Assay ID | Title | Year | Journal | Article |
AID1178317 | Binding affinity to induced myeloid leukemia cell differentiation protein 1 (unknown origin) | 2014 | Bioorganic & medicinal chemistry, Aug-15, Volume: 22, Issue:16
| Biased and unbiased strategies to identify biologically active small molecules. |
AID1320544 | Inhibition of 5-FAM-Bid peptide binding to Bcl-2 (unknown origin) by fluorescence polarization assay | 2016 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
| Design, synthesis, and activity evaluation of selective inhibitors of anti-apoptotic Bcl-2 proteins: The effects on the selectivity of the P1 pockets in the active sites. |
AID1816664 | Cytotoxicity against MCL-1deficient MEF cells assessed as release of cytochrome c from mitochondria at 2.5 uM FACS analysis | | | |
AID701530 | Induction of apoptosis in human RS4:11 cells at 10 uM incubated for 24 hrs by Annexin V and propidium iodide staining based FACS method | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis and biological activities of polyquinoline derivatives: new Bcl-2 family protein modulators. |
AID1690752 | Antiproliferative activity against human MOLT-4 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay | | | |
AID721471 | Binding affinity to Bcl-2 (unknown origin) fluorescence polarization assay | 2013 | Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1
| 3-Thiomorpholin-8-oxo-8H-acenaphtho [1,2-b] pyrrole-9-carbonitrile (S1) derivatives as pan-Bcl-2-inhibitors of Bcl-2, Bcl-xL and Mcl-1. |
AID1690776 | Induction of apoptosis in human MOLT-4 cells assessed as viable cells at 100 nM measured after 48 hrs by Alexa Fluor 647-Annexin V/propidium iodide staining based flow cytometry (Rvb = 97.1 to 97.3%) | | | |
AID330751 | Induction of apoptosis in mouse Eu-Myc cells overexpressing BCL2 assessed as inhibition of colony formation at 1 uM | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-04, Volume: 104, Issue:49
| Small molecule obatoclax (GX15-070) antagonizes MCL-1 and overcomes MCL-1-mediated resistance to apoptosis. |
AID277492 | Inhibition of cell growth in human RS11380 cells overexpressing Bcl2 in presence of 10% HS | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
| Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL. |
AID654462 | Binding affinity to Bcl-xL | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Structure-activity relationship of selected polyphenol derivatives as inhibitors of Bax/Bcl-xL interaction. |
AID1296620 | Cell cycle arrest in human HCT116 p53-/- cells assessed as accumulation at G1 phase at 10 uM after 24 hrs by propidium iodide staining-based flow cytometric method (Rvb = 28%) | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics. |
AID1816652 | Inhibition of GST tagged human/mouse chimeric MCL-1 using biotin-DLRPEIRIAQELRIZIGDEFNETYTRR as substrate incubated for 40 mins followed by substrate addition measured after 4 hrs by AlphaSCREEN assay | | | |
AID628484 | Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 V141A mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay | 2011 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 21, Issue:17
| Biochemical and pharmacological profiling of the pro-survival protein Bcl-xL. |
AID1580122 | Inhibition of Bcl-xL (unknown origin) by surface plasmon resonance assay | 2020 | Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3
| Hot-Spots of Mcl-1 Protein. |
AID421428 | Cytotoxicity against human BP3 cells expressing Bfl1/Mcl1 by FITC-annexin V and propidium iodide assay | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Apogossypol derivatives as pan-active inhibitors of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins. |
AID389262 | Cytotoxicity against IL3-dependent mouse FL5.12 cells overexpressing human Bcl2 assessed as cell viability after 24 hrs by MTS assay in absence of serum | 2008 | Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
| Discovery of an orally bioavailable small molecule inhibitor of prosurvival B-cell lymphoma 2 proteins. |
AID1352851 | Cytotoxicity against human K562 cells assessed as reduction in cell viability at 1 to 2 uM by CellTiter-Glo luminescent assay relative to control | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Small-molecule Mcl-1 inhibitors: Emerging anti-tumor agents. |
AID628398 | Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 F97V mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay | 2011 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 21, Issue:17
| Biochemical and pharmacological profiling of the pro-survival protein Bcl-xL. |
AID277485 | Displacement of Bad-derived peptide from Bcl-xL by fluorescence polarization assay | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
| Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL. |
AID462447 | Inhibition of Bcl-xL | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Fragment-based deconstruction of Bcl-xL inhibitors. |
AID640028 | Binding affinity to Bcl-2 by competitive fluorescence polarization assay | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
| Design, synthesis, and activity evaluation of broad-spectrum small-molecule inhibitors of anti-apoptotic Bcl-2 family proteins: characteristics of broad-spectrum protein binding and its effects on anti-tumor activity. |
AID1483465 | Binding affinity to Mcl-1 (unknown origin) | 2017 | Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3
| Expanding the Cancer Arsenal with Targeted Therapies: Disarmament of the Antiapoptotic Bcl-2 Proteins by Small Molecules. |
AID587011 | Displacement of wild type mBimBH3 from human Bcl-w by solution competition assay | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
| Quinazoline sulfonamides as dual binders of the proteins B-cell lymphoma 2 and B-cell lymphoma extra long with potent proapoptotic cell-based activity. |
AID640029 | Binding affinity to Mcl-1 by competitive fluorescence polarization assay | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
| Design, synthesis, and activity evaluation of broad-spectrum small-molecule inhibitors of anti-apoptotic Bcl-2 family proteins: characteristics of broad-spectrum protein binding and its effects on anti-tumor activity. |
AID1178315 | Binding affinity to Bcl-w (unknown origin) | 2014 | Bioorganic & medicinal chemistry, Aug-15, Volume: 22, Issue:16
| Biased and unbiased strategies to identify biologically active small molecules. |
AID701519 | Inhibition of GST-tagged recombinant Bcl-XL interaction with biotinylated Bim peptide by ELISA based competitive binding assay | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis and biological activities of polyquinoline derivatives: new Bcl-2 family protein modulators. |
AID587087 | Cytotoxicity against mouse mcl-1 deficient MEF cells after 24 hrs by Cell titer glo assay in presence of 10% fetal bovine serum | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
| Quinazoline sulfonamides as dual binders of the proteins B-cell lymphoma 2 and B-cell lymphoma extra long with potent proapoptotic cell-based activity. |
AID654460 | Inhibition of Rluc-Bax/eYFP-Bcl-xL interaction expressed in human HeLa cells at 10 uM after 16 hrs by BRET assay | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Structure-activity relationship of selected polyphenol derivatives as inhibitors of Bax/Bcl-xL interaction. |
AID1635029 | Inhibition of His-tagged Mcl-1/5-carboxyfluorescein-Bid (unknown origin) after 1 hr by fluorescence polarization assay | 2016 | Journal of natural products, Apr-22, Volume: 79, Issue:4
| Anacardic Acids from Knema hookeriana as Modulators of Bcl-xL/Bak and Mcl-1/Bid Interactions. |
AID1851858 | Selectivity ratio, Ki for inhibition of MCL-1 (unknown origin) to Ki for inhibition of BCL-2 (unknown origin) | 2022 | RSC medicinal chemistry, Aug-17, Volume: 13, Issue:8
| Scaffold hopping from indoles to indazoles yields dual MCL-1/BCL-2 inhibitors from MCL-1 selective leads. |
AID1545357 | Inhibition of BCL-W (unknown origin) in presence of 10% human serum incubated for 15 mins by fluorescence polarization assay | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Clinical candidates modulating protein-protein interactions: The fragment-based experience. |
AID1224377 | Displacement of fluorescein-labeled BAK from His-tagged BCL-XL (unknown origin) after 1 hr by fluorescence polarization assay | 2014 | Journal of natural products, Jun-27, Volume: 77, Issue:6
| Endiandric acid analogues from Beilschmiedia ferruginea as dual inhibitors of Bcl-xL/Bak and Mcl-1/Bid interactions. |
AID281476 | Induction of cell death in human MDA-MB-231 cells after 96 hrs by trypan blue exclusion assay | 2007 | Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8
| Pyrogallol-based molecules as potent inhibitors of the antiapoptotic Bcl-2 proteins. |
AID687164 | Ratio of IC50 for doxorubicin-resistant human K562 cells to IC50 for human K562 cells | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
| Structure-activity relationship (SAR) study of ethyl 2-amino-6-(3,5-dimethoxyphenyl)-4-(2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate (CXL017) and the potential of the lead against multidrug resistance in cancer treatment. |
AID701528 | Binding affinity to Bcl-XL | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis and biological activities of polyquinoline derivatives: new Bcl-2 family protein modulators. |
AID727588 | Induction of apoptosis in human Toledo cells | 2013 | ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
| The role of the acidity of N-heteroaryl sulfonamides as inhibitors of bcl-2 family protein-protein interactions. |
AID1893751 | Selectivity ratio of IC50 for inhibition of biotin-linker-Bax BH3 peptide binding to human C-terminal 6His-tagged Bcl-2 (1 to 218 residues) expressed in Escherichia coli BL21 Star (DE3) pLysS to IC50 for inhibition of biotin-linker-Beclin 1 BH3 peptide bi | 2022 | ACS medicinal chemistry letters, Sep-08, Volume: 13, Issue:9
| Novel Bcl-2 Inhibitors Selectively Disrupt the Autophagy-Specific Bcl-2-Beclin 1 Protein-Protein Interaction. |
AID1851857 | Inhibition of BCL-xL (unknown origin) by fluorescence polarization competition assay | 2022 | RSC medicinal chemistry, Aug-17, Volume: 13, Issue:8
| Scaffold hopping from indoles to indazoles yields dual MCL-1/BCL-2 inhibitors from MCL-1 selective leads. |
AID330776 | Binding affinity to BCL2 | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-04, Volume: 104, Issue:49
| Small molecule obatoclax (GX15-070) antagonizes MCL-1 and overcomes MCL-1-mediated resistance to apoptosis. |
AID687160 | Ratio of IC50 for human HL60/MX2 cells to IC50 for human HL60 cells | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
| Structure-activity relationship (SAR) study of ethyl 2-amino-6-(3,5-dimethoxyphenyl)-4-(2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate (CXL017) and the potential of the lead against multidrug resistance in cancer treatment. |
AID330756 | Cytotoxicity in human siRNA-mediated-MCL1-kncok down KB cells overexpressing BCL2 at 0.5 uM | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-04, Volume: 104, Issue:49
| Small molecule obatoclax (GX15-070) antagonizes MCL-1 and overcomes MCL-1-mediated resistance to apoptosis. |
AID628399 | Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 R100E mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay | 2011 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 21, Issue:17
| Biochemical and pharmacological profiling of the pro-survival protein Bcl-xL. |
AID675723 | Growth inhibition of human NCI-H146 cells after 4 days by WST8 assay | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
| Design of Bcl-2 and Bcl-xL inhibitors with subnanomolar binding affinities based upon a new scaffold. |
AID330758 | Cytotoxicity in human KB cells overexpressing BCL2 at 0.1 uM | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-04, Volume: 104, Issue:49
| Small molecule obatoclax (GX15-070) antagonizes MCL-1 and overcomes MCL-1-mediated resistance to apoptosis. |
AID389265 | Cmax in Sprague-Dawley rat at 5 mg/kg, po | 2008 | Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
| Discovery of an orally bioavailable small molecule inhibitor of prosurvival B-cell lymphoma 2 proteins. |
AID1296624 | Cell cycle arrest in human HCT116 p53+/+ cells assessed as accumulation at G1 phase at 5 uM after 24 hrs by propidium iodide staining-based flow cytometric method (Rvb = 31%) | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics. |
AID1881901 | Inhibition of PKM2 (unknown origin) Leu180, Asp177, Lys207, Hie78, Thr328, GIn329, Gly363, Lys367 residues | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
| A Perspective on Medicinal Chemistry Approaches for Targeting Pyruvate Kinase M2. |
AID694161 | Antagonist activity at recombinant Bcl-XL assessed as restoration of BIM BH3-induced cytochrome c release in mitochondria isolated from MDA-MB-231 cells at 0.03 to 1 uM after 1 hr by Western blot analysis | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Structure-based design of potent Bcl-2/Bcl-xL inhibitors with strong in vivo antitumor activity. |
AID652718 | Induction of Bcl-xL-mediated apoptosis in doxycyclin-stimulated human HeLa cells expressing GFP at 1 uM after 12 hrs by Hoechst staining | 2012 | Bioorganic & medicinal chemistry, Apr-01, Volume: 20, Issue:7
| Perturbing pro-survival proteins using quinoxaline derivatives: a structure-activity relationship study. |
AID1690759 | Antiproliferative activity against human NCI-H146 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay | | | |
AID1690761 | Selectivity index, ratio of IC50 for human platelet to IC50 for human MOLT-4 cells | | | |
AID431392 | Cytotoxicity against human SU-8686 cells after 48 hrs by cell titer-blue assay | 2009 | Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
| Structure-activity relationship and molecular mechanisms of ethyl 2-amino-4-(2-ethoxy-2-oxoethyl)-6-phenyl-4h-chromene-3-carboxylate (sha 14-1) and its analogues. |
AID1296627 | Induction of apoptosis in human HCT116 p53+/+ cells after 48 hrs by Annexin V-FITC staining-based flow cytometric method | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics. |
AID687157 | Cytotoxicity against human HL60 cells assessed as cell viability after 48 hrs by celltiter-blue assay | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
| Structure-activity relationship (SAR) study of ethyl 2-amino-6-(3,5-dimethoxyphenyl)-4-(2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate (CXL017) and the potential of the lead against multidrug resistance in cancer treatment. |
AID1690780 | Induction of apoptosis in human MOLT-4 cells assessed as viable cells at 100 nM measured after 48 hrs in presence of pan-caspase inhibitor QVD by Alexa Fluor 647-Annexin V/propidium iodide staining based flow cytometry (Rvb = 97.1 to 97.3%) | | | |
AID389266 | AUC in Sprague-Dawley rat at 5 mg/kg, po | 2008 | Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
| Discovery of an orally bioavailable small molecule inhibitor of prosurvival B-cell lymphoma 2 proteins. |
AID1194221 | Inhibition of GST-tagged Bcl-xL (unknown origin) measured after 1 hr incubation by fluorescence polarization assay | 2015 | Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8
| A combination of in silico and SAR studies to identify binding hot spots of Bcl-xL inhibitors. |
AID1353864 | Cytotoxicity against human BL2 cells assessed as reduction in cell viability after 24 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Dual inhibitors of the pro-survival proteins Bcl-2 and Mcl-1 derived from natural compound meiogynin A. |
AID1296626 | Cell cycle arrest in human HCT116 p53-/- cells assessed as accumulation at G2/M phase at 10 uM after 24 hrs by propidium iodide staining-based flow cytometric method (Rvb = 35%) | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics. |
AID1320551 | Growth inhibition of human MCF7 cells after 72 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
| Design, synthesis, and activity evaluation of selective inhibitors of anti-apoptotic Bcl-2 proteins: The effects on the selectivity of the P1 pockets in the active sites. |
AID277489 | Inhibition of cell growth in human DoHH2 cells overexpressing Bcl2 in presence of 3% FBS | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
| Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL. |
AID1483464 | Inhibition of Bcl-w (unknown origin) | 2017 | Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3
| Expanding the Cancer Arsenal with Targeted Therapies: Disarmament of the Antiapoptotic Bcl-2 Proteins by Small Molecules. |
AID1296636 | Induction of apoptosis in human DMS53 cells harboring p53 mutant assessed as caspase-3 cleavage at 5 to 10 uM after 12 hrs by immunoblotting method | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics. |
AID389268 | Ratio of AUC for Sprague-Dawley rat at 5 mg/kg, po to EC50 for human NCI-H146 cells in presence of 10% human serum | 2008 | Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
| Discovery of an orally bioavailable small molecule inhibitor of prosurvival B-cell lymphoma 2 proteins. |
AID1293715 | Inhibition of human Bcl-2 deltaC22 mutant by surface plasmon resonance method | 2016 | Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
| Selective inhibitors of Bcl-2 and Bcl-xL: Balancing antitumor activity with on-target toxicity. |
AID1635028 | Inhibition of His-tagged Bcl-xL/5-carboxyfluorescein-Bak (unknown origin) after 1 hr by fluorescence polarization assay | 2016 | Journal of natural products, Apr-22, Volume: 79, Issue:4
| Anacardic Acids from Knema hookeriana as Modulators of Bcl-xL/Bak and Mcl-1/Bid Interactions. |
AID1816660 | Cytotoxicity against MCL-1/BAX/BAK deficient mouse embryonic fibroblast cells assessed as reduction in cell viability in presence of 1 % fetal calf serum measured after 24 hrs propidium iodide staining based flow cytometric analysis | | | |
AID694155 | Antiproliferative activity against human NCI-H1417 cells after 4 days by WST8 assay | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Structure-based design of potent Bcl-2/Bcl-xL inhibitors with strong in vivo antitumor activity. |
AID1320546 | Inhibition of 5-FAM-Bid peptide binding to MCL-1 (unknown origin) by fluorescence polarization assay | 2016 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
| Design, synthesis, and activity evaluation of selective inhibitors of anti-apoptotic Bcl-2 proteins: The effects on the selectivity of the P1 pockets in the active sites. |
AID277494 | Inhibition of cell growth in human SUDHL4 cells overexpressing Bcl2 in presence of 10% HS | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
| Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL. |
AID675721 | Binding affinity to N-terminus 8X His-tagged human Bcl-xL expressed in Escherichia coli BL21 (DE3) cells after 2 hrs by fluorescence polarization assay | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
| Design of Bcl-2 and Bcl-xL inhibitors with subnanomolar binding affinities based upon a new scaffold. |
AID1545370 | Half life in mouse | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Clinical candidates modulating protein-protein interactions: The fragment-based experience. |
AID694168 | Antagonist activity at recombinant Mcl1 assessed as restoration of BIM BH3-induced Smac protein release in mitochondria isolated from MDA-MB-231 cells at 10 uM after 1 hr by Western blot analysis | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Structure-based design of potent Bcl-2/Bcl-xL inhibitors with strong in vivo antitumor activity. |
AID727589 | Solubility of compound in fasted state simulated intestinal fluid | 2013 | ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
| The role of the acidity of N-heteroaryl sulfonamides as inhibitors of bcl-2 family protein-protein interactions. |
AID526646 | Binding affinity to BCl2 | 2010 | Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19
| Toward the development of innovative bifunctional agents to induce differentiation and to promote apoptosis in leukemia: clinical candidates and perspectives. |
AID431390 | Cytotoxicity against human H460 cells after 48 hrs by cell titer-blue assay | 2009 | Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
| Structure-activity relationship and molecular mechanisms of ethyl 2-amino-4-(2-ethoxy-2-oxoethyl)-6-phenyl-4h-chromene-3-carboxylate (sha 14-1) and its analogues. |
AID1296632 | Inhibition of BCl-2/Bim interaction in human DMS53 cells harboring p53 mutant at 5 to 10 uM after 12 hrs by immunoprecipitation method | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics. |
AID389261 | Displacement of fluorescein labeled Bax peptide from Bcl2 by fluorescence polarization assay | 2008 | Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
| Discovery of an orally bioavailable small molecule inhibitor of prosurvival B-cell lymphoma 2 proteins. |
AID1677971 | Inhibition of N-His6-tagged human AspH (315-755) expressed in Escherichia coli BL21 (DE3) at 20uM using 1 uM hFX-CP as substrate mixture with 3 uM 2OG, 100 uM L-ascorbic acid and 2 uM FAS incubated for 35 mins by MS analysis | 2020 | Bioorganic & medicinal chemistry, 10-15, Volume: 28, Issue:20
| Small-molecule active pharmaceutical ingredients of approved cancer therapeutics inhibit human aspartate/asparagine-β-hydroxylase. |
AID694152 | Inhibition of human N-terminal His8-tagged Bcl-XL expressed in Escherichia coli BL21(DE3) assessed as inhibition of Fluorescein-labeled BAK binding after 1 to 2 hrs by fluorescence polarization assay | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Structure-based design of potent Bcl-2/Bcl-xL inhibitors with strong in vivo antitumor activity. |
AID431384 | Cytotoxicity against human Jurkat cells after 48 hrs by cell titer-blue assay | 2009 | Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
| Structure-activity relationship and molecular mechanisms of ethyl 2-amino-4-(2-ethoxy-2-oxoethyl)-6-phenyl-4h-chromene-3-carboxylate (sha 14-1) and its analogues. |
AID1296638 | Induction of apoptosis in human DMS53 cells harboring p53 mutant assessed as PARP cleavage at 5 to 10 uM after 12 hrs by immunoblotting method | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics. |
AID431388 | Cytotoxicity against human HCT116 cells after 48 hrs by cell titer-blue assay | 2009 | Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
| Structure-activity relationship and molecular mechanisms of ethyl 2-amino-4-(2-ethoxy-2-oxoethyl)-6-phenyl-4h-chromene-3-carboxylate (sha 14-1) and its analogues. |
AID587008 | Displacement of biotinylated Bim-BH3 from GST-tagged Bcl-Xl by AlphaScreen competitive assay | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
| Quinazoline sulfonamides as dual binders of the proteins B-cell lymphoma 2 and B-cell lymphoma extra long with potent proapoptotic cell-based activity. |
AID1816654 | Inhibition of human BCL-2 deltaC22 by surface plasmon resonance assay | | | |
AID694167 | Antagonist activity at recombinant Mcl1 assessed as restoration of BIM BH3-induced cytochrome c release in mitochondria isolated from MDA-MB-231 cells at 10 uM after 1 hr by Western blot analysis | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Structure-based design of potent Bcl-2/Bcl-xL inhibitors with strong in vivo antitumor activity. |
AID330752 | Induction of apoptosis in mouse Eu-Myc cells overexpressing A1 assessed as inhibition of colony formation at 1 uM | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-04, Volume: 104, Issue:49
| Small molecule obatoclax (GX15-070) antagonizes MCL-1 and overcomes MCL-1-mediated resistance to apoptosis. |
AID628349 | Binding affinity for GST-tagged mouse MCL1 expressed in Escherichia coli BL21 cells | 2011 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 21, Issue:17
| Biochemical and pharmacological profiling of the pro-survival protein Bcl-xL. |
AID710843 | Binding affinity to Bcl-2 | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
| An anthraquinone scaffold for putative, two-face Bim BH3 α-helix mimic. |
AID756761 | Binding affinity to human/mouse chimeric Mcl-1 by luminescence proximity assay | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
| Discovery of potent and selective benzothiazole hydrazone inhibitors of Bcl-XL. |
AID756759 | Binding affinity to human GST-tagged Bcl-Xl by luminescence proximity assay | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
| Discovery of potent and selective benzothiazole hydrazone inhibitors of Bcl-XL. |
AID1545367 | Oral bioavailability in monkey | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Clinical candidates modulating protein-protein interactions: The fragment-based experience. |
AID1677972 | Inhibition of N-His6-tagged human AspH (315-755) expressed in Escherichia coli BL21 (DE3) using 1 uM hFX-CP as substrate mixture with 3 uM 2OG, 100 uM L-ascorbic acid and 2 uM FAS incubated for 35 mins by MS analysis | 2020 | Bioorganic & medicinal chemistry, 10-15, Volume: 28, Issue:20
| Small-molecule active pharmaceutical ingredients of approved cancer therapeutics inhibit human aspartate/asparagine-β-hydroxylase. |
AID1353865 | Cytotoxicity against human Remb1 cells assessed as reduction in cell viability after 24 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Dual inhibitors of the pro-survival proteins Bcl-2 and Mcl-1 derived from natural compound meiogynin A. |
AID701526 | Binding affinity to Bcl-w | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis and biological activities of polyquinoline derivatives: new Bcl-2 family protein modulators. |
AID587090 | Cytotoxicity against mouse mcl-1 deficient MEF cells after 24 hrs by Cell titer glo assay in presence of 1% serum | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
| Quinazoline sulfonamides as dual binders of the proteins B-cell lymphoma 2 and B-cell lymphoma extra long with potent proapoptotic cell-based activity. |
AID694153 | Inhibition of human N-terminal His8-tagged Mcl1 expressed in Escherichia coli BL21(DE3) assessed as inhibition of Fluorescein-labeled BID binding after 1 to 2 hrs by fluorescence polarization assay | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Structure-based design of potent Bcl-2/Bcl-xL inhibitors with strong in vivo antitumor activity. |
AID628487 | Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 Y195F mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay | 2011 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 21, Issue:17
| Biochemical and pharmacological profiling of the pro-survival protein Bcl-xL. |
AID701518 | Inhibition of GST-tagged recombinant Bcl2 interaction with biotinylated Bim peptide by ELISA based competitive binding assay | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis and biological activities of polyquinoline derivatives: new Bcl-2 family protein modulators. |
AID587089 | Cytotoxicity against mouse MEF cells expressing mcl-1 fl/fl after 24 hrs by Cell titer glo assay in presence of 1% serum | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
| Quinazoline sulfonamides as dual binders of the proteins B-cell lymphoma 2 and B-cell lymphoma extra long with potent proapoptotic cell-based activity. |
AID330762 | Cytotoxicity against BCL2 overexpressing human KB cells transfected with MCL1 siRNA assessed as propidium iodide uptake at 0.5 uM after 72 hrs by flow cytometry | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-04, Volume: 104, Issue:49
| Small molecule obatoclax (GX15-070) antagonizes MCL-1 and overcomes MCL-1-mediated resistance to apoptosis. |
AID526652 | Aqueous solubility of the compound | 2010 | Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19
| Toward the development of innovative bifunctional agents to induce differentiation and to promote apoptosis in leukemia: clinical candidates and perspectives. |
AID701531 | Induction of apoptosis in human IM9 cells at 10 uM incubated for 24 hrs by Annexin V and propidium iodide staining based FACS method | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis and biological activities of polyquinoline derivatives: new Bcl-2 family protein modulators. |
AID727591 | Inhibition of Bcl-2/biotinylated BAK (unknown origin) interaction incubated for 1 hr by surface plasmon resonance analysis | 2013 | ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
| The role of the acidity of N-heteroaryl sulfonamides as inhibitors of bcl-2 family protein-protein interactions. |
AID515598 | Inhibition of GST-tagged Bel-xl/FITC-conjugated Bak interaction by fluorescence polarisation assay | 2010 | Bioorganic & medicinal chemistry, Oct-01, Volume: 18, Issue:19
| Synthesis and biological activities of new di- and trimeric quinoline derivatives. |
AID628489 | Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 A142Gdelta136T mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay | 2011 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 21, Issue:17
| Biochemical and pharmacological profiling of the pro-survival protein Bcl-xL. |
AID728130 | Cytotoxicity against human NCI-H187 cells assessed as growth inhibition after 4 days by WST assay | 2013 | Journal of medicinal chemistry, Apr-11, Volume: 56, Issue:7
| A potent and highly efficacious Bcl-2/Bcl-xL inhibitor. |
AID694151 | Inhibition of human N-terminal His6-tagged Bcl2 isoform 2 expressed in Escherichia coli BL21(DE3) assessed as inhibition of Fluorescein-labeled BIM binding after 1 to 2 hrs by fluorescence polarization assay | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Structure-based design of potent Bcl-2/Bcl-xL inhibitors with strong in vivo antitumor activity. |
AID587096 | Displacement of wild type mBimBH3 from Mcl-1 by solution competition assay | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
| Quinazoline sulfonamides as dual binders of the proteins B-cell lymphoma 2 and B-cell lymphoma extra long with potent proapoptotic cell-based activity. |
AID721795 | Induction of apoptosis in Mcl1 dependent human K562 cells after 48 hrs by Annexin V staining based flow cytometry | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Fragment-based design, synthesis, and biological evaluation of N-substituted-5-(4-isopropylthiophenol)-2-hydroxynicotinamide derivatives as novel Mcl-1 inhibitors. |
AID1545371 | Oral bioavailability in mouse | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Clinical candidates modulating protein-protein interactions: The fragment-based experience. |
AID701517 | Inhibition of GST-tagged recombinant Mcl1 interaction with biotinylated Bim peptide by ELISA based competitive binding assay | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis and biological activities of polyquinoline derivatives: new Bcl-2 family protein modulators. |
AID640093 | Cytotoxicity against human MDA-MB-435 cells expressing Bcl-xL, Bcl-2 and Mcl-1 after 72 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
| Design, synthesis, and activity evaluation of broad-spectrum small-molecule inhibitors of anti-apoptotic Bcl-2 family proteins: characteristics of broad-spectrum protein binding and its effects on anti-tumor activity. |
AID701521 | Induction of cell death in mouse MEF cells containing Bax/Bak double knock out at 10 uM by Annexin V and propidium iodide staining based FACS method | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis and biological activities of polyquinoline derivatives: new Bcl-2 family protein modulators. |
AID1388439 | Inhibition of Bcl-xL (unknown origin) | 2018 | Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
| Beyond the Rule of 5: Lessons Learned from AbbVie's Drugs and Compound Collection. |
AID694171 | Induction of apoptosis in human NCI-H146 cells assessed as caspase3 activation after 24 hrs by Western blot analysis | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Structure-based design of potent Bcl-2/Bcl-xL inhibitors with strong in vivo antitumor activity. |
AID1296633 | Inhibition of BCl-2/Bax interaction in human DMS53 cells harboring p53 mutant at 5 to 10 uM after 12 hrs by immunoprecipitation method | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics. |
AID756749 | Cytotoxicity against mcl-1 deficient MFF assessed as cell viability after overnight incubation by celltiter-blue assay in presence of 10% FBS | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
| Discovery of potent and selective benzothiazole hydrazone inhibitors of Bcl-XL. |
AID1816659 | Cytotoxicity against wild type mouse embryonic fibroblast cells assessed as reduction in cell viability in presence of 1 % fetal calf serum measured after 24 hrs propidium iodide staining based flow cytometric analysis | | | |
AID628402 | Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 L130A mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay | 2011 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 21, Issue:17
| Biochemical and pharmacological profiling of the pro-survival protein Bcl-xL. |
AID628404 | Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 L130V mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay | 2011 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 21, Issue:17
| Biochemical and pharmacological profiling of the pro-survival protein Bcl-xL. |
AID1483463 | Inhibition of Bcl-xL (unknown origin) | 2017 | Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3
| Expanding the Cancer Arsenal with Targeted Therapies: Disarmament of the Antiapoptotic Bcl-2 Proteins by Small Molecules. |
AID1690782 | Induction of apoptosis in human MOLT-4 cells assessed as late apoptotic cells at 100 nM measured after 48 hrs in presence of pan-caspase inhibitor QVD by Alexa Fluor 647-Annexin V/propidium iodide staining based flow cytometry (Rvb = 1.1 to 1.4%) | | | |
AID640030 | Cytotoxicity against human Raji cells expressing Bcl-xL, Bcl-2 and Mcl-1 at 100 ug/ml after 72 hrs by MTT assay relative to control | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
| Design, synthesis, and activity evaluation of broad-spectrum small-molecule inhibitors of anti-apoptotic Bcl-2 family proteins: characteristics of broad-spectrum protein binding and its effects on anti-tumor activity. |
AID675720 | Binding affinity to N-terminus 6X His-tagged human Bcl2 expressed in Escherichia coli BL21 (DE3) cells after 2 hrs by fluorescence polarization assay | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
| Design of Bcl-2 and Bcl-xL inhibitors with subnanomolar binding affinities based upon a new scaffold. |
AID721796 | Induction of apoptosis in Bcl2 dependent human RS4:11 cells after 48 hrs by Annexin V staining based flow cytometry | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Fragment-based design, synthesis, and biological evaluation of N-substituted-5-(4-isopropylthiophenol)-2-hydroxynicotinamide derivatives as novel Mcl-1 inhibitors. |
AID1545366 | Half life in monkey | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Clinical candidates modulating protein-protein interactions: The fragment-based experience. |
AID687162 | Ratio of IC50 for daunorubicin-resistant human HL60 cells to IC50 for human HL60 cells | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
| Structure-activity relationship (SAR) study of ethyl 2-amino-6-(3,5-dimethoxyphenyl)-4-(2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate (CXL017) and the potential of the lead against multidrug resistance in cancer treatment. |
AID1677973 | Inhibition of N-His6-tagged human AspH (315-755) expressed in Escherichia coli BL21 (DE3) using 1 uM hFX-CP as substrate mixture with high 200 uM 2OG, 100 uM L-ascorbic acid and 2 uM FAS incubated for 35 mins by MS analysis | 2020 | Bioorganic & medicinal chemistry, 10-15, Volume: 28, Issue:20
| Small-molecule active pharmaceutical ingredients of approved cancer therapeutics inhibit human aspartate/asparagine-β-hydroxylase. |
AID1296623 | Cell cycle arrest in human HCT116 p53+/+ cells assessed as accumulation at S phase at 5 uM after 24 hrs by propidium iodide staining-based flow cytometric method (Rvb = 42%) | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics. |
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AID1388440 | Antiproliferative activity against human RS4:11 cells in presence of 10% human serum | 2018 | Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
| Beyond the Rule of 5: Lessons Learned from AbbVie's Drugs and Compound Collection. |
AID1677974 | Inhibition of N-His6-tagged human AspH (315-755) expressed in Escherichia coli BL21 (DE3) using 1 uM hFX-CP as substrate mixture with 3 uM 2OG, 100 uM L-ascorbic acid and high 20 uM FAS incubated for 35 mins by MS analysis | 2020 | Bioorganic & medicinal chemistry, 10-15, Volume: 28, Issue:20
| Small-molecule active pharmaceutical ingredients of approved cancer therapeutics inhibit human aspartate/asparagine-β-hydroxylase. |
AID318565 | Binding affinity to Bcl-XL assessed as inhibition of Bcl-XL-BAD derived peptide interaction | 2007 | Nature, Dec-13, Volume: 450, Issue:7172
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AID431387 | Cytotoxicity against human DU145 cells after 48 hrs by cell titer-blue assay | 2009 | Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
| Structure-activity relationship and molecular mechanisms of ethyl 2-amino-4-(2-ethoxy-2-oxoethyl)-6-phenyl-4h-chromene-3-carboxylate (sha 14-1) and its analogues. |
AID687167 | Ratio of IC50 for human CCRF-CEM/VM-1-5 cells IC50 for human CCRF-CEM cells | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
| Structure-activity relationship (SAR) study of ethyl 2-amino-6-(3,5-dimethoxyphenyl)-4-(2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate (CXL017) and the potential of the lead against multidrug resistance in cancer treatment. |
AID1296625 | Cell cycle arrest in human HCT116 p53-/- cells assessed as accumulation at S phase at 10 uM after 24 hrs by propidium iodide staining-based flow cytometric method (Rvb = 36%) | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics. |
AID671072 | Inhibition of Bcl-XL | 2012 | Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
| Structure-based design of rhodanine-based acylsulfonamide derivatives as antagonists of the anti-apoptotic Bcl-2 protein. |
AID683534 | Inhibition of Mcl1-BAK interaction | 2012 | ACS medicinal chemistry letters, Jul-12, Volume: 3, Issue:7
| Lipophilic Isosteres of a π-π Stacking Interaction: New Inhibitors of the Bcl-2-Bak Protein-Protein Interaction. |
AID1690773 | Induction of apoptosis in human MOLT-4 cells assessed as early apoptotic cells at 10 nM measured after 48 hrs by Alexa Fluor 647-Annexin V/propidium iodide staining based flow cytometry (Rvb = 1.5 to 1.7%) | | | |
AID1296621 | Cell cycle arrest in human HCT116 p53-/- cells assessed as accumulation at 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics. | |
AID431401 | Inhibition of recombinant His6-tagged Bcl-XL expressed in Escherichia coli BL21 (DE3) and Flu-Bak peptide interaction by fluorescence polarization assay | 2009 | Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
| Structure-activity relationship and molecular mechanisms of ethyl 2-amino-4-(2-ethoxy-2-oxoethyl)-6-phenyl-4h-chromene-3-carboxylate (sha 14-1) and its analogues. |
AID1851855 | Inhibition of MCL-1 (unknown origin) by fluorescence polarization competition assay | 2022 | RSC medicinal chemistry, Aug-17, Volume: 13, Issue:8
| Scaffold hopping from indoles to indazoles yields dual MCL-1/BCL-2 inhibitors from MCL-1 selective leads. |
AID654461 | Binding affinity to Bcl-2 | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Structure-activity relationship of selected polyphenol derivatives as inhibitors of Bax/Bcl-xL interaction. |
AID1545373 | Oral bioavailability in dog | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Clinical candidates modulating protein-protein interactions: The fragment-based experience. |
AID539959 | Inhibition of Bcl-XL | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11
| 3D-QSAR pharmacophore modeling and in silico screening of new Bcl-xl inhibitors. |
AID515601 | Inhibition of GST-tagged Bcl-xl/FITC-conjugated PUMA interaction by fluorescence polarisation assay | 2010 | Bioorganic & medicinal chemistry, Oct-01, Volume: 18, Issue:19
| Synthesis and biological activities of new di- and trimeric quinoline derivatives. |
AID687158 | Cytotoxicity against human K562 cells assessed as cell viability after 48 hrs by celltiter-blue assay | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
| Structure-activity relationship (SAR) study of ethyl 2-amino-6-(3,5-dimethoxyphenyl)-4-(2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate (CXL017) and the potential of the lead against multidrug resistance in cancer treatment. |
AID652722 | Induction of Mcl-1-mediated apoptosis in doxycyclin-stimulated human HeLa cells overexpressing Bad3SA at 1 uM after 12 hrs by Hoechst staining | 2012 | Bioorganic & medicinal chemistry, Apr-01, Volume: 20, Issue:7
| Perturbing pro-survival proteins using quinoxaline derivatives: a structure-activity relationship study. |
AID277486 | Displacement of Bax-derived peptide from Bcl2 by fluorescence polarization assay | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
| Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL. |
AID277495 | Inhibition of tumor growth in SUDHL4 xenografted SCID mouse at 50 mg/kg, ip twice daily relative to control | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
| Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL. |
AID1690778 | Induction of apoptosis in human MOLT-4 cells assessed as late apoptotic cells at 100 nM measured after 48 hrs by Alexa Fluor 647-Annexin V/propidium iodide staining based flow cytometry (Rvb = 1.1 to 1.4%) | | | |
AID728146 | Cytotoxicity against human NCI-H1963 cells assessed as growth inhibition after 4 days by WST assay | 2013 | Journal of medicinal chemistry, Apr-11, Volume: 56, Issue:7
| A potent and highly efficacious Bcl-2/Bcl-xL inhibitor. |
AID389267 | Oral bioavailability in Sprague-Dawley rat at 5 mg/kg | 2008 | Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
| Discovery of an orally bioavailable small molecule inhibitor of prosurvival B-cell lymphoma 2 proteins. |
AID710850 | Binding affinity to Bcl-XL | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
| An anthraquinone scaffold for putative, two-face Bim BH3 α-helix mimic. |
AID1353867 | Cytotoxicity against human NCI-H929 cells assessed as reduction in cell viability after 24 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Dual inhibitors of the pro-survival proteins Bcl-2 and Mcl-1 derived from natural compound meiogynin A. |
AID628401 | Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 E129H mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay | 2011 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 21, Issue:17
| Biochemical and pharmacological profiling of the pro-survival protein Bcl-xL. |
AID1690781 | Induction of apoptosis in human MOLT-4 cells assessed as early apoptotic cells at 100 nM measured after 48 hrs in presence of pan-caspase inhibitor QVD by Alexa Fluor 647-Annexin V/propidium iodide staining based flow cytometry (Rvb = 1.5 to 1.7%) | | | |
AID1504724 | Inhibition of His-tagged MCL1 (unknown origin)/5-carboxyfluorescein-labeled Bid (unknown origin) protein protein interaction after 1 hr by fluorescence polarization assay | 2017 | Journal of natural products, 12-22, Volume: 80, Issue:12
| (+)- and (-)-Ecarlottones, Uncommon Chalconoids from Fissistigma latifolium with Pro-Apoptotic Activity. |
AID389260 | Displacement of fluorescein labeled BAD peptide from Bcl-XL by fluorescence polarization assay | 2008 | Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
| Discovery of an orally bioavailable small molecule inhibitor of prosurvival B-cell lymphoma 2 proteins. |
AID640092 | Cytotoxicity against human Raji cells expressing Bcl-xL, Bcl-2 and Mcl-1 after 72 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
| Design, synthesis, and activity evaluation of broad-spectrum small-molecule inhibitors of anti-apoptotic Bcl-2 family proteins: characteristics of broad-spectrum protein binding and its effects on anti-tumor activity. |
AID687165 | Ratio of IC50 for human K562/HHT300 cells to IC50 for human K562 cells | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
| Structure-activity relationship (SAR) study of ethyl 2-amino-6-(3,5-dimethoxyphenyl)-4-(2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate (CXL017) and the potential of the lead against multidrug resistance in cancer treatment. |
AID1483466 | Binding affinity to Bcl2A1 (unknown origin) | 2017 | Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3
| Expanding the Cancer Arsenal with Targeted Therapies: Disarmament of the Antiapoptotic Bcl-2 Proteins by Small Molecules. |
AID1178316 | Binding affinity to Bcl-b (unknown origin) | 2014 | Bioorganic & medicinal chemistry, Aug-15, Volume: 22, Issue:16
| Biased and unbiased strategies to identify biologically active small molecules. |
AID431385 | Cytotoxicity against human NALM6 cells after 48 hrs by cell titer-blue assay | 2009 | Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
| Structure-activity relationship and molecular mechanisms of ethyl 2-amino-4-(2-ethoxy-2-oxoethyl)-6-phenyl-4h-chromene-3-carboxylate (sha 14-1) and its analogues. |
AID1690774 | Induction of apoptosis in human MOLT-4 cells assessed as late apoptotic cells at 10 nM measured after 48 hrs by Alexa Fluor 647-Annexin V/propidium iodide staining based flow cytometry (Rvb = 1.1 to 1.4%) | | | |
AID756765 | Binding affinity to human GST-tagged Bcl-Xl by fluorescence polarization assay | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
| Discovery of potent and selective benzothiazole hydrazone inhibitors of Bcl-XL. |
AID277496 | Displacement of Bad-derived peptide from Bcl-xL by FPA in presence of 10% human serum | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
| Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL. |
AID1893747 | Inhibition of biotin-linker-Beclin 1 BH3 peptide binding to human C-terminal 6His-tagged Bcl-2 (1 to 218 residues) expressed in Escherichia coli BL21 Star (DE3) pLysS measured after 3 hrs by AlphaLISA assay | 2022 | ACS medicinal chemistry letters, Sep-08, Volume: 13, Issue:9
| Novel Bcl-2 Inhibitors Selectively Disrupt the Autophagy-Specific Bcl-2-Beclin 1 Protein-Protein Interaction. |
AID1690772 | Induction of apoptosis in human MOLT-4 cells assessed as viable cells at 10 nM measured after 48 hrs by Alexa Fluor 647-Annexin V/propidium iodide staining based flow cytometry (Rvb = 97.1 to 97.3%) | | | |
AID1483462 | Inhibition of Bcl-2 (unknown origin) | 2017 | Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3
| Expanding the Cancer Arsenal with Targeted Therapies: Disarmament of the Antiapoptotic Bcl-2 Proteins by Small Molecules. |
AID1690775 | Induction of apoptosis in human MOLT-4 cells assessed as necrotic cells at 10 nM measured after 48 hrs by Alexa Fluor 647-Annexin V/propidium iodide staining based flow cytometry (Rvb = 0.3 to 0.4%) | | | |
AID1851856 | Inhibition of BCL-2 (unknown origin) by fluorescence polarization competition assay | 2022 | RSC medicinal chemistry, Aug-17, Volume: 13, Issue:8
| Scaffold hopping from indoles to indazoles yields dual MCL-1/BCL-2 inhibitors from MCL-1 selective leads. |
AID330779 | Cytotoxicity against BCL2 overexpressing human KB cells transfected with luciferase siRNA assessed as annexin 5 uptake at 0.5 uM after 72 hrs by flow cytometry | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-04, Volume: 104, Issue:49
| Small molecule obatoclax (GX15-070) antagonizes MCL-1 and overcomes MCL-1-mediated resistance to apoptosis. |
AID515599 | Inhibition of GST-tagged Bcl-xl/FITC-conjugated Bid interaction by fluorescence polarisation assay | 2010 | Bioorganic & medicinal chemistry, Oct-01, Volume: 18, Issue:19
| Synthesis and biological activities of new di- and trimeric quinoline derivatives. |
AID694156 | Antiproliferative activity against human NCI-H1963 cells after 4 days by WST8 assay | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Structure-based design of potent Bcl-2/Bcl-xL inhibitors with strong in vivo antitumor activity. |
AID330750 | Induction of apoptosis in mouse Eu-Myc cells overexpressing MCL1 assessed as inhibition of colony formation at 1 uM | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-04, Volume: 104, Issue:49
| Small molecule obatoclax (GX15-070) antagonizes MCL-1 and overcomes MCL-1-mediated resistance to apoptosis. |
AID277500 | Reversal of cytokine withdrawal protection in IL3 dependent Bcl-xL overexpressing mouse FL5.12 cells in presence of 3% FBS | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
| Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL. |
AID701516 | Inhibition of GST-tagged recombinant Bfl1 interaction with biotinylated Bim peptide by ELISA based competitive binding assay | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis and biological activities of polyquinoline derivatives: new Bcl-2 family protein modulators. |
AID756752 | Binding affinity to human GST-tagged Bcl-Xl assessed as dissociation rate by surface plasmon resonance assay | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
| Discovery of potent and selective benzothiazole hydrazone inhibitors of Bcl-XL. |
AID330757 | Cytotoxicity in human KB cells overexpressing BCL2 at 0.5 uM | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-04, Volume: 104, Issue:49
| Small molecule obatoclax (GX15-070) antagonizes MCL-1 and overcomes MCL-1-mediated resistance to apoptosis. |
AID1178318 | Binding affinity to bovine beta-casein A1 | 2014 | Bioorganic & medicinal chemistry, Aug-15, Volume: 22, Issue:16
| Biased and unbiased strategies to identify biologically active small molecules. |
AID1690760 | Toxicity in human platelet assessed as reduction in cell viability measured after 48 hrs by MTS assay | | | |
AID694169 | Induction of cell death in human NCI-H146 cells after 24 hrs by trypan blue assay | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Structure-based design of potent Bcl-2/Bcl-xL inhibitors with strong in vivo antitumor activity. |
AID1296622 | Cell cycle arrest in human HCT116 p53+/+ cells assessed as accumulation at G2/M phase at 5 uM after 24 hrs by propidium iodide staining-based flow cytometric method (Rvb = 26%) | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics. |
AID1599454 | Inhibition of Bcl2 (unknown origin) | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | The chemical biology of apoptosis: Revisited after 17 years. |
AID431391 | Cytotoxicity against human MCF7 cells after 48 hrs by cell titer-blue assay | 2009 | Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
| Structure-activity relationship and molecular mechanisms of ethyl 2-amino-4-(2-ethoxy-2-oxoethyl)-6-phenyl-4h-chromene-3-carboxylate (sha 14-1) and its analogues. |
AID1320548 | Selectivity index, ratio of Ki for Bcl-2 (unknown origin) to Ki for MCL-1 (unknown origin) | 2016 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
| Design, synthesis, and activity evaluation of selective inhibitors of anti-apoptotic Bcl-2 proteins: The effects on the selectivity of the P1 pockets in the active sites. |
AID671073 | Inhibition of Bcl2 | 2012 | Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
| Structure-based design of rhodanine-based acylsulfonamide derivatives as antagonists of the anti-apoptotic Bcl-2 protein. |
AID1352853 | Cytotoxicity against human HL60/VCR cells assessed as reduction in cell viability at 1 to 2 uM by CellTiter-Glo luminescent assay relative to control | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Small-molecule Mcl-1 inhibitors: Emerging anti-tumor agents. |
AID628396 | Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 A93V mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay | 2011 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 21, Issue:17
| Biochemical and pharmacological profiling of the pro-survival protein Bcl-xL. |
AID526645 | Binding affinity to Bcl-xl | 2010 | Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19
| Toward the development of innovative bifunctional agents to induce differentiation and to promote apoptosis in leukemia: clinical candidates and perspectives. |
AID652711 | Induction of apoptosis in human HeLa cells assessed as caspase activation at 1 uM by Hoechst staining | 2012 | Bioorganic & medicinal chemistry, Apr-01, Volume: 20, Issue:7
| Perturbing pro-survival proteins using quinoxaline derivatives: a structure-activity relationship study. |
AID640032 | Cytotoxicity against human HCT116 cells expressing Bcl-xL, Bcl-2 and Mcl-1 after 72 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
| Design, synthesis, and activity evaluation of broad-spectrum small-molecule inhibitors of anti-apoptotic Bcl-2 family proteins: characteristics of broad-spectrum protein binding and its effects on anti-tumor activity. |
AID701532 | Induction of apoptosis in human BP3 cells at 10 uM incubated for 24 hrs by Annexin V and propidium iodide staining based FACS method | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis and biological activities of polyquinoline derivatives: new Bcl-2 family protein modulators. |
AID683531 | Inhibition of Bcl2-BAK interaction after 1 hr by surface plasmon resonance assay | 2012 | ACS medicinal chemistry letters, Jul-12, Volume: 3, Issue:7
| Lipophilic Isosteres of a π-π Stacking Interaction: New Inhibitors of the Bcl-2-Bak Protein-Protein Interaction. |
AID694172 | Induction of apoptosis in human NCI-H146 cells assessed as PARP cleavage after 24 hrs by Western blot analysis | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Structure-based design of potent Bcl-2/Bcl-xL inhibitors with strong in vivo antitumor activity. |
AID1545355 | Inhibition of BCL-2 (unknown origin) in presence of 10% human serum incubated for 15 mins by fluorescence polarization assay | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Clinical candidates modulating protein-protein interactions: The fragment-based experience. |
AID277501 | Inhibition of tumor growth in SUDHL4 xenografted SCID mouse at 50 mg/kg, ip in combination with etoposide at 20 mg/kg, ip | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
| Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL. |
AID277497 | Reversal of cytokine withdrawal protection in IL3 dependent Bcl2 overexpressing mouse FL5.12 cells in presence of bovine gelatin | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
| Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL. |
AID687161 | Ratio of IC50 for human HL60/ADR cells to IC50 for human HL60 cells | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
| Structure-activity relationship (SAR) study of ethyl 2-amino-6-(3,5-dimethoxyphenyl)-4-(2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate (CXL017) and the potential of the lead against multidrug resistance in cancer treatment. |
AID628395 | Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Wild type Bcl-2-like protein 1 expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay | 2011 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 21, Issue:17
| Biochemical and pharmacological profiling of the pro-survival protein Bcl-xL. |
AID1296637 | Induction of apoptosis in human DMS53 cells harboring p53 mutant assessed as cytochrome c release at 5 to 10 uM after 12 hrs by immunoblotting method | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics. |
AID587009 | Binding affinity to Bcl-Xl assessed as association rate constant by surface plasmon resonance assay | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
| Quinazoline sulfonamides as dual binders of the proteins B-cell lymphoma 2 and B-cell lymphoma extra long with potent proapoptotic cell-based activity. |
AID1599455 | Inhibition of Bcl-xL (unknown origin) | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | The chemical biology of apoptosis: Revisited after 17 years. |
AID277491 | Inhibition of cell growth in human RS11380 cells overexpressing Bcl2 in presence of 3% FBS | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
| Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL. |
AID1816656 | Inhibition of GST tagged human/mouse chimeric MCL-1 by surface plasmon resonance assay | | | |
AID1388438 | Inhibition of Bcl2 (unknown origin) | 2018 | Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
| Beyond the Rule of 5: Lessons Learned from AbbVie's Drugs and Compound Collection. |
AID1545356 | Inhibition of BCL-XL (unknown origin) in presence of 10% human serum incubated for 15 mins by fluorescence polarization assay | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Clinical candidates modulating protein-protein interactions: The fragment-based experience. |
AID1353866 | Cytotoxicity against human RS4:11 cells assessed as reduction in cell viability after 24 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Dual inhibitors of the pro-survival proteins Bcl-2 and Mcl-1 derived from natural compound meiogynin A. |
AID671074 | Inhibition of Bcl-w | 2012 | Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
| Structure-based design of rhodanine-based acylsulfonamide derivatives as antagonists of the anti-apoptotic Bcl-2 protein. |
AID675724 | Growth inhibition of human NCI-H1417 cells after 4 days by WST8 assay | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
| Design of Bcl-2 and Bcl-xL inhibitors with subnanomolar binding affinities based upon a new scaffold. |
AID628403 | Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 L130G mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay | 2011 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 21, Issue:17
| Biochemical and pharmacological profiling of the pro-survival protein Bcl-xL. |
AID1891304 | Antiproliferative activity against cisplatin-resistant human MCF7-CR cells assessed as reduction in cell viability after 24 hrs by MTT assay | 2022 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 67 | New synthetic phenylquinazoline derivatives induce apoptosis by targeting the pro-survival members of the BCL-2 family. |
AID1224379 | Displacement of fluorescein-labeled BID from His-tagged MCL-1 (unknown origin) after 1 hr by fluorescence polarization assay | 2014 | Journal of natural products, Jun-27, Volume: 77, Issue:6
| Endiandric acid analogues from Beilschmiedia ferruginea as dual inhibitors of Bcl-xL/Bak and Mcl-1/Bid interactions. |
AID1178313 | Binding affinity to Bcl-xL (unknown origin) | 2014 | Bioorganic & medicinal chemistry, Aug-15, Volume: 22, Issue:16
| Biased and unbiased strategies to identify biologically active small molecules. |
AID687166 | Ratio of IC50 for human CCRF-CEM/C2 cells IC50 for human CCRF-CEM cells | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
| Structure-activity relationship (SAR) study of ethyl 2-amino-6-(3,5-dimethoxyphenyl)-4-(2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate (CXL017) and the potential of the lead against multidrug resistance in cancer treatment. |
AID1893748 | Inhibition of biotin-linker-Bax BH3 peptide binding to human C-terminal 6His-tagged Bcl-2 (1 to 218 residues) expressed in Escherichia coli BL21 Star (DE3) pLysS measured after 3 hrs by AlphaLISA assay | 2022 | ACS medicinal chemistry letters, Sep-08, Volume: 13, Issue:9
| Novel Bcl-2 Inhibitors Selectively Disrupt the Autophagy-Specific Bcl-2-Beclin 1 Protein-Protein Interaction. |
AID587092 | Cytotoxicity against mouse mcl-1 deficient MEF cells after 24 hrs by Cell titer glo assay in presence of 10% serum | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
| Quinazoline sulfonamides as dual binders of the proteins B-cell lymphoma 2 and B-cell lymphoma extra long with potent proapoptotic cell-based activity. |
AID1296608 | Cell cycle arrest in human HCT116 p53+/+ cells assessed as accumulation at 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics. | |
AID756757 | Binding affinity to human GST-tagged Bcl-Xl by surface plasmon resonance assay | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
| Discovery of potent and selective benzothiazole hydrazone inhibitors of Bcl-XL. |
AID1690779 | Induction of apoptosis in human MOLT-4 cells assessed as necrotic cells at 100 nM measured after 48 hrs by Alexa Fluor 647-Annexin V/propidium iodide staining based flow cytometry (Rvb = 0.3 to 0.4%) | | | |
AID1388441 | Antiproliferative activity against human MOLT4 cells in presence of 10% human serum | 2018 | Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
| Beyond the Rule of 5: Lessons Learned from AbbVie's Drugs and Compound Collection. |
AID1296611 | Inhibition of MDM2-p53 interaction in human HCT116 p53+/+ cells assessed as upregulation of p53 expression at 5 to 10 uM after 12 hrs by immunoblotting method | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics. |
AID526651 | Induction of apoptosis in human CLL cells | 2010 | Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19
| Toward the development of innovative bifunctional agents to induce differentiation and to promote apoptosis in leukemia: clinical candidates and perspectives. |
AID756747 | Cytotoxicity against bax and bak deficient MFF assessed as cell viability after overnight incubation by celltiter-blue assay in presence of 1% FBS | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
| Discovery of potent and selective benzothiazole hydrazone inhibitors of Bcl-XL. |
AID1690777 | Induction of apoptosis in human MOLT-4 cells assessed as early apoptotic cells at 100 nM measured after 48 hrs by Alexa Fluor 647-Annexin V/propidium iodide staining based flow cytometry (Rvb = 1.5 to 1.7%) | | | |
AID727592 | Binding affinity to Bcl-2 (unknown origin) by surface plasmon resonance analysis | 2013 | ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
| The role of the acidity of N-heteroaryl sulfonamides as inhibitors of bcl-2 family protein-protein interactions. |
AID277490 | Inhibition of cell growth in human DoHH2 cells overexpressing Bcl2 in presence of 10% HS | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
| Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL. |
AID628350 | Binding affinity for GST-tagged human BCL2A1 expressed in Escherichia coli BL21 cells | 2011 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 21, Issue:17
| Biochemical and pharmacological profiling of the pro-survival protein Bcl-xL. |
AID687163 | Ratio of IC50 for doxorubicin-resistant human HL60 cells to IC50 for human HL60 cells | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
| Structure-activity relationship (SAR) study of ethyl 2-amino-6-(3,5-dimethoxyphenyl)-4-(2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate (CXL017) and the potential of the lead against multidrug resistance in cancer treatment. |
AID1816653 | Inhibition of GST tagged human BCL-XL deltaC25 by surface plasmon resonance assay | | | |
AID687159 | Cytotoxicity against human CCRF-CEM cells assessed as cell viability after 48 hrs by celltiter-blue assay | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
| Structure-activity relationship (SAR) study of ethyl 2-amino-6-(3,5-dimethoxyphenyl)-4-(2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate (CXL017) and the potential of the lead against multidrug resistance in cancer treatment. |
AID728129 | Cytotoxicity against human NCI-H1417 cells assessed as growth inhibition after 4 days by WST assay | 2013 | Journal of medicinal chemistry, Apr-11, Volume: 56, Issue:7
| A potent and highly efficacious Bcl-2/Bcl-xL inhibitor. |
AID1320545 | Inhibition of 5-FAM-Bid peptide binding to Bcl-XL (unknown origin) by fluorescence polarization assay | 2016 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
| Design, synthesis, and activity evaluation of selective inhibitors of anti-apoptotic Bcl-2 proteins: The effects on the selectivity of the P1 pockets in the active sites. |
AID277493 | Inhibition of cell growth in human SUDHL4 cells overexpressing Bcl2 in presence of 3% FBS | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
| Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL. |
AID756754 | Binding affinity to Bcl-2 (unknown origin) by surface plasmon resonance assay | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
| Discovery of potent and selective benzothiazole hydrazone inhibitors of Bcl-XL. |
AID1545369 | Oral bioavailability in rat | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Clinical candidates modulating protein-protein interactions: The fragment-based experience. |
AID628488 | Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 G196A mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay | 2011 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 21, Issue:17
| Biochemical and pharmacological profiling of the pro-survival protein Bcl-xL. |
AID1599456 | Inhibition of Bcl-w (unknown origin) | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | The chemical biology of apoptosis: Revisited after 17 years. |
AID1320552 | Growth inhibition of human SKOV3 cells after 72 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
| Design, synthesis, and activity evaluation of selective inhibitors of anti-apoptotic Bcl-2 proteins: The effects on the selectivity of the P1 pockets in the active sites. |
AID1296613 | Inhibition of MDM2-p53 interaction in human HCT116 p53+/+ cells assessed as upregulation of p21 expression at 5 to 10 uM after 12 hrs by immunoblotting method | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics. |
AID1504723 | Inhibition of His-tagged Bcl-xL (unknown origin)/5-carboxyfluorescein-labeled Bak (unknown origin) protein protein interaction after 1 hr by fluorescence polarization assay | 2017 | Journal of natural products, 12-22, Volume: 80, Issue:12
| (+)- and (-)-Ecarlottones, Uncommon Chalconoids from Fissistigma latifolium with Pro-Apoptotic Activity. |
AID675722 | Binding affinity to N-terminus 8X His-tagged human Mcl1 expressed in Escherichia coli BL21 (DE3) cells after 2 hrs by fluorescence polarization assay | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
| Design of Bcl-2 and Bcl-xL inhibitors with subnanomolar binding affinities based upon a new scaffold. |
AID694157 | Antagonist activity at recombinant Bcl2 assessed as restoration of BIM BH3-induced cytochrome c release in mitochondria isolated from MDA-MB-231 cells after 1 hr by Western blot analysis | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Structure-based design of potent Bcl-2/Bcl-xL inhibitors with strong in vivo antitumor activity. |
AID654459 | Binding affinity to Mcl-1 | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Structure-activity relationship of selected polyphenol derivatives as inhibitors of Bax/Bcl-xL interaction. |
AID652720 | Induction of Bcl-xL-mediated apoptosis in doxycyclin-stimulated human HeLa cells overexpressing Noxa at 1 uM after 12 hrs by Hoechst staining | 2012 | Bioorganic & medicinal chemistry, Apr-01, Volume: 20, Issue:7
| Perturbing pro-survival proteins using quinoxaline derivatives: a structure-activity relationship study. |
AID1545368 | Half life in rat | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Clinical candidates modulating protein-protein interactions: The fragment-based experience. |
AID1320549 | Growth inhibition of human HL60 cells after 72 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
| Design, synthesis, and activity evaluation of selective inhibitors of anti-apoptotic Bcl-2 proteins: The effects on the selectivity of the P1 pockets in the active sites. |
AID389264 | Cytotoxicity against human NCI-H146 cells assessed as cell viability after 48 hrs in presence of 10% human serum | 2008 | Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
| Discovery of an orally bioavailable small molecule inhibitor of prosurvival B-cell lymphoma 2 proteins. |
AID628486 | Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 A142T mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay | 2011 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 21, Issue:17
| Biochemical and pharmacological profiling of the pro-survival protein Bcl-xL. |
AID587010 | Displacement of wild type mBimBH3 from human Bcl-2 by solution competition assay | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
| Quinazoline sulfonamides as dual binders of the proteins B-cell lymphoma 2 and B-cell lymphoma extra long with potent proapoptotic cell-based activity. |
AID1677975 | Inhibition of N-His6-tagged human AspH (315-755) expressed in Escherichia coli BL21 (DE3) using high 10 uM hFX-CP as substrate mixture with 10 uM 2OG, 100 uM L-ascorbic acid and 2 uM FAS incubated for 35 mins by MS analysis | 2020 | Bioorganic & medicinal chemistry, 10-15, Volume: 28, Issue:20
| Small-molecule active pharmaceutical ingredients of approved cancer therapeutics inhibit human aspartate/asparagine-β-hydroxylase. |
AID628485 | Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 A142G mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay | 2011 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 21, Issue:17
| Biochemical and pharmacological profiling of the pro-survival protein Bcl-xL. |
AID1545372 | Half life in dog | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Clinical candidates modulating protein-protein interactions: The fragment-based experience. |
AID694162 | Antagonist activity at recombinant Bcl-XL assessed as restoration of BIM BH3-induced Smac protein release in mitochondria isolated from MDA-MB-231 cells at 0.03 to 1 uM after 1 hr by Western blot analysis | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Structure-based design of potent Bcl-2/Bcl-xL inhibitors with strong in vivo antitumor activity. |
AID587088 | Cytotoxicity against mouse MEF cells expressing mcl-1 fl/fl at 10 uM after 24 hrs by Cell titer glo assay in presence of 10% fetal bovine serum | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
| Quinazoline sulfonamides as dual binders of the proteins B-cell lymphoma 2 and B-cell lymphoma extra long with potent proapoptotic cell-based activity. |
AID330761 | Cytotoxicity against BCL2 overexpressing human KB cells transfected with MCL1 siRNA assessed as annexin 5 reactivity at 0.5 uM after 72 hrs by flow cytometry | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-04, Volume: 104, Issue:49
| Small molecule obatoclax (GX15-070) antagonizes MCL-1 and overcomes MCL-1-mediated resistance to apoptosis. |
AID389263 | Cytotoxicity against IL3-dependent mouse FL5.12 cells overexpressing human Bcl-XL assessed as cell viability after 24 hrs by MTS assay in absence of serum | 2008 | Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
| Discovery of an orally bioavailable small molecule inhibitor of prosurvival B-cell lymphoma 2 proteins. |
AID694158 | Antagonist activity at recombinant Bcl2 assessed as restoration of BIM BH3-induced Smac protein release in mitochondria isolated from MDA-MB-231 cells after 1 hr by Western blot analysis | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Structure-based design of potent Bcl-2/Bcl-xL inhibitors with strong in vivo antitumor activity. |
AID756766 | Cytotoxicity against mcl-1 deficient MFF assessed as cell viability after overnight incubation by celltiter-blue assay in presence of 1% FBS | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
| Discovery of potent and selective benzothiazole hydrazone inhibitors of Bcl-XL. |
AID431386 | Cytotoxicity against human REH cells after 48 hrs by cell titer-blue assay | 2009 | Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
| Structure-activity relationship and molecular mechanisms of ethyl 2-amino-4-(2-ethoxy-2-oxoethyl)-6-phenyl-4h-chromene-3-carboxylate (sha 14-1) and its analogues. |
AID431389 | Cytotoxicity against mouse Hepa-1c1c7 cells after 48 hrs by cell titer-blue assay | 2009 | Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
| Structure-activity relationship and molecular mechanisms of ethyl 2-amino-4-(2-ethoxy-2-oxoethyl)-6-phenyl-4h-chromene-3-carboxylate (sha 14-1) and its analogues. |
AID628405 | Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 delta136T mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay | 2011 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 21, Issue:17
| Biochemical and pharmacological profiling of the pro-survival protein Bcl-xL. |
AID1352852 | Cytotoxicity against human Raji cells assessed as reduction in cell viability at 1 to 2 uM by CellTiter-Glo luminescent assay relative to control | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Small-molecule Mcl-1 inhibitors: Emerging anti-tumor agents. |
AID1320553 | Growth inhibition of human NCI-H23 cells after 72 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
| Design, synthesis, and activity evaluation of selective inhibitors of anti-apoptotic Bcl-2 proteins: The effects on the selectivity of the P1 pockets in the active sites. |
AID640031 | Cytotoxicity against human MDA-MB-435 cells expressing Bcl-xL, Bcl-2 and Mcl-1 at 100 ug/ml after 72 hrs by MTT assay relative to control | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
| Design, synthesis, and activity evaluation of broad-spectrum small-molecule inhibitors of anti-apoptotic Bcl-2 family proteins: characteristics of broad-spectrum protein binding and its effects on anti-tumor activity. |
AID1816658 | Cytotoxicity against MCL deficient mouse embryonic fibroblast cells assessed as reduction in cell viability in presence of 1 % fetal calf serum measured after 24 hrs by propidium iodide staining based flow cytometric analysis | | | |
AID1320550 | Growth inhibition of human U266 cells after 72 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
| Design, synthesis, and activity evaluation of selective inhibitors of anti-apoptotic Bcl-2 proteins: The effects on the selectivity of the P1 pockets in the active sites. |
AID628397 | Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 E96G mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay | 2011 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 21, Issue:17
| Biochemical and pharmacological profiling of the pro-survival protein Bcl-xL. |
AID277499 | Reversal of cytokine withdrawal protection in IL3 dependent Bcl-xL overexpressing mouse FL5.12 cells in presence of bovine gelatin | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
| Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL. |
AID587091 | Cytotoxicity against mouse MEF cells expressing mcl-1 fl/fl after 24 hrs by Cell titer glo assay in presence of 10% serum | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
| Quinazoline sulfonamides as dual binders of the proteins B-cell lymphoma 2 and B-cell lymphoma extra long with potent proapoptotic cell-based activity. |
AID756748 | Cytotoxicity against wild type MFF assessed as cell viability after overnight incubation by celltiter-blue assay in presence of 10% FBS | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
| Discovery of potent and selective benzothiazole hydrazone inhibitors of Bcl-XL. |
AID587007 | Binding affinity to Bcl-Xl | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
| Quinazoline sulfonamides as dual binders of the proteins B-cell lymphoma 2 and B-cell lymphoma extra long with potent proapoptotic cell-based activity. |
AID1320547 | Selectivity index, ratio of Ki for Bcl-2 (unknown origin) to Ki for Bcl-XL (unknown origin) | 2016 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
| Design, synthesis, and activity evaluation of selective inhibitors of anti-apoptotic Bcl-2 proteins: The effects on the selectivity of the P1 pockets in the active sites. |
AID1296612 | Inhibition of MDM2-p53 interaction in human HCT116 p53+/+ cells assessed as upregulation of MDM2 expression at 5 to 10 uM after 12 hrs by immunoblotting method | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics. |
AID640027 | Binding affinity to Bcl-xL by competitive fluorescence polarization assay | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
| Design, synthesis, and activity evaluation of broad-spectrum small-molecule inhibitors of anti-apoptotic Bcl-2 family proteins: characteristics of broad-spectrum protein binding and its effects on anti-tumor activity. |
AID687168 | Ratio of IC50 for human CCRF-CEM/VLB100 cells IC50 for human CCRF-CEM cells | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
| Structure-activity relationship (SAR) study of ethyl 2-amino-6-(3,5-dimethoxyphenyl)-4-(2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate (CXL017) and the potential of the lead against multidrug resistance in cancer treatment. |
AID1816651 | Inhibition of GST tagged human BCL-XL deltaC25 using biotin-DLRPEIRIAQELRIZIGDEFNETYTRR as substrate incubated for 40 mins followed by substrate addition measured after 4 hrs by AlphaSCREEN assay | | | |
AID628400 | Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 Y101H mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay | 2011 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 21, Issue:17
| Biochemical and pharmacological profiling of the pro-survival protein Bcl-xL. |
AID701259 | Induction of apoptosis in human NCI-H146 cells assessed as cell viability at 30 to 100 nM after 24 hrs by trypan blue exclusion assay | 2012 | Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19
| Structure-based discovery of BM-957 as a potent small-molecule inhibitor of Bcl-2 and Bcl-xL capable of achieving complete tumor regression. |
AID701261 | Induction of apoptosis in human NCI-H146 cells assessed as cell viability after 24 hrs by trypan blue exclusion assay | 2012 | Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19
| Structure-based discovery of BM-957 as a potent small-molecule inhibitor of Bcl-2 and Bcl-xL capable of achieving complete tumor regression. |
AID515600 | Inhibition of GST-tagged Bcl-xl/FITC-conjugated Bim interaction by fluorescence polarisation assay | 2010 | Bioorganic & medicinal chemistry, Oct-01, Volume: 18, Issue:19
| Synthesis and biological activities of new di- and trimeric quinoline derivatives. |
AID1178314 | Binding affinity to Bcl-2 (unknown origin) | 2014 | Bioorganic & medicinal chemistry, Aug-15, Volume: 22, Issue:16
| Biased and unbiased strategies to identify biologically active small molecules. |
AID515597 | Inhibition of GST-tagged Bcl-xl/FITC-conjugated Bax interaction by fluorescence polarisation assay | 2010 | Bioorganic & medicinal chemistry, Oct-01, Volume: 18, Issue:19
| Synthesis and biological activities of new di- and trimeric quinoline derivatives. |
AID1690783 | Induction of apoptosis in human MOLT-4 cells assessed as necrotic cells at 100 nM measured after 48 hrs in presence of pan-caspase inhibitor QVD by Alexa Fluor 647-Annexin V/propidium iodide staining based flow cytometry (Rvb = 0.3 to 0.4%) | | | |
AID1816655 | Inhibition of human BCL-W deltaC23 C29S/A128E mutant by surface plasmon resonance assay | | | |
AID1293716 | Inhibition of human Bcl-XL deltaC24 mutant at 25 degC by surface plasmon resonance method | 2016 | Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
| Selective inhibitors of Bcl-2 and Bcl-xL: Balancing antitumor activity with on-target toxicity. |
AID694154 | Antiproliferative activity against human NCI-H146 cells after 4 days by WST8 assay | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Structure-based design of potent Bcl-2/Bcl-xL inhibitors with strong in vivo antitumor activity. |
AID756756 | Binding affinity to Bcl-w (unknown origin) by surface plasmon resonance assay | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
| Discovery of potent and selective benzothiazole hydrazone inhibitors of Bcl-XL. |
AID277498 | Reversal of cytokine withdrawal protection in IL3 dependent Bcl2 overexpressing mouse FL5.12 cells in presence of 3% FBS | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
| Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL. |
AID330778 | Cytotoxicity against BCL2 overexpressing human KB cells transfected with luciferase siRNA assessed as propidium iodide uptake at 0.5 uM after 72 hrs by flow cytometry | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-04, Volume: 104, Issue:49
| Small molecule obatoclax (GX15-070) antagonizes MCL-1 and overcomes MCL-1-mediated resistance to apoptosis. |
AID701527 | Binding affinity to Bcl2 | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis and biological activities of polyquinoline derivatives: new Bcl-2 family protein modulators. |
AID756755 | Binding affinity to human/mouse chimeric Mcl-1 by surface plasmon resonance assay | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
| Discovery of potent and selective benzothiazole hydrazone inhibitors of Bcl-XL. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
AID1347164 | 384 well plate NINDS Rhodamine confirmatory 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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | | | |
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. |
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. |
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. |
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. |
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. |
AID1347158 | ZIKV-mCherry secondary 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. |
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. |
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. |
AID1347156 | DAPI mCherry counterscreen 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. |
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. |
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. |
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. |
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. |
AID1347163 | 384 well plate NINDS AMC confirmatory 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. |
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. |
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. |
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. |
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. |
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. |
AID1346193 | Human BCL2, apoptosis regulator (B-cell lymphoma 2 (Bcl-2) protein family) | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
| Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL. |
AID1346232 | Human Bcl-2-like 1 (B-cell lymphoma 2 (Bcl-2) protein family) | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
| Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL. |
AID1346192 | Human Bcl-2-like 2 (B-cell lymphoma 2 (Bcl-2) protein family) | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
| Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL. |
AID1798080 | Fluorescence Polarization Assay and FL5.12 Cellular Assay from Article 10.1021/jm061152t: \\Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL.\\ | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
| Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL. |
AID1800239 | SPR Directy Binding Assay (Biacore 4000) from Article 10.1038/nchembio.1246: \\Structure-guided design of a selective BCL-X(L) inhibitor.\\ | 2013 | Nature chemical biology, Jun, Volume: 9, Issue:6
| Structure-guided design of a selective BCL-X(L) inhibitor. |
AID1800237 | AlphaScreen Assay (AS) from Article 10.1038/nchembio.1246: \\Structure-guided design of a selective BCL-X(L) inhibitor.\\ | 2013 | Nature chemical biology, Jun, Volume: 9, Issue:6
| Structure-guided design of a selective BCL-X(L) inhibitor. |
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. |
AID1347170 | Vero cells viability counterscreen for qRT-PCR qHTS assay of selected 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. |
AID1347172 | Secondary qRT-PCR qHTS assay for selected 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. |
AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 2007 | Cell death and differentiation, Sep, Volume: 14, Issue:9
| Crystal structure of ABT-737 complexed with Bcl-xL: implications for selectivity of antagonists of the Bcl-2 family. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |