| Assay ID | Title | Year | Journal | Article |
|---|
| AID1359762 | Antiproliferative activity against human LNCAP cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer. |
| AID1368370 | Cytotoxicity against human Loucy cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay | 2018 | Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1
| Exploiting a water network to achieve enthalpy-driven, bromodomain-selective BET inhibitors. |
| AID1286358 | Binding affinity to human His6-tagged BRD2 bromodomain 1 (K77 to N194 residues) expressed in Escherichia coli BL21(DE3) cells at 200 uM incubated for 30 mins by SYPRO orange staining based fluorescence thermal shift assay | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Discovery of Benzo[cd]indol-2(1H)-ones as Potent and Specific BET Bromodomain Inhibitors: Structure-Based Virtual Screening, Optimization, and Biological Evaluation. |
| AID1690279 | Antitumour activity against human MV4-11 cells xenografted in NOD-SCID mouse assessed as tumour growth inhibition at 50 mg/kg, po for 18 days by vernier caliper method relative to control | 2020 | European journal of medicinal chemistry, Apr-01, Volume: 191 | Design, synthesis, and biological evaluation of 4,5-dihydro-[1,2,4]triazolo[4,3-f]pteridine derivatives as novel dual-PLK1/BRD4 inhibitors. |
| AID1821747 | Binding affinity to human BRD4 BD1 E151A mutant assessed as change in melting temperature at 6:8 compound to protein ratio by thermal shift assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site. |
| AID1357993 | Inhibition of BRD2 BD1 (unknown origin) after 1 hr by TR-FRET assay | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation. |
| AID1878584 | Antiproliferative activity against human SW1990 cells assessed as inhibition of cell growth measured after 5 days by MTT assay | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1371236 | Growth inhibition of human MOLM13 cells after 4 days by WST-8 assay | 2017 | Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
| Structure-Based Discovery of 4-(6-Methoxy-2-methyl-4-(quinolin-4-yl)-9H-pyrimido[4,5-b]indol-7-yl)-3,5-dimethylisoxazole (CD161) as a Potent and Orally Bioavailable BET Bromodomain Inhibitor. |
| AID1664731 | Cell cycle arrest in human MV4-11 cells assessed as accumulation at G2/M phase at 0.5 uM after 12 hrs by propidium iodide staining based flow cytometric analysis (Rvb = 18.19%) | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15
| Design, synthesis and biological evaluation of novel 6-phenyl-1,3a,4,10b-tetrahydro-2H-benzo[c]thiazolo[4,5-e]azepin-2-one derivatives as potential BRD4 inhibitors. |
| AID1821729 | Binding affinity BRD3 BD2 (unknown origin) incubated for 1 hr by TR-FRET assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site. |
| AID1762765 | Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation at 2 uM incubated for 48 hrs by MTT assay relative to control | 2021 | Bioorganic & medicinal chemistry, 06-01, Volume: 39 | Discovery of 3,5-dimethylisoxazole derivatives as novel, potent inhibitors for bromodomain and extraterminal domain (BET) family. |
| AID1905948 | Inhibition of C-terminal His6-tagged BRD4 BD2 (unknown origin) using H-YSGRGK(Ac)GGK(Ac)GLGK(Ac)-GGAK(Ac)RHRK-Biotin-OH as substrate incubated for 1 hrs by HTRF assay | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
| Structure-Based Discovery and Optimization of Furo[3,2- |
| AID1821713 | Binding affinity to wild type human BRD4 BD1 (44 to 168 residues) assessed as change in melting temperature at 1:3 compound to protein ratio by thermal shift assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site. |
| AID1409978 | Binding affinity to human His6-tagged BRD4 BD1 (N44 to E168 residues) expressed in Escherichia coli BL21 (DE3) cells assessed as change in melting temperature at 200 uM after 30 mins by SYPRO Orange-dye based fluorescence thermal shift assay | 2018 | ACS medicinal chemistry letters, Mar-08, Volume: 9, Issue:3
| Y08060: A Selective BET Inhibitor for Treatment of Prostate Cancer. |
| AID1547271 | Inhibition of HDAC7 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
| Discovery of Thieno[2,3- |
| AID1807759 | Inhibition of PLK1 in HEK293T cells assessed as reduction in phosphorylation of TCTP at S46 residue at 30 to 100 nM incubated for 6 hrs by immunoblotting analysis | 2021 | Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
| Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors. |
| 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. |
| AID1229998 | Displacement of FAM-labeled ZBA248 from BRD4 BD2 (333 to 460 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay | 2015 | Journal of medicinal chemistry, Jun-25, Volume: 58, Issue:12
| Structure-Based Design of γ-Carboline Analogues as Potent and Specific BET Bromodomain Inhibitors. |
| AID1535636 | Antitumor activity against human MM1S cells xenografted in mouse assessed as tumor growth inhibition at 50 mg/kg, ip administered once daily for 14 days relative to control | 2019 | Bioorganic & medicinal chemistry, 02-01, Volume: 27, Issue:3
| Structure-guided discovery of a novel, potent, and orally bioavailable 3,5-dimethylisoxazole aryl-benzimidazole BET bromodomain inhibitor. |
| AID1664734 | Cell cycle arrest in human MV4-11 cells assessed as accumulation at G2/M phase at 5 uM after 12 hrs by propidium iodide staining based flow cytometric analysis (Rvb = 18.19%) | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15
| Design, synthesis and biological evaluation of novel 6-phenyl-1,3a,4,10b-tetrahydro-2H-benzo[c]thiazolo[4,5-e]azepin-2-one derivatives as potential BRD4 inhibitors. |
| AID1359756 | Binding affinity to His6-tagged human BAZ2B (S1858 to S1972 residues) expressed in Escherichia coli BL21(DE3) assessed as change in melting temperature at 200 uM by SYPRO orange dye based fluorescence assay | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer. |
| AID1242390 | Cytotoxicity against human MV4-11 cells after 24 hrs by CellTiter-Blue assay | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7
| BRD4 Structure-Activity Relationships of Dual PLK1 Kinase/BRD4 Bromodomain Inhibitor BI-2536. |
| AID1821861 | Inhibition of BRD3 D1 (unknown origin) by competitive fluorescence anisotropy assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| A Structure-based Design Approach for Generating High Affinity BRD4 D1-Selective Chemical Probes. |
| AID1196541 | Growth inhibition of human MV4-11 cells after 72 hrs by SRB assay | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
| Fragment-based drug discovery of 2-thiazolidinones as BRD4 inhibitors: 2. Structure-based optimization. |
| AID1400167 | Inhibition of N-terminal His-tagged BRD4 (BD1) (unknown origin) using biotinylated tetra-acetylated histone H4 peptide after 30 mins by alpha-screen assay | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
| Design and Characterization of Novel Covalent Bromodomain and Extra-Terminal Domain (BET) Inhibitors Targeting a Methionine. |
| AID1371238 | Inhibition of FAM-labeled ZBA248 binding to recombinant human N-terminal His6-tagged BRD4 bromodomain 2 (333 to 460 residues) expressed in Rosetta2 DE3 cells after 30 mins by Flourescence polarization assay | 2017 | Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
| Structure-Based Discovery of 4-(6-Methoxy-2-methyl-4-(quinolin-4-yl)-9H-pyrimido[4,5-b]indol-7-yl)-3,5-dimethylisoxazole (CD161) as a Potent and Orally Bioavailable BET Bromodomain Inhibitor. |
| AID1718523 | Growth inhibition of human HL60 cells after 72 hrs by CellTiter 96S AQeous non-radioactive cell proliferation assay | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24
| 4-Acyl Pyrroles as Dual BET-BRD7/9 Bromodomain Inhibitors Address BETi Insensitive Human Cancer Cell Lines. |
| AID1544786 | Induction of cell cycle arrest in human MV4-11 cells assessed as accumulation at G1 phase incubated for 24 hrs by propidium iodide staining based flow cytometry | 2019 | Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
| Design, synthesis and biological evaluation of novel 4,5-dihydro-[1,2,4]triazolo[4,3-f]pteridine derivatives as potential BRD4 inhibitors. |
| AID1387967 | Proteolysis targeting chimera activity in human HeLa cells assessed as induction of VCB-mediated delivery of BRD4 short isoform for protein degradation by proteasome at 30 to 10000 nM incubated for 24 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. |
| AID1878713 | Effect on FOXM1 gene expression in human SW1990 cells at 4 uM by Q-PCR analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1196546 | Binding affinity to BRG1 (unknown origin) assessed as increase in protein melting temperature at 50 umol by real-time PCR system based thermal shift assay | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
| Fragment-based drug discovery of 2-thiazolidinones as BRD4 inhibitors: 2. Structure-based optimization. |
| AID1905964 | Binding affinity to TAF1 BD2 (unknown origin) assessed as change in melting temperature at 100 uM incubated for 30 mins by thermal shift assay | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
| Structure-Based Discovery and Optimization of Furo[3,2- |
| AID1462230 | Inhibition of BRD4 (unknown origin) | 2017 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
| Structure-based design, synthesis and in vitro antiproliferative effects studies of novel dual BRD4/HDAC inhibitors. |
| AID1831220 | Induction of apoptosis in human SW1990 cells assessed as necrotic cells at 1 uM after 4 days in presence of 3 uM Olaparib by Annexin V-FITC and propidium iodide staining based flow cytometry (Rvb = 1.89%) | | | |
| AID1831272 | Induction of DNA damage in human SW1990 cells assessed as tail DNA at 1 uM incubated for 4 days in presence of 3 uM Olaparib by comet assay | | | |
| AID1831154 | Inhibition of recombinant BRD2 BD2 (unknown origin) incubated for 120 mins by TR-FRET assay | | | |
| AID1368367 | Cytotoxicity against human NALM6 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay | 2018 | Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1
| Exploiting a water network to achieve enthalpy-driven, bromodomain-selective BET inhibitors. |
| AID1460619 | Inhibition of recombinant human His6-tagged BRD4 bromodomain 1 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells preincubated for 30 mins followed by H4K5acK8acK12acK16ac peptide substrate addition after 30 mins by alphascreen assay | 2017 | Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
| Drug Discovery Targeting Bromodomain-Containing Protein 4. |
| AID1359764 | Antiproliferative activity against human 22Rv1 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer. |
| AID1286365 | Binding affinity to human His6-tagged TAF1 bromodomain 1 (R1377 to D1503 residues) expressed in Escherichia coli BL21(DE3) cells at 200 uM incubated for 30 mins by SYPRO orange staining based fluorescence thermal shift assay | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Discovery of Benzo[cd]indol-2(1H)-ones as Potent and Specific BET Bromodomain Inhibitors: Structure-Based Virtual Screening, Optimization, and Biological Evaluation. |
| AID1831199 | Toxicity in BALB/c mouse xenografted with human SW1990 cells assessed as heart damage at 15 mg/kg, ip administered for 28 consecutive days in presence of 45 mg/kg Olaparib | | | |
| AID1559432 | Displacement of tetra-acetylated histone H4 peptide (1-21) from recombinant human N-terminal His-tagged BRD4 BD2 (349 to 460 residues) expressed in Escherichia coli incubated for 30 mins followed by further incubation with tetra-acetylated histone H4 pept | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Discovery of Benzo[ |
| AID1878605 | Toxicity in nude mouse xenografted with human SW1990 cells assessed as liver damage at 15 mg/kg, ip administered for 28 days in presence of 45 mg/kg Olaparib by H and E staining based fluorescence microscopic analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1881930 | Inhibition of recombinant his tagged BRD4 BD1 (unknown origin) by Alpha screen assay | | | |
| AID1594421 | Inhibition of BRD4 in human HLF1 cells assessed as reduction in collagen-1 protein expression at 10 uM measured after 24 hrs by Western blot analysis | 2019 | Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
| Binding pocket-based design, synthesis and biological evaluation of novel selective BRD4-BD1 inhibitors. |
| AID1878596 | Inhibition of colony formation in human SW1990 cells at 0.5 uM incubated for 14 days in presence of 1.5 uM Olaparib by crystal violet staining based microscopic analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1652229 | Displacement of APC-labeled biotinylated-avidin from Euphorium-chelated recombinant human BRD4 bromodomain 1 expressed in Escherichia coli preincubated for 15 mins followed by APC-labeled biotinylated-avidin addition and measured after 1 hr under dark con | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
| Novel Pyrrolopyridone Bromodomain and Extra-Terminal Motif (BET) Inhibitors Effective in Endocrine-Resistant ER+ Breast Cancer with Acquired Resistance to Fulvestrant and Palbociclib. |
| AID1762764 | Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation at 2 uM incubated for 48 hrs by MTT assay relative to control | 2021 | Bioorganic & medicinal chemistry, 06-01, Volume: 39 | Discovery of 3,5-dimethylisoxazole derivatives as novel, potent inhibitors for bromodomain and extraterminal domain (BET) family. |
| AID1762762 | Cytotoxicity against human MCF-10A cells assessed as inhibition of cell proliferation at 2 uM incubated for 48 hrs by MTT assay | 2021 | Bioorganic & medicinal chemistry, 06-01, Volume: 39 | Discovery of 3,5-dimethylisoxazole derivatives as novel, potent inhibitors for bromodomain and extraterminal domain (BET) family. |
| AID1196559 | Inhibition of CYP2C19 in human liver microsomes at 10 uM using mephenytoin substrate preincubated for 5 mins before NADPH addition and measured after 20 mins post NADPH addition | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
| Fragment-based drug discovery of 2-thiazolidinones as BRD4 inhibitors: 2. Structure-based optimization. |
| 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. |
| 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. |
| AID1286394 | Inhibition of human His-tagged BRD4 bromodomain 1 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells using biotin-H4K5acK8acK12acK16ac as substrate preincubated for 30 mins followed by substrate addition measured after 30 mins by alphascreen assay | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Discovery of Benzo[cd]indol-2(1H)-ones as Potent and Specific BET Bromodomain Inhibitors: Structure-Based Virtual Screening, Optimization, and Biological Evaluation. |
| AID1718527 | Growth inhibition of human SK-MEL-5 cells after 72 hrs by CellTiter 96S AQeous non-radioactive cell proliferation assay | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24
| 4-Acyl Pyrroles as Dual BET-BRD7/9 Bromodomain Inhibitors Address BETi Insensitive Human Cancer Cell Lines. |
| AID1831537 | Inhibition of CK1 (unknown origin) | 2021 | Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
| Discovery of Novel Dual-Target Inhibitor of Bromodomain-Containing Protein 4/Casein Kinase 2 Inducing Apoptosis and Autophagy-Associated Cell Death for Triple-Negative Breast Cancer Therapy. |
| AID1683136 | Binding affinity to polybromo-1 (6) (unknown origin) assessed as change in melting temperature at 20 uM by SYPRO orange dye based DSF assay | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
| Pan-SMARCA/PB1 Bromodomain Inhibitors and Their Role in Regulating Adipogenesis. |
| AID1878603 | Toxicity in nude mouse xenografted with human SW1990 cells assessed as lung damage at 15 mg/kg, ip administered for 28 days by H and E staining based fluorescence microscopic analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1359770 | Antiproliferative activity against human MCF7 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer. |
| AID1878573 | Induction of cell cycle arrest in human SW1990 cells assessed as accumulation of cells at G0/G1 phase at 4 uM incubated for 4 days by propidium iodide staining based flow cytometry (Rvb = 64.79%) | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1905949 | Inhibition of C-terminal His6-tagged BRD3 BD2 (unknown origin) using H-YSGRGK(Ac)GGK(Ac)GLGK(Ac)-GGAK(Ac)RHRK-Biotin-OH as substrate incubated for 1 hrs by HTRF assay | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
| Structure-Based Discovery and Optimization of Furo[3,2- |
| AID1454054 | Growth inhibition of human MDA-MB-231 cells after 3 days by WST1 assay | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
| Synthesis and evaluation of novel dual BRD4/HDAC inhibitors. |
| AID1454055 | Growth inhibition of human T47D cells after 3 days by WST1 assay | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
| Synthesis and evaluation of novel dual BRD4/HDAC inhibitors. |
| AID1725786 | Antiproliferation activity against human HCT116 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | 2020 | ACS medicinal chemistry letters, Nov-12, Volume: 11, Issue:11
| Identification of 3,5-Dimethylisoxazole Derivatives as BRD4 Inhibitors for the Treatment of Colorectal Cancer. |
| AID1650236 | Binding affinity to recombinant human N-terminal His-tagged BRD4 BD2 (349 to 460 residues) expressed in Escherichia coli measured after 30 mins by AlphaScreen assay | 2020 | Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
| Discovery of novel small molecule induced selective degradation of the bromodomain and extra-terminal (BET) bromodomain protein BRD4 and BRD2 with cellular potencies. |
| AID1513795 | Inhibition of human 6x-His-tagged BRD3 bromodomain 2 expressed in Escherichia coli | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
| Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor. |
| AID1821749 | Binding affinity to human BRD4 BD1 E151A mutant assessed as change in melting temperature at 3:0 compound to protein ratio by thermal shift assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site. |
| AID1286363 | Binding affinity to human His6-tagged ASH1L (E2433 to E2564 residues) expressed in Escherichia coli BL21(DE3) cells at 200 uM incubated for 30 mins by SYPRO orange staining based fluorescence thermal shift assay | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Discovery of Benzo[cd]indol-2(1H)-ones as Potent and Specific BET Bromodomain Inhibitors: Structure-Based Virtual Screening, Optimization, and Biological Evaluation. |
| AID1905950 | Inhibition of C-terminal His6-tagged BRD2 BD2 (unknown origin) using H-YSGRGK(Ac)GGK(Ac)GLGK(Ac)-GGAK(Ac)RHRK-Biotin-OH as substrate incubated for 1 hrs by HTRF assay | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
| Structure-Based Discovery and Optimization of Furo[3,2- |
| AID1383800 | Antiproliferative activity against human TY82 cells after 72 hrs by CCK8 assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Structure-based optimization of a series of selective BET inhibitors containing aniline or indoline groups. |
| AID1496422 | Inhibition of BRD4 in human MCF7 cells assessed as decrease in MYC protein expression at 10 uM incubated for 190 to 48 hrs by Western blot method | 2018 | Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
| BET bromodomain ligands: Probing the WPF shelf to improve BRD4 bromodomain affinity and metabolic stability. |
| AID1368371 | Cytotoxicity against human BJ cells assessed as reduction in cell viability after 3 days by CellTiter-Glo assay | 2018 | Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1
| Exploiting a water network to achieve enthalpy-driven, bromodomain-selective BET inhibitors. |
| AID1905962 | Binding affinity to TRIM24 (unknown origin) assessed as change in melting temperature at 100 uM incubated for 30 mins by thermal shift assay | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
| Structure-Based Discovery and Optimization of Furo[3,2- |
| AID1878710 | Effect on BRCA2 gene expression in human SW1990 cells at 4 uM by Q-PCR analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1357999 | Inhibition of CBP (unknown origin) after 1 hr by TR-FRET assay | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation. |
| AID1821716 | Binding affinity to wild type human BRD4 BD2 (349 to 461 residues) assessed as change in melting temperature at 0:4 compound to protein ratio by thermal shift assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site. |
| AID1878579 | Inhibition of BRD4-BD1/2 (unknown origin) | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1831529 | Inhibition of BRD2 BD2 (unknown origin) incubated for 2 hrs by TR-FRET assay | 2021 | Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
| Discovery of Novel Dual-Target Inhibitor of Bromodomain-Containing Protein 4/Casein Kinase 2 Inducing Apoptosis and Autophagy-Associated Cell Death for Triple-Negative Breast Cancer Therapy. |
| AID1230003 | Binding affinity to biotinylated BRD2 BD1 (72 to 205 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometry method | 2015 | Journal of medicinal chemistry, Jun-25, Volume: 58, Issue:12
| Structure-Based Design of γ-Carboline Analogues as Potent and Specific BET Bromodomain Inhibitors. |
| AID1650532 | Antiproliferative activity against human THP1 cells assessed as reduction in cell viability at 2.5 uM incubated for 72 hrs by cell titer glo assay | 2020 | Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
| Discovery of a new class of PROTAC BRD4 degraders based on a dihydroquinazolinone derivative and lenalidomide/pomalidomide. |
| AID1615991 | Antiproliferative activity against human MDA-MB-436 cells after 72 hrs by CCK8 or SRB assay | 2019 | Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18
| Structure-Based Discovery and Development of a Series of Potent and Selective Bromodomain and Extra-Terminal Protein Inhibitors. |
| AID1409980 | Inhibition of human His6-tagged BRD4 BD1 (N44 to E168 residues) expressed in Escherichia coli BL21 (DE3) cells using H-SGRGK(Ac)GGK(Ac)GLGK(Ac)GGAK(Ac)RHRK-Biotin-OH as substrate after 2.5 hrs by AlphaScreen assay | 2018 | ACS medicinal chemistry letters, Mar-08, Volume: 9, Issue:3
| Y08060: A Selective BET Inhibitor for Treatment of Prostate Cancer. |
| 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. |
| AID1831189 | Toxicity in BALB/c mouse xenografted with human SW1990 cells assessed as heart damage at 15 mg/kg, ip administered for 28 consecutive days by H and E staining based fluorescence microscopic analysis | | | |
| AID1387853 | Induction of human His-tagged CRBN-DDB1/GST-tagged BRD4 (49 to 170 residues) interaction assessed as CRBN/DDB1/BRD4/compound ternary complex formation preincubated for 60 mins and measured after 60 mins by luminescence based Alphascreen proximity assay re | 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. |
| AID1460682 | Binding affinity to recombinant human His6-tagged BRDT bromodomain 1 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells assessed as change in melting temperature by SYPRO orange dye based fluorescence assay | 2017 | Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
| Drug Discovery Targeting Bromodomain-Containing Protein 4. |
| AID1683138 | Binding affinity to polybromo-1 (5) (unknown origin) assessed as change in melting temperature at 20 uM by SYPRO orange dye based DSF assay | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
| Pan-SMARCA/PB1 Bromodomain Inhibitors and Their Role in Regulating Adipogenesis. |
| AID1878587 | Antiproliferative activity against human SW1990 cells assessed as inhibition of cell growth measured after 7 days by MTT assay | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1600703 | Antiproliferative activity against human BT474 cells | 2019 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 29, Issue:19
| Design, synthesis and biological evaluation of 3,5-dimethylisoxazole and pyridone derivatives as BRD4 inhibitors. |
| AID1559435 | Inhibition of LPS-induced NO overproduction in mouse RAW264.7 cells at 1 uM incubated for 2 hrs followed by LPS stimulation and measured after 22 hrs by Griess reagent based assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Discovery of Benzo[ |
| AID1878628 | Induction of apoptosis in human SW1990 cells assessed as late apoptotic cells at 4 uM measured after 4 days by Annexin V-FITC and propidium iodide staining based flow cytometry (Rvb = 7.23%) | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1650528 | Inhibition of recombinant human GST-tagged BRD4 BD1 (44 to 168 residues) expressed in Escherichia coli at 500 nM incubated for 60 mins by alphascreen assay relative to control | 2020 | Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
| Discovery of a new class of PROTAC BRD4 degraders based on a dihydroquinazolinone derivative and lenalidomide/pomalidomide. |
| AID1725785 | Antiproliferation activity against human HCT116 cells assessed as reduction in cell viability at 2 uM incubated for 48 hrs by MTT assay relative to control | 2020 | ACS medicinal chemistry letters, Nov-12, Volume: 11, Issue:11
| Identification of 3,5-Dimethylisoxazole Derivatives as BRD4 Inhibitors for the Treatment of Colorectal Cancer. |
| AID1878641 | Induction of cell cycle arrest in human SW1990 cells assessed as accumulation of cells at G2/M phase at 4 uM incubated for 4 days by propidium iodide staining based flow cytometry (Rvb = 5.89%) | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1230020 | Cytotoxicity against human K562 cells harboring BCR-ABL fusion gene assessed as growth inhibition after 4 days by CellTiter-Glo luminescent assay | 2015 | Journal of medicinal chemistry, Jun-25, Volume: 58, Issue:12
| Structure-Based Design of γ-Carboline Analogues as Potent and Specific BET Bromodomain Inhibitors. |
| AID1594411 | Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
| Binding pocket-based design, synthesis and biological evaluation of novel selective BRD4-BD1 inhibitors. |
| AID1821737 | Binding affinity to wild type human BRD4 BD1 (44 to 168 residues) assessed as change in melting temperature at 6:8 compound to protein ratio by thermal shift assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site. |
| AID1600700 | Antiproliferative activity against human SW480 cells | 2019 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 29, Issue:19
| Design, synthesis and biological evaluation of 3,5-dimethylisoxazole and pyridone derivatives as BRD4 inhibitors. |
| AID1465514 | Inhibition of BRD4 in human H1299 cells assessed as decrease in HPV LCR-E2-EP400-mediated transcriptional repression after 24 hrs by Bright-Glo luciferase reporter gene assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of N-(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor. |
| AID1544781 | Induction of apoptosis in human MV4-11 cells assessed as early apoptotic cells level at 5 uM incubated for 24 hrs by Annexin V-FITC and propidium iodide staining based flow cytometry (Rvb = 0.8%) | 2019 | Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
| Design, synthesis and biological evaluation of novel 4,5-dihydro-[1,2,4]triazolo[4,3-f]pteridine derivatives as potential BRD4 inhibitors. |
| AID1831525 | Inhibition of CK2 (unknown origin) at 1 uM relative to control | 2021 | Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
| Discovery of Novel Dual-Target Inhibitor of Bromodomain-Containing Protein 4/Casein Kinase 2 Inducing Apoptosis and Autophagy-Associated Cell Death for Triple-Negative Breast Cancer Therapy. |
| AID1357987 | Inhibition of BRD4 in human SAE cells assessed as reduction in TLR3 agonist poly(I:C) -induced ISG54 RNA expression preincubated for 24 hrs followed by poly(I:C) addition and measured after 4 hrs by SYBR green dye-based qRT-PCR analysis | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation. |
| AID731331 | Cytotoxicity against human MV4-11 cells after 72 hrs by MTS assay | 2013 | Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
| Optimization of 3,5-dimethylisoxazole derivatives as potent bromodomain ligands. |
| AID1594409 | Antiproliferative activity against human HepG2 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
| Binding pocket-based design, synthesis and biological evaluation of novel selective BRD4-BD1 inhibitors. |
| AID1547256 | Inhibition of human recombinant His-tagged BRDT BD1 domain expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells by AlphaScreen assay | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
| Discovery of Thieno[2,3- |
| AID1308519 | Binding affinity to human PCAF expressed in Escherichia coli BL21(DE3)-R3-pRARE2 assessed as change in melting temperature at 25 uM by SYPRO orange based protein stability shift assay | 2016 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
| Targeting epigenetic reader and eraser: Rational design, synthesis and in vitro evaluation of dimethylisoxazoles derivatives as BRD4/HDAC dual inhibitors. |
| AID1831233 | Induction of cell cycle arrest in human SW1990 cells assessed as accumulation of cells at G0/G1 phase at 1 uM incubated for 4 days in presence of 3 uM Olaparib by propidium iodide staining based flow cytometry (Rvb = 64.79%) | | | |
| AID1409982 | Antiproliferative activity against human C4-2B cells after 96 hrs by Cell-Titer glo reagent based luminescence assay | 2018 | ACS medicinal chemistry letters, Mar-08, Volume: 9, Issue:3
| Y08060: A Selective BET Inhibitor for Treatment of Prostate Cancer. |
| AID1831530 | Inhibition of BRD3 BD1 (unknown origin) incubated for 2 hrs by TR-FRET assay | 2021 | Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
| Discovery of Novel Dual-Target Inhibitor of Bromodomain-Containing Protein 4/Casein Kinase 2 Inducing Apoptosis and Autophagy-Associated Cell Death for Triple-Negative Breast Cancer Therapy. |
| AID1831138 | Induction of autophagy in human SW1990 cells assessed as reduction in p62 expression at 4 uM incubated for 4 days by immunofluorescence assay | | | |
| AID1690281 | Toxicity in NOD-SCID mouse xenografted with human MV4-11 cells assessed as reduction in body weight at 50 mg/kg, po for 18 days | 2020 | European journal of medicinal chemistry, Apr-01, Volume: 191 | Design, synthesis, and biological evaluation of 4,5-dihydro-[1,2,4]triazolo[4,3-f]pteridine derivatives as novel dual-PLK1/BRD4 inhibitors. |
| AID1878770 | Effect on MDC1 gene expression in human SW1990 cells at 1 uM in presence of Olaparib by Q-PCR analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1831187 | Toxicity in BALB/c mouse xenografted with human SW1990 cells assessed as spleen damage at 15 mg/kg, ip administered for 28 consecutive days by H and E staining based fluorescence microscopic analysis | | | |
| AID1359757 | Binding affinity to His6-tagged human TAF1 (R1377 to D1503 residues) expressed in Escherichia coli BL21(DE3) assessed as change in melting temperature at 200 uM by SYPRO orange dye based fluorescence assay | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer. |
| AID1547261 | Inhibition of human recombinant His-tagged BRD2 BD2 domain expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells by AlphaScreen assay | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
| Discovery of Thieno[2,3- |
| AID1878576 | Antiproliferative activity against BRCA-proficient human MDA-MB-231 cells assessed as inhibition of cell growth measured after 7 days by MTT assay | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1544774 | Inhibition of bovine BRD4 bromodomain 1 incubated for 60 mins by TR-FRET assay | 2019 | Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
| Design, synthesis and biological evaluation of novel 4,5-dihydro-[1,2,4]triazolo[4,3-f]pteridine derivatives as potential BRD4 inhibitors. |
| AID1368361 | Binding affinity to His-tagged BRD2 bromodomain 2 (unknown origin) by SPR assay | 2018 | Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1
| Exploiting a water network to achieve enthalpy-driven, bromodomain-selective BET inhibitors. |
| AID1615983 | Antiproliferative activity against human Hep3B cells after 72 hrs by CCK8 or SRB assay | 2019 | Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18
| Structure-Based Discovery and Development of a Series of Potent and Selective Bromodomain and Extra-Terminal Protein Inhibitors. |
| AID1831209 | Invivo inhibition of PARP1 expression in human SW1900 cells xenografted in BALB/c mouse assessed as reversal of Olaparib-induced PARP1 accumulation at 15 mg/kg, ip administered for 28 consecutive days in presence of 45 mg/kg Olaparib by Q-PCR analysis | | | |
| AID1594410 | Antiproliferative activity against human A375 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
| Binding pocket-based design, synthesis and biological evaluation of novel selective BRD4-BD1 inhibitors. |
| AID1359774 | Antiproliferative activity against human U2OS cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer. |
| AID1905956 | Binding affinity to His6-fused BRDT BD1 (unknown origin) assessed as change in melting temperature at 100 uM incubated for 30 mins by thermal shift assay | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
| Structure-Based Discovery and Optimization of Furo[3,2- |
| AID1547257 | Inhibition of human recombinant His-tagged BRD4 BD2 domain using H-SGRGK(Ac)GGK(Ac)GLGK-(Ac)GGAK(Ac)RHRK(Biotin)-OH as substrate preincubated with enzyme for 30 mins followed by substrate addition measured after 30 mins by AlphaScreen assay | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
| Discovery of Thieno[2,3- |
| AID1359744 | Binding affinity to His6-tagged human BRD4 bromodomain-1 (N44 to E168 residues) expressed in Escherichia coli BL21(DE3) assessed as change in melting temperature at 200 uM by SYPRO orange dye based fluorescence assay | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer. |
| AID1831141 | Antiproliferative activity against human CFPAC-1 cells assessed as reduction in cell viability after 4 days by MTT assay | | | |
| AID1615980 | Antiproliferative activity against human TY82 cells after 72 hrs by CCK8 or SRB assay | 2019 | Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18
| Structure-Based Discovery and Development of a Series of Potent and Selective Bromodomain and Extra-Terminal Protein Inhibitors. |
| AID692860 | Binding affinity to first bromodomain of BRD4 | 2012 | ACS medicinal chemistry letters, Sep-13, Volume: 3, Issue:9
| Bromodomains: are readers right for epigenetic therapy? |
| AID1664726 | Induction of apoptosis in human MV4-11 cells assessed as late apoptotic cell at 5 uM after 12 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 1.28 %) | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15
| Design, synthesis and biological evaluation of novel 6-phenyl-1,3a,4,10b-tetrahydro-2H-benzo[c]thiazolo[4,5-e]azepin-2-one derivatives as potential BRD4 inhibitors. |
| AID1387717 | Inhibition of FAM-labeled ZBA248 binding to recombinant N-terminal His6-tagged BRD4 bromodomain 1 (44 to 168 residues) (unknown origin) expressed in Escherichia coli Rosetta2 DE3 after 30 mins by fluorescence polarization assay | 2018 | Journal of medicinal chemistry, 01-25, Volume: 61, Issue:2
| Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression. |
| AID1357986 | Inhibition of BRD4 in human SAE cells assessed as reduction in TLR3 agonist poly(I:C) -induced grobeta RNA expression at 10 uM preincubated for 24 hrs followed by poly(I:C) addition and measured after 4 hrs by SYBR green dye-based qRT-PCR analysis relativ | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation. |
| AID1191950 | Inhibition of BRD4 bromodomain-1 (unknown origin) by europium based LANCE TR-FRET assay | 2015 | Bioorganic & medicinal chemistry, Mar-01, Volume: 23, Issue:5
| Discovery and structure-activity relationship studies of N6-benzoyladenine derivatives as novel BRD4 inhibitors. |
| AID1878602 | Toxicity in nude mouse xenografted with human SW1990 cells assessed as spleen damage at 15 mg/kg, ip administered for 28 days by H and E staining based fluorescence microscopic analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1308514 | Inhibition of human BRD4 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 by bromodomain alphascreen peptide displacement assay | 2016 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
| Targeting epigenetic reader and eraser: Rational design, synthesis and in vitro evaluation of dimethylisoxazoles derivatives as BRD4/HDAC dual inhibitors. |
| AID1286362 | Binding affinity to human His6-tagged PCAF (G715 to D831 residues) expressed in Escherichia coli BL21(DE3) cells at 200 uM incubated for 30 mins by SYPRO orange staining based fluorescence thermal shift assay | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Discovery of Benzo[cd]indol-2(1H)-ones as Potent and Specific BET Bromodomain Inhibitors: Structure-Based Virtual Screening, Optimization, and Biological Evaluation. |
| AID1878601 | Toxicity in nude mouse xenografted with human SW1990 cells assessed as liver damage at 15 mg/kg, ip administered for 28 days by H and E staining based fluorescence microscopic analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1594413 | Inhibition of BRD4 in human A375 cells assessed as reduction in c-MYC mRNA expression at 10 uM measured after 24 hrs by RT-PCR analysis | 2019 | Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
| Binding pocket-based design, synthesis and biological evaluation of novel selective BRD4-BD1 inhibitors. |
| AID1570916 | Binding affinity to BRD4 bromodomain 1 (unknown origin) by isothermal titration calorimetry | 2018 | MedChemComm, Nov-01, Volume: 9, Issue:11
| Targeting Brd4 for cancer therapy: inhibitors and degraders. |
| AID1807758 | Inhibition of cell growth in HEK293T cells incubated for 72 hrs by CellTiter-blue reagent based assay | 2021 | Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
| Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors. |
| 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. |
| AID1520159 | Antiproliferative activity against human BxPC3 cells assessed as reduction in cell viability at 2 uM by MTT assay relative to control | 2019 | ACS medicinal chemistry letters, Dec-12, Volume: 10, Issue:12
| Pharmacokinetics-Driven Optimization of 7-Methylimidazo[1,5- |
| AID1831162 | Inhibition of recombinant BRDT BD1 (unknown origin) incubated for 120 mins by TR-FRET assay | | | |
| AID1878763 | Effect on BRCA1 gene expression in human SW1990 cells at 1 uM in presence of Olaparib by Q-PCR analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1359772 | Antiproliferative activity against human MV4-11 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer. |
| AID1878592 | Antiproliferative activity against human CFPAC-1 cells assessed as inhibition of cell growth measured after 3 days by MTT assay | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1387979 | Binding affinity to human BRD4 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells 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. |
| AID1831524 | Inhibition of BRD4 (unknown origin) at 1 uM incubated for 2 hrs by TR-FRET assay relative to control | 2021 | Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
| Discovery of Novel Dual-Target Inhibitor of Bromodomain-Containing Protein 4/Casein Kinase 2 Inducing Apoptosis and Autophagy-Associated Cell Death for Triple-Negative Breast Cancer Therapy. |
| AID1547272 | Inhibition of HDAC6 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
| Discovery of Thieno[2,3- |
| AID1368358 | Inhibition of recombinant human BRD2 bromodomain 2 (342 to 460 residues) using biotin labeled peptide substrate preincubated for 15 mins followed by substrate addition measured after 1 hr by TR-FRET assay | 2018 | Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1
| Exploiting a water network to achieve enthalpy-driven, bromodomain-selective BET inhibitors. |
| AID1831235 | Induction of cell cycle arrest in human SW1990 cells assessed as accumulation of cells at G2/M phase at 1 uM incubated for 4 days in presence of 3 uM Olaparib by propidium iodide staining based flow cytometry (Rvb = 5.89%) | | | |
| AID1831289 | Inhibition of homologous recombinant repair in human SW1990 cells assessed as reduction in Olaparib-induced Rad51 expression at 1 uM after 4 days in presence of Olaparib by Western blot analysis | | | |
| AID1387713 | Inhibition of FAM-labeled ZBA248 binding to recombinant N-terminal His6-tagged BRD2 bromodomain 1 (72 to 205 residues) (unknown origin) expressed in Escherichia coli Rosetta2 DE3 after 30 mins by fluorescence polarization assay | 2018 | Journal of medicinal chemistry, 01-25, Volume: 61, Issue:2
| Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression. |
| AID1878706 | Effect on CCND1 gene expression in human SW1990 cells at 4 uM by Q-PCR analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1358022 | Anti-inflammatory activity in poly(I:C)-induced airway inflammation C57BL/6 mouse model assessed as reduction in mISG54 expression in lung at 10 mg/kg, ip administered 1 day prior to poly(I:C) stimulation and redosed on day 2 followed by poly(I:C) stimula | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation. |
| AID649999 | Displacement of acetylated histone peptide from BRD4-BD2 by luminescence proximity homogenous assay | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| Development of live-cell imaging probes for monitoring histone modifications. |
| AID1547264 | Inhibition of HDAC10 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
| Discovery of Thieno[2,3- |
| AID1544778 | Induction of apoptosis in human MV4-11 cells assessed as late apoptotic cells level at 1 uM incubated for 24 hrs by Annexin V-FITC and propidium iodide staining based flow cytometry (Rvb = 1.5%) | 2019 | Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
| Design, synthesis and biological evaluation of novel 4,5-dihydro-[1,2,4]triazolo[4,3-f]pteridine derivatives as potential BRD4 inhibitors. |
| AID1454056 | Growth inhibition of human A2780 cells after 3 days by WST1 assay | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
| Synthesis and evaluation of novel dual BRD4/HDAC inhibitors. |
| AID1905963 | Binding affinity to TAF1 BD1(unknown origin) assessed as change in melting temperature at 100 uM incubated for 30 mins by thermal shift assay | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
| Structure-Based Discovery and Optimization of Furo[3,2- |
| AID1831295 | Inhibition of homologous recombinant repair in human SW1990 cells assessed as reduction in Rad51 expression at 4 uM after 4 days by Western blot analysis | | | |
| AID1821868 | Binding affinity to BRD4 D2 (unknown origin) assessed as dissociation constant by isothermal titration calorimetry | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| A Structure-based Design Approach for Generating High Affinity BRD4 D1-Selective Chemical Probes. |
| AID1821732 | Binding affinity CBP (unknown origin) incubated for 1 hr by TR-FRET assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site. |
| AID1821724 | Binding affinity recombinant human BRD4 BD1 (42 to 168 residues) expressed in Escherichia coli BL21(DE3) incubated for 1 hr by TR-FRET assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site. |
| AID1387715 | Inhibition of FAM-labeled ZBA248 binding to recombinant N-terminal His6-tagged BRD3 bromodomain 1 (24 to 144 residues) (unknown origin) expressed in Escherichia coli Rosetta2 DE3 after 30 mins by fluorescence polarization assay | 2018 | Journal of medicinal chemistry, 01-25, Volume: 61, Issue:2
| Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression. |
| AID1230007 | Binding affinity to biotinylated BRD4 BD1 (44 to 168 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometry method | 2015 | Journal of medicinal chemistry, Jun-25, Volume: 58, Issue:12
| Structure-Based Design of γ-Carboline Analogues as Potent and Specific BET Bromodomain Inhibitors. |
| AID1821748 | Binding affinity to human BRD4 BD1 E151A mutant assessed as change in melting temperature at 4:5 compound to protein ratio by thermal shift assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site. |
| AID1359748 | Binding affinity to His6-tagged human BRD3 bromodomain-1 (P24 to E144 residues) expressed in Escherichia coli BL21(DE3) assessed as change in melting temperature at 200 uM by SYPRO orange dye based fluorescence assay | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer. |
| AID1831254 | Effect on cell cycle progression in human SW1990 cells assessed as reduction in Olaparib-induced CDK6 expression at 1 uM after 4 days in presence of Olaparib by Western blot analysis | | | |
| AID1169318 | Cytotoxicity against BRD4-NUT-expressing human NMC-797 cells assessed as reduction in cell viability after 3 days by ATPlite assay | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
| Biased multicomponent reactions to develop novel bromodomain inhibitors. |
| AID1683139 | Binding affinity to polybromo-1 (3) (unknown origin) assessed as change in melting temperature at 20 uM by SYPRO orange dye based DSF assay | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
| Pan-SMARCA/PB1 Bromodomain Inhibitors and Their Role in Regulating Adipogenesis. |
| AID1650531 | Antiproliferative activity against human Raji cells assessed as reduction in cell viability at 2.5 uM incubated for 72 hrs by cell titer glo assay | 2020 | Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
| Discovery of a new class of PROTAC BRD4 degraders based on a dihydroquinazolinone derivative and lenalidomide/pomalidomide. |
| AID1831153 | Inhibition of recombinant BRD2 BD1 (unknown origin) incubated for 120 mins by TR-FRET assay | | | |
| AID1547263 | Inhibition of HDAC11 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
| Discovery of Thieno[2,3- |
| AID1169317 | Inhibition of BRD4 (unknown origin) by biotinylated-JQ1 based AlphaScreen BRD binding assay | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
| Biased multicomponent reactions to develop novel bromodomain inhibitors. |
| AID1615931 | Displacement of 5-FITC labelled (+)-JQ1 from His6-tagged human BRD4 bromodomain 1 expressed in Escherichia coli BL21(DE3) )-codon plus-RIL cells incubated for 4 hrs in dark condition by fluorescence anisotropy binding assay | 2019 | Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18
| Structure-Based Discovery and Development of a Series of Potent and Selective Bromodomain and Extra-Terminal Protein Inhibitors. |
| AID1905968 | Binding affinity to SMARCA4 (unknown origin) assessed as change in melting temperature at 100 uM incubated for 30 mins by thermal shift assay | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
| Structure-Based Discovery and Optimization of Furo[3,2- |
| AID1652275 | Growth inhibition of fulvestrant-resistant human MCF7:CFR 3D spheroid cells at 100 nM supplemented with fresh medium containing compound every 2 to 3 days for 9 days by celltitre-glo assay relative to control | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
| Novel Pyrrolopyridone Bromodomain and Extra-Terminal Motif (BET) Inhibitors Effective in Endocrine-Resistant ER+ Breast Cancer with Acquired Resistance to Fulvestrant and Palbociclib. |
| AID1359755 | Binding affinity to TIF1 (unknown origin) assessed as change in melting temperature at 200 uM by SYPRO orange dye based fluorescence assay | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer. |
| AID1831258 | Effect on cell cycle progression in human SW1990 cells assessed as reduction in Olaparib-induced PLK1 expression at 1 uM after 4 days in presence of Olaparib by Western blot analysis | | | |
| AID1196549 | Inhibition of BRD4 in human HT-29 cells assessed as reduction in c-Myc protein expression at 0.3125 uM to 5 uM uM after 24 hrs by Western blotting method | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
| Fragment-based drug discovery of 2-thiazolidinones as BRD4 inhibitors: 2. Structure-based optimization. |
| AID1496414 | Inhibition of recombinant His-tagged human BRD4 bromodomain 1 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells preincubated for 30 mins followed by H4K5acK8acK12acK16ac substrate addition measured after 30 mins by AlphaScreen assay | 2018 | Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
| BET bromodomain ligands: Probing the WPF shelf to improve BRD4 bromodomain affinity and metabolic stability. |
| AID705343 | Inhibition of human N-terminal BRD4 bromodomain expressed in Escherichia coli BL21(DE3) after 30 mins by luminescence proximity homogeneous assay | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2
| Fragment-based discovery of bromodomain inhibitors part 2: optimization of phenylisoxazole sulfonamides. |
| AID1385734 | Inhibition of BRD4-BD1 (unknown origin) incubated for 1 hr by AlphaScreen biotin-JQ1 competition assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
| Structure-Guided Design and Development of Potent and Selective Dual Bromodomain 4 (BRD4)/Polo-like Kinase 1 (PLK1) Inhibitors. |
| AID1878627 | Induction of apoptosis in human SW1990 cells assessed as necrotic cells at 4 uM measured after 4 days by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 2.45%) | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1196564 | Time dependent inhibition of CYP2C19 in human liver microsomes at 10 uM using mephenytoin substrate preincubated for 5 mins before NADPH addition and measured after 20 mins post NADPH addition | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
| Fragment-based drug discovery of 2-thiazolidinones as BRD4 inhibitors: 2. Structure-based optimization. |
| AID1878716 | Effect on MDC1 gene expression in human SW1990 cells at 4 uM by Q-PCR analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1845309 | Inhibition of recombinant BRD4-BD1 (unknown origin) by TR-FRET assay | 2021 | Bioorganic & medicinal chemistry letters, 01-01, Volume: 31 | Current status in the discovery of dual BET/HDAC inhibitors. |
| AID1594406 | Inhibition of biotinylated H4 K5,8,12,16Ac peptide binding to GST-tagged BRD4 bromodomain2 (unknown origin) measured after 60 mins by AlphaScreen assay | 2019 | Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
| Binding pocket-based design, synthesis and biological evaluation of novel selective BRD4-BD1 inhibitors. |
| AID1831287 | Inhibition of homologous recombinant repair in human SW1990 cells assessed as reduction in Olaparib-induced BRCA1 expression at 1 uM after 4 days in presence of Olaparib by Western blot analysis | | | |
| AID1807752 | Binding affinity to recombinant human N-terminal hexaHis-tagged BRD4 expressed in Escherichia coli BL21 (DE3) cells by ITC analysis | 2021 | Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
| Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors. |
| AID1513787 | Inhibition of human 6x-His-tagged BRD4 bromodomain 1 expressed in Escherichia coli | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
| Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor. |
| AID1456303 | Antiproliferative activity against BRD4-independent human K562 cells after 72 hrs by CCK8 assay | 2017 | Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8
| Design, synthesis and biological evaluation of 7-methylimidazo[1,5-a]pyrazin-8(7H)-one derivatives as BRD4 inhibitors. |
| AID1196540 | Growth inhibition of human HT-29 cells after 72 hrs by SRB assay | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
| Fragment-based drug discovery of 2-thiazolidinones as BRD4 inhibitors: 2. Structure-based optimization. |
| AID1762759 | Inhibition of BRD4-BD1 (unknown origin) at 1 uM preincubated for 15 mins followed by substrate addition and measured after 1 hr relative to control | 2021 | Bioorganic & medicinal chemistry, 06-01, Volume: 39 | Discovery of 3,5-dimethylisoxazole derivatives as novel, potent inhibitors for bromodomain and extraterminal domain (BET) family. |
| AID1845939 | Reactivation of HIV-1 latency in human U1 cells assessed as fold increase in HIV transcription by measuring GFP expression at 2 uM incubated for 24 hrs in presence of PEP005 by flow cytometry | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | HIV latency reversal agents: A potential path for functional cure? |
| AID1387970 | Proteolysis targeting chimera activity in human HeLa cells assessed as induction of VCB-mediated delivery of BRD2 for protein degradation by proteasome at 30 to 10000 nM incubated for 24 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. |
| AID1859890 | Inhibition of His tagged human BRD4 BD1 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells using biotinylated H4K5acK8acK12acK16ac peptide as substrate pretreated for 30 mins followed by substrate addition and measured after 30 mins by Alphascreen an | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Discovery of 2-((2-methylbenzyl)thio)-6-oxo-4-(3,4,5-trimethoxyphenyl)-1,6-dihydropyrimidine-5-carbonitrile as a novel and effective bromodomain and extra-terminal (BET) inhibitor for the treatment of sepsis. |
| AID648852 | Binding affinity to BRD4-BD1 assessed as change in melting temperature by isothermal titration calorimetry | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family. |
| AID1465448 | Binding affinity to human N-terminal His6-tagged BRD4 BD1-BD2 (K57 to K550 residues) after 1 hr using alexa-647 conjugated probe by TR-FRET assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of N-(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor. |
| AID1383799 | Antiproliferative activity against human MM1S cells after 72 hrs by CCK8 assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Structure-based optimization of a series of selective BET inhibitors containing aniline or indoline groups. |
| AID1664724 | Induction of apoptosis in human MV4-11 cells assessed as early apoptotic cell at 0.5 uM after 12 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 0.56 %) | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15
| Design, synthesis and biological evaluation of novel 6-phenyl-1,3a,4,10b-tetrahydro-2H-benzo[c]thiazolo[4,5-e]azepin-2-one derivatives as potential BRD4 inhibitors. |
| AID1556856 | Inhibition of recombinant human His-tagged BRD4 bromodomain 1/2 (2 to 1362 residues) expressed in s9f insect cells using biotinylated H4(1 to 21)K5/8/12/16Ac peptide as substrate preincubated for 30 mins followed by substrate addition and measured after 3 | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Novel phenanthridin-6(5H)-one derivatives as potent and selective BET bromodomain inhibitors: Rational design, synthesis and biological evaluation. |
| AID1615989 | Antiproliferative activity against human BT549 cells after 72 hrs by CCK8 or SRB assay | 2019 | Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18
| Structure-Based Discovery and Development of a Series of Potent and Selective Bromodomain and Extra-Terminal Protein Inhibitors. |
| AID1881932 | Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition incubated for 72 hrs by CellTiter-Glo assay | | | |
| AID1821750 | Binding affinity to human BRD4 BD1 E151A mutant assessed as change in melting temperature at 2:0 compound to protein ratio by thermal shift assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site. |
| AID1544780 | Induction of apoptosis in human MV4-11 cells assessed as viable cells level at 5 uM incubated for 24 hrs by Annexin V-FITC and propidium iodide staining based flow cytometry (Rvb = 97.7%) | 2019 | Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
| Design, synthesis and biological evaluation of novel 4,5-dihydro-[1,2,4]triazolo[4,3-f]pteridine derivatives as potential BRD4 inhibitors. |
| AID1368363 | Binding affinity to BRD2 bromodomain 1 (74 to 194 residues) (unknown origin) by ITC | 2018 | Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1
| Exploiting a water network to achieve enthalpy-driven, bromodomain-selective BET inhibitors. |
| AID1357997 | Inhibition of BRDT BD1 (unknown origin) after 1 hr by TR-FRET assay | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation. |
| AID1359758 | Binding affinity to His6-tagged human ASH1L (E2433 to E2564 residues) expressed in Escherichia coli BL21(DE3) assessed as change in melting temperature at 200 uM by SYPRO orange dye based fluorescence assay | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer. |
| AID1878632 | Induction of apoptosis in human SW1990 cells assessed as necrotic cells at 1 uM measured after 4 days in presence of 3 uM Olaparib by Annexin V-FITC and propidium iodide staining based flow cytometry (Rvb = 2.45%) | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1808919 | Displacement of FITC-conjugated JQ1 from wildtype BRD4 BD1 (unknown origin) expressed in Escherichia coli BL21-DE3 rosetta cells incubated for 15 mins by competitive fluorescence polarization assay | 2021 | Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
| Structure-Guided Design of a "Bump-and-Hole" Bromodomain-Based Degradation Tag. |
| AID1359763 | Antiproliferative activity against human C4-2B cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer. |
| AID1831144 | Synergistic antiproliferative activity against human SW1990 cells assessed as combination index at compound to Olaparib ratio of 1:3 measured after 4 days by MTT assay | | | |
| AID1878640 | Induction of cell cycle arrest in human SW1990 cells assessed as accumulation of cells at S phase at 4 uM incubated for 4 days by propidium iodide staining based flow cytometry (Rvb = 29.32%) | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1821770 | Antiinflammatory activity in C57BL/6 mouse model of poly(I:C)-induced acute airway inflammation assessed as decrease in H3K122Ac accumulation in lung tissue at 10 mg/kg, po administered 1 day prior to poly(I:C) stimulation by immunofluorescence analysis | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site. |
| AID1762768 | Antiproliferative activity against human CT26 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay | 2021 | Bioorganic & medicinal chemistry, 06-01, Volume: 39 | Discovery of 3,5-dimethylisoxazole derivatives as novel, potent inhibitors for bromodomain and extraterminal domain (BET) family. |
| AID1230002 | Displacement of FAM-labeled ZBA248 from BRD3 BD2 (306 to 417 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay | 2015 | Journal of medicinal chemistry, Jun-25, Volume: 58, Issue:12
| Structure-Based Design of γ-Carboline Analogues as Potent and Specific BET Bromodomain Inhibitors. |
| AID1831186 | Toxicity in BALB/c mouse xenografted with human SW1990 cells assessed as lung damage at 15 mg/kg, ip administered for 28 consecutive days by H and E staining based fluorescence microscopic analysis | | | |
| AID1448424 | Cytotoxicity against human MM1S cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
| BET Bromodomain Inhibitors with One-Step Synthesis Discovered from Virtual Screen. |
| AID1359769 | Antiproliferative activity against human PC3 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer. |
| AID1664732 | Cell cycle arrest in human MV4-11 cells assessed as accumulation at S phase at 0.5 uM after 12 hrs by propidium iodide staining based flow cytometric analysis (Rvb = 38.62%) | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15
| Design, synthesis and biological evaluation of novel 6-phenyl-1,3a,4,10b-tetrahydro-2H-benzo[c]thiazolo[4,5-e]azepin-2-one derivatives as potential BRD4 inhibitors. |
| AID1359740 | Inhibition of BRD4 bromodomain-1 (unknown origin) by AlphaScreen assay | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer. |
| AID1544783 | Induction of apoptosis in human MV4-11 cells assessed as necrotic cells level at 5 uM incubated for 24 hrs by Annexin V-FITC and propidium iodide staining based flow cytometry (Rvb = 0.0%) | 2019 | Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
| Design, synthesis and biological evaluation of novel 4,5-dihydro-[1,2,4]triazolo[4,3-f]pteridine derivatives as potential BRD4 inhibitors. |
| AID1878759 | Effect on CDK1 to 2 gene expression in human SW1990 cells at 1 uM in presence of Olaparib by Q-PCR analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1606740 | Binding affinity to recombinant BRD4 BD1 (unknown origin) incubated for 1 hr by TR-FRET assay | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation. |
| AID1821865 | Inhibition of BRD4 D2 (unknown origin) by competitive fluorescence anisotropy assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| A Structure-based Design Approach for Generating High Affinity BRD4 D1-Selective Chemical Probes. |
| AID1520154 | Antiproliferative activity against human Raji cells assessed as reduction in cell viability at 2 uM by MTT assay relative to control | 2019 | ACS medicinal chemistry letters, Dec-12, Volume: 10, Issue:12
| Pharmacokinetics-Driven Optimization of 7-Methylimidazo[1,5- |
| AID1359777 | Antiproliferative activity against human NCI-H1975 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer. |
| AID1821850 | Inhibition of BRD4 D1 (unknown origin) by competitive fluorescence anisotropy assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| A Structure-based Design Approach for Generating High Affinity BRD4 D1-Selective Chemical Probes. |
| AID1515646 | Ratio of drug concentration in unbound HEK293 cell to media | 2019 | MedChemComm, Jun-01, Volume: 10, Issue:6
| Controlling cellular distribution of drugs with permeability modifying moieties. |
| AID1409987 | Antiproliferative activity against human DU145 cells after 96 hrs by Cell-Titer glo reagent based luminescence assay | 2018 | ACS medicinal chemistry letters, Mar-08, Volume: 9, Issue:3
| Y08060: A Selective BET Inhibitor for Treatment of Prostate Cancer. |
| AID1375120 | Chromatographic hydrophobicity index, log D of the compound at pH 7.4 by HPLC method | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
| Discovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain. |
| AID1878765 | Effect on Rad51 gene expression in human SW1990 cells at 1 uM in presence of Olaparib by Q-PCR analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1821856 | Anti-inflammatory activity in human A549 cells assessed as residual IL-8 levels at 1 uM preincubated for 6 hrs followed by TNFalpha induction and measured after 24 hrs by ELISA | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| A Structure-based Design Approach for Generating High Affinity BRD4 D1-Selective Chemical Probes. |
| AID1383779 | Inhibition of BRD4 in human TY82 cells assessed as reduction in c-Myc protein expression at 0.2 to 1 uM after 24 hrs by Western blot analysis | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Structure-based optimization of a series of selective BET inhibitors containing aniline or indoline groups. |
| 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. |
| AID1831299 | Inhibition of homologous recombinant repair in human SW1990 cells assessed as reduction in c-Myc expression at 4 uM after 4 days by Western blot analysis | | | |
| AID1705272 | Inhibition of BRD2 BD1 (unknown origin) preincubated for 15 mins followed by peptide addition and measured after 60 mins by TR-FRET assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Design, synthesis and biological evaluation of indole-2-one derivatives as potent BRD4 inhibitors. |
| AID1570915 | Inhibition of BRD4 bromodomain 1 (unknown origin) by alpha-screen method | 2018 | MedChemComm, Nov-01, Volume: 9, Issue:11
| Targeting Brd4 for cancer therapy: inhibitors and degraders. |
| AID1831290 | Inhibition of homologous recombinant repair in human SW1990 cells assessed as reduction in FOXM1 expression at 4 uM after 4 days by Q-PCR analysis | | | |
| AID1358021 | Anti-inflammatory activity in poly(I:C)-induced airway inflammation C57BL/6 mouse model assessed as reduction in mKC expression in lung at 10 mg/kg, ip administered 1 day prior to poly(I:C) stimulation and redosed on day 2 followed by poly(I:C) stimulatio | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation. |
| AID1831274 | Induction of DNA damage in human SW1990 cells assessed as increase in gammaH2AX at 4 uM incubated for 4 days by immunofluorescence assay | | | |
| AID649989 | Binding affinity to BRD3-BD2 by isothermal titration calorimetry | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| Development of live-cell imaging probes for monitoring histone modifications. |
| AID1878711 | Effect on Rad51 gene expression in human SW1990 cells at 4 uM by Q-PCR analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1357998 | Inhibition of BRDT BD2 (unknown origin) after 1 hr by TR-FRET assay | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation. |
| AID1513830 | Inhibition of BRD4 bromodomain 1 in human MM1S cells assessed as reduction in c-myc levels at 0.1 to 10 uM by Western blot analysis | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
| Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor. |
| AID1286348 | Inhibition of human His6-tagged BRD4 bromodomain 1 (N44 to E168 residues) expressed in Escherichia coli BL21(DE3) cells using biotin-H4KAc4 as substrate incubated for 2 hrs by alphascreen assay | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Discovery of Benzo[cd]indol-2(1H)-ones as Potent and Specific BET Bromodomain Inhibitors: Structure-Based Virtual Screening, Optimization, and Biological Evaluation. |
| AID1359765 | Antiproliferative activity against human VCaP cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer. |
| AID1831535 | Inhibition of BRDT BD1 (unknown origin) incubated for 2 hrs by TR-FRET assay | 2021 | Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
| Discovery of Novel Dual-Target Inhibitor of Bromodomain-Containing Protein 4/Casein Kinase 2 Inducing Apoptosis and Autophagy-Associated Cell Death for Triple-Negative Breast Cancer Therapy. |
| AID1831135 | Induction of apoptosis in human SW1990 cells assessed as early apoptotic cells at 4 uM after 4 days by Annexin V-FITC and propidium iodide staining based flow cytometry (Rvb = 1.91%) | | | |
| AID706721 | Binding affinity to BRD4 isoform 1 | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Progress in the development and application of small molecule inhibitors of bromodomain-acetyl-lysine interactions. |
| AID1547269 | Inhibition of HDAC3 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
| Discovery of Thieno[2,3- |
| AID1383803 | Inhibition of BRD4 in human TY82 or NCI-H1299 cells assessed as reduction in PD-L1 mRNA expression at 0.2 to 1 uM after 24 hrs by RT-PCR analysis | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Structure-based optimization of a series of selective BET inhibitors containing aniline or indoline groups. |
| AID1368357 | Inhibition of recombinant human BRD2 bromodomain 1 (49 to 170 residues) using biotin labeled peptide substrate preincubated for 15 mins followed by substrate addition measured after 1 hr by TR-FRET assay | 2018 | Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1
| Exploiting a water network to achieve enthalpy-driven, bromodomain-selective BET inhibitors. |
| AID1666861 | Inhibition of BRD4 (unknown origin) | 2020 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 30, Issue:6
| BET proteins: Investigating BRDT as a potential target for male contraception. |
| AID1594419 | Selectivity index, ratio of IC50 for cytotoxicity against human LO2 cells to IC50 for antifibrotic activity against human LX2 cells | 2019 | Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
| Binding pocket-based design, synthesis and biological evaluation of novel selective BRD4-BD1 inhibitors. |
| AID1831298 | Inhibition of homologous recombinant repair in human SW1990 cells assessed as reduction in c-Myc expression at 4 uM after 4 days by Q-PCR analysis | | | |
| AID1664735 | Cell cycle arrest in human MV4-11 cells assessed as accumulation at S phase at 5 uM after 12 hrs by propidium iodide staining based flow cytometric analysis (Rvb = 38.62%) | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15
| Design, synthesis and biological evaluation of novel 6-phenyl-1,3a,4,10b-tetrahydro-2H-benzo[c]thiazolo[4,5-e]azepin-2-one derivatives as potential BRD4 inhibitors. |
| AID1196562 | Time dependent inhibition of CYP2C9 in human liver microsomes at 10 uM using diclofenac substrate preincubated for 5 mins before NADPH addition and measured after 20 mins post NADPH addition | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
| Fragment-based drug discovery of 2-thiazolidinones as BRD4 inhibitors: 2. Structure-based optimization. |
| AID1878755 | Effect on CDC25B gene expression in human SW1990 cells at 1 uM in presence of Olaparib by Q-PCR analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1831538 | Inhibition of CK2 (unknown origin) | 2021 | Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
| Discovery of Novel Dual-Target Inhibitor of Bromodomain-Containing Protein 4/Casein Kinase 2 Inducing Apoptosis and Autophagy-Associated Cell Death for Triple-Negative Breast Cancer Therapy. |
| AID1368365 | Selectivity index, ratio of Kd for BRD2 bromodomain 1 (74 to 194 residues) (unknown origin to Kd for BRD2 bromodomain 2 (348 to 455 residues) (unknown origin) | 2018 | Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1
| Exploiting a water network to achieve enthalpy-driven, bromodomain-selective BET inhibitors. |
| AID1831293 | Inhibition of homologous recombinant repair in human SW1990 cells assessed as reduction in BRCA1 expression at 4 uM after 4 days by Western blot analysis | | | |
| AID1878633 | Induction of apoptosis in human SW1990 cells assessed as early apoptotic cells at 1 uM measured after 4 days in presence of 3 uM Olaparib by Annexin V-FITC and propidium iodide staining based flow cytometry (Rvb = 1.62%) | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1831532 | Inhibition of BRD4 BD1 (unknown origin) incubated for 2 hrs by TR-FRET assay | 2021 | Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
| Discovery of Novel Dual-Target Inhibitor of Bromodomain-Containing Protein 4/Casein Kinase 2 Inducing Apoptosis and Autophagy-Associated Cell Death for Triple-Negative Breast Cancer Therapy. |
| AID1400169 | Inhibition of N-terminal His-tagged BRD4 (BD1/BD2) (unknown origin) using biotinylated tetra-acetylated histone H4 peptide after 30 mins by alpha-screen assay | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
| Design and Characterization of Novel Covalent Bromodomain and Extra-Terminal Domain (BET) Inhibitors Targeting a Methionine. |
| AID1513797 | Inhibition of human 6x-His-tagged BRD2 bromodomain 1 expressed in Escherichia coli | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
| Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor. |
| AID1762769 | Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay | 2021 | Bioorganic & medicinal chemistry, 06-01, Volume: 39 | Discovery of 3,5-dimethylisoxazole derivatives as novel, potent inhibitors for bromodomain and extraterminal domain (BET) family. |
| AID772237 | Inhibition of BRD4 in human Raji cells assessed as reduction of MYC expression after 4 hrs | 2013 | ACS medicinal chemistry letters, Sep-12, Volume: 4, Issue:9
| Discovery, Design, and Optimization of Isoxazole Azepine BET Inhibitors. |
| AID1831526 | Antiproliferative activity against human MDA-MB-231 cells incubated for 24 hrs by MTT assay | 2021 | Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
| Discovery of Novel Dual-Target Inhibitor of Bromodomain-Containing Protein 4/Casein Kinase 2 Inducing Apoptosis and Autophagy-Associated Cell Death for Triple-Negative Breast Cancer Therapy. |
| AID1606742 | Binding affinity to recombinant BRD2 BD1 (unknown origin) incubated for 1 hr by TR-FRET assay | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation. |
| AID1831212 | Invivo inhibition of BRD4 expression in human SW1900 cells xenografted in BALB/c mouse assessed as reversal of Olaparib-induced BRD4 accumulation at 15 mg/kg, ip administered for 28 consecutive days in presence of 45 mg/kg Olaparib by Western blot analysi | | | |
| 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. |
| AID1821714 | Binding affinity to wild type human BRD4 BD1 (44 to 168 residues) assessed as change in melting temperature at 3:0 compound to protein ratio by thermal shift assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site. |
| AID1196555 | Inhibition of CYP3A4 in human liver microsomes at 10 uM preincubated for 5 mins before NADPH addition and measured after 20 mins post NADPH addition | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
| Fragment-based drug discovery of 2-thiazolidinones as BRD4 inhibitors: 2. Structure-based optimization. |
| AID1878595 | Antiproliferative activity against human CFPAC-1 cells assessed as inhibition of cell growth measured after 7 days by MTT assay | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1831227 | Induction of cell cycle arrest in human SW1990 cells assessed as accumulation of cells at G0/G1 phase at 4 uM incubated for 4 days by propidium iodide staining based flow cytometry (Rvb = 64.79%) | | | |
| AID1878582 | Antiproliferative activity against human SW1990 cells assessed as inhibition of cell growth after 3 days by MTT assay | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1594417 | Antifibrotic activity against rat NRK-49F cells assessed as reduction in cell growth measured after 48 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
| Binding pocket-based design, synthesis and biological evaluation of novel selective BRD4-BD1 inhibitors. |
| AID1831196 | Toxicity in BALB/c mouse xenografted with human SW1990 cells assessed as lung damage at 15 mg/kg, ip administered for 28 consecutive days in presence of 45 mg/kg Olaparib | | | |
| AID1905951 | Binding affinity to His6-fused BRD4 BD2 (unknown origin) assessed as change in melting temperature at 100 uM incubated for 30 mins by thermal shift assay | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
| Structure-Based Discovery and Optimization of Furo[3,2- |
| AID1652288 | Up regulation of CDKN1B gene expression in fulvestrant-resistant human MCF7:CFR cells at 100 nM measured after 24 hrs | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
| Novel Pyrrolopyridone Bromodomain and Extra-Terminal Motif (BET) Inhibitors Effective in Endocrine-Resistant ER+ Breast Cancer with Acquired Resistance to Fulvestrant and Palbociclib. |
| AID1456302 | Antiproliferative activity against BRD4-sensitive human HL60 cells after 72 hrs by CCK8 assay | 2017 | Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8
| Design, synthesis and biological evaluation of 7-methylimidazo[1,5-a]pyrazin-8(7H)-one derivatives as BRD4 inhibitors. |
| AID1909960 | Inhibition of EZH2/BRD4 in human A549 cell lysate assessed as ternary complex formation at 1 uM preincubated for 24 hrs for 30 mins followed by DSP treatment by co-immunoprecipitation method | 2022 | Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
| Design and Synthesis of Dual EZH2/BRD4 Inhibitors to Target Solid Tumors. |
| AID649993 | Binding affinity to BRDT-BD1 by isothermal titration calorimetry | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| Development of live-cell imaging probes for monitoring histone modifications. |
| AID1664728 | Induction of apoptosis in human MV4-11 cells assessed as early apoptotic cell at 5 uM after 12 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 0.56 %) | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15
| Design, synthesis and biological evaluation of novel 6-phenyl-1,3a,4,10b-tetrahydro-2H-benzo[c]thiazolo[4,5-e]azepin-2-one derivatives as potential BRD4 inhibitors. |
| AID1196545 | Binding affinity to EP300 (unknown origin) assessed as increase in protein melting temperature at 50 umol by real-time PCR system based thermal shift assay | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
| Fragment-based drug discovery of 2-thiazolidinones as BRD4 inhibitors: 2. Structure-based optimization. |
| AID1594404 | Inhibition of biotinylated H4 K5,8,12,16Ac peptide binding to GST-tagged BRD4 bromodomain1 (unknown origin) measured after 60 mins by AlphaScreen assay | 2019 | Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
| Binding pocket-based design, synthesis and biological evaluation of novel selective BRD4-BD1 inhibitors. |
| AID1831276 | Induction of DNA damage in human SW1990 cells assessed as increase in gammaH2AX at 1 uM incubated for 4 days in presence of Olaparib by immunofluorescence assay | | | |
| AID706720 | Displacement of H4(1-21)KAc5,8,12,16 peptide from BRD4 isoform 1 bead based amplified luminescent proximity homogeneous assay | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Progress in the development and application of small molecule inhibitors of bromodomain-acetyl-lysine interactions. |
| AID1821744 | Binding affinity to wild type human BRD4 BD2 (349 to 461 residues) assessed as change in melting temperature at 0:7 compound to protein ratio by thermal shift assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site. |
| AID1318693 | Inhibition of human His-tagged BRD4 BD1 (49 to 170 residues) using H-SGRGK(Ac)GGK(Ac)GLGK-(Ac)GGAK(Ac)RHRK(Biotin)-OH as substrate preincubated for 30 mins followed by substrate addition measured after 30 mins by TR-FRET assay | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Development of 4,5-dihydro-benzodiazepinone derivatives as a new chemical series of BRD4 inhibitors. |
| AID1196542 | Growth inhibition of human MM1S cells after 72 hrs by SRB assay | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
| Fragment-based drug discovery of 2-thiazolidinones as BRD4 inhibitors: 2. Structure-based optimization. |
| AID1368373 | Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 3 days by CellTiter-Glo assay | 2018 | Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1
| Exploiting a water network to achieve enthalpy-driven, bromodomain-selective BET inhibitors. |
| AID1808921 | Displacement of FITC-conjugated JQ1 from BRD4 BD2 L387V mutant (unknown origin) expressed in Escherichia coli BL21-DE3 rosetta cells incubated for 15 mins by competitive fluorescence polarization assay | 2021 | Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
| Structure-Guided Design of a "Bump-and-Hole" Bromodomain-Based Degradation Tag. |
| AID1594414 | Induction of apoptosis in human A375 cells at 10 uM measured after 24 hrs by Annexin V-FITC/propidium iodide staining based fluorescence microscopic analysis | 2019 | Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
| Binding pocket-based design, synthesis and biological evaluation of novel selective BRD4-BD1 inhibitors. |
| AID1905944 | Binding affinity to BAZ2B (unknown origin) assessed as change in melting temperature at 100 uM incubated for 30 mins by thermal shift assay | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
| Structure-Based Discovery and Optimization of Furo[3,2- |
| AID1831291 | Inhibition of homologous recombinant repair in human SW1990 cells assessed as reduction in FOXM1 expression at 4 uM after 4 days by Western blot analysis | | | |
| AID1368369 | Cytotoxicity against human 697 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay | 2018 | Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1
| Exploiting a water network to achieve enthalpy-driven, bromodomain-selective BET inhibitors. |
| AID1831534 | Inhibition of BRD4 BD1/BD2 (unknown origin) incubated for 2 hrs by TR-FRET assay | 2021 | Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
| Discovery of Novel Dual-Target Inhibitor of Bromodomain-Containing Protein 4/Casein Kinase 2 Inducing Apoptosis and Autophagy-Associated Cell Death for Triple-Negative Breast Cancer Therapy. |
| AID1878758 | Effect on CCNB1 gene expression in human SW1990 cells at 1 uM in presence of Olaparib by Q-PCR analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID649992 | Binding affinity to BRD4-BD2 by isothermal titration calorimetry | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| Development of live-cell imaging probes for monitoring histone modifications. |
| 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. |
| AID1547260 | Inhibition of human recombinant His-tagged BRD3 BD1 domain expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells by AlphaScreen assay | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
| Discovery of Thieno[2,3- |
| AID1196558 | Inhibition of CYP1A2 in human liver microsomes at 10 uM using phenacetin substrate preincubated for 5 mins before NADPH addition and measured after 20 mins post NADPH addition | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
| Fragment-based drug discovery of 2-thiazolidinones as BRD4 inhibitors: 2. Structure-based optimization. |
| AID1878593 | Antiproliferative activity against human CFPAC-1 cells assessed as inhibition of cell growth measured after 4 days by MTT assay | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1807753 | Binding affinity to recombinant human N-terminal hexaHis-tagged BRDT expressed in Escherichia coli BL21 (DE3) cells assessed as change in melting temperature by DSF assay | 2021 | Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
| Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors. |
| AID1705257 | Inhibition of BRD4 BD1 (unknown origin) at 1 uM preincubated for 15 mins followed by peptide addition and measured after 60 mins by TR-FRET assay relative to control | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Design, synthesis and biological evaluation of indole-2-one derivatives as potent BRD4 inhibitors. |
| AID1652289 | Down regulation of cyclin-D gene expression in fulvestrant-resistant human MCF7:CFR cells at 100 nM measured after 24 hrs | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
| Novel Pyrrolopyridone Bromodomain and Extra-Terminal Motif (BET) Inhibitors Effective in Endocrine-Resistant ER+ Breast Cancer with Acquired Resistance to Fulvestrant and Palbociclib. |
| AID1359750 | Binding affinity to His6-tagged human BRD4 bromodomain-2 expressed in Escherichia coli BL21(DE3) assessed as change in melting temperature at 200 uM by SYPRO orange dye based fluorescence assay | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer. |
| AID1606745 | Binding affinity to recombinant BRD3 BD2 (unknown origin) incubated for 1 hr by TR-FRET assay | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation. |
| AID1664717 | Displacement of APC-labeled biotinylated-avidin from Euphorium-chelated recombinant human N-terminal GST-tagged BRD4 bromodomain 1 expressed in Escherichia coli preincubated for 15 mins followed by APC-labeled biotinylated-avidin addition and measured aft | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15
| Design, synthesis and biological evaluation of novel 6-phenyl-1,3a,4,10b-tetrahydro-2H-benzo[c]thiazolo[4,5-e]azepin-2-one derivatives as potential BRD4 inhibitors. |
| AID1606746 | Binding affinity to recombinant BRDT BD1 (unknown origin) incubated for 1 hr by TR-FRET assay | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation. |
| AID1368372 | Cytotoxicity against HEK293 cells assessed as reduction in cell viability after 3 days by CellTiter-Glo assay | 2018 | Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1
| Exploiting a water network to achieve enthalpy-driven, bromodomain-selective BET inhibitors. |
| AID1383801 | Inhibition of BRD4 in human TY82 cells assessed as reduction in c-Myc mRNA expression at 0.2 to 1 uM after 24 hrs by RT-PCR analysis | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Structure-based optimization of a series of selective BET inhibitors containing aniline or indoline groups. |
| AID1705260 | Antiproliferative activity against human HT29 cells incubated for 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Design, synthesis and biological evaluation of indole-2-one derivatives as potent BRD4 inhibitors. |
| AID1905969 | Binding affinity to PHIP-2 (unknown origin) assessed as change in melting temperature at 100 uM incubated for 30 mins by thermal shift assay | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
| Structure-Based Discovery and Optimization of Furo[3,2- |
| AID1846146 | Inhibition of BRD4 (unknown origin) incubated for 30 mins by ELISA method | 2021 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 38 | Current status in the discovery of dual BET/HDAC inhibitors. |
| AID1831155 | Inhibition of recombinant BRD3 BD1 (unknown origin) incubated for 120 mins by TR-FRET assay | | | |
| AID1513810 | Displacement of Fl-JQ1 from BRD4 C-terminal bromodomain 2 H437D mutant (unknown origin) expressed in Escherichia coli Bl21(DE3) by fluorescence polarization assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
| Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor. |
| AID1878685 | Induction of DNA damage in human SW1990 cells assessed as increase in gammaH2AX expression at 1 uM incubated for 4 days in presence of Olaparib by DAPI staining based laser confocal microscopic analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1905993 | Binding affinity to His6-fused BRD4 BD1 (unknown origin) assessed as increase in thermal stability at 100 uM incubated for 30 mins by thermal shift assay | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
| Structure-Based Discovery and Optimization of Furo[3,2- |
| AID1308512 | Inhibition of BRD4(1) (unknown origin) | 2016 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
| Targeting epigenetic reader and eraser: Rational design, synthesis and in vitro evaluation of dimethylisoxazoles derivatives as BRD4/HDAC dual inhibitors. |
| AID1600697 | Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent cell viability assay | 2019 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 29, Issue:19
| Design, synthesis and biological evaluation of 3,5-dimethylisoxazole and pyridone derivatives as BRD4 inhibitors. |
| AID1878588 | Antiproliferative activity against human CAPAN-1 cells assessed as inhibition of cell growth measured after 3 days by MTT assay | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1762760 | Inhibition of BRD4-BD1 (unknown origin) preincubated for 15 mins followed by substrate addition and measured after 1 hr | 2021 | Bioorganic & medicinal chemistry, 06-01, Volume: 39 | Discovery of 3,5-dimethylisoxazole derivatives as novel, potent inhibitors for bromodomain and extraterminal domain (BET) family. |
| AID1878565 | Synergistic antiproliferative activity against human SW1990 cells assessed as combination index at compound to Olaparib ratio of 1:3 measured after 4 days by MTT assay | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1308517 | Binding affinity to human CECR2 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 assessed as change in melting temperature at 25 uM by SYPRO orange based protein stability shift assay | 2016 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
| Targeting epigenetic reader and eraser: Rational design, synthesis and in vitro evaluation of dimethylisoxazoles derivatives as BRD4/HDAC dual inhibitors. |
| AID1878608 | Toxicity in nude mouse xenografted with human SW1990 cells assessed as kidney damage at 15 mg/kg, ip administered for 28 days in presence of 45 mg/kg Olaparib by H and E staining based fluorescence microscopic analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1286357 | Binding affinity to human His6-tagged BRDT bromodomain 1 (N21 to E137 residues) expressed in Escherichia coli BL21(DE3) cells at 200 uM incubated for 30 mins by SYPRO orange staining based fluorescence thermal shift assay | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Discovery of Benzo[cd]indol-2(1H)-ones as Potent and Specific BET Bromodomain Inhibitors: Structure-Based Virtual Screening, Optimization, and Biological Evaluation. |
| AID1387969 | Proteolysis targeting chimera activity in human HeLa cells assessed as induction of VCB-mediated delivery of BRD3 for protein degradation by proteasome at 30 to 10000 nM incubated for 24 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. |
| AID1683141 | Binding affinity to polybromo-1 (1) (unknown origin) assessed as change in melting temperature at 20 uM by SYPRO orange dye based DSF assay | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
| Pan-SMARCA/PB1 Bromodomain Inhibitors and Their Role in Regulating Adipogenesis. |
| AID1831172 | Inhibition of PARP1 in human SW1990 cells assessed as reversal of Olaparib-induced PARP1 accumulation in nucleus at 1 uM after 4 days by Western blot analysis | | | |
| AID1831163 | Inhibition of recombinant BRDT BD2 (unknown origin) incubated for 120 mins by TR-FRET assay | | | |
| AID1600701 | Antiproliferative activity against human DU145 cells | 2019 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 29, Issue:19
| Design, synthesis and biological evaluation of 3,5-dimethylisoxazole and pyridone derivatives as BRD4 inhibitors. |
| AID1878772 | Downregulation of Ki67 expression in human SW1990 cells at 15 mg/kg, ip measured after 28 days by immuno histochemical staining based fluorescence microscopic analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1513824 | Inhibition of p38alpha in human MM1S cells assessed as reduction in MSK1 phosphorylation at T581 up to 10 uM by Western blot analysis | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
| Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor. |
| AID1547265 | Inhibition of HDAC9 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
| Discovery of Thieno[2,3- |
| AID1725782 | Inhibition of BRD4 bromodomain1 (unknown origin) using peptide histone H4 (SGRGACKGGACKGLGAC-KGGAACKRHGSGSK-biotin) as substrate incubated for 15 mins followed by substrate addition at 0.5 uM measured after 1 hr by alphascreen assay relative to control | 2020 | ACS medicinal chemistry letters, Nov-12, Volume: 11, Issue:11
| Identification of 3,5-Dimethylisoxazole Derivatives as BRD4 Inhibitors for the Treatment of Colorectal Cancer. |
| AID1547266 | Inhibition of HDAC8 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
| Discovery of Thieno[2,3- |
| AID1878703 | Effect on CDK1 gene expression in human SW1990 cells at 4 uM by Q-PCR analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| 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. |
| AID1831160 | Inhibition of recombinant BRD4 BD1 (unknown origin) incubated for 120 mins by TR-FRET assay | | | |
| AID1606741 | Binding affinity to recombinant BRD4 BD2 (unknown origin) incubated for 1 hr by TR-FRET assay | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation. |
| AID1878589 | Antiproliferative activity against human CAPAN-1 cells assessed as inhibition of cell growth measured after 4 days by MTT assay | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1807757 | Inhibition of cell growth in human MM1.S cells incubated for 72 hrs by CellTiter-blue reagent based assay | 2021 | Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
| Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors. |
| AID1520155 | Inhibition of BRD4 bromodomain1 (unknown origin) using peptide H4 as substrate incubated for 15 mins followed by substrate addition and measured after 1 hr by alphascreen assay | 2019 | ACS medicinal chemistry letters, Dec-12, Volume: 10, Issue:12
| Pharmacokinetics-Driven Optimization of 7-Methylimidazo[1,5- |
| AID1664719 | Antiproliferative activity against human HL60 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15
| Design, synthesis and biological evaluation of novel 6-phenyl-1,3a,4,10b-tetrahydro-2H-benzo[c]thiazolo[4,5-e]azepin-2-one derivatives as potential BRD4 inhibitors. |
| AID1878580 | Antiproliferative activity against BRCA2-mutated human HCT-116 cells assessed as inhibition of cell growth measured after 7 days by MTT assay | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1905961 | Binding affinity to His6-fused BRD7 (unknown origin) assessed as change in melting temperature at 100 uM incubated for 30 mins by thermal shift assay | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
| Structure-Based Discovery and Optimization of Furo[3,2- |
| AID1601806 | Induction of CRBN-mediated BRD4 degradation in human 22RV1 cells assessed as downregulation of c-Myc protein expression up to 1000 nM by immunoblotting analysis | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | A novel cereblon modulator for targeted protein degradation. |
| AID1878581 | Antiproliferative activity against human THP-1 cells expressing BRD4 assessed as inhibition of cell growth measured after 3 days by MTT assay | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1368368 | Cytotoxicity against human NALM16 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay | 2018 | Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1
| Exploiting a water network to achieve enthalpy-driven, bromodomain-selective BET inhibitors. |
| AID1878756 | Effect on CDC25A gene expression in human SW1990 cells at 1 uM in presence of Olaparib by Q-PCR analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1821739 | Binding affinity to wild type human BRD4 BD2 (349 to 461 residues) assessed as change in melting temperature at 5:1 compound to protein ratio by thermal shift assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site. |
| AID1559433 | Selectivity index, ratio of IC50 for recombinant human N-terminal His-tagged BRD4 BD1 (44 to 170 residues) expressed in Escherichia coli to IC50 for recombinant human N-terminal His-tagged BRD4 BD2 (349 to 460 residues) expressed in Escherichia coli | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Discovery of Benzo[ |
| AID1584507 | Binding affinity to human BRD4 BD1 (44 to 168 residues) by fluorescence polarization assay | 2018 | Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
| 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. |
| AID1615979 | Antiproliferative activity against human MV4-11 cells after 72 hrs by CCK8 or SRB assay | 2019 | Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18
| Structure-Based Discovery and Development of a Series of Potent and Selective Bromodomain and Extra-Terminal Protein Inhibitors. |
| AID1359746 | Binding affinity to His6-tagged human BRD2 bromodomain-1 (K77 to N194 residues) expressed in Escherichia coli BL21(DE3) assessed as change in melting temperature at 200 uM by SYPRO orange dye based fluorescence assay | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer. |
| AID1821741 | Binding affinity to wild type human BRD4 BD2 (349 to 461 residues) assessed as change in melting temperature at 2:3 compound to protein ratio by thermal shift assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site. |
| AID731327 | Cytotoxicity against human HeLa cells after 24 hrs by WST-1 assay | 2013 | Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
| Optimization of 3,5-dimethylisoxazole derivatives as potent bromodomain ligands. |
| AID1878590 | Antiproliferative activity against human CAPAN-1 cells assessed as inhibition of cell growth measured after 5 days by MTT assay | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1878714 | Effect on TOPBP1 gene expression in human SW1990 cells at 4 uM by Q-PCR analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1409979 | Inhibition of human His6-tagged BRD4 BD1 (N44 to E168 residues) expressed in Escherichia coli BL21 (DE3) cells at 20 uM using H-SGRGK(Ac)GGK(Ac)GLGK(Ac)GGAK(Ac)RHRK-Biotin-OH as substrate after 2.5 hrs by AlphaScreen assay relative to control | 2018 | ACS medicinal chemistry letters, Mar-08, Volume: 9, Issue:3
| Y08060: A Selective BET Inhibitor for Treatment of Prostate Cancer. |
| AID1308510 | Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by Alamar blue assay | 2016 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
| Targeting epigenetic reader and eraser: Rational design, synthesis and in vitro evaluation of dimethylisoxazoles derivatives as BRD4/HDAC dual inhibitors. |
| AID1357991 | Inhibition of BRD4 BD1 (unknown origin) after 1 hr by TR-FRET assay | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation. |
| AID1368360 | Binding affinity to His-tagged BRD2 bromodomain 1 (unknown origin) by SPR assay | 2018 | Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1
| Exploiting a water network to achieve enthalpy-driven, bromodomain-selective BET inhibitors. |
| AID1878757 | Effect on CDK1 gene expression in human SW1990 cells at 1 uM in presence of Olaparib by Q-PCR analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1230001 | Displacement of FAM-labeled ZBA248 from BRD3 BD1 (24 to 144 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay | 2015 | Journal of medicinal chemistry, Jun-25, Volume: 58, Issue:12
| Structure-Based Design of γ-Carboline Analogues as Potent and Specific BET Bromodomain Inhibitors. |
| AID1286354 | Antiproliferative activity against human HL60 cells after 72 hrs by CCK8 assay | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Discovery of Benzo[cd]indol-2(1H)-ones as Potent and Specific BET Bromodomain Inhibitors: Structure-Based Virtual Screening, Optimization, and Biological Evaluation. |
| AID1229997 | Displacement of FAM-labeled ZBA248 from BRD4 BD1 (44 to 168 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay | 2015 | Journal of medicinal chemistry, Jun-25, Volume: 58, Issue:12
| Structure-Based Design of γ-Carboline Analogues as Potent and Specific BET Bromodomain Inhibitors. |
| AID1387714 | Inhibition of FAM-labeled ZBA248 binding to recombinant N-terminal His6-tagged BRD2 bromodomain 2 (349 to 460 residues) (unknown origin) expressed in Escherichia coli Rosetta2 DE3 after 30 mins by fluorescence polarization assay | 2018 | Journal of medicinal chemistry, 01-25, Volume: 61, Issue:2
| Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression. |
| AID1359754 | Binding affinity to His6-tagged human BRD9 (L14 to Q134 residues) expressed in Escherichia coli BL21(DE3) assessed as change in melting temperature at 200 uM by SYPRO orange dye based fluorescence assay | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer. |
| AID1359752 | Binding affinity to His6-tagged human EP300 (A1040 to G1161 residues) expressed in Escherichia coli BL21(DE3) assessed as change in melting temperature at 200 uM by SYPRO orange dye based fluorescence assay | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer. |
| AID1878586 | Effect on CDC25B gene expression in human SW1990 cells at 4 uM by Q-PCR analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1735644 | Inhibition of HYSGRGK(Ac)GGK(Ac)GLGK(Ac)GGAK(Ac)RHRK(Biotin)-OH binding to recombinant human His6-tagged BRD4 bromodomain 1 (N44 to E168 residues) expressed in Escherichia coli BL21 (DE3) cells measured after 2 hrs by Alphascreen assay | 2018 | Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
| Structure-Based Discovery and Optimization of Benzo[ d]isoxazole Derivatives as Potent and Selective BET Inhibitors for Potential Treatment of Castration-Resistant Prostate Cancer (CRPC). |
| AID1807756 | Binding affinity to recombinant human N-terminal hexaHis-tagged BRDT expressed in Escherichia coli BL21 (DE3) cells by ITC analysis | 2021 | Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
| Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors. |
| AID1831288 | Inhibition of homologous recombinant repair in human SW1990 cells assessed as reduction in Olaparib-induced Rad51 expression at 1 uM after 4 days in presence of Olaparib by Q-PCR analysis | | | |
| AID1600698 | Inhibition of BRD4 bromodomain 1/2 (unknown origin) by alphascreen assay | 2019 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 29, Issue:19
| Design, synthesis and biological evaluation of 3,5-dimethylisoxazole and pyridone derivatives as BRD4 inhibitors. |
| AID1821731 | Binding affinity BRDT BD2 (unknown origin) incubated for 1 hr by TR-FRET assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site. |
| AID1196547 | Binding affinity to ATAD2 (unknown origin) assessed as increase in protein melting temperature at 50 umol by real-time PCR system based thermal shift assay | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
| Fragment-based drug discovery of 2-thiazolidinones as BRD4 inhibitors: 2. Structure-based optimization. |
| AID1456299 | Inhibition of BRD4-BD1 (44 to 168 residues) (unknown origin) at 1 uM using histone H4 peptide as substrate preincubated for 15 mins followed by addition of substrate measured after 60 mins by AlphaScreen assay | 2017 | Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8
| Design, synthesis and biological evaluation of 7-methylimidazo[1,5-a]pyrazin-8(7H)-one derivatives as BRD4 inhibitors. |
| AID1821721 | Antiinflammatory activity in human SAEC assessed as inhibition of Poly(I:C) induced CIG5 expression pretreated for 24 hrs followed by Poly(I:C) addition for 4 hrs by qRT-PCR analysis | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site. |
| AID1705259 | Antiproliferative activity against human HL60 cells incubated for 72 hrs by CCK8 assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Design, synthesis and biological evaluation of indole-2-one derivatives as potent BRD4 inhibitors. |
| AID1831208 | Invivo inhibition of BRD4 expression in human SW1900 cells xenografted in BALB/c mouse assessed as reversal of Olaparib-induced BRD4 accumulation at 15 mg/kg, ip administered for 28 consecutive days in presence of 45 mg/kg Olaparib by immunohistochemical | | | |
| AID1807751 | Binding affinity to recombinant human N-terminal hexaHis-tagged BRD4 expressed in Escherichia coli BL21 (DE3) cells by qPCR assay | 2021 | Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
| Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors. |
| AID1807749 | Binding affinity to recombinant human N-terminal hexaHis-tagged BRD4 expressed in Escherichia coli BL21 (DE3) cells assessed as change in melting temperature by DSF assay | 2021 | Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
| Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors. |
| AID1878623 | Reversal of Olaparib-induced PARP1 expression in nucleus of human SW1990 cells at 1 uM measured after 4 days by Western blot analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID648853 | Binding affinity to BRD4-BD1 by isothermal titration calorimetry | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family. |
| AID1831213 | Induction of apoptosis in human SW1990 cells assessed as late apoptotic cells at 4 uM after 4 days by Annexin V-FITC and propidium iodide staining based flow cytometry (Rvb = 6.22%) | | | |
| AID648860 | Binding affinity to BRD4 by isothermal titration calorimetry | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family. |
| AID1513788 | Inhibition of human 6x-His-tagged BRD4 bromodomain 2 expressed in Escherichia coli | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
| Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor. |
| AID1821742 | Binding affinity to wild type human BRD4 BD2 (349 to 461 residues) assessed as change in melting temperature at 1:5 compound to protein ratio by thermal shift assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site. |
| AID1357985 | Inhibition of BRD4 in human SAE cells assessed as reduction in TLR3 agonist poly(I:C) -induced IL-8 RNA expression at 10 uM preincubated for 24 hrs followed by poly(I:C) addition and measured after 4 hrs by SYBR green dye-based qRT-PCR analysis relative t | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation. |
| AID1705261 | Antiproliferative activity against human WI-38 cells incubated for 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Design, synthesis and biological evaluation of indole-2-one derivatives as potent BRD4 inhibitors. |
| AID1878771 | Effect on Rad52 gene expression in human SW1990 cells at 1 uM in presence of Olaparib by Q-PCR analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1357984 | Inhibition of BRD4 in human SAE cells assessed as reduction in TLR3 agonist poly(I:C) -induced ISG56 RNA expression at 10 uM preincubated for 24 hrs followed by poly(I:C) addition and measured after 4 hrs by SYBR green dye-based qRT-PCR analysis relative | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation. |
| AID1878567 | Induction of apoptosis in human SW1990 cells assessed as early apoptotic cells at 4 uM measured after 4 days by Annexin V-FITC and propidium iodide staining based flow cytometry (Rvb = 1.62%) | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1318694 | Inhibition of human BRD4 BD2 (342 to 460 residues) at 30 uM preincubated for 30 mins followed by substrate addition measured after 30 mins by TR-FRET assay | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Development of 4,5-dihydro-benzodiazepinone derivatives as a new chemical series of BRD4 inhibitors. |
| AID1499131 | Inhibition of JQ1-FITC binding to His6-tagged BRD4-BD1 (unknown origin) expressed in Escherichia coli BL21 (DE3)-codon plus-RIL cells incubated in dark for 4 hrs by fluorescence anisotropy assay | 2017 | European journal of medicinal chemistry, Sep-08, Volume: 137 | Discovery of a series of dihydroquinoxalin-2(1H)-ones as selective BET inhibitors from a dual PLK1-BRD4 inhibitor. |
| AID1718524 | Binding affinity to human BRD4 BD1 (N44 to E168 aa residues) by bromoKdELECT Discover assay | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24
| 4-Acyl Pyrroles as Dual BET-BRD7/9 Bromodomain Inhibitors Address BETi Insensitive Human Cancer Cell Lines. |
| AID1666862 | Binding affinity to BRD4 (unknown origin) | 2020 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 30, Issue:6
| BET proteins: Investigating BRDT as a potential target for male contraception. |
| AID1821735 | Binding affinity to wild type human BRD4 BD1 (44 to 168 residues) assessed as change in melting temperature at 15:2 compound to protein ratio by thermal shift assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site. |
| AID1831528 | Inhibition of BRD2 BD1 (unknown origin) incubated for 2 hrs by TR-FRET assay | 2021 | Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
| Discovery of Novel Dual-Target Inhibitor of Bromodomain-Containing Protein 4/Casein Kinase 2 Inducing Apoptosis and Autophagy-Associated Cell Death for Triple-Negative Breast Cancer Therapy. |
| AID1358020 | Anti-inflammatory activity in poly(I:C)-induced airway inflammation C57BL/6 mouse model assessed as reduction in neutrophils recruitment into bronchoalveolar lavage fluid at 10 mg/kg, ip administered 1 day prior to poly(I:C) stimulation and redosed on day | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation. |
| AID1890891 | Antiinflammatory activity against human THP-1 cells assessed as inhibition of LPS-induced IL-6 production incubated for 18 hrs by ELISA | 2022 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 64 | Development of BRD4 inhibitors as anti-inflammatory agents and antidotes for arsenicals. |
| AID1878704 | Effect on CCNB1 gene expression in human SW1990 cells at 4 uM by Q-PCR analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1615992 | Antiproliferative activity against human HuTu 80 cells after 72 hrs by CCK8 or SRB assay | 2019 | Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18
| Structure-Based Discovery and Development of a Series of Potent and Selective Bromodomain and Extra-Terminal Protein Inhibitors. |
| AID1615981 | Antiproliferative activity against human KG1 cells after 72 hrs by CCK8 or SRB assay | 2019 | Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18
| Structure-Based Discovery and Development of a Series of Potent and Selective Bromodomain and Extra-Terminal Protein Inhibitors. |
| AID1286351 | Binding affinity to human His6-tagged EP300 (A1040 to G1161 residues) expressed in Escherichia coli BL21(DE3) cells at 200 uM incubated for 30 mins by SYPRO orange staining based fluorescence thermal shift assay | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Discovery of Benzo[cd]indol-2(1H)-ones as Potent and Specific BET Bromodomain Inhibitors: Structure-Based Virtual Screening, Optimization, and Biological Evaluation. |
| AID1375118 | Displacement of (+)-JQ1 from 6H-Thr BRD4 Y97A mutant BD2 (unknown origin) after 30 mins by TR-FRET assay | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
| Discovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain. |
| AID1383802 | Inhibition of BRD4 in human TY82 or NCI-H1299 cells assessed as reduction in PD-L1 protein expression at 0.2 to 1 uM after 24 hrs by Western blot analysis | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Structure-based optimization of a series of selective BET inhibitors containing aniline or indoline groups. |
| AID1357990 | Inhibition of BRD4 in human SAE cells assessed as reduction in TLR3 agonist poly(I:C) -induced grobeta RNA expression preincubated for 24 hrs followed by poly(I:C) addition and measured after 4 hrs by SYBR green dye-based qRT-PCR analysis | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation. |
| AID1878680 | Induction of DNA damage in human SW1990 cells assessed as increase in tail DNA at 4 uM incubated for 4 days by comet assay | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1409983 | Antiproliferative activity against human LNCAP cells after 96 hrs by Cell-Titer glo reagent based luminescence assay | 2018 | ACS medicinal chemistry letters, Mar-08, Volume: 9, Issue:3
| Y08060: A Selective BET Inhibitor for Treatment of Prostate Cancer. |
| AID1229999 | Displacement of FAM-labeled ZBA248 from BRD2 BD1 (72 to 205 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay | 2015 | Journal of medicinal chemistry, Jun-25, Volume: 58, Issue:12
| Structure-Based Design of γ-Carboline Analogues as Potent and Specific BET Bromodomain Inhibitors. |
| AID1513791 | Inhibition of BRD4 bromodomain 2 (unknown origin) expressed in Escherichia coli Bl21(DE3) by fluorescence anisotropy | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
| Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor. |
| AID1357996 | Inhibition of BRD3 BD2 (unknown origin) after 1 hr by TR-FRET assay | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation. |
| AID1831297 | Inhibition of homologous recombinant repair in human SW1990 cells assessed as increase in HEX1M1 expression at 4 uM after 4 days by Western blot analysis | | | |
| AID1286355 | Antiproliferative activity against human HT-29 cells after 72 hrs by CCK8 assay | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Discovery of Benzo[cd]indol-2(1H)-ones as Potent and Specific BET Bromodomain Inhibitors: Structure-Based Virtual Screening, Optimization, and Biological Evaluation. |
| 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. |
| 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. |
| AID1909972 | Induction of apoptosis in human HCT116 cells assessed as early apoptotic cells at 10 uM measured after 72 hrs by flow cytometry (Rvb = 2.8 %) | 2022 | Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
| Design and Synthesis of Dual EZH2/BRD4 Inhibitors to Target Solid Tumors. |
| 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. |
| AID1808922 | Displacement of FITC-conjugated JQ1 from BRD4 BD2 L383V mutant (unknown origin) expressed in Escherichia coli BL21-DE3 rosetta cells incubated for 15 mins by competitive fluorescence polarization assay | 2021 | Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
| Structure-Guided Design of a "Bump-and-Hole" Bromodomain-Based Degradation Tag. |
| AID1513829 | Binding affinity to BRD4 C-terminal bromodomain 2 (unknown origin) expressed in Escherichia coli Bl21(DE3) | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
| Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor. |
| AID1878766 | Effect on FOXO1 gene expression in human SW1990 cells at 1 uM in presence of Olaparib by Q-PCR analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1683135 | Binding affinity to SMARCA2 (unknown origin) assessed as change in melting temperature at 20 uM by SYPRO orange dye based DSF assay | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
| Pan-SMARCA/PB1 Bromodomain Inhibitors and Their Role in Regulating Adipogenesis. |
| AID1711598 | Inhibition of His/FLAG-tagged BRD4 BD1 (unknown origin) using histone H4-TetraAcetylated-biotin peptide as substrate incubated for 20 mins by AlphaLISA assay | 2016 | ACS medicinal chemistry letters, Feb-11, Volume: 7, Issue:2
| Discovery of Benzotriazolo[4,3-d][1,4]diazepines as Orally Active Inhibitors of BET Bromodomains. |
| AID1878646 | Induction of cell cycle arrest in human SW1990 cells assessed as accumulation of cells at S phase at 1 uM incubated for 4 days in presence of 3 uM Olaparib by propidium iodide staining based flow cytometry (Rvb = 29.32%) | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1460620 | Inhibition of recombinant human His6-tagged BRD4 bromodomain 2 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells preincubated for 30 mins followed by HSGRGK(Ac)GGK(Ac)GLGK(Ac)GGAK(Ac)RHRK(Biotin)-OH peptide substrate addition after 30 mins by alphas | 2017 | Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
| Drug Discovery Targeting Bromodomain-Containing Protein 4. |
| AID649998 | Displacement of acetylated histone peptide from BRD4-BD1 by luminescence proximity homogenous assay | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| Development of live-cell imaging probes for monitoring histone modifications. |
| AID1831228 | Induction of cell cycle arrest in human SW1990 cells assessed as accumulation of cells at S phase at 4 uM incubated for 4 days by propidium iodide staining based flow cytometry (Rvb = 29.32%) | | | |
| AID1357988 | Inhibition of BRD4 in human SAE cells assessed as reduction in TLR3 agonist poly(I:C) -induced ISG56 RNA expression preincubated for 24 hrs followed by poly(I:C) addition and measured after 4 hrs by SYBR green dye-based qRT-PCR analysis | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation. |
| AID1196544 | Binding affinity to BRD2(1) (unknown origin) assessed as increase in protein melting temperature at 50 umol by real-time PCR system based thermal shift assay | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
| Fragment-based drug discovery of 2-thiazolidinones as BRD4 inhibitors: 2. Structure-based optimization. |
| AID1513945 | Inhibition of fluorescent-tagged ligand from nanoLuc fused full length BRD4 (unknown origin) expressed in 293T cells by luciferase reporter gene based BRET engagement assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
| GNE-371, a Potent and Selective Chemical Probe for the Second Bromodomains of Human Transcription-Initiation-Factor TFIID Subunit 1 and Transcription-Initiation-Factor TFIID Subunit 1-like. |
| AID1725781 | Inhibition of BRD4 bromodomain1 (unknown origin) using peptide histone H4 (SGRGACKGGACKGLGAC-KGGAACKRHGSGSK-biotin) as substrate incubated for 15 mins followed by substrate addition measured after 1 hr by alphascreen assay | 2020 | ACS medicinal chemistry letters, Nov-12, Volume: 11, Issue:11
| Identification of 3,5-Dimethylisoxazole Derivatives as BRD4 Inhibitors for the Treatment of Colorectal Cancer. |
| AID1230008 | Binding affinity to biotinylated BRD4 BD2 (333 to 460 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometry method | 2015 | Journal of medicinal chemistry, Jun-25, Volume: 58, Issue:12
| Structure-Based Design of γ-Carboline Analogues as Potent and Specific BET Bromodomain Inhibitors. |
| AID1859891 | Inhibition of His tagged human BRD4 BD2 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells using HSGRGK(Ac)GGK(Ac)GLGK(Ac)GGAK(Ac)RHRK(Biotin)-OH peptide as substrate pretreated for 30 mins followed by substrate addition and measured after 30 mins by | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Discovery of 2-((2-methylbenzyl)thio)-6-oxo-4-(3,4,5-trimethoxyphenyl)-1,6-dihydropyrimidine-5-carbonitrile as a novel and effective bromodomain and extra-terminal (BET) inhibitor for the treatment of sepsis. |
| AID1814807 | Binding affinity to BRD4 BD1 (unknown origin) by fluorescence anisotropy method | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
| 4-Methyl-1,2,3-Triazoles as |
| AID1359759 | Binding affinity to His6-tagged human PCAF (G715 to D831 residues) expressed in Escherichia coli BL21(DE3) assessed as change in melting temperature at 200 uM by SYPRO orange dye based fluorescence assay | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer. |
| AID1196554 | Inhibition of CYP3A4 in human liver microsomes at 10 uM using midazolam substrate preincubated for 5 mins before NADPH addition and measured after 20 mins post NADPH addition | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
| Fragment-based drug discovery of 2-thiazolidinones as BRD4 inhibitors: 2. Structure-based optimization. |
| AID1905955 | Binding affinity to His6-fused BRD2 BD1 (unknown origin) assessed as change in melting temperature at 100 uM incubated for 30 mins by thermal shift assay | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
| Structure-Based Discovery and Optimization of Furo[3,2- |
| AID1878577 | Toxicity in nude mouse xenografted with human SW1990 cells assessed as heart damage at 15 mg/kg, ip administered for 28 days in presence of 45 mg/kg Olaparib by H and E staining based fluorescence microscopic analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1831198 | Toxicity in BALB/c mouse xenografted with human SW1990 cells assessed as liver damage at 15 mg/kg, ip administered for 28 consecutive days in presence of 45 mg/kg Olaparib | | | |
| AID1878709 | Effect on BRCA1 gene expression in human SW1990 cells at 4 uM by Q-PCR analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1683134 | Binding affinity to SMARCA4 (unknown origin) assessed as change in melting temperature at 20 uM by SYPRO orange dye based DSF assay | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
| Pan-SMARCA/PB1 Bromodomain Inhibitors and Their Role in Regulating Adipogenesis. |
| AID1846022 | Antiproliferative activity against human Medulloblastoma cells expressing wild type SMO assessed as reduction in cell viability | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | Medulloblastoma drugs in development: Current leads, trials and drawbacks. |
| AID1454053 | Growth inhibition of human MCF7 cells after 3 days by WST1 assay | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
| Synthesis and evaluation of novel dual BRD4/HDAC inhibitors. |
| AID1547268 | Inhibition of HDAC4 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
| Discovery of Thieno[2,3- |
| AID1544777 | Induction of apoptosis in human MV4-11 cells assessed as early apoptotic cells level at 1 uM incubated for 24 hrs by Annexin V-FITC and propidium iodide staining based flow cytometry (Rvb = 0.8%) | 2019 | Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
| Design, synthesis and biological evaluation of novel 4,5-dihydro-[1,2,4]triazolo[4,3-f]pteridine derivatives as potential BRD4 inhibitors. |
| AID1831259 | Effect on cell cycle progression in human SW1990 cells assessed as reduction in Olaparib-induced PLK1 expression at 1 uM after 4 days in presence of Olaparib by Q-PCR analysis | | | |
| AID1664722 | Induction of apoptosis in human MV4-11 cells assessed as late apoptotic cell at 0.5 uM after 12 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 1.28 %) | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15
| Design, synthesis and biological evaluation of novel 6-phenyl-1,3a,4,10b-tetrahydro-2H-benzo[c]thiazolo[4,5-e]azepin-2-one derivatives as potential BRD4 inhibitors. |
| AID1230006 | Binding affinity to biotinylated BRD3 BD2 (306 to 417 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometry method | 2015 | Journal of medicinal chemistry, Jun-25, Volume: 58, Issue:12
| Structure-Based Design of γ-Carboline Analogues as Potent and Specific BET Bromodomain Inhibitors. |
| AID1650529 | Inhibition of recombinant human GST-tagged BRD4 BD1 (44 to 168 residues) expressed in Escherichia coli incubated for 60 mins by alphascreen assay | 2020 | Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
| Discovery of a new class of PROTAC BRD4 degraders based on a dihydroquinazolinone derivative and lenalidomide/pomalidomide. |
| AID1762763 | Antiproliferative activity against human CT26 cells assessed as inhibition of cell proliferation at 2 uM incubated for 48 hrs by MTT assay relative to control | 2021 | Bioorganic & medicinal chemistry, 06-01, Volume: 39 | Discovery of 3,5-dimethylisoxazole derivatives as novel, potent inhibitors for bromodomain and extraterminal domain (BET) family. |
| AID1821727 | Binding affinity BRD2 BD2 (unknown origin) incubated for 1 hr by TR-FRET assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site. |
| AID1559436 | Inhibition of BRD4 BD1 in HUVEC assessed as downregulation of NF-kappaB activity at 0.1 to 10 uM incubated for 24 hrs by dual luciferase reporter gene assay | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Discovery of Benzo[ |
| AID1905959 | Binding affinity to CECR2 (unknown origin) assessed as change in melting temperature at 100 uM incubated for 30 mins by thermal shift assay | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
| Structure-Based Discovery and Optimization of Furo[3,2- |
| AID1831229 | Induction of cell cycle arrest in human SW1990 cells assessed as accumulation of cells at G2/M phase at 4 uM incubated for 4 days by propidium iodide staining based flow cytometry (Rvb = 5.89%) | | | |
| AID1878715 | Effect on ALDH1A1 gene expression in human SW1990 cells at 4 uM by Q-PCR analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1448426 | Inhibition of BRD4 bromodomain in human MM1S cells assessed as upregulation of p21Cip1 levels after 6 hrs by Western blot analysis | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
| BET Bromodomain Inhibitors with One-Step Synthesis Discovered from Virtual Screen. |
| AID1594416 | Antifibrotic activity against human HLF1 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
| Binding pocket-based design, synthesis and biological evaluation of novel selective BRD4-BD1 inhibitors. |
| AID1652231 | Displacement of APC-labeled biotinylated-avidin from Euphorium-chelated recombinant human BRD4 bromodomain 2 expressed in Escherichia coli preincubated for 15 mins followed by APC-labeled biotinylated-avidin addition and measured after 1 hr under dark con | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
| Novel Pyrrolopyridone Bromodomain and Extra-Terminal Motif (BET) Inhibitors Effective in Endocrine-Resistant ER+ Breast Cancer with Acquired Resistance to Fulvestrant and Palbociclib. |
| AID1615993 | Antiproliferative activity against human SW620 cells after 72 hrs by CCK8 or SRB assay | 2019 | Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18
| Structure-Based Discovery and Development of a Series of Potent and Selective Bromodomain and Extra-Terminal Protein Inhibitors. |
| AID1368366 | Cytotoxicity against human HD-MB03 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay | 2018 | Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1
| Exploiting a water network to achieve enthalpy-driven, bromodomain-selective BET inhibitors. |
| AID1705271 | Inhibition of BRD4 BD2 (unknown origin) preincubated for 15 mins followed by peptide addition and measured after 60 mins by TR-FRET assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Design, synthesis and biological evaluation of indole-2-one derivatives as potent BRD4 inhibitors. |
| AID1878767 | Effect on FOXM1 gene expression in human SW1990 cells at 1 uM in presence of Olaparib by Q-PCR analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1600699 | Antiproliferative activity against human HCT116 cells | 2019 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 29, Issue:19
| Design, synthesis and biological evaluation of 3,5-dimethylisoxazole and pyridone derivatives as BRD4 inhibitors. |
| AID1462227 | Inhibition of BRD4/HDAC1 in human OCI-AML2 cells assessed as reduction in myc expression levels at 1 uM after 24 hrs by Western blot analysis | 2017 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
| Structure-based design, synthesis and in vitro antiproliferative effects studies of novel dual BRD4/HDAC inhibitors. |
| AID1460683 | Binding affinity to recombinant human His6-tagged BRD4 bromodomain 1 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells assessed as change in melting temperature by SYPRO orange dye based fluorescence assay | 2017 | Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
| Drug Discovery Targeting Bromodomain-Containing Protein 4. |
| AID1594408 | Antiproliferative activity against human HT-29 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
| Binding pocket-based design, synthesis and biological evaluation of novel selective BRD4-BD1 inhibitors. |
| AID1594422 | Inhibition of BRD4 in human HLF1 cells assessed as reduction in collagen-1 mRNA expression at 10 uM measured after 24 hrs by RT-PCR analysis | 2019 | Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
| Binding pocket-based design, synthesis and biological evaluation of novel selective BRD4-BD1 inhibitors. |
| AID1831211 | Invivo inhibition of PARP1 expression in human SW1900 cells xenografted in BALB/c mouse assessed as reversal of Olaparib-induced PARP1 accumulation at 15 mg/kg, ip administered for 28 consecutive days in presence of 45 mg/kg Olaparib by Western blot analy | | | |
| AID1878591 | Antiproliferative activity against human CAPAN-1 cells assessed as inhibition of cell growth measured after 7 days by MTT assay | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1720096 | Inhibition of HDAC (unknown origin) | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
| Dual-Target Inhibitors Based on HDACs: Novel Antitumor Agents for Cancer Therapy. |
| AID1878600 | Toxicity in nude mouse xenografted with human SW1990 cells assessed as heart damage at 15 mg/kg, ip administered for 28 days by H and E staining based fluorescence microscopic analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1664716 | Induction of apoptosis in human MV4-11 cells assessed as necrotic cell at 0.5 uM after 12 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 0.17 %) | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15
| Design, synthesis and biological evaluation of novel 6-phenyl-1,3a,4,10b-tetrahydro-2H-benzo[c]thiazolo[4,5-e]azepin-2-one derivatives as potential BRD4 inhibitors. |
| AID650000 | Displacement of acetylated histone peptide from CREBBP by luminescence proximity homogenous assay | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| Development of live-cell imaging probes for monitoring histone modifications. |
| AID1652230 | Growth inhibition of fulvestrant-resistant human MCF7:CFR cells measured after 5 days by Hoechst 33342 dye based imaging analysis | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
| Novel Pyrrolopyridone Bromodomain and Extra-Terminal Motif (BET) Inhibitors Effective in Endocrine-Resistant ER+ Breast Cancer with Acquired Resistance to Fulvestrant and Palbociclib. |
| AID1878647 | Induction of cell cycle arrest in human SW1990 cells assessed as accumulation of cells at G2/M phase at 1 uM incubated for 4 days in presence of 3 uM Olaparib by propidium iodide staining based flow cytometry (Rvb = 5.89%) | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1499135 | Antiproliferative activity against human MM1S cells after 72 hrs by CCK8 assay | 2017 | European journal of medicinal chemistry, Sep-08, Volume: 137 | Discovery of a series of dihydroquinoxalin-2(1H)-ones as selective BET inhibitors from a dual PLK1-BRD4 inhibitor. |
| AID1357992 | Inhibition of BRD4 BD2 (unknown origin) after 1 hr by TR-FRET assay | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation. |
| AID1881993 | Inhibition of BRD4 BD2 (unknown origin) by Alpha screen assay | | | |
| AID1831142 | Antiproliferative activity against human CAPAN-1 cells assessed as reduction in cell viability after 4 days by MTT assay | | | |
| AID1878583 | Antiproliferative activity against human SW1990 cells assessed as inhibition of cell growth measured after 4 days by MTT assay | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1286360 | Binding affinity to human His6-tagged BRD1 (E556 to A688 residues) expressed in Escherichia coli BL21(DE3) cells at 200 uM incubated for 30 mins by SYPRO orange staining based fluorescence thermal shift assay | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Discovery of Benzo[cd]indol-2(1H)-ones as Potent and Specific BET Bromodomain Inhibitors: Structure-Based Virtual Screening, Optimization, and Biological Evaluation. |
| AID1358023 | Anti-inflammatory activity in poly(I:C)-induced airway inflammation C57BL/6 mouse model assessed as reduction in mIL6 expression in lung at 10 mg/kg, ip administered 1 day prior to poly(I:C) stimulation and redosed on day 2 followed by poly(I:C) stimulati | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation. |
| AID1725783 | Antiproliferation activity against human BxPC3 cells assessed as reduction in cell viability at 2.5 uM incubated for 48 hrs by MTT assay relative to control | 2020 | ACS medicinal chemistry letters, Nov-12, Volume: 11, Issue:11
| Identification of 3,5-Dimethylisoxazole Derivatives as BRD4 Inhibitors for the Treatment of Colorectal Cancer. |
| AID1385736 | Inhibition of BRDT-BD1 (unknown origin) incubated for 1 hr by AlphaScreen biotin-JQ1 competition assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
| Structure-Guided Design and Development of Potent and Selective Dual Bromodomain 4 (BRD4)/Polo-like Kinase 1 (PLK1) Inhibitors. |
| AID1831185 | Toxicity in BALB/c mouse xenografted with human SW1990 cells assessed as kidney damage at 15 mg/kg, ip administered for 28 consecutive days by H and E staining based fluorescence microscopic analysis | | | |
| AID1359768 | Antiproliferative activity against human DU145 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer. |
| AID1878712 | Effect on FOXO1 gene expression in human SW1990 cells at 4 uM by Q-PCR analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1465449 | Antiproliferative activity against human MX1 cells after 72 hrs by Cell Titer Glo assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of N-(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor. |
| AID1705286 | Inhibition of human His-tagged BRD4 BD2 domain using H-SGRGK(Ac)GGK(Ac)GLGK-(Ac)GGAK(Ac)RHRK(Biotin)-OH as substrate preincubated for 30 mins followed by substrate addition measured after 30 mins by AlphaScreen assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Design, synthesis and biological evaluation of indole-2-one derivatives as potent BRD4 inhibitors. |
| AID731328 | Cytotoxicity against human U2OS cells after 24 hrs by WST-1 assay | 2013 | Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
| Optimization of 3,5-dimethylisoxazole derivatives as potent bromodomain ligands. |
| AID1230018 | Cytotoxicity against human MV4-11 cells harboring MLL1 fusion gene assessed as growth inhibition after 4 days by CellTiter-Glo luminescent assay | 2015 | Journal of medicinal chemistry, Jun-25, Volume: 58, Issue:12
| Structure-Based Design of γ-Carboline Analogues as Potent and Specific BET Bromodomain Inhibitors. |
| AID1821746 | Binding affinity to human BRD4 BD1 E151A mutant assessed as change in melting temperature at 10:1 compound to protein ratio by thermal shift assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site. |
| AID1368359 | Selectivity index, ratio of IC50 for recombinant human BRD2 bromodomain 1 (49 to 170 residues) to IC50 for recombinant human BRD2 bromodomain 2 (342 to 460 residues) | 2018 | Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1
| Exploiting a water network to achieve enthalpy-driven, bromodomain-selective BET inhibitors. |
| AID1831234 | Induction of cell cycle arrest in human SW1990 cells assessed as accumulation of cells at S phase at 1 uM incubated for 4 days in presence of 3 uM Olaparib by propidium iodide staining based flow cytometry (Rvb = 29.32%) | | | |
| AID1664718 | Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15
| Design, synthesis and biological evaluation of novel 6-phenyl-1,3a,4,10b-tetrahydro-2H-benzo[c]thiazolo[4,5-e]azepin-2-one derivatives as potential BRD4 inhibitors. |
| AID1831255 | Effect on cell cycle progression in human SW1990 cells assessed as reduction in Olaparib-induced CDK6 expression at 1 uM after 4 days in presence of Olaparib by Q-PCR analysis | | | |
| AID1821715 | Binding affinity to wild type human BRD4 BD1 (44 to 168 residues) assessed as change in melting temperature at 2:0 compound to protein ratio by thermal shift assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site. |
| AID1652287 | Down regulation of n-MYC gene expression in fulvestrant-resistant human MCF7:CFR cells at 100 nM measured after 24 hrs | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
| Novel Pyrrolopyridone Bromodomain and Extra-Terminal Motif (BET) Inhibitors Effective in Endocrine-Resistant ER+ Breast Cancer with Acquired Resistance to Fulvestrant and Palbociclib. |
| AID1318695 | Cytotoxicity against human U937 cells assessed as decrease in cell viability after 24 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Development of 4,5-dihydro-benzodiazepinone derivatives as a new chemical series of BRD4 inhibitors. |
| AID1652337 | Growth inhibition of fulvestrant-resistant human MCF7:CFR cells at < 300 nM treated for 3 hrs followed by compound washout and measured after 5 days by Hoechst 33342 dye based imaging analysis | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
| Novel Pyrrolopyridone Bromodomain and Extra-Terminal Motif (BET) Inhibitors Effective in Endocrine-Resistant ER+ Breast Cancer with Acquired Resistance to Fulvestrant and Palbociclib. |
| AID1383780 | Displacement of FITC-JQ1 from His6-tagged BRD4 bromodomain-1 (unknown origin) expressed in Escherichia coli BL21(DE3) after 4 hrs by fluorescence anisotropy method | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Structure-based optimization of a series of selective BET inhibitors containing aniline or indoline groups. |
| AID1831285 | Inhibition of homologous recombinant repair in human SW1990 cells assessed as reduction in Olaparib-induced FOXM1 expression at 1 uM after 4 days in presence of Olaparib by Western blot analysis | | | |
| AID1286353 | Antiproliferative activity against human MV4-11 cells after 72 hrs by CCK8 assay | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Discovery of Benzo[cd]indol-2(1H)-ones as Potent and Specific BET Bromodomain Inhibitors: Structure-Based Virtual Screening, Optimization, and Biological Evaluation. |
| AID1308515 | Binding affinity to human BRD4 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 assessed as change in melting temperature at 25 uM by SYPRO orange based protein stability shift assay | 2016 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
| Targeting epigenetic reader and eraser: Rational design, synthesis and in vitro evaluation of dimethylisoxazoles derivatives as BRD4/HDAC dual inhibitors. |
| AID1308516 | Binding affinity to human BRD9 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 assessed as change in melting temperature at 25 uM by SYPRO orange based protein stability shift assay | 2016 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
| Targeting epigenetic reader and eraser: Rational design, synthesis and in vitro evaluation of dimethylisoxazoles derivatives as BRD4/HDAC dual inhibitors. |
| AID1831218 | Induction of apoptosis in human SW1990 cells assessed as early apoptotic cells at 1 uM after 4 days in presence of 3 uM Olaparib by Annexin V-FITC and propidium iodide staining based flow cytometry (Rvb = 1.91%) | | | |
| AID1814808 | Binding affinity to BRD4 BD2 (unknown origin) by fluorescence anisotropy method | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
| 4-Methyl-1,2,3-Triazoles as |
| AID1720097 | Inhibition of BRD4 (unknown origin) at 10 uM relative to control | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
| Dual-Target Inhibitors Based on HDACs: Novel Antitumor Agents for Cancer Therapy. |
| AID1454034 | Growth inhibition of human HL60 cells after 3 days by counting method | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
| Synthesis and evaluation of novel dual BRD4/HDAC inhibitors. |
| AID1762770 | Antiproliferative activity against human U-266 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay | 2021 | Bioorganic & medicinal chemistry, 06-01, Volume: 39 | Discovery of 3,5-dimethylisoxazole derivatives as novel, potent inhibitors for bromodomain and extraterminal domain (BET) family. |
| AID1878705 | Effect on CDK6 gene expression in human SW1990 cells at 4 uM by Q-PCR analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1821722 | Antiinflammatory activity in human SAEC assessed as inhibition of Poly(I:C) induced IL-6 expression pretreated for 24 hrs followed by Poly(I:C) addition for 4 hrs by qRT-PCR analysis | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site. |
| AID1460634 | Antiproliferative activity against human MV4-11 cells | 2017 | Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
| Drug Discovery Targeting Bromodomain-Containing Protein 4. |
| AID1359773 | Antiproliferative activity against human HT-29 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer. |
| AID1722822 | Inhibition of BRD4 in human HCT-116 cells assessed as reduction in c-Myc protein expression at 50 to 500 nM after 24 hrs by Western blot analysis | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
| Rational Design and Evaluation of 6-(Pyrimidin-2-ylamino)-3,4-dihydroquinoxalin-2(1 |
| AID1196543 | Binding affinity to BRD4(1) (unknown origin) assessed as increase in protein melting temperature at 50 umol by real-time PCR system based thermal shift assay | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
| Fragment-based drug discovery of 2-thiazolidinones as BRD4 inhibitors: 2. Structure-based optimization. |
| AID1821771 | Antiinflammatory activity in human SAEC assessed as decrease in H3K122Ac accumulation by immunofluorescence analysis | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site. |
| AID649991 | Binding affinity to BRD4-BD1 by isothermal titration calorimetry | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| Development of live-cell imaging probes for monitoring histone modifications. |
| AID1807577 | AUC in mouse at 3 mg/kg, po measured after 24 hrs | 2021 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 51 | Development of BET inhibitors as potential treatments for cancer: A new carboline chemotype. |
| AID1831257 | Effect on cell cycle progression in human SW1990 cells assessed as reduction in Olaparib-induced CCND1 expression at 1 uM after 4 days in presence of Olaparib by Q-PCR analysis | | | |
| AID1359747 | Binding affinity to His6-tagged human BRD2 bromodomain-2 expressed in Escherichia coli BL21(DE3) assessed as change in melting temperature at 200 uM by SYPRO orange dye based fluorescence assay | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer. |
| AID1615982 | Antiproliferative activity against human RKO cells after 72 hrs by CCK8 or SRB assay | 2019 | Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18
| Structure-Based Discovery and Development of a Series of Potent and Selective Bromodomain and Extra-Terminal Protein Inhibitors. |
| AID1909992 | Antiproliferative activity against human ASPC1 cells assessed as cell growth inhibition incubated for 6 days by MTS assay | 2022 | Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
| Design and Synthesis of Dual EZH2/BRD4 Inhibitors to Target Solid Tumors. |
| AID1831270 | Induction of DNA damage in human SW1990 cells assessed as tail DNA at 4 uM incubated for 4 days by comet assay | | | |
| AID1606744 | Binding affinity to recombinant BRD3 BD1 (unknown origin) incubated for 1 hr by TR-FRET assay | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation. |
| 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. |
| AID1286352 | Binding affinity to human His6-tagged BRD4 bromodomain 1 (N44 to E168 residues) expressed in Escherichia coli BL21(DE3) cells by isothermal titration calorimetry | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Discovery of Benzo[cd]indol-2(1H)-ones as Potent and Specific BET Bromodomain Inhibitors: Structure-Based Virtual Screening, Optimization, and Biological Evaluation. |
| AID1683137 | Binding affinity to polybromo-1 (4) (unknown origin) assessed as change in melting temperature at 20 uM by SYPRO orange dye based DSF assay | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
| Pan-SMARCA/PB1 Bromodomain Inhibitors and Their Role in Regulating Adipogenesis. |
| AID1286361 | Binding affinity to human His6-tagged BRD9 (L14 to Q134 residues) expressed in Escherichia coli BL21(DE3) cells at 200 uM incubated for 30 mins by SYPRO orange staining based fluorescence thermal shift assay | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Discovery of Benzo[cd]indol-2(1H)-ones as Potent and Specific BET Bromodomain Inhibitors: Structure-Based Virtual Screening, Optimization, and Biological Evaluation. |
| AID1831533 | Inhibition of BRD4 BD2 (unknown origin) incubated for 2 hrs by TR-FRET assay | 2021 | Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
| Discovery of Novel Dual-Target Inhibitor of Bromodomain-Containing Protein 4/Casein Kinase 2 Inducing Apoptosis and Autophagy-Associated Cell Death for Triple-Negative Breast Cancer Therapy. |
| AID1359775 | Antiproliferative activity against human HeLa cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer. |
| AID1515645 | Permeability of compound in 5% DMSO after 7 hrs by PAMPA | 2019 | MedChemComm, Jun-01, Volume: 10, Issue:6
| Controlling cellular distribution of drugs with permeability modifying moieties. |
| AID1196553 | Stability in human liver microsomes assessed as clearance at 1 uM pre-incubated for 5 mins followed by NADPH addition and measured after 5 to 30 mins post NADPH addition by LC/MS/MS method | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
| Fragment-based drug discovery of 2-thiazolidinones as BRD4 inhibitors: 2. Structure-based optimization. |
| AID1615932 | Antiproliferative activity against human MM1S cells after 72 hrs by CCK8 or SRB assay | 2019 | Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18
| Structure-Based Discovery and Development of a Series of Potent and Selective Bromodomain and Extra-Terminal Protein Inhibitors. |
| AID1400168 | Inhibition of N-terminal His-tagged BRD4 (BD2) (unknown origin) using biotinylated tetra-acetylated histone H4 peptide after 30 mins by alpha-screen assay | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
| Design and Characterization of Novel Covalent Bromodomain and Extra-Terminal Domain (BET) Inhibitors Targeting a Methionine. |
| 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. |
| AID1359743 | Inhibition of His6-tagged human BRD4 bromodomain-1 (N44 to E168 residues) expressed in Escherichia coli BL21(DE3) using biotinylated-H4KAc4 as substrate by AlphaScreen assay | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer. |
| AID1368362 | Selectivity index, ratio of Kd for His-tagged BRD2 bromodomain 1 (unknown origin) to Kd for His-tagged BRD2 bromodomain 2 (unknown origin) | 2018 | Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1
| Exploiting a water network to achieve enthalpy-driven, bromodomain-selective BET inhibitors. |
| AID1905947 | Selectivity index, ratio of IC50 for BRD4 BD1 (unknown origin) to IC50 of BRD4 BD2 (unknown origin) | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
| Structure-Based Discovery and Optimization of Furo[3,2- |
| AID1831296 | Inhibition of homologous recombinant repair in human SW1990 cells assessed as increase in HEX1M1 expression at 4 uM after 4 days by Q-PCR analysis | | | |
| AID1456301 | Inhibition of BRD4-BD2 (333 to 460 residues) (unknown origin) using histone H4 peptide as substrate preincubated for 15 mins followed by addition of substrate measured after 60 mins by AlphaScreen assay | 2017 | Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8
| Design, synthesis and biological evaluation of 7-methylimidazo[1,5-a]pyrazin-8(7H)-one derivatives as BRD4 inhibitors. |
| AID1831137 | Induction of autophagy in human SW1990 cells assessed as increase in LC3B expression at 4 uM incubated for 4 days by immunofluorescence assay | | | |
| AID1594407 | Antiproliferative activity against human A549 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
| Binding pocket-based design, synthesis and biological evaluation of novel selective BRD4-BD1 inhibitors. |
| AID1762766 | Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation at 2 uM incubated for 48 hrs by MTT assay relative to control | 2021 | Bioorganic & medicinal chemistry, 06-01, Volume: 39 | Discovery of 3,5-dimethylisoxazole derivatives as novel, potent inhibitors for bromodomain and extraterminal domain (BET) family. |
| AID1831294 | Inhibition of homologous recombinant repair in human SW1990 cells assessed as reduction in Rad51 expression at 4 uM after 4 days by Q-PCR analysis | | | |
| AID1878568 | Induction of apoptosis in human SW1990 cells assessed as late apoptotic cells at 1 uM measured after 4 days in presence of 3 uM Olaparib by Annexin V-FITC and propidium iodide staining based flow cytometry (Rvb = 7.23%) | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1808920 | Displacement of FITC-conjugated JQ1 from BRD4 BD1 L94V mutant (unknown origin) expressed in Escherichia coli BL21-DE3 rosetta cells incubated for 15 mins by competitive fluorescence polarization assay | 2021 | Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
| Structure-Guided Design of a "Bump-and-Hole" Bromodomain-Based Degradation Tag. |
| AID1308521 | Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by Alamar blue assay | 2016 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
| Targeting epigenetic reader and eraser: Rational design, synthesis and in vitro evaluation of dimethylisoxazoles derivatives as BRD4/HDAC dual inhibitors. |
| AID1831161 | Inhibition of recombinant BRD4 BD2 (unknown origin) incubated for 120 mins by TR-FRET assay | | | |
| AID1878575 | Antiproliferative activity against BRCA-proficient human MDA-MB-468 cells assessed as inhibition of cell growth measured after 7 days by MTT assay | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1544782 | Induction of apoptosis in human MV4-11 cells assessed as late apoptotic cells level at 5 uM incubated for 24 hrs by Annexin V-FITC and propidium iodide staining based flow cytometry (Rvb = 1.5%) | 2019 | Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
| Design, synthesis and biological evaluation of novel 4,5-dihydro-[1,2,4]triazolo[4,3-f]pteridine derivatives as potential BRD4 inhibitors. |
| 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. |
| AID1821751 | Binding affinity to human BRD4 BD1 E151A mutant assessed as change in melting temperature at 1:3 compound to protein ratio by thermal shift assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site. |
| AID1808923 | Displacement of FITC-conjugated JQ1 from BRD4 BD2 (unknown origin) expressed in Escherichia coli BL21-DE3 rosetta cells incubated for 15 mins by competitive fluorescence polarization assay | 2021 | Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
| Structure-Guided Design of a "Bump-and-Hole" Bromodomain-Based Degradation Tag. |
| AID1196556 | Inhibition of CYP2D6 in human liver microsomes at 10 uM using dextromethorphan substrate preincubated for 5 mins before NADPH addition and measured after 20 mins post NADPH addition | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
| Fragment-based drug discovery of 2-thiazolidinones as BRD4 inhibitors: 2. Structure-based optimization. |
| AID1881992 | Inhibition of BRD4 BD1 (unknown origin) by Alpha screen assay | | | |
| AID1846021 | Antiproliferative activity against human Med1 cells assessed as reduction in cell viability | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | Medulloblastoma drugs in development: Current leads, trials and drawbacks. |
| AID1515644 | Inhibition of BRD4 in human H1229 cells transfected with HPV-E2 assessed as transrepression of HPV-long control region by luciferase reporter assay | 2019 | MedChemComm, Jun-01, Volume: 10, Issue:6
| Controlling cellular distribution of drugs with permeability modifying moieties. |
| AID1289188 | Displacement of biotinylated tetra-acetylated histone H4 from human his-tagged BRD4 bromodomain1 by alphascreen assay | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Disrupting Acetyl-Lysine Recognition: Progress in the Development of Bromodomain Inhibitors. |
| AID1878645 | Induction of cell cycle arrest in human SW1990 cells assessed as accumulation of cells at G0/G1 phase at 1 uM incubated for 4 days in presence of 3 uM Olaparib by propidium iodide staining based flow cytometry (Rvb = 64.79%) | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1831143 | Antiproliferative activity against human SW1990 cells assessed as reduction in cell viability after 4 days by MTT assay | | | |
| 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. |
| AID1286349 | Binding affinity to human His6-tagged BRD4 bromodomain 1 (N44 to E168 residues) expressed in Escherichia coli BL21(DE3) cells at 200 uM incubated for 30 mins by SYPRO orange staining based fluorescence thermal shift assay | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Discovery of Benzo[cd]indol-2(1H)-ones as Potent and Specific BET Bromodomain Inhibitors: Structure-Based Virtual Screening, Optimization, and Biological Evaluation. |
| AID1878768 | Effect on TOPBP1 gene expression in human SW1990 cells at 1 uM in presence of Olaparib by Q-PCR analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1664729 | Inhibition of BRD4 in human MV4-11 cells assessed as reduction in c-Myc expression level at 0.5 uM to 5 uM after 4 hrs by Western blot analysis | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15
| Design, synthesis and biological evaluation of novel 6-phenyl-1,3a,4,10b-tetrahydro-2H-benzo[c]thiazolo[4,5-e]azepin-2-one derivatives as potential BRD4 inhibitors. |
| AID1831148 | Inhibition of recombinant BRD4 (unknown origin) incubated for 120 mins by TR-FRET assay | | | |
| AID1308520 | Binding affinity to human TAF1 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 assessed as change in melting temperature at 25 uM by SYPRO orange based protein stability shift assay | 2016 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
| Targeting epigenetic reader and eraser: Rational design, synthesis and in vitro evaluation of dimethylisoxazoles derivatives as BRD4/HDAC dual inhibitors. |
| AID1371243 | Inhibition of FAM-labeled ZBA248 binding to recombinant human N-terminal His6-tagged BRD4 bromodomain 1 (44 to 168 residues) expressed in Rosetta2 DE3 cells after 30 mins by Flourescence polarization assay | 2017 | Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
| Structure-Based Discovery of 4-(6-Methoxy-2-methyl-4-(quinolin-4-yl)-9H-pyrimido[4,5-b]indol-7-yl)-3,5-dimethylisoxazole (CD161) as a Potent and Orally Bioavailable BET Bromodomain Inhibitor. |
| AID1821867 | Binding affinity to BRD4 D1 (unknown origin) assessed as dissociation constant by isothermal titration calorimetry | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| A Structure-based Design Approach for Generating High Affinity BRD4 D1-Selective Chemical Probes. |
| AID1890890 | Displacement of biotinylated acetylated histone H4 peptide from human recombinant N-terminal GST-tagged BRD4 BD1 (49 to 170 residues) expressed in Escherichia coli expression system incubated for 30 mins by AlphaScreen assay | 2022 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 64 | Development of BRD4 inhibitors as anti-inflammatory agents and antidotes for arsenicals. |
| AID1831195 | Toxicity in BALB/c mouse xenografted with human SW1990 cells assessed as kidney damage at 15 mg/kg, ip administered for 28 consecutive days in presence of 45 mg/kg Olaparib | | | |
| AID1821864 | Inhibition of BRD3 D2 (unknown origin) by competitive fluorescence anisotropy assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| A Structure-based Design Approach for Generating High Affinity BRD4 D1-Selective Chemical Probes. |
| AID1905954 | Binding affinity to His6-fused BRD3 BD1 (unknown origin) assessed as change in melting temperature at 100 uM incubated for 30 mins by thermal shift assay | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
| Structure-Based Discovery and Optimization of Furo[3,2- |
| AID1664727 | Induction of apoptosis in human MV4-11 cells assessed as live cell at 5 uM after 12 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 97.99 %) | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15
| Design, synthesis and biological evaluation of novel 6-phenyl-1,3a,4,10b-tetrahydro-2H-benzo[c]thiazolo[4,5-e]azepin-2-one derivatives as potential BRD4 inhibitors. |
| AID1845320 | Inhibition of BRD4 (unknown origin) by ELISA | 2021 | Bioorganic & medicinal chemistry letters, 01-01, Volume: 31 | Current status in the discovery of dual BET/HDAC inhibitors. |
| AID1664720 | Cell cycle arrest in human MV4-11 cells assessed as accumulation at G1 phase after 12 hrs by propidium iodide staining based flow cytometric analysis | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15
| Design, synthesis and biological evaluation of novel 6-phenyl-1,3a,4,10b-tetrahydro-2H-benzo[c]thiazolo[4,5-e]azepin-2-one derivatives as potential BRD4 inhibitors. |
| AID649988 | Binding affinity to BRD2-BD1 by isothermal titration calorimetry | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| Development of live-cell imaging probes for monitoring histone modifications. |
| AID1359751 | Binding affinity to His6-tagged human BRDT bromodomain-1 (N21 to E137 residues) expressed in Escherichia coli BL21(DE3) assessed as change in melting temperature at 200 uM by SYPRO orange dye based fluorescence assay | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer. |
| AID1409985 | Antiproliferative activity against human PC3 cells after 96 hrs by Cell-Titer glo reagent based luminescence assay | 2018 | ACS medicinal chemistry letters, Mar-08, Volume: 9, Issue:3
| Y08060: A Selective BET Inhibitor for Treatment of Prostate Cancer. |
| AID1594415 | Antifibrotic activity against human LX2 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
| Binding pocket-based design, synthesis and biological evaluation of novel selective BRD4-BD1 inhibitors. |
| AID1720098 | Growth inhibition of human THP-1 cells | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
| Dual-Target Inhibitors Based on HDACs: Novel Antitumor Agents for Cancer Therapy. |
| AID1831256 | Effect on cell cycle progression in human SW1990 cells assessed as reduction in Olaparib-induced CCND1 expression at 1 uM after 4 days in presence of Olaparib by Western blot analysis | | | |
| AID1905960 | Binding affinity to PCAF (unknown origin) assessed as change in melting temperature at 100 uM incubated for 30 mins by thermal shift assay | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
| Structure-Based Discovery and Optimization of Furo[3,2- |
| AID1831173 | Inhibition of BRD4 expression in human SW1990 cells at 4 uM after 4 days by Western blot analysis | | | |
| AID1905967 | Binding affinity to SMARCA2B (unknown origin) assessed as change in melting temperature at 100 uM incubated for 30 mins by thermal shift assay | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
| Structure-Based Discovery and Optimization of Furo[3,2- |
| AID1615994 | Antiproliferative activity against human A549 cells after 72 hrs by CCK8 or SRB assay | 2019 | Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18
| Structure-Based Discovery and Development of a Series of Potent and Selective Bromodomain and Extra-Terminal Protein Inhibitors. |
| AID1387718 | Inhibition of FAM-labeled ZBA248 binding to recombinant N-terminal His6-tagged BRD4 bromodomain 2 (333 to 460 residues) (unknown origin) expressed in Escherichia coli Rosetta2 DE3 after 30 mins by fluorescence polarization assay | 2018 | Journal of medicinal chemistry, 01-25, Volume: 61, Issue:2
| Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression. |
| AID1196557 | Inhibition of CYP2C9 in human liver microsomes at 10 uM using diclofenac substrate preincubated for 5 mins before NADPH addition and measured after 20 mins post NADPH addition | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
| Fragment-based drug discovery of 2-thiazolidinones as BRD4 inhibitors: 2. Structure-based optimization. |
| AID1462226 | Inhibition of BRD4/HDAC1 in human OCI-AML3 cells assessed as reduction in myc expression levels at 1 uM after 24 hrs by Western blot analysis | 2017 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
| Structure-based design, synthesis and in vitro antiproliferative effects studies of novel dual BRD4/HDAC inhibitors. |
| AID1359749 | Binding affinity to His6-tagged human BRD3 bromodomain-2 expressed in Escherichia coli BL21(DE3) assessed as change in melting temperature at 200 uM by SYPRO orange dye based fluorescence assay | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer. |
| AID1831527 | Antiproliferative activity against human MDA-MB-468 cells incubated for 24 hrs by MTT assay | 2021 | Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
| Discovery of Novel Dual-Target Inhibitor of Bromodomain-Containing Protein 4/Casein Kinase 2 Inducing Apoptosis and Autophagy-Associated Cell Death for Triple-Negative Breast Cancer Therapy. |
| AID1605851 | Inhibition of HSGRGK(Ac)GGK(Ac)GLGK(Ac)GGAK(Ac)RHRK(Biotin)-OH binding to recombinant human His6-tagged BRD4 bromodomain 1 expressed in Escherichia coli BL21 (DE3)-R3-pRARE2 cells preincubated for 30 mins followed by HSGRGK(Ac)GGK(Ac)GLGK(Ac)GGAK(Ac)RHRK( | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
| Discovery of 8-Methyl-pyrrolo[1,2- |
| AID1547259 | Inhibition of human recombinant His-tagged BRD3 BD2 domain expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells by AlphaScreen assay | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
| Discovery of Thieno[2,3- |
| AID1448425 | Inhibition of BRD4 bromodomain in human MM1S cells assessed as reduction in c-Myc levels after 6 hrs by Western blot analysis | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
| BET Bromodomain Inhibitors with One-Step Synthesis Discovered from Virtual Screen. |
| AID1905953 | Binding affinity to His6-fused BRD2 BD2 (unknown origin) assessed as change in melting temperature at 100 uM incubated for 30 mins by thermal shift assay | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
| Structure-Based Discovery and Optimization of Furo[3,2- |
| AID1724646 | Permeability of the compound in phosphate buffer containing 5% DMSO at pH 7.4 incubated for 7 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. |
| AID1600702 | Antiproliferative activity against human Capan1 cells | 2019 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 29, Issue:19
| Design, synthesis and biological evaluation of 3,5-dimethylisoxazole and pyridone derivatives as BRD4 inhibitors. |
| AID1905943 | Binding affinity to BRPF1 (unknown origin) assessed as change in melting temperature at 100 uM incubated for 30 mins by thermal shift assay | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
| Structure-Based Discovery and Optimization of Furo[3,2- |
| AID1821720 | Antiinflammatory activity in human SAEC assessed as inhibition of Poly(I:C) induced IL-6 expression by measuring residual activity rate at 10 uM pretreated for 24 hrs followed by Poly(I:C) addition for 4 hrs by qRT-PCR analysis | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site. |
| AID1878684 | Induction of DNA damage in human SW1990 cells assessed as increase in gammaH2AX expression at 4 uM incubated for 4 days by DAPI staining based laser confocal microscopic analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1606738 | Inhibition of BRD4 in poly(I:C)-stimulated human SAECs TLR3-inducible CIG5 gene expression pre-incubated for 24 hrs before poly(I:C) stimulation for 4 hrs by qRT-PCR analysis | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation. |
| AID1831146 | Inhibition of PARP1 (unknown origin) incubated for 45 mins in presence of biotinylated-NAD+ by microplate reader analysis | | | |
| AID1831188 | Toxicity in BALB/c mouse xenografted with human SW1990 cells assessed as liver damage at 15 mg/kg, ip administered for 28 consecutive days by H and E staining based fluorescence microscopic analysis | | | |
| AID1705285 | Inhibition of human His-tagged BRD4 BD1 domain using H4K5acK8acK12acK16ac as substrate preincubated for 30 mins followed by substrate addition measured after 30 mins by AlphaScreen assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Design, synthesis and biological evaluation of indole-2-one derivatives as potent BRD4 inhibitors. |
| AID1650237 | Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured after 48 hrs by CellTiter-Glo assay | 2020 | Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
| Discovery of novel small molecule induced selective degradation of the bromodomain and extra-terminal (BET) bromodomain protein BRD4 and BRD2 with cellular potencies. |
| AID1606747 | Binding affinity to recombinant BRDT BD2 (unknown origin) incubated for 1 hr by TR-FRET assay | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation. |
| AID1544779 | Induction of apoptosis in human MV4-11 cells assessed as necrotic cells level at 1 uM incubated for 24 hrs by Annexin V-FITC and propidium iodide staining based flow cytometry (Rvb = 0.0%) | 2019 | Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
| Design, synthesis and biological evaluation of novel 4,5-dihydro-[1,2,4]triazolo[4,3-f]pteridine derivatives as potential BRD4 inhibitors. |
| AID1705273 | Inhibition of BRD2 BD2 (unknown origin) preincubated for 15 mins followed by peptide addition and measured after 60 mins by TR-FRET assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Design, synthesis and biological evaluation of indole-2-one derivatives as potent BRD4 inhibitors. |
| AID705342 | Inhibition of human C-terminal BRD4 bromodomain expressed in Escherichia coli BL21(DE3) after 30 mins by luminescence proximity homogeneous assay | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2
| Fragment-based discovery of bromodomain inhibitors part 2: optimization of phenylisoxazole sulfonamides. |
| AID1831531 | Inhibition of BRD3 BD2 (unknown origin) incubated for 2 hrs by TR-FRET assay | 2021 | Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
| Discovery of Novel Dual-Target Inhibitor of Bromodomain-Containing Protein 4/Casein Kinase 2 Inducing Apoptosis and Autophagy-Associated Cell Death for Triple-Negative Breast Cancer Therapy. |
| AID1409984 | Antiproliferative activity against human 22Rv1 cells after 96 hrs by Cell-Titer glo reagent based luminescence assay | 2018 | ACS medicinal chemistry letters, Mar-08, Volume: 9, Issue:3
| Y08060: A Selective BET Inhibitor for Treatment of Prostate Cancer. |
| AID1547262 | Inhibition of human recombinant His-tagged BRD2 BD1 domain expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells by AlphaScreen assay | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
| Discovery of Thieno[2,3- |
| AID1831286 | Inhibition of homologous recombinant repair in human SW1990 cells assessed as reduction in Olaparib-induced BRCA1 expression at 1 uM after 4 days in presence of Olaparib by Q-PCR analysis | | | |
| AID1615987 | Antiproliferative activity against human HT-29 cells after 72 hrs by CCK8 or SRB assay | 2019 | Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18
| Structure-Based Discovery and Development of a Series of Potent and Selective Bromodomain and Extra-Terminal Protein Inhibitors. |
| AID1831174 | Inhibition of BRD4 in human SW1990 cells assessed as reversal of Olaparib-induced BRD4 accumulation in nucleus at 1 uM after 4 days by Western blot analysis | | | |
| AID1807750 | Binding affinity to recombinant human N-terminal hexaHis-tagged BRD4 expressed in Escherichia coli BL21 (DE3) cells by MST assay | 2021 | Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
| Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors. |
| AID1905942 | Binding affinity to His6-fused BRD9 (unknown origin) assessed as change in melting temperature at 100 uM incubated for 30 mins by thermal shift assay | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
| Structure-Based Discovery and Optimization of Furo[3,2- |
| AID1357983 | Inhibition of BRD4 in human SAE cells assessed as reduction in TLR3 agonist poly(I:C) -induced ISG54 RNA expression at 10 uM preincubated for 24 hrs followed by poly(I:C) addition and measured after 4 hrs by SYBR green dye-based qRT-PCR analysis relative | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation. |
| AID1544776 | Induction of apoptosis in human MV4-11 cells assessed as viable cells level at 1 uM incubated for 24 hrs by Annexin V-FITC and propidium iodide staining based flow cytometry (Rvb = 97.7%) | 2019 | Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
| Design, synthesis and biological evaluation of novel 4,5-dihydro-[1,2,4]triazolo[4,3-f]pteridine derivatives as potential BRD4 inhibitors. |
| AID1368364 | Binding affinity to BRD2 bromodomain 2 (348 to 455 residues) (unknown origin) by ITC | 2018 | Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1
| Exploiting a water network to achieve enthalpy-driven, bromodomain-selective BET inhibitors. |
| AID1606743 | Binding affinity to recombinant BRD2 BD2 (unknown origin) incubated for 1 hr by TR-FRET assay | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation. |
| AID1650530 | Antiproliferative activity against human HL60 cells assessed as reduction in cell viability at 2.5 uM incubated for 72 hrs by cell titer glo assay | 2020 | Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
| Discovery of a new class of PROTAC BRD4 degraders based on a dihydroquinazolinone derivative and lenalidomide/pomalidomide. |
| AID1559431 | Displacement of tetra-acetylated histone H4 peptide (1-21) from recombinant human N-terminal His-tagged BRD4 BD1 (44 to 170 residues) expressed in Escherichia coli incubated for 30 mins followed by further incubation with tetra-acetylated histone H4 pepti | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Discovery of Benzo[ |
| AID1196539 | Inhibition of BRD4(1) (unknown origin) incubated for 4 hrs by (+)-JQ1 fluorescent ligand based fluorescence anisotrophy | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
| Fragment-based drug discovery of 2-thiazolidinones as BRD4 inhibitors: 2. Structure-based optimization. |
| AID1358024 | Anti-inflammatory activity in poly(I:C)-induced airway inflammation C57BL/6 mouse model assessed as reduction in mCIG5 expression in lung at 10 mg/kg, ip administered 1 day prior to poly(I:C) stimulation and redosed on day 2 followed by poly(I:C) stimulat | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation. |
| AID1515642 | Inhibition of BRD4 (unknown origin) by TR-FRET assay | 2019 | MedChemComm, Jun-01, Volume: 10, Issue:6
| Controlling cellular distribution of drugs with permeability modifying moieties. |
| AID1606748 | Binding affinity to recombinant CBP (unknown origin) incubated for 1 hr by TR-FRET assay | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation. |
| AID1831214 | Induction of apoptosis in human SW1990 cells assessed as necrotic cells at 4 uM after 4 days by Annexin V-FITC and propidium iodide staining based flow cytometry (Rvb = 1.89%) | | | |
| AID1878762 | Effect on HEXIM1 gene expression in human SW1990 cells at 1 uM in presence of Olaparib by Q-PCR analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1831207 | Invivo inhibition of PARP1 expression in human SW1900 cells xenografted in BALB/c mouse assessed as reversal of Olaparib-induced PARP1 accumulation at 15 mg/kg, ip administered for 28 consecutive days in presence of 45 mg/kg Olaparib by immunohistochemica | | | |
| AID1821860 | Inhibition of BRD2 D1 (unknown origin) by competitive fluorescence anisotropy assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| A Structure-based Design Approach for Generating High Affinity BRD4 D1-Selective Chemical Probes. |
| AID1387716 | Inhibition of FAM-labeled ZBA248 binding to recombinant N-terminal His6-tagged BRD3 bromodomain 2 (306 to 417residues) (unknown origin) expressed in Escherichia coli Rosetta2 DE3 after 30 mins by fluorescence polarization assay | 2018 | Journal of medicinal chemistry, 01-25, Volume: 61, Issue:2
| Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression. |
| AID1359741 | Antiproliferative activity against human LNCAP cells | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer. |
| AID1878708 | Effect on HEXIM1 gene expression in human SW1990 cells at 4 uM by Q-PCR analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1831292 | Inhibition of homologous recombinant repair in human SW1990 cells assessed as reduction in BRCA1 expression at 4 uM after 4 days by Q-PCR analysis | | | |
| AID1454057 | Growth inhibition of human OVCAR5 cells after 3 days by WST1 assay | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
| Synthesis and evaluation of novel dual BRD4/HDAC inhibitors. |
| AID1878615 | Inhibition of BRD4 expression in nude mouse xenografted with human SW1900 cells assessed as reversal of olaparib-induced PARP1 expression at 15 mg/kg, ip administered for 28 days by DAPI staining based laser confocal microscopic analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1359776 | Antiproliferative activity against human A549 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer. |
| AID1230019 | Cytotoxicity against human MOLM13 cells harboring MLL1 fusion gene assessed as growth inhibition after 4 days by CellTiter-Glo luminescent assay | 2015 | Journal of medicinal chemistry, Jun-25, Volume: 58, Issue:12
| Structure-Based Design of γ-Carboline Analogues as Potent and Specific BET Bromodomain Inhibitors. |
| AID1821726 | Binding affinity BRD2 BD1 (unknown origin) incubated for 1 hr by TR-FRET assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site. |
| AID1821730 | Binding affinity BRDT BD1 (unknown origin) incubated for 1 hr by TR-FRET assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site. |
| AID1821743 | Binding affinity to wild type human BRD4 BD2 (349 to 461 residues) assessed as change in melting temperature at 1:0 compound to protein ratio by thermal shift assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site. |
| AID1821862 | Inhibition of BRDT D1 (unknown origin) by competitive fluorescence anisotropy assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| A Structure-based Design Approach for Generating High Affinity BRD4 D1-Selective Chemical Probes. |
| AID1513798 | Inhibition of human 6x-His-tagged BRD2 bromodomain 2 expressed in Escherichia coli | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
| Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor. |
| AID1544772 | Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by CCK-8 assay | 2019 | Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
| Design, synthesis and biological evaluation of novel 4,5-dihydro-[1,2,4]triazolo[4,3-f]pteridine derivatives as potential BRD4 inhibitors. |
| AID1878594 | Antiproliferative activity against human CFPAC-1 cells assessed as inhibition of cell growth measured after 5 days by MTT assay | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1664723 | Induction of apoptosis in human MV4-11 cells assessed as live cell at 0.5 uM after 12 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 97.99 %) | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15
| Design, synthesis and biological evaluation of novel 6-phenyl-1,3a,4,10b-tetrahydro-2H-benzo[c]thiazolo[4,5-e]azepin-2-one derivatives as potential BRD4 inhibitors. |
| AID1905957 | Binding affinity to CBP (unknown origin) assessed as change in melting temperature at 100 uM incubated for 30 mins by thermal shift assay | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
| Structure-Based Discovery and Optimization of Furo[3,2- |
| AID1807754 | Binding affinity to recombinant human N-terminal hexaHis-tagged BRDT expressed in Escherichia coli BL21 (DE3) cells by MST assay | 2021 | Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
| Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors. |
| AID1357989 | Inhibition of BRD4 in human SAE cells assessed as reduction in TLR3 agonist poly(I:C) -induced IL-8 RNA expression preincubated for 24 hrs followed by poly(I:C) addition and measured after 4 hrs by SYBR green dye-based qRT-PCR analysis | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation. |
| AID1821719 | Antiinflammatory activity in human SAEC assessed as inhibition of Poly(I:C) induced CIG5 expression by measuring residual activity rate at 10 uM pretreated for 24 hrs followed by Poly(I:C) addition for 4 hrs by qRT-PCR analysis | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site. |
| AID1831182 | Toxicity in BALB/c mouse xenografted with human SW1990 cells assessed as effect on body weight at 15 mg/kg, ip administered for 28 consecutive days | | | |
| AID1454051 | Inhibition of BRD4 in human HL60 cells assessed as reduction in C-myc production after 24 hrs by ELISA | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
| Synthesis and evaluation of novel dual BRD4/HDAC inhibitors. |
| AID1515643 | Inhibition of BRD4 in human MX1 cells assessed as decrease in cell proliferation after 3 days by Celltiter-Glo assay | 2019 | MedChemComm, Jun-01, Volume: 10, Issue:6
| Controlling cellular distribution of drugs with permeability modifying moieties. |
| AID1858164 | Binding affinity towards BRD4-BD1 (unknown origin) measured by isothermal titration calorimetry (ITC) method | 2022 | ACS medicinal chemistry letters, Oct-13, Volume: 13, Issue:10
| Development of an N-Terminal BRD4 Bromodomain-Targeted Degrader. |
| AID1821745 | Binding affinity to human BRD4 BD1 E151A mutant assessed as change in melting temperature at 15:2 compound to protein ratio by thermal shift assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site. |
| AID1878585 | Effect on c-Myc gene expression in human SW1990 cells at 4 uM by Q-PCR analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1499136 | Antiproliferative activity against human TY82 cells after 72 hrs by CCK8 assay | 2017 | European journal of medicinal chemistry, Sep-08, Volume: 137 | Discovery of a series of dihydroquinoxalin-2(1H)-ones as selective BET inhibitors from a dual PLK1-BRD4 inhibitor. |
| AID1454033 | Inhibition of HDAC in human HeLa nuclear extract at 10 uM using Fluor de Lys as substrate by fluorimetric method | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
| Synthesis and evaluation of novel dual BRD4/HDAC inhibitors. |
| AID1513826 | Inhibition of BRD4 bromodomain 1 in human A549 cells assessed as reduction in TNFalpha-induced IL8 levels at 1 uM after 24 hrs by ELISA relative to control | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
| Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor. |
| AID1594418 | Cytotoxicity against human LO2 cells assessed as reduction in cell growth measured after 24 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
| Binding pocket-based design, synthesis and biological evaluation of novel selective BRD4-BD1 inhibitors. |
| AID1821736 | Binding affinity to wild type human BRD4 BD1 (44 to 168 residues) assessed as change in melting temperature at 10:1 compound to protein ratio by thermal shift assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site. |
| AID1454030 | Inhibition of recombinant human N-terminal His-tagged BRD4 bromodomain 1 (49 to 170 residues) expressed in Escherichia coli using biotinylated peptide containing acetylated lysine as substrate pretreated for 15 mins followed by substrate addition after 1 | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
| Synthesis and evaluation of novel dual BRD4/HDAC inhibitors. |
| AID1515641 | Inhibition of BRD3 (unknown origin) by TR-FRET assay | 2019 | MedChemComm, Jun-01, Volume: 10, Issue:6
| Controlling cellular distribution of drugs with permeability modifying moieties. |
| AID1547267 | Inhibition of HDAC5 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
| Discovery of Thieno[2,3- |
| AID1281631 | Immunosuppressive activity in BALB/c mouse splenic T cells assessed as inhibition of PMA/CD28 induced cell proliferation after 24 hrs by [methyl-3H]thymidine incorporation assay | 2016 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 26, Issue:5
| A phenotypic drug discovery study on thienodiazepine derivatives as inhibitors of T cell proliferation induced by CD28 co-stimulation leads to the discovery of a first bromodomain inhibitor. |
| AID1718526 | Growth inhibition of human MCF7 cells after 72 hrs by CellTiter 96S AQeous non-radioactive cell proliferation assay | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24
| 4-Acyl Pyrroles as Dual BET-BRD7/9 Bromodomain Inhibitors Address BETi Insensitive Human Cancer Cell Lines. |
| AID1357995 | Inhibition of BRD3 BD1 (unknown origin) after 1 hr by TR-FRET assay | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation. |
| AID1831165 | Inhibition of P300 (unknown orign) using acetyl-CoA as substrate preincubated for 30 mins followed by substrate addition measured after 1 hr by microplate reader analysis | | | |
| AID1454050 | Induction of ATRA-induced human HL60 cell differentiation pretreated for 1 hr followed by ATRA addition measured after 3 days by Wright-Giemsa staining based microscopic analysis | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
| Synthesis and evaluation of novel dual BRD4/HDAC inhibitors. |
| AID1821738 | Binding affinity to wild type human BRD4 BD1 (44 to 168 residues) assessed as change in melting temperature at 4:5 compound to protein ratio by thermal shift assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site. |
| AID1821863 | Inhibition of BRD2 D2 (unknown origin) by competitive fluorescence anisotropy assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| A Structure-based Design Approach for Generating High Affinity BRD4 D1-Selective Chemical Probes. |
| AID1547270 | Inhibition of HDAC1 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
| Discovery of Thieno[2,3- |
| AID1615986 | Antiproliferative activity against human MDA-MB-468 cells after 72 hrs by CCK8 or SRB assay | 2019 | Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18
| Structure-Based Discovery and Development of a Series of Potent and Selective Bromodomain and Extra-Terminal Protein Inhibitors. |
| AID1878764 | Effect on BRCA2 gene expression in human SW1990 cells at 1 uM in presence of Olaparib by Q-PCR analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1762767 | Antiproliferative activity against human U-266 cells assessed as inhibition of cell proliferation at 0.1 uM incubated for 48 hrs by MTT assay relative to control | 2021 | Bioorganic & medicinal chemistry, 06-01, Volume: 39 | Discovery of 3,5-dimethylisoxazole derivatives as novel, potent inhibitors for bromodomain and extraterminal domain (BET) family. |
| AID1547258 | Inhibition of human recombinant His-tagged BRD4 BD1 domain using H-SGRGK(Ac)GGK(Ac)GLGK-(Ac)GGAK(Ac)RHRK(Biotin)-OH as substrate preincubated with enzyme for 30 mins followed by substrate addition measured after 30 mins by AlphaScreen assay | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
| Discovery of Thieno[2,3- |
| AID1359778 | Antiproliferative activity against HFL1 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer. |
| AID1905952 | Binding affinity to His6-fused BRD3 BD2 (unknown origin) assessed as change in melting temperature at 100 uM incubated for 30 mins by thermal shift assay | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
| Structure-Based Discovery and Optimization of Furo[3,2- |
| AID1878702 | Effect on CDC25A gene expression in human SW1990 cells at 4 uM by Q-PCR analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1544775 | Antiproliferative activity against human HL60 cells incubated for 72 hrs by CCK-8 assay | 2019 | Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
| Design, synthesis and biological evaluation of novel 4,5-dihydro-[1,2,4]triazolo[4,3-f]pteridine derivatives as potential BRD4 inhibitors. |
| AID1878761 | Effect on E2F2 gene expression in human SW1990 cells at 1 uM in presence of Olaparib by Q-PCR analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1831184 | Toxicity in BALB/c mouse xenografted with human SW1990 cells assessed as effect on body weight at 15 mg/kg, ip administered for 28 consecutive days in presence of 45 mg/kg Olaparib | | | |
| AID1807755 | Binding affinity to recombinant human N-terminal hexaHis-tagged BRDT expressed in Escherichia coli BL21 (DE3) cells by qPCR assay | 2021 | Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
| Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors. |
| AID1286364 | Binding affinity to human His6-tagged BAZ2B (S1858 to S1972 residues) expressed in Escherichia coli BL21(DE3) cells at 200 uM incubated for 30 mins by SYPRO orange staining based fluorescence thermal shift assay | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Discovery of Benzo[cd]indol-2(1H)-ones as Potent and Specific BET Bromodomain Inhibitors: Structure-Based Virtual Screening, Optimization, and Biological Evaluation. |
| AID1615990 | Antiproliferative activity against human SKOV3 cells after 72 hrs by CCK8 or SRB assay | 2019 | Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18
| Structure-Based Discovery and Development of a Series of Potent and Selective Bromodomain and Extra-Terminal Protein Inhibitors. |
| AID1600707 | Inhibition of human recombinant N-terminal 6his-tagged BRD4 expressed in Escherichia coli BL21(DE3) using H4 peptide as substrate by alphascreen assay | 2019 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 29, Issue:19
| Design, synthesis and biological evaluation of 3,5-dimethylisoxazole and pyridone derivatives as BRD4 inhibitors. |
| AID1409981 | Binding affinity to human His6-tagged BRD4 BD1 (N44 to E168 residues) expressed in Escherichia coli BL21 (DE3) cells by isothermal titration calorimetry method | 2018 | ACS medicinal chemistry letters, Mar-08, Volume: 9, Issue:3
| Y08060: A Selective BET Inhibitor for Treatment of Prostate Cancer. |
| AID1878607 | Toxicity in nude mouse xenografted with human SW1990 cells assessed as lung damage at 15 mg/kg, ip administered for 28 days in presence of 45 mg/kg Olaparib by H and E staining based fluorescence microscopic analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1318696 | Cytotoxicity against human HL60 cells assessed as decrease in cell viability after 24 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Development of 4,5-dihydro-benzodiazepinone derivatives as a new chemical series of BRD4 inhibitors. |
| 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. |
| AID1371237 | Growth inhibition of human MV4-11 cells after 4 days by WST-8 assay | 2017 | Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
| Structure-Based Discovery of 4-(6-Methoxy-2-methyl-4-(quinolin-4-yl)-9H-pyrimido[4,5-b]indol-7-yl)-3,5-dimethylisoxazole (CD161) as a Potent and Orally Bioavailable BET Bromodomain Inhibitor. |
| AID1725784 | Antiproliferation activity against human MIAPaCa2 cells assessed as reduction in cell viability at 2.5 uM incubated for 48 hrs by MTT assay relative to control | 2020 | ACS medicinal chemistry letters, Nov-12, Volume: 11, Issue:11
| Identification of 3,5-Dimethylisoxazole Derivatives as BRD4 Inhibitors for the Treatment of Colorectal Cancer. |
| AID1683140 | Binding affinity to polybromo-1 (2) (unknown origin) assessed as change in melting temperature at 20 uM by SYPRO orange dye based DSF assay | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
| Pan-SMARCA/PB1 Bromodomain Inhibitors and Their Role in Regulating Adipogenesis. |
| AID1831164 | Inhibition of recombinant BRD1 (unknown origin) incubated for 120 mins by TR-FRET assay | | | |
| AID1230000 | Displacement of FAM-labeled ZBA248 from BRD2 BD2 (349 to 460 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay | 2015 | Journal of medicinal chemistry, Jun-25, Volume: 58, Issue:12
| Structure-Based Design of γ-Carboline Analogues as Potent and Specific BET Bromodomain Inhibitors. |
| AID1359771 | Antiproliferative activity against human Hs578T cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer. |
| AID1831284 | Inhibition of homologous recombinant repair in human SW1990 cells assessed as reduction in Olaparib-induced FOXM1 expression at 1 uM after 4 days in presence of Olaparib by Q-PCR analysis | | | |
| AID1286359 | Binding affinity to human His6-tagged CREBBP (R1081 to G1197 residues) expressed in Escherichia coli BL21(DE3) cells at 200 uM incubated for 30 mins by SYPRO orange staining based fluorescence thermal shift assay | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Discovery of Benzo[cd]indol-2(1H)-ones as Potent and Specific BET Bromodomain Inhibitors: Structure-Based Virtual Screening, Optimization, and Biological Evaluation. |
| AID1615988 | Antiproliferative activity against human AGS cells after 72 hrs by CCK8 or SRB assay | 2019 | Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18
| Structure-Based Discovery and Development of a Series of Potent and Selective Bromodomain and Extra-Terminal Protein Inhibitors. |
| AID1664725 | Induction of apoptosis in human MV4-11 cells assessed as necrotic cell at 5 uM after 12 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 0.17 %) | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15
| Design, synthesis and biological evaluation of novel 6-phenyl-1,3a,4,10b-tetrahydro-2H-benzo[c]thiazolo[4,5-e]azepin-2-one derivatives as potential BRD4 inhibitors. |
| AID1878760 | Effect on CCND1 gene expression in human SW1990 cells at 1 uM in presence of Olaparib by Q-PCR analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1652286 | Down regulation of c-MYC gene expression in fulvestrant-resistant human MCF7:CFR cells at 100 nM measured after 24 hrs | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
| Novel Pyrrolopyridone Bromodomain and Extra-Terminal Motif (BET) Inhibitors Effective in Endocrine-Resistant ER+ Breast Cancer with Acquired Resistance to Fulvestrant and Palbociclib. |
| AID1905965 | Binding affinity to His6-fused BRDT BD2 (unknown origin) assessed as change in melting temperature at 100 uM incubated for 30 mins by thermal shift assay | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
| Structure-Based Discovery and Optimization of Furo[3,2- |
| AID1615985 | Antiproliferative activity against human NCI-H522 cells after 72 hrs by CCK8 or SRB assay | 2019 | Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18
| Structure-Based Discovery and Development of a Series of Potent and Selective Bromodomain and Extra-Terminal Protein Inhibitors. |
| AID1664730 | Cell cycle arrest in human MV4-11 cells assessed as accumulation at G0/G1 phase at 0.5 uM after 12 hrs by propidium iodide staining based flow cytometric analysis (Rvb = 43.91%) | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15
| Design, synthesis and biological evaluation of novel 6-phenyl-1,3a,4,10b-tetrahydro-2H-benzo[c]thiazolo[4,5-e]azepin-2-one derivatives as potential BRD4 inhibitors. |
| AID1831168 | Inhibition of colony formation in human SW1990 cells at 0.5 uM after 14 days in presence of 1.5 uM Olaparib by crystal violet staining based microscopic analysis | | | |
| AID1650235 | Binding affinity to recombinant human N-terminal His-tagged BRD4 BD1 (44 to 170 residues) expressed in Escherichia coli using H4K5AcK8Ac as substrate measured after 30 mins by AlphaScreen assay | 2020 | Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
| Discovery of novel small molecule induced selective degradation of the bromodomain and extra-terminal (BET) bromodomain protein BRD4 and BRD2 with cellular potencies. |
| AID1878624 | Reversal of Olaparib-induced BRD4 expression in nucleus of human SW1990 cells at 1 uM measured after 4 days by Western blot analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1878707 | Effect on E2F2 gene expression in human SW1990 cells at 4 uM by Q-PCR analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1456300 | Inhibition of BRD4-BD1 (44 to 168 residues) (unknown origin) using histone H4 peptide as substrate preincubated for 15 mins followed by addition of substrate measured after 60 mins by AlphaScreen assay | 2017 | Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8
| Design, synthesis and biological evaluation of 7-methylimidazo[1,5-a]pyrazin-8(7H)-one derivatives as BRD4 inhibitors. |
| AID1513794 | Inhibition of human 6x-His-tagged BRD3 bromodomain 1 expressed in Escherichia coli | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
| Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor. |
| AID1905966 | Binding affinity to SMARCA2A (unknown origin) assessed as change in melting temperature at 100 uM incubated for 30 mins by thermal shift assay | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
| Structure-Based Discovery and Optimization of Furo[3,2- |
| AID1905946 | Inhibition of C-terminal His6-tagged BRD4 BD1 (unknown origin) using H-YSGRGK(Ac)GGK(Ac)GLGK(Ac)-GGAK(Ac)RHRK-Biotin-OH as substrate incubated for 1 hrs by HTRF assay | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
| Structure-Based Discovery and Optimization of Furo[3,2- |
| AID1831536 | Inhibition of BRDT BD2 (unknown origin) incubated for 2 hrs by TR-FRET assay | 2021 | Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
| Discovery of Novel Dual-Target Inhibitor of Bromodomain-Containing Protein 4/Casein Kinase 2 Inducing Apoptosis and Autophagy-Associated Cell Death for Triple-Negative Breast Cancer Therapy. |
| AID1831219 | Induction of apoptosis in human SW1990 cells assessed as late apoptotic cells at 1 uM after 4 days in presence of 3 uM Olaparib by Annexin V-FITC and propidium iodide staining based flow cytometry (Rvb = 6.22%) | | | |
| AID1821728 | Binding affinity BRD3 BD1 (unknown origin) incubated for 1 hr by TR-FRET assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site. |
| AID772239 | Inhibition of His-FLAG-tagged BRD4 binding domain1 (unknown origin) binding to H4-TetraAc-biotin peptide after 20 mins by AlphaLISA | 2013 | ACS medicinal chemistry letters, Sep-12, Volume: 4, Issue:9
| Discovery, Design, and Optimization of Isoxazole Azepine BET Inhibitors. |
| AID1821851 | Inhibition of BRD4 D1 (unknown origin) by alphascreen assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| A Structure-based Design Approach for Generating High Affinity BRD4 D1-Selective Chemical Probes. |
| AID1878717 | Effect on Rad52 gene expression in human SW1990 cells at 4 uM by Q-PCR analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1705258 | Inhibition of BRD4 BD1 (unknown origin) preincubated for 15 mins followed by peptide addition and measured after 60 mins by TR-FRET assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Design, synthesis and biological evaluation of indole-2-one derivatives as potent BRD4 inhibitors. |
| AID1286350 | Binding affinity to human His6-tagged BRD3 bromodomain 1 (P24 to E144 residues) expressed in Escherichia coli BL21(DE3) cells at 200 uM incubated for 30 mins by SYPRO orange staining based fluorescence thermal shift assay | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Discovery of Benzo[cd]indol-2(1H)-ones as Potent and Specific BET Bromodomain Inhibitors: Structure-Based Virtual Screening, Optimization, and Biological Evaluation. |
| AID1357994 | Inhibition of BRD2 BD2 (unknown origin) after 1 hr by TR-FRET assay | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation. |
| AID1878775 | Downregulation of Ki67 expression in human SW1990 cells at 15 mg/kg, ip in presence of 45 mg/kg, ip Olaparib measured after 28 days by immuno histochemical staining based fluorescence microscopic analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1392194 | Inhibition of BRD4-BD1 in human Raji cells assessed as downregulation of MYC gene expression by PCR method | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10
| Design, synthesis and biological evaluation of novel 4-phenylisoquinolinone BET bromodomain inhibitors. |
| AID1230004 | Binding affinity to biotinylated BRD2 BD2 (349 to 460 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometry method | 2015 | Journal of medicinal chemistry, Jun-25, Volume: 58, Issue:12
| Structure-Based Design of γ-Carboline Analogues as Potent and Specific BET Bromodomain Inhibitors. |
| AID1456304 | Antiproliferative activity against BRD4-sensitive human MV411 cells after 72 hrs by CCK8 assay | 2017 | Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8
| Design, synthesis and biological evaluation of 7-methylimidazo[1,5-a]pyrazin-8(7H)-one derivatives as BRD4 inhibitors. |
| AID1878604 | Toxicity in nude mouse xenografted with human SW1990 cells assessed as kidney damage at 15 mg/kg, ip administered for 28 days by H and E staining based fluorescence microscopic analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1905958 | Inhibition of EP300 (unknown origin) assessed as change in melting temperature at 100 uM incubated for 30 mins by thermal shift assay | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
| Structure-Based Discovery and Optimization of Furo[3,2- |
| AID1454052 | Growth inhibition of human K562 cells after 3 days by counting method | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
| Synthesis and evaluation of novel dual BRD4/HDAC inhibitors. |
| AID1878614 | Inhibition of PARP1 expression in nude mouse xenografted with human SW1900 cells assessed as reversal of olaparib-induced PARP1 expression at 15 mg/kg, ip administered for 28 days by DAPI staining based laser confocal microscopic analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID731808 | Binding affinity to human BRD4 bromodomain 1 using H4Ac4 peptide by amplified luminescent proximity homogeneous assay | 2013 | Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
| Optimization of 3,5-dimethylisoxazole derivatives as potent bromodomain ligands. |
| AID1308518 | Binding affinity to human CREBBP expressed in Escherichia coli BL21(DE3)-R3-pRARE2 assessed as change in melting temperature at 25 uM by SYPRO orange based protein stability shift assay | 2016 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
| Targeting epigenetic reader and eraser: Rational design, synthesis and in vitro evaluation of dimethylisoxazoles derivatives as BRD4/HDAC dual inhibitors. |
| AID1515640 | Inhibition of BRD2 (unknown origin) by TR-FRET assay | 2019 | MedChemComm, Jun-01, Volume: 10, Issue:6
| Controlling cellular distribution of drugs with permeability modifying moieties. |
| AID1520158 | Antiproliferative activity against human HL60 cells assessed as reduction in cell viability by MTT assay | 2019 | ACS medicinal chemistry letters, Dec-12, Volume: 10, Issue:12
| Pharmacokinetics-Driven Optimization of 7-Methylimidazo[1,5- |
| AID1387968 | Proteolysis targeting chimera activity in human HeLa cells assessed as induction of VCB-mediated delivery of BRD4 long isoform for protein degradation by proteasome at 30 to 10000 nM incubated for 24 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. |
| AID1831210 | Invivo inhibition of BRD4 expression in human SW1900 cells xenografted in BALB/c mouse assessed as reversal of Olaparib-induced BRD4 accumulation at 15 mg/kg, ip administered for 28 consecutive days in presence of 45 mg/kg Olaparib by Q-PCR analysis | | | |
| AID1308513 | Inhibition of recombinant HDAC1 (unknown origin) using of Fluor-de-Lys substrate incubated for 10 mins by fluorimetric assay | 2016 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
| Targeting epigenetic reader and eraser: Rational design, synthesis and in vitro evaluation of dimethylisoxazoles derivatives as BRD4/HDAC dual inhibitors. |
| AID1547273 | Inhibition of HDAC2 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
| Discovery of Thieno[2,3- |
| AID1878681 | Induction of DNA damage in human SW1990 cells assessed as increase in tail DNA at 1 uM incubated for 4 days in presence of 3 uM Olaparib by comet assay | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1821855 | Cytotoxicity against human A549 cells assessed as viable cells incubated for 23 hrs by alamar blue assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| A Structure-based Design Approach for Generating High Affinity BRD4 D1-Selective Chemical Probes. |
| AID1878606 | Toxicity in nude mouse xenografted with human SW1990 cells assessed as spleen damage at 15 mg/kg, ip administered for 28 days in presence of 45 mg/kg Olaparib by H and E staining based fluorescence microscopic analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1606739 | Inhibition of BRD4 in poly(I:C)-stimulated human SAECs TLR3-inducible IL-6 gene expression pre-incubated for 24 hrs before poly(I:C) stimulation for 4 hrs by qRT-PCR analysis | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation. |
| AID1375117 | Displacement of (+)-JQ1 from 6H-Thr BRD4 Y390A mutant BD1 (unknown origin) after 30 mins by TR-FRET assay | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
| Discovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain. |
| AID1878769 | Effect on ALDH1A1 gene expression in human SW1990 cells at 1 uM in presence of Olaparib by Q-PCR analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1878754 | Effect on c-Myc gene expression in human SW1990 cells at 1 uM in presence of Olaparib by Q-PCR analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. |
| AID1664733 | Cell cycle arrest in human MV4-11 cells assessed as accumulation at G0/G1 phase at 5 uM after 12 hrs by propidium iodide staining based flow cytometric analysis (Rvb = 43.91%) | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15
| Design, synthesis and biological evaluation of novel 6-phenyl-1,3a,4,10b-tetrahydro-2H-benzo[c]thiazolo[4,5-e]azepin-2-one derivatives as potential BRD4 inhibitors. |
| AID1230005 | Binding affinity to biotinylated BRD3 BD1 (24 to 144 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometry method | 2015 | Journal of medicinal chemistry, Jun-25, Volume: 58, Issue:12
| Structure-Based Design of γ-Carboline Analogues as Potent and Specific BET Bromodomain Inhibitors. |
| AID1318697 | Cytotoxicity against human MV4-11 cells assessed as decrease in cell viability after 24 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Development of 4,5-dihydro-benzodiazepinone derivatives as a new chemical series of BRD4 inhibitors. |
| AID1909994 | Displacement of fluorescein-labeled JQ1 from His6/TEV cleavage site fused human BRD4 (residues N44 to E168) expressed in Escherichia coli BL21 (DE3) incubated for 60 min by Fluorescence polarization assay | 2022 | Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
| Design and Synthesis of Dual EZH2/BRD4 Inhibitors to Target Solid Tumors. |
| AID1615984 | Antiproliferative activity against human NCI-H1299 cells after 72 hrs by CCK8 or SRB assay | 2019 | Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18
| Structure-Based Discovery and Development of a Series of Potent and Selective Bromodomain and Extra-Terminal Protein Inhibitors. |
| AID1821740 | Binding affinity to wild type human BRD4 BD2 (349 to 461 residues) assessed as change in melting temperature at 3:4 compound to protein ratio by thermal shift assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site. |
| AID1831152 | Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 7 days | | | |
| AID1359753 | Binding affinity to His6-tagged human CREBBP (R1081 to G1197 residues) expressed in Escherichia coli BL21(DE3) assessed as change in melting temperature at 200 uM by SYPRO orange dye based fluorescence assay | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer. |
| AID1520156 | Inhibition of BRD4 bromodomain2 (unknown origin) using peptide H4 as substrate incubated for 15 mins followed by substrate addition and measured after 1 hr by alphascreen assay | 2019 | ACS medicinal chemistry letters, Dec-12, Volume: 10, Issue:12
| Pharmacokinetics-Driven Optimization of 7-Methylimidazo[1,5- |
| AID1513811 | Binding affinity to BRD4 C-terminal bromodomain 2 H437D mutant (unknown origin) expressed in Escherichia coli Bl21(DE3) by fluorescence polarization assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
| Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor. |
| AID1821866 | Binding affinity to BRD2 D1 (unknown origin) assessed as dissociation constant by isothermal titration calorimetry | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| A Structure-based Design Approach for Generating High Affinity BRD4 D1-Selective Chemical Probes. |
| AID649990 | Binding affinity to BRD3-BD1 by isothermal titration calorimetry | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| Development of live-cell imaging probes for monitoring histone modifications. |
| AID1831156 | Inhibition of recombinant BRD3 BD2 (unknown origin) incubated for 120 mins by TR-FRET assay | | | |
| AID1831197 | Toxicity in BALB/c mouse xenografted with human SW1990 cells assessed as spleen damage at 15 mg/kg, ip administered for 28 consecutive days in presence of 45 mg/kg Olaparib | | | |
| AID1821725 | Binding affinity human BRD4 BD2 incubated for 1 hr by TR-FRET assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site. |
| AID1802797 | Thermal Shift Assay (TSA) from Article 10.1074/jbc.M113.523019: \\Affinity map of bromodomain protein 4 (BRD4) interactions with the histone H4 tail and the small molecule inhibitor JQ1.\\ | 2014 | The Journal of biological chemistry, Mar-28, Volume: 289, Issue:13
| Affinity map of bromodomain protein 4 (BRD4) interactions with the histone H4 tail and the small molecule inhibitor JQ1. |
| AID1802799 | Fluorescence Polarization Assay from Article 10.1074/jbc.M113.523019: \\Affinity map of bromodomain protein 4 (BRD4) interactions with the histone H4 tail and the small molecule inhibitor JQ1.\\ | 2014 | The Journal of biological chemistry, Mar-28, Volume: 289, Issue:13
| Affinity map of bromodomain protein 4 (BRD4) interactions with the histone H4 tail and the small molecule inhibitor JQ1. |
| AID1802798 | TR-FRET Competition Assay from Article 10.1074/jbc.M113.523019: \\Affinity map of bromodomain protein 4 (BRD4) interactions with the histone H4 tail and the small molecule inhibitor JQ1.\\ | 2014 | The Journal of biological chemistry, Mar-28, Volume: 289, Issue:13
| Affinity map of bromodomain protein 4 (BRD4) interactions with the histone H4 tail and the small molecule inhibitor JQ1. |
| AID1802213 | ITC experiments (Isothermal titration calorimetry) from Article 10.1038/nchembio.2209: \\Design and characterization of bivalent BET inhibitors.\\ | 2016 | Nature chemical biology, Dec, Volume: 12, Issue:12
| Design and characterization of bivalent BET inhibitors. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
| Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347123 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347129 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347116 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1508591 | NCATS Rat Liver Microsome Stability Profiling | 2020 | Scientific reports, 11-26, Volume: 10, Issue:1
| Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models. |
| AID1347128 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347122 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347117 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347126 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID686947 | qHTS for small molecule inhibitors of Yes1 kinase: Primary Screen | 2013 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15
| Identification of potent Yes1 kinase inhibitors using a library screening approach. |
| AID1347119 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4
| A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | | | |
| AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347124 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347118 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347113 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347125 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347115 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347109 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1508612 | NCATS Parallel Artificial Membrane Permeability Assay (PAMPA) Profiling | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
| Highly predictive and interpretable models for PAMPA permeability. |
| AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347110 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347114 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347112 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347127 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347111 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347121 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1346051 | Mouse bromodomain testis associated (Non-enzymatic BRD containing proteins) | 2012 | Cell, Aug-17, Volume: 150, Issue:4
| Small-molecule inhibition of BRDT for male contraception. |
| AID1345665 | Human bromodomain containing 4 (Bromodomain kinase (BRDK) family) | 2010 | Nature, Dec-23, Volume: 468, Issue:7327
| Selective inhibition of BET bromodomains. |
| AID1347017 | Human bromodomain testis associated (Non-enzymatic BRD containing proteins) | 2012 | Cell, Aug-17, Volume: 150, Issue:4
| Small-molecule inhibition of BRDT for male contraception. |
| AID977611 | Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB | 2014 | ACS chemical biology, Dec-19, Volume: 9, Issue:12
| Fluorinated aromatic amino acids are sensitive 19F NMR probes for bromodomain-ligand interactions. |
| AID1347414 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Secondary screen by immunofluorescence | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1645848 | NCATS Kinetic Aqueous Solubility Profiling | 2019 | Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
| Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity. |
| AID1347412 | qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1745855 | NCATS anti-infectives library activity on the primary C. elegans qHTS viability assay | 2023 | Disease models & mechanisms, 03-01, Volume: 16, Issue:3
| In vivo quantitative high-throughput screening for drug discovery and comparative toxicology. |
| AID1745854 | NCATS anti-infectives library activity on HEK293 viability as a counter-qHTS vs the C. elegans viability qHTS | 2023 | Disease models & mechanisms, 03-01, Volume: 16, Issue:3
| In vivo quantitative high-throughput screening for drug discovery and comparative toxicology. |
| AID977611 | Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB | 2010 | Nature, Dec-23, Volume: 468, Issue:7327
| Selective inhibition of BET bromodomains. |
| AID977611 | Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB | 2012 | Cell, Aug-17, Volume: 150, Issue:4
| Small-molecule inhibition of BRDT for male contraception. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |