| Assay ID | Title | Year | Journal | Article |
|---|
| AID1909166 | Inhibition of homologous recombinant repair in human MDA-MB-468 cells assessed as reversal of olaparib-induced upregulation of Rad51 expression at 1 uM in by Western blot analysis | 2022 | Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
| Discovery of 4-Hydroxyquinazoline Derivatives as Small Molecular BET/PARP1 Inhibitors That Induce Defective Homologous Recombination and Lead to Synthetic Lethality for Triple-Negative Breast Cancer Therapy. |
| AID1909160 | Induction of apoptosis in human MDA-MB-468 cells assessed as downregulation of Bcl-2 protein level incubated for 72 hrs in presence of olaparib by Western blot analysis | 2022 | Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
| Discovery of 4-Hydroxyquinazoline Derivatives as Small Molecular BET/PARP1 Inhibitors That Induce Defective Homologous Recombination and Lead to Synthetic Lethality for Triple-Negative Breast Cancer Therapy. |
| AID1478010 | Inhibition of recombinant human N-terminal GST-tagged BRDT bromodomain-1 (22 to 138 residues) expressed in Escherichia coli expression system after 120 mins by TR-FRET assay | 2017 | Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24
| Discovery of a Small-Molecule Bromodomain-Containing Protein 4 (BRD4) Inhibitor That Induces AMP-Activated Protein Kinase-Modulated Autophagy-Associated Cell Death in Breast Cancer. |
| AID1909176 | Induction of DNA damage in human MDA-MB-468 cells assessed as up-regulation of gammaH2AX expression level at 1 uM incubated for 60 mins by DAPI staining based immunofluorescence assay | 2022 | Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
| Discovery of 4-Hydroxyquinazoline Derivatives as Small Molecular BET/PARP1 Inhibitors That Induce Defective Homologous Recombination and Lead to Synthetic Lethality for Triple-Negative Breast Cancer Therapy. |
| AID1909182 | Induction of DNA damage in human MDA-MB-231 cells assessed as increase in tail DNA at 1 uM measured after 3 days in presence of olaparib by comet assay | 2022 | Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
| Discovery of 4-Hydroxyquinazoline Derivatives as Small Molecular BET/PARP1 Inhibitors That Induce Defective Homologous Recombination and Lead to Synthetic Lethality for Triple-Negative Breast Cancer Therapy. |
| AID1478044 | Induction of autophagy in human MDA-MB-231 cells assessed as downregulation of p62/SQSTM1 expression at 10 uM by Western blot analysis | 2017 | Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24
| Discovery of a Small-Molecule Bromodomain-Containing Protein 4 (BRD4) Inhibitor That Induces AMP-Activated Protein Kinase-Modulated Autophagy-Associated Cell Death in Breast Cancer. |
| AID1909178 | Induction of DNA damage in human MDA-MB-468 cells assessed as up-regulation of gammaH2AX expression level at 1 uM in presence of olaparib by DAPI staining based immunofluorescence assay | 2022 | Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
| Discovery of 4-Hydroxyquinazoline Derivatives as Small Molecular BET/PARP1 Inhibitors That Induce Defective Homologous Recombination and Lead to Synthetic Lethality for Triple-Negative Breast Cancer Therapy. |
| AID1349406 | Antiproliferative activity against human MLL-AF9 cells after 72 hrs by Cell-TiterGlo assay | 2017 | ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12
| Design, Synthesis, and Biological Activity of 1,2,3-Triazolobenzodiazepine BET Bromodomain Inhibitors. |
| AID1909229 | Synergistic antiproliferative activity against human MDA-MB-468 cells at compound to Olaparib ratio of 1:3 | 2022 | Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
| Discovery of 4-Hydroxyquinazoline Derivatives as Small Molecular BET/PARP1 Inhibitors That Induce Defective Homologous Recombination and Lead to Synthetic Lethality for Triple-Negative Breast Cancer Therapy. |
| AID1909142 | Cell cycle arrest in human MDA-MB-468 cells assessed as accumulation at G0/G1 phase incubated for 72 hrs in presence of olaparib by propidium iodide staining-based flow cytometry analysis (Rvb = 61.4%) | 2022 | Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
| Discovery of 4-Hydroxyquinazoline Derivatives as Small Molecular BET/PARP1 Inhibitors That Induce Defective Homologous Recombination and Lead to Synthetic Lethality for Triple-Negative Breast Cancer Therapy. |
| AID1477945 | Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay | 2017 | Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24
| Discovery of a Small-Molecule Bromodomain-Containing Protein 4 (BRD4) Inhibitor That Induces AMP-Activated Protein Kinase-Modulated Autophagy-Associated Cell Death in Breast Cancer. |
| AID1852005 | Inhibition of c-MYC G4 quadruplex DNA in HEK293T cells co-transfected with Renilla and firefly luciferase assessed as decrease in relative luciferase at 2.5 to 5 uM measured after 24 hrs by dual luciferase reporter assay | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
| Design, Synthesis, and Evaluation of New Sugar-Substituted Imidazole Derivatives as Selective |
| AID1349400 | Inhibition of human His-tagged Brd4 bromodomain 1 expressed in Escherichia coli BL21 (DE3) preincubated for 30 mins followed by addition of biotinylated acetyl-histone H4 peptide and measured after 1 hr by AlphaScreen assay | 2017 | ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12
| Design, Synthesis, and Biological Activity of 1,2,3-Triazolobenzodiazepine BET Bromodomain Inhibitors. |
| AID1478007 | Inhibition of recombinant human N-terminal GST-tagged BRD3 bromodomain-2 (306 to 417 residues) expressed in Escherichia coli expression system after 120 mins by TR-FRET assay | 2017 | Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24
| Discovery of a Small-Molecule Bromodomain-Containing Protein 4 (BRD4) Inhibitor That Induces AMP-Activated Protein Kinase-Modulated Autophagy-Associated Cell Death in Breast Cancer. |
| AID1909227 | Inhibition of BRD4 BD2 (unknown origin) | 2022 | Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
| Discovery of 4-Hydroxyquinazoline Derivatives as Small Molecular BET/PARP1 Inhibitors That Induce Defective Homologous Recombination and Lead to Synthetic Lethality for Triple-Negative Breast Cancer Therapy. |
| AID1349410 | Antiproliferative activity against human RPMI8226 cells after 72 hrs by Cell-TiterGlo assay | 2017 | ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12
| Design, Synthesis, and Biological Activity of 1,2,3-Triazolobenzodiazepine BET Bromodomain Inhibitors. |
| AID1598103 | Activation of Tat-mediated HIV1 transcription in J-Lat 10.6 cells harboring LTR driven GFP reporter co-expressing CMV driven RFP reporter assessed as LTR-driven gene expression incubated for 48 hr by FACSCalibur flow cytometry | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
| Identification of 5-Substituted 2-Acylaminothiazoles That Activate Tat-Mediated Transcription in HIV-1 Latency Models. |
| AID1477968 | Inhibition of recombinant human N-terminal GST-tagged BRD2 bromodomain-1 (65 to 187 residues) expressed in Escherichia coli expression system after 120 mins by TR-FRET assay | 2017 | Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24
| Discovery of a Small-Molecule Bromodomain-Containing Protein 4 (BRD4) Inhibitor That Induces AMP-Activated Protein Kinase-Modulated Autophagy-Associated Cell Death in Breast Cancer. |
| AID1909150 | Cell cycle arrest in human MDA-MB-468 cells assessed as accumulation at S phase incubated for 72 hrs in presence of olaparib by propidium iodide staining-based flow cytometry analysis (Rvb=16.1%) | 2022 | Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
| Discovery of 4-Hydroxyquinazoline Derivatives as Small Molecular BET/PARP1 Inhibitors That Induce Defective Homologous Recombination and Lead to Synthetic Lethality for Triple-Negative Breast Cancer Therapy. |
| AID1337144 | Inhibition of N-terminal 6His-tagged human BRD4 bromodomain 1 (44 to 168 residues) expressed in Escherichia coli BL21 (DE3) using biotinylated histone H4 peptide (1 to 21 residues) containing KAc (K5/8/12/16Ac) as substrate by Alpha screen assay | 2017 | Nature reviews. Drug discovery, Jun, Volume: 16, Issue:6
| Non-kinase targets of protein kinase inhibitors. |
| AID1477943 | Inhibition of His/thioredoxin-tagged human recombinant BRD4 bromodomain-1 (43 to 166 residues) expressed in Escherichia coli BL21 Star (DE3) pre-incubated for 30 mins followed by biotinylated histone peptide H4 addition measured after 30 mins by AlphaScre | 2017 | Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24
| Discovery of a Small-Molecule Bromodomain-Containing Protein 4 (BRD4) Inhibitor That Induces AMP-Activated Protein Kinase-Modulated Autophagy-Associated Cell Death in Breast Cancer. |
| AID1852007 | Inhibition of c-MYC G4 quadruplex DNA mutant in HEK293T cells co-transfected with Renilla and firefly luciferase assessed as decrease in relative luciferase at 2.5 to 5 uM measured after 24 hrs by dual luciferase reporter assay | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
| Design, Synthesis, and Evaluation of New Sugar-Substituted Imidazole Derivatives as Selective |
| AID1909164 | Induction of apoptosis in human MDA-MB-468 cells assessed as up-regulation of cleaved caspase 3 protein level incubated for 72 hrs in presence of olaparib by Western blot analysis | 2022 | Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
| Discovery of 4-Hydroxyquinazoline Derivatives as Small Molecular BET/PARP1 Inhibitors That Induce Defective Homologous Recombination and Lead to Synthetic Lethality for Triple-Negative Breast Cancer Therapy. |
| AID1478055 | Effect on VDAC2 expression in human MCF7 cells at 10 uM measured up to 24 hrs by Western blot analysis | 2017 | Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24
| Discovery of a Small-Molecule Bromodomain-Containing Protein 4 (BRD4) Inhibitor That Induces AMP-Activated Protein Kinase-Modulated Autophagy-Associated Cell Death in Breast Cancer. |
| AID1909226 | Inhibition of BRD4 BD1 (unknown origin) | 2022 | Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
| Discovery of 4-Hydroxyquinazoline Derivatives as Small Molecular BET/PARP1 Inhibitors That Induce Defective Homologous Recombination and Lead to Synthetic Lethality for Triple-Negative Breast Cancer Therapy. |
| AID1478049 | Downregulation of HMGB1 expression in human MCF7 cells at 10 uM measured up to 24 hrs by Western blot analysis | 2017 | Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24
| Discovery of a Small-Molecule Bromodomain-Containing Protein 4 (BRD4) Inhibitor That Induces AMP-Activated Protein Kinase-Modulated Autophagy-Associated Cell Death in Breast Cancer. |
| AID1598096 | Activation of Tat-mediated HIV1 transcription in HEK293- FlpIn-FM cells harboring LTR driven CBR reporter co-expressing CMV driven CBG reporter assessed as maximum LTR activity at 5 uM incubated for 48 hr using Chroma-Glo substrate by luciferase dual repo | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
| Identification of 5-Substituted 2-Acylaminothiazoles That Activate Tat-Mediated Transcription in HIV-1 Latency Models. |
| AID1349413 | Antiproliferative activity against human Raji cells after 72 hrs by Cell-TiterGlo assay | 2017 | ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12
| Design, Synthesis, and Biological Activity of 1,2,3-Triazolobenzodiazepine BET Bromodomain Inhibitors. |
| AID1478004 | Upregulation of VDAC2 expression in human MDA-MB-231 cells at 3 uM measured up to 36 hrs by Western blot analysis | 2017 | Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24
| Discovery of a Small-Molecule Bromodomain-Containing Protein 4 (BRD4) Inhibitor That Induces AMP-Activated Protein Kinase-Modulated Autophagy-Associated Cell Death in Breast Cancer. |
| AID1478003 | Downregulation of EF2 phosphorylation in human MDA-MB-231 cells at 3 uM measured up to 36 hrs by Western blot analysis | 2017 | Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24
| Discovery of a Small-Molecule Bromodomain-Containing Protein 4 (BRD4) Inhibitor That Induces AMP-Activated Protein Kinase-Modulated Autophagy-Associated Cell Death in Breast Cancer. |
| AID1909180 | Induction of DNA damage in human MDA-MB-231 cells assessed as increase in tail DNA measured at 1 uM after 3 days by comet assay | 2022 | Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
| Discovery of 4-Hydroxyquinazoline Derivatives as Small Molecular BET/PARP1 Inhibitors That Induce Defective Homologous Recombination and Lead to Synthetic Lethality for Triple-Negative Breast Cancer Therapy. |
| AID1478002 | Downregulation of EF2 phosphorylation in human MCF7 cells at 1.5 uM measured up to 36 hrs by Western blot analysis | 2017 | Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24
| Discovery of a Small-Molecule Bromodomain-Containing Protein 4 (BRD4) Inhibitor That Induces AMP-Activated Protein Kinase-Modulated Autophagy-Associated Cell Death in Breast Cancer. |
| AID1478052 | Effect on EF2 phosphorylation in human MDA-MB-231 cells at 10 uM measured up to 24 hrs by Western blot analysis | 2017 | Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24
| Discovery of a Small-Molecule Bromodomain-Containing Protein 4 (BRD4) Inhibitor That Induces AMP-Activated Protein Kinase-Modulated Autophagy-Associated Cell Death in Breast Cancer. |
| AID1478009 | Inhibition of recombinant human BRD4 bromodomain-1 (342 to 460 residues) expressed in Escherichia coli expression system after 120 mins by TR-FRET assay | 2017 | Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24
| Discovery of a Small-Molecule Bromodomain-Containing Protein 4 (BRD4) Inhibitor That Induces AMP-Activated Protein Kinase-Modulated Autophagy-Associated Cell Death in Breast Cancer. |
| AID1478000 | Downregulation of HMGB1 expression in human MCF7 cells at 1.5 uM measured up to 36 hrs by Western blot analysis | 2017 | Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24
| Discovery of a Small-Molecule Bromodomain-Containing Protein 4 (BRD4) Inhibitor That Induces AMP-Activated Protein Kinase-Modulated Autophagy-Associated Cell Death in Breast Cancer. |
| AID1909146 | Cell cycle arrest in human MDA-MB-468 cells assessed as accumulation at S phase incubated for 72 hrs in presence of olaparib by propidium iodide staining-based flow cytometry analysis (Rvb = 21.1%) | 2022 | Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
| Discovery of 4-Hydroxyquinazoline Derivatives as Small Molecular BET/PARP1 Inhibitors That Induce Defective Homologous Recombination and Lead to Synthetic Lethality for Triple-Negative Breast Cancer Therapy. |
| AID1852006 | Inhibition of c-MYC G4 quadruplex DNA in HEK293T cells co-transfected with Renilla and firefly luciferase assessed as decrease in relative luciferase measured after 24 hrs by dual luciferase reporter assay | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
| Design, Synthesis, and Evaluation of New Sugar-Substituted Imidazole Derivatives as Selective |
| AID1477998 | Induction of autophagy in GFP/mRFP treated human MDA-MB-231 cells assessed as induction of LC3 puncta at 10 uM by fluorescence microscopic analysis | 2017 | Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24
| Discovery of a Small-Molecule Bromodomain-Containing Protein 4 (BRD4) Inhibitor That Induces AMP-Activated Protein Kinase-Modulated Autophagy-Associated Cell Death in Breast Cancer. |
| AID1349414 | Antiproliferative activity against human HEL 92.1.7 cells after 72 hrs by Cell-TiterGlo assay | 2017 | ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12
| Design, Synthesis, and Biological Activity of 1,2,3-Triazolobenzodiazepine BET Bromodomain Inhibitors. |
| AID1349421 | Inhibition of BRD4 in human MV4-11 cells assessed as downregulation of BCL2 RNA expression by RNA-seq analysis | 2017 | ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12
| Design, Synthesis, and Biological Activity of 1,2,3-Triazolobenzodiazepine BET Bromodomain Inhibitors. |
| AID1349416 | Antiproliferative activity against mouse 494H cells after 72 hrs by Cell-TiterGlo assay | 2017 | ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12
| Design, Synthesis, and Biological Activity of 1,2,3-Triazolobenzodiazepine BET Bromodomain Inhibitors. |
| AID1852009 | Downregulation of c-MYC mRNA level in human MDA-MB-231 cells measured after 24 hrs by RT-PCR analysis | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
| Design, Synthesis, and Evaluation of New Sugar-Substituted Imidazole Derivatives as Selective |
| AID1349422 | Inhibition of binding of a tetra-acetylated histone H4 peptide to His-tagged human BRD4(D1) expressed in bacteria | 2017 | ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12
| Design, Synthesis, and Biological Activity of 1,2,3-Triazolobenzodiazepine BET Bromodomain Inhibitors. |
| AID1909158 | Induction of apoptosis in human MDA-MB-468 cells assessed as late apoptotic cells at 1 uM incubated for 72 hrs in presence of olaparib by annexin V/propidium iodide staining-based flow cytometry analysis (Rvb = 1.34%) | 2022 | Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
| Discovery of 4-Hydroxyquinazoline Derivatives as Small Molecular BET/PARP1 Inhibitors That Induce Defective Homologous Recombination and Lead to Synthetic Lethality for Triple-Negative Breast Cancer Therapy. |
| AID1478053 | Effect on VDAC1 expression in human MCF7 cells at 10 uM measured up to 24 hrs by Western blot analysis | 2017 | Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24
| Discovery of a Small-Molecule Bromodomain-Containing Protein 4 (BRD4) Inhibitor That Induces AMP-Activated Protein Kinase-Modulated Autophagy-Associated Cell Death in Breast Cancer. |
| AID1598093 | Cytotoxicity against human HepG2 cells assessed as reduction in cell growth incubated for 48 hrs by CellTiter-Glo assay | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
| Identification of 5-Substituted 2-Acylaminothiazoles That Activate Tat-Mediated Transcription in HIV-1 Latency Models. |
| AID1598094 | Cytotoxicity against HEK293 cells assessed as reduction in cell growth incubated for 48 hrs by MTS assay | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
| Identification of 5-Substituted 2-Acylaminothiazoles That Activate Tat-Mediated Transcription in HIV-1 Latency Models. |
| AID1909162 | Induction of apoptosis in human MDA-MB-468 cells assessed as up-regulation of Bax protein level at incubated for 72 hrs in presence of olaparib by Western blot analysis | 2022 | Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
| Discovery of 4-Hydroxyquinazoline Derivatives as Small Molecular BET/PARP1 Inhibitors That Induce Defective Homologous Recombination and Lead to Synthetic Lethality for Triple-Negative Breast Cancer Therapy. |
| AID1337145 | Inhibition of N-terminal 6His-tagged human BRDT bromodomain 1 (21 to 137 residues) expressed in Escherichia coli BL21 (DE3) using biotinylated histone H4 peptide (1 to 21 residues) containing KAc (K5/8/12/16Ac) as substrate by Alpha screen assay | 2017 | Nature reviews. Drug discovery, Jun, Volume: 16, Issue:6
| Non-kinase targets of protein kinase inhibitors. |
| AID1477944 | Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay | 2017 | Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24
| Discovery of a Small-Molecule Bromodomain-Containing Protein 4 (BRD4) Inhibitor That Induces AMP-Activated Protein Kinase-Modulated Autophagy-Associated Cell Death in Breast Cancer. |
| AID1349397 | Inhibition of human His-tagged Brd2 bromodomain 1 expressed in Escherichia coli BL21 (DE3) preincubated for 30 mins followed by addition of biotinylated acetyl-histone H4 peptide and measured after 1 hr by AlphaScreen assay | 2017 | ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12
| Design, Synthesis, and Biological Activity of 1,2,3-Triazolobenzodiazepine BET Bromodomain Inhibitors. |
| AID1478050 | Downregulation of HMGB1 expression in human MDA-MB-231 cells at 10 uM measured up to 24 hrs by Western blot analysis | 2017 | Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24
| Discovery of a Small-Molecule Bromodomain-Containing Protein 4 (BRD4) Inhibitor That Induces AMP-Activated Protein Kinase-Modulated Autophagy-Associated Cell Death in Breast Cancer. |
| AID1451722 | Inhibition of hedgehog signaling pathway in mouse NIH/3T3 cells harboring sufu shRNA assessed as downregulation of Gli1 mRNA expression at 1 uM by RT-qPCR analysis | 2017 | Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
| Discovery of Novel Macrocyclic Hedgehog Pathway Inhibitors Acting by Suppressing the Gli-Mediated Transcription. |
| AID1349411 | Antiproliferative activity against human SU-DHL4 cells after 72 hrs by Cell-TiterGlo assay | 2017 | ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12
| Design, Synthesis, and Biological Activity of 1,2,3-Triazolobenzodiazepine BET Bromodomain Inhibitors. |
| AID1477952 | Inhibition of BRD4 bromodomain-1 interaction with AMPK in human MCF7 cells assessed as induction of autophagy activity by measuring MDC positive cells at 5 uM after 6 hrs by MDC-fluorescence based flow cytometric analysis relative to control | 2017 | Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24
| Discovery of a Small-Molecule Bromodomain-Containing Protein 4 (BRD4) Inhibitor That Induces AMP-Activated Protein Kinase-Modulated Autophagy-Associated Cell Death in Breast Cancer. |
| AID1451723 | Inhibition of hedgehog signaling pathway in mouse NIH/3T3 cells harboring sufu shRNA assessed as downregulation of ptch1 mRNA expression at 1 uM by RT-qPCR analysis | 2017 | Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
| Discovery of Novel Macrocyclic Hedgehog Pathway Inhibitors Acting by Suppressing the Gli-Mediated Transcription. |
| AID1478005 | Inhibition of recombinant human N-terminal GST-tagged BRD2 bromodomain-2 (339 to 459 residues) expressed in Escherichia coli expression system after 120 mins by TR-FRET assay | 2017 | Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24
| Discovery of a Small-Molecule Bromodomain-Containing Protein 4 (BRD4) Inhibitor That Induces AMP-Activated Protein Kinase-Modulated Autophagy-Associated Cell Death in Breast Cancer. |
| AID1478051 | Effect on EF2 phosphorylation in human MCF7 cells at 10 uM measured up to 24 hrs by Western blot analysis | 2017 | Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24
| Discovery of a Small-Molecule Bromodomain-Containing Protein 4 (BRD4) Inhibitor That Induces AMP-Activated Protein Kinase-Modulated Autophagy-Associated Cell Death in Breast Cancer. |
| AID1852011 | Downregulation of VEGF expression in human MDA-MB-231 cells measured after 48 hrs by western blot analysis | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
| Design, Synthesis, and Evaluation of New Sugar-Substituted Imidazole Derivatives as Selective |
| AID1349420 | Inhibition of BRD4 in human MV4-11 cells assessed as downregulation of cMYC RNA expression by RNA-seq analysis | 2017 | ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12
| Design, Synthesis, and Biological Activity of 1,2,3-Triazolobenzodiazepine BET Bromodomain Inhibitors. |
| AID1478006 | Inhibition of recombinant human N-terminal GST-tagged BRD3 bromodomain-1 (29 to 145 residues) expressed in Escherichia coli expression system after 120 mins by TR-FRET assay | 2017 | Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24
| Discovery of a Small-Molecule Bromodomain-Containing Protein 4 (BRD4) Inhibitor That Induces AMP-Activated Protein Kinase-Modulated Autophagy-Associated Cell Death in Breast Cancer. |
| AID1349401 | Inhibition of human His-tagged Brd4 bromodomain 2 expressed in Escherichia coli BL21 (DE3) preincubated for 30 mins followed by addition of biotinylated acetyl-histone H4 peptide and measured after 1 hr by AlphaScreen assay | 2017 | ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12
| Design, Synthesis, and Biological Activity of 1,2,3-Triazolobenzodiazepine BET Bromodomain Inhibitors. |
| AID1852010 | Downregulation of c-MYC expression in human MDA-MB-231 cells measured after 48 hrs by western blot analysis | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
| Design, Synthesis, and Evaluation of New Sugar-Substituted Imidazole Derivatives as Selective |
| AID1478001 | Upregulation of VDAC1 expression in human MCF7 cells at 1.5 uM measured up to 36 hrs by Western blot analysis | 2017 | Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24
| Discovery of a Small-Molecule Bromodomain-Containing Protein 4 (BRD4) Inhibitor That Induces AMP-Activated Protein Kinase-Modulated Autophagy-Associated Cell Death in Breast Cancer. |
| AID1349408 | Antiproliferative activity against human MV4-11 cells after 72 hrs by Cell-TiterGlo assay | 2017 | ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12
| Design, Synthesis, and Biological Activity of 1,2,3-Triazolobenzodiazepine BET Bromodomain Inhibitors. |
| AID1349415 | Antiproliferative activity against human K562 cells after 72 hrs by Cell-TiterGlo assay | 2017 | ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12
| Design, Synthesis, and Biological Activity of 1,2,3-Triazolobenzodiazepine BET Bromodomain Inhibitors. |
| AID1909225 | Inhibition of BRD4 (unknown origin) | 2022 | Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
| Discovery of 4-Hydroxyquinazoline Derivatives as Small Molecular BET/PARP1 Inhibitors That Induce Defective Homologous Recombination and Lead to Synthetic Lethality for Triple-Negative Breast Cancer Therapy. |
| AID1598104 | Activation of non-specific gene expression in human J-Lat 10.6 cells harboring LTR driven GFP reporter co-expressing CMV driven RFP reporter assessed as CMV driven gene expression incubated for 48 hr by FACSCalibur flow cytometry | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
| Identification of 5-Substituted 2-Acylaminothiazoles That Activate Tat-Mediated Transcription in HIV-1 Latency Models. |
| AID1349409 | Antiproliferative activity against human DOHH2 cells after 72 hrs by Cell-TiterGlo assay | 2017 | ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12
| Design, Synthesis, and Biological Activity of 1,2,3-Triazolobenzodiazepine BET Bromodomain Inhibitors. |
| AID1478054 | Effect on VDAC1 expression in human MDA-MB-231 cells at 10 uM measured up to 24 hrs by Western blot analysis | 2017 | Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24
| Discovery of a Small-Molecule Bromodomain-Containing Protein 4 (BRD4) Inhibitor That Induces AMP-Activated Protein Kinase-Modulated Autophagy-Associated Cell Death in Breast Cancer. |
| AID1598140 | Activation of Tat-mediated HIV1 transcription in CD4 positive cells derived from HIV-infected patient on suppressive anti-retroviral therapy assessed as increase in unspliced HIV transcripts at 1 uM incubated for 72 hrs by RT-qPCR method | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
| Identification of 5-Substituted 2-Acylaminothiazoles That Activate Tat-Mediated Transcription in HIV-1 Latency Models. |
| AID1477996 | Induction of autophagy in GFP/mRFP treated human MCF7 cells assessed as induction of LC3 puncta at 10 uM by fluorescence microscopic analysis | 2017 | Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24
| Discovery of a Small-Molecule Bromodomain-Containing Protein 4 (BRD4) Inhibitor That Induces AMP-Activated Protein Kinase-Modulated Autophagy-Associated Cell Death in Breast Cancer. |
| AID1909154 | Induction of apoptosis in human MDA-MB-468 cells assessed as early apoptotic cells at 1 uM incubated for 72 hrs in presence of olaparib by annexin V/propidium iodide staining-based flow cytometry analysis (Rvb = 4.07%) | 2022 | Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
| Discovery of 4-Hydroxyquinazoline Derivatives as Small Molecular BET/PARP1 Inhibitors That Induce Defective Homologous Recombination and Lead to Synthetic Lethality for Triple-Negative Breast Cancer Therapy. |
| AID1349407 | Antiproliferative activity against human HL60 cells after 72 hrs by Cell-TiterGlo assay | 2017 | ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12
| Design, Synthesis, and Biological Activity of 1,2,3-Triazolobenzodiazepine BET Bromodomain Inhibitors. |
| AID1478008 | Inhibition of recombinant human BRD4 bromodomain-1 (49 to 170 residues) expressed in Escherichia coli expression system after 120 mins by TR-FRET assay | 2017 | Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24
| Discovery of a Small-Molecule Bromodomain-Containing Protein 4 (BRD4) Inhibitor That Induces AMP-Activated Protein Kinase-Modulated Autophagy-Associated Cell Death in Breast Cancer. |
| AID1349417 | Antiproliferative activity against mouse 148I cells after 72 hrs by Cell-TiterGlo assay | 2017 | ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12
| Design, Synthesis, and Biological Activity of 1,2,3-Triazolobenzodiazepine BET Bromodomain Inhibitors. |
| AID1478043 | Induction of autophagy in human MCF7 cells assessed as downregulation of p62/SQSTM1 expression at 10 uM by Western blot analysis | 2017 | Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24
| Discovery of a Small-Molecule Bromodomain-Containing Protein 4 (BRD4) Inhibitor That Induces AMP-Activated Protein Kinase-Modulated Autophagy-Associated Cell Death in Breast Cancer. |
| AID1349412 | Antiproliferative activity against human CCRF-CEM cells after 72 hrs by Cell-TiterGlo assay | 2017 | ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12
| Design, Synthesis, and Biological Activity of 1,2,3-Triazolobenzodiazepine BET Bromodomain Inhibitors. |
| AID1478056 | Effect on VDAC2 expression in human MDA-MB-231 cells at 10 uM measured up to 24 hrs by Western blot analysis | 2017 | Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24
| Discovery of a Small-Molecule Bromodomain-Containing Protein 4 (BRD4) Inhibitor That Induces AMP-Activated Protein Kinase-Modulated Autophagy-Associated Cell Death in Breast Cancer. |
| AID1349399 | Inhibition of human His-tagged Brd3 bromodomain 1 expressed in Escherichia coli BL21 (DE3) preincubated for 30 mins followed by addition of biotinylated acetyl-histone H4 peptide and measured after 1 hr by AlphaScreen assay | 2017 | ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12
| Design, Synthesis, and Biological Activity of 1,2,3-Triazolobenzodiazepine BET Bromodomain Inhibitors. |
| AID1598136 | Activation of Tat-mediated HIV1 transcription in J-Lat 10.6 cells harboring LTR driven GFP reporter co-expressing CMV driven RFP reporter assessed as maximum LTR activity at 2.5 uM incubated for 48 hr by FACSCalibur flow cytometry relative to control | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
| Identification of 5-Substituted 2-Acylaminothiazoles That Activate Tat-Mediated Transcription in HIV-1 Latency Models. |
| AID1909167 | Inhibition of homologous recombinant repair in human MDA-MB-468 cells assessed as reversal of olaparib-induced upregulation of Mre11 expression at 1 uM in by Western blot analysis | 2022 | Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
| Discovery of 4-Hydroxyquinazoline Derivatives as Small Molecular BET/PARP1 Inhibitors That Induce Defective Homologous Recombination and Lead to Synthetic Lethality for Triple-Negative Breast Cancer Therapy. |
| AID1349398 | Inhibition of human His-tagged Brd2 bromodomain 2 expressed in Escherichia coli BL21 (DE3) preincubated for 30 mins followed by addition of biotinylated acetyl-histone H4 peptide and measured after 1 hr by AlphaScreen assay | 2017 | ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12
| Design, Synthesis, and Biological Activity of 1,2,3-Triazolobenzodiazepine BET Bromodomain 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. |
| AID1347160 | Primary screen NINDS Rhodamine 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. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 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. |
| 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. |
| 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. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |