ki for displacement of ( | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| Estimating the cooperativity of PROTAC-induced ternary complexes using |
| AID1813764 | Binding affinity to N-terminal His6-tagged VHL (54 to 213 residues) (unknown origin) expressed in Escherichia coli assessed as displacement of HIF-1alpha by binary binding competitive fluorescence polarization assay | 2021 | Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
| Amide-to-Ester Substitution as a Strategy for Optimizing PROTAC Permeability and Cellular Activity. |
| AID1387854 | Induction of human His-tagged VHL(1 to 154)/GST-tagged BRD4 (49 to 170 residues) interaction assessed as VHL/BRD4/compound complex formation preincubated for 60 mins and measured after 60 mins by luminescence based Alphascreen proximity assay relative to | 2018 | Journal of medicinal chemistry, 01-25, Volume: 61, Issue:2
| A "Click Chemistry Platform" for the Rapid Synthesis of Bispecific Molecules for Inducing Protein Degradation. |
| AID1387959 | Proteolysis targeting chimera activity in human HeLa cells assessed as induction of VCB-mediated delivery of BRD2 for protein degradation by proteasome by measuring drug level causing 50% cellular protein depletion incubated for 24 hrs by Western blotting | 2018 | Journal of medicinal chemistry, 01-25, Volume: 61, Issue:2
| 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. |
| AID1853514 | Co-operativity factor, ratio of Ki for displacement of (2S,4R)-N-(4-bromobenzyl)-4-hydroxy-1-(3,3,3-trifluoropropanoyl)pyrrolidine-2-carboxamide from VBC E3 ligase (unknown origin) binary complex assessed as inhibition constant to Ki for displacement of ( | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| Estimating the cooperativity of PROTAC-induced ternary complexes using |
| AID1830808 | Half life in C57BL/6 mouse at 5 mg/kg, iv measured up to 8 hrs by LC-MS analysis | 2021 | Journal of medicinal chemistry, 10-28, Volume: 64, Issue:20
| Development of BromoTag: A "Bump-and-Hole"-PROTAC System to Induce Potent, Rapid, and Selective Degradation of Tagged Target Proteins. |
| AID1387958 | Proteolysis targeting chimera activity in human HeLa cells assessed as induction of VCB-mediated delivery of BRD3 for protein degradation by proteasome by measuring drug level causing 50% cellular protein depletion incubated for 24 hrs by Western blotting | 2018 | Journal of medicinal chemistry, 01-25, Volume: 61, Issue:2
| 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. |
| AID1387955 | Antiproliferative activity against human HL60 cells after 48 hrs by CellTiter-Glo luminescent cell viability assay | 2018 | Journal of medicinal chemistry, 01-25, Volume: 61, Issue:2
| 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. |
| AID1853527 | Displacement of (2S,4R)-N-(4-bromobenzyl)-4-hydroxy-1-(3,3,3-trifluoropropanoyl)pyrrolidine-2-carboxamide from VBC E3 ligase (unknown origin) binary complex assessed as inhibition constant by 19F NMR assay | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| Estimating the cooperativity of PROTAC-induced ternary complexes using |
| AID1813760 | Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 24 hrs by Celltiter-Glo cell viability assay | 2021 | Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
| Amide-to-Ester Substitution as a Strategy for Optimizing PROTAC Permeability and Cellular Activity. |
| AID1387952 | Proteolysis targeting chimera activity in human HeLa cells assessed as induction of VCB-mediated delivery of BRD3 for protein degradation by proteasome by measuring drug level causing 50% cellular protein depletion incubated for 24 hrs by Western blotting | 2018 | Journal of medicinal chemistry, 01-25, Volume: 61, Issue:2
| 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. |
| AID1907467 | Protac activity at BRD4 short isoform in human MV4-11 cells assessed as recovery of BRD4S expression at 100 nM for 24 hrs by immunoblot analysis | 2022 | European journal of medicinal chemistry, Jun-05, Volume: 236 | Adjusted degradation of BRD4 S and BRD4 L based on fine structural modifications of the pyrrolopyridone scaffold. |
| AID1830807 | Volume of distribution at steady state in C57BL/6 mouse at 5 mg/kg, iv measured up to 8 hrs by LC-MS analysis | 2021 | Journal of medicinal chemistry, 10-28, Volume: 64, Issue:20
| Development of BromoTag: A "Bump-and-Hole"-PROTAC System to Induce Potent, Rapid, and Selective Degradation of Tagged Target Proteins. |
| AID1387951 | Proteolysis targeting chimera activity in human HeLa cells assessed as induction of VCB-mediated delivery of BRD4 long isoform for protein degradation by proteasome by measuring drug level causing 50% cellular protein depletion incubated for 24 hrs by Wes | 2018 | Journal of medicinal chemistry, 01-25, Volume: 61, Issue:2
| 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. |
| AID1853505 | Co-operativity factor, ratio of Ki for displacement of (2S,4R)-N-(4-bromobenzyl)-4-hydroxy-1-(3,3,3-trifluoropropanoyl)pyrrolidine-2-carboxamide from VBC E3 ligase (unknown origin) binary complex assessed as inhibition constant to Ki for displacement of ( | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| Estimating the cooperativity of PROTAC-induced ternary complexes using |
| AID1387956 | Proteolysis targeting chimera activity in human HeLa cells assessed as induction of VCB-mediated delivery of BRD4 short isoform for protein degradation by proteasome by measuring drug level causing 50% cellular protein depletion incubated for 24 hrs by We | 2018 | Journal of medicinal chemistry, 01-25, Volume: 61, Issue:2
| 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. |
| AID1830812 | AUC (0 to infinity) in C57BL/6 mouse at 5 mg/kg, iv measured up to 8 hrs by LC-MS analysis | 2021 | Journal of medicinal chemistry, 10-28, Volume: 64, Issue:20
| Development of BromoTag: A "Bump-and-Hole"-PROTAC System to Induce Potent, Rapid, and Selective Degradation of Tagged Target Proteins. |
| AID1853493 | Displacement of (2S,4R)-N-(4-bromobenzyl)-4-hydroxy-1-(3,3,3-trifluoropropanoyl)pyrrolidine-2-carboxamide from BRD3 bromodomain 2/VBC E3 ligase (unknown origin) ternary complex by 19F NMR assay | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| Estimating the cooperativity of PROTAC-induced ternary complexes using |
| AID1853512 | Co-operativity factor, ratio of Ki for displacement of (2S,4R)-N-(4-bromobenzyl)-4-hydroxy-1-(3,3,3-trifluoropropanoyl)pyrrolidine-2-carboxamide from VBC E3 ligase (unknown origin) binary complex assessed as inhibition constant to Ki for displacement of ( | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| Estimating the cooperativity of PROTAC-induced ternary complexes using |
| AID1853516 | Co-operativity factor, ratio of Ki for displacement of (2S,4R)-N-(4-bromobenzyl)-4-hydroxy-1-(3,3,3-trifluoropropanoyl)pyrrolidine-2-carboxamide from VBC E3 ligase (unknown origin) binary complex assessed as inhibition constant to Ki for displacement of ( | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| Estimating the cooperativity of PROTAC-induced ternary complexes using |
| AID1853500 | Displacement of (2S,4R)-N-(4-bromobenzyl)-4-hydroxy-1-(3,3,3-trifluoropropanoyl)pyrrolidine-2-carboxamide from BRD4 bromodomain 1/VBC E3 ligase (unknown origin) ternary complex assessed as inhibition constant by 19F NMR assay | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| Estimating the cooperativity of PROTAC-induced ternary complexes using |
| AID1853524 | Co-operativity factor, ratio of Ki for displacement of (2S,4R)-N-(4-bromobenzyl)-4-hydroxy-1-(3,3,3-trifluoropropanoyl)pyrrolidine-2-carboxamide from VBC E3 ligase (unknown origin) binary complex assessed as inhibition constant to Ki for displacement of ( | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| Estimating the cooperativity of PROTAC-induced ternary complexes using |
| AID1387957 | Proteolysis targeting chimera activity in human HeLa cells assessed as induction of VCB-mediated delivery of BRD4 long isoform for protein degradation by proteasome by measuring drug level causing 50% cellular protein depletion incubated for 24 hrs by Wes | 2018 | Journal of medicinal chemistry, 01-25, Volume: 61, Issue:2
| 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. |
| AID1387843 | Induction of CRBN/DDB1-mediated BRD4 protein degradation in human NCI-H661 cells assessed as drug level causing 50% cellular protein depletion incubated for 4 hrs by MSD assay | 2018 | Journal of medicinal chemistry, 01-25, Volume: 61, Issue:2
| A "Click Chemistry Platform" for the Rapid Synthesis of Bispecific Molecules for Inducing Protein Degradation. |
| AID1853509 | Co-operativity factor, ratio of Ki for displacement of (2S,4R)-N-(4-bromobenzyl)-4-hydroxy-1-(3,3,3-trifluoropropanoyl)pyrrolidine-2-carboxamide from VBC E3 ligase (unknown origin) binary complex assessed as inhibition constant to Ki for displacement of ( | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| Estimating the cooperativity of PROTAC-induced ternary complexes using |
| AID1853515 | Co-operativity factor, ratio of Ki for displacement of (2S,4R)-N-(4-bromobenzyl)-4-hydroxy-1-(3,3,3-trifluoropropanoyl)pyrrolidine-2-carboxamide from VBC E3 ligase (unknown origin) binary complex assessed as inhibition constant to Ki for displacement of ( | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| Estimating the cooperativity of PROTAC-induced ternary complexes using |
| AID1853508 | Co-operativity factor, ratio of Ki for displacement of (2S,4R)-N-(4-bromobenzyl)-4-hydroxy-1-(3,3,3-trifluoropropanoyl)pyrrolidine-2-carboxamide from VBC E3 ligase (unknown origin) binary complex assessed as inhibition constant to Ki for displacement of ( | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| Estimating the cooperativity of PROTAC-induced ternary complexes using |
| AID1853523 | Co-operativity factor, ratio of Ki for displacement of (2S,4R)-N-(4-bromobenzyl)-4-hydroxy-1-(3,3,3-trifluoropropanoyl)pyrrolidine-2-carboxamide from VBC E3 ligase (unknown origin) binary complex assessed as inhibition constant to Ki for displacement of ( | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| Estimating the cooperativity of PROTAC-induced ternary complexes using |
| AID1724645 | Permeability of the compound in phosphate buffer containing 5% DMSO at pH 7.4 incubated for 15 hrs by PAMPA based LC/MS analysis | 2020 | ACS medicinal chemistry letters, Sep-10, Volume: 11, Issue:9
| Understanding and Improving the Membrane Permeability of VH032-Based PROTACs. |
| AID1813759 | Protac activity at VHL/Brd2 in HEK293 cells assessed as Brd2 degradation after 4 hrs by Western blotting analysis | 2021 | Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
| Amide-to-Ester Substitution as a Strategy for Optimizing PROTAC Permeability and Cellular Activity. |
| AID1387966 | Induction of interaction of N-terminal His6-tagged recombinant human VHL (54 to 213 residues)/elongin C (17 to 112 residues)/elongin B (1 to 104 residues) co-expressed in Escherichia coli BL21 (DE3) with recombinant human Brd4 BD2 assessed as VCB/BRD4/com | 2018 | Journal of medicinal chemistry, 01-25, Volume: 61, Issue:2
| 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. |
| AID1853511 | Co-operativity factor, ratio of Ki for displacement of (2S,4R)-N-(4-bromobenzyl)-4-hydroxy-1-(3,3,3-trifluoropropanoyl)pyrrolidine-2-carboxamide from VBC E3 ligase (unknown origin) binary complex assessed as inhibition constant to Ki for displacement of ( | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| Estimating the cooperativity of PROTAC-induced ternary complexes using |
| AID1853503 | Co-operativity factor, ratio of Ki for displacement of (2S,4R)-N-(4-bromobenzyl)-4-hydroxy-1-(3,3,3-trifluoropropanoyl)pyrrolidine-2-carboxamide from VBC E3 ligase (unknown origin) binary complex assessed as inhibition constant to Ki for displacement of ( | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| Estimating the cooperativity of PROTAC-induced ternary complexes using |
| AID1830806 | Clearance in C57BL/6 mouse at 5 mg/kg, iv measured up to 8 hrs by LC-MS analysis | 2021 | Journal of medicinal chemistry, 10-28, Volume: 64, Issue:20
| Development of BromoTag: A "Bump-and-Hole"-PROTAC System to Induce Potent, Rapid, and Selective Degradation of Tagged Target Proteins. |
| AID1387846 | Solubility of the compound in 0.01 N HCl | 2018 | Journal of medicinal chemistry, 01-25, Volume: 61, Issue:2
| A "Click Chemistry Platform" for the Rapid Synthesis of Bispecific Molecules for Inducing Protein Degradation. |
| AID1387856 | Proteolysis targeting chimera activity in human HeLa cells assessed as induction of VHL-mediated delivery of BRD4 for protein degradation by proteasome by measuring drug level causing 50% cellular protein depletion incubated for 24 hrs by Western blot ana | 2018 | Journal of medicinal chemistry, 01-25, Volume: 61, Issue:2
| A "Click Chemistry Platform" for the Rapid Synthesis of Bispecific Molecules for Inducing Protein Degradation. |
| AID1853494 | Displacement of (2S,4R)-N-(4-bromobenzyl)-4-hydroxy-1-(3,3,3-trifluoropropanoyl)pyrrolidine-2-carboxamide from BRD4 bromodomain 1/VBC E3 ligase (unknown origin) ternary complex by 19F NMR assay | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| Estimating the cooperativity of PROTAC-induced ternary complexes using |
| AID1589949 | Protac activity at VHL/BRD4 in human HeLa cells assessed as induction of BRD4 protein degradation incubated for 24 hrs by Western blot analysis | 2019 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 29, Issue:13
| Proteolysis targeting chimeras (PROTACs) in 'beyond rule-of-five' chemical space: Recent progress and future challenges. |
| AID1409614 | Overall antiviral activity against SARS-CoV-2 (isolate France/IDF0372/2020) in the Vero E6 cell line at 48 h based on three assays 1) detection of viral RNA by qRT-PCR (targeting the N-gene), 2) plaque assay using lysate 3 days after addition of compound | 2020 | Nature, 07, Volume: 583, Issue:7816
| A SARS-CoV-2 protein interaction map reveals targets for drug repurposing. |
| AID1853495 | Displacement of (2S,4R)-N-(4-bromobenzyl)-4-hydroxy-1-(3,3,3-trifluoropropanoyl)pyrrolidine-2-carboxamide from BRD4 bromodomain 2/VBC E3 ligase (unknown origin) ternary complex by 19F NMR assay | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| Estimating the cooperativity of PROTAC-induced ternary complexes using |
| AID1387954 | Proteolysis targeting chimera activity in human MV4-11 cells assessed as induction of VCB-mediated delivery of BRD4 for protein degradation by proteasome by measuring cellular protein depletion at 50 nM incubated for 4 hrs by Western blotting method | 2018 | Journal of medicinal chemistry, 01-25, Volume: 61, Issue:2
| 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. |
| AID1813758 | Protac activity at VHL/Brd3 in HEK293 cells assessed as Brd3 degradation after 4 hrs by Western blotting analysis | 2021 | Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
| Amide-to-Ester Substitution as a Strategy for Optimizing PROTAC Permeability and Cellular Activity. |
| AID1387845 | Solubility of the compound in fasted state simulated intestinal fluid | 2018 | Journal of medicinal chemistry, 01-25, Volume: 61, Issue:2
| A "Click Chemistry Platform" for the Rapid Synthesis of Bispecific Molecules for Inducing Protein Degradation. |
| AID1830814 | MRT (0 to infinity) in C57BL/6 mouse at 5 mg/kg, sc measured up to 8 hrs by LC-MS analysis | 2021 | Journal of medicinal chemistry, 10-28, Volume: 64, Issue:20
| Development of BromoTag: A "Bump-and-Hole"-PROTAC System to Induce Potent, Rapid, and Selective Degradation of Tagged Target Proteins. |
| AID1409613 | Selectivity ratio: ratio of AUC (viral infection %) of SARS-CoV-2 in the Vero E6 cell line compared to AUC (cytotoxicity %) of compound against Vero E6 cells by MTT assay. | 2020 | Nature, 07, Volume: 583, Issue:7816
| A SARS-CoV-2 protein interaction map reveals targets for drug repurposing. |
| AID1853492 | Displacement of (2S,4R)-N-(4-bromobenzyl)-4-hydroxy-1-(3,3,3-trifluoropropanoyl)pyrrolidine-2-carboxamide from BRD3 bromodomain 1/VBC E3 ligase (unknown origin) ternary complex by 19F NMR assay | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| Estimating the cooperativity of PROTAC-induced ternary complexes using |
| AID1813763 | Binding affinity to N-terminal His6-tagged VHL (54 to 213 residues)/BRD4 BD2 (333 to 460 residues) (unknown origin) expressed in Escherichia coli assessed as displacement of HIF-1alpha preincubated with Brd4 BD2 by ternary binding competitive fluorescence | 2021 | Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
| Amide-to-Ester Substitution as a Strategy for Optimizing PROTAC Permeability and Cellular Activity. |
| AID1813757 | Protac activity at VHL/Brd4 in HEK293 cells assessed as Brd4 degradation after 4 hrs by Western blotting analysis | 2021 | Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
| Amide-to-Ester Substitution as a Strategy for Optimizing PROTAC Permeability and Cellular Activity. |
| AID1409608 | AUC (viral infection %) for SARS-CoV-2 in the Vero E6 cell line at 48 h by immunofluorescence-based assay (detecting the viral NP protein in the nucleus of the Vero E6 cells). | 2020 | Nature, 07, Volume: 583, Issue:7816
| A SARS-CoV-2 protein interaction map reveals targets for drug repurposing. |
| AID1409611 | AUC (cytotoxicity %) of compound against Vero E6 cells by MTT assay. | 2020 | Nature, 07, Volume: 583, Issue:7816
| A SARS-CoV-2 protein interaction map reveals targets for drug repurposing. |
| AID1853498 | Displacement of (2S,4R)-N-(4-bromobenzyl)-4-hydroxy-1-(3,3,3-trifluoropropanoyl)pyrrolidine-2-carboxamide from BRD3 bromodomain 1/VBC E3 ligase (unknown origin) ternary complex assessed as inhibition constant by 19F NMR assay | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| Estimating the cooperativity of PROTAC-induced ternary complexes using |
| AID1853521 | Co-operativity factor, ratio of Ki for displacement of (2S,4R)-N-(4-bromobenzyl)-4-hydroxy-1-(3,3,3-trifluoropropanoyl)pyrrolidine-2-carboxamide from VBC E3 ligase (unknown origin) binary complex assessed as inhibition constant to Ki for displacement of ( | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| Estimating the cooperativity of PROTAC-induced ternary complexes using |
| AID1813762 | Permeability of the compound in PBS at pH 7.4 after 16 hrs by PAMPA | 2021 | Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
| Amide-to-Ester Substitution as a Strategy for Optimizing PROTAC Permeability and Cellular Activity. |
| AID1853518 | Co-operativity factor, ratio of Ki for displacement of (2S,4R)-N-(4-bromobenzyl)-4-hydroxy-1-(3,3,3-trifluoropropanoyl)pyrrolidine-2-carboxamide from VBC E3 ligase (unknown origin) binary complex assessed as inhibition constant to Ki for displacement of ( | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| Estimating the cooperativity of PROTAC-induced ternary complexes using |
| AID1387961 | Proteolysis targeting chimera activity in human MV4-11 cells assessed as induction of VCB-mediated delivery of BRD4 for protein degradation by proteasome by measuring cellular cMyc protein depletion at 50 nM incubated for 4 hrs by Western blotting method | 2018 | Journal of medicinal chemistry, 01-25, Volume: 61, Issue:2
| 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. |
| AID1813761 | Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell viability incubated for 72 hrs by Celltiter-Glo cell viability assay | 2021 | Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
| Amide-to-Ester Substitution as a Strategy for Optimizing PROTAC Permeability and Cellular Activity. |
| AID1830809 | Half life in C57BL/6 mouse at 5 mg/kg, sc measured up to 8 hrs by LC-MS analysis | 2021 | Journal of medicinal chemistry, 10-28, Volume: 64, Issue:20
| Development of BromoTag: A "Bump-and-Hole"-PROTAC System to Induce Potent, Rapid, and Selective Degradation of Tagged Target Proteins. |
| AID1387950 | Proteolysis targeting chimera activity in human HeLa cells assessed as induction of VCB-mediated delivery of BRD4 short isoform for protein degradation by proteasome by measuring drug level causing 50% cellular protein depletion incubated for 24 hrs by We | 2018 | Journal of medicinal chemistry, 01-25, Volume: 61, Issue:2
| 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. |
| AID1853499 | Displacement of (2S,4R)-N-(4-bromobenzyl)-4-hydroxy-1-(3,3,3-trifluoropropanoyl)pyrrolidine-2-carboxamide from BRD3 bromodomain 2/VBC E3 ligase (unknown origin) ternary complex assessed as inhibition constant by 19F NMR assay | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| Estimating the cooperativity of PROTAC-induced ternary complexes using |
| AID1853491 | Displacement of (2S,4R)-N-(4-bromobenzyl)-4-hydroxy-1-(3,3,3-trifluoropropanoyl)pyrrolidine-2-carboxamide from BRD2 bromodomain 2/VBC E3 ligase (unknown origin) ternary complex by 19F NMR assay | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| Estimating the cooperativity of PROTAC-induced ternary complexes using |
| AID1830817 | Bioavailability in C57BL/6 mouse at 5 mg/kg, sc measured up to 8 hrs by LC-MS analysis | 2021 | Journal of medicinal chemistry, 10-28, Volume: 64, Issue:20
| Development of BromoTag: A "Bump-and-Hole"-PROTAC System to Induce Potent, Rapid, and Selective Degradation of Tagged Target Proteins. |
| AID1724644 | Partition coefficient, logD of the compound in 1,9-decadiene and phosphate buffer at pH 7.4 measured after 30 mins under shaking condition by LC-MS analysis | 2020 | ACS medicinal chemistry letters, Sep-10, Volume: 11, Issue:9
| Understanding and Improving the Membrane Permeability of VH032-Based PROTACs. |
| AID1853497 | Displacement of (2S,4R)-N-(4-bromobenzyl)-4-hydroxy-1-(3,3,3-trifluoropropanoyl)pyrrolidine-2-carboxamide from BRD2 bromodomain 2/VBC E3 ligase (unknown origin) ternary complex assessed as inhibition constant by 19F NMR assay | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| Estimating the cooperativity of PROTAC-induced ternary complexes using |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |