Assay ID | Title | Year | Journal | Article |
AID350571 | Cytotoxicity against human MCF7 cells after 72 hrs by celltiter-glo assay | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Potent cytotoxic C-11 modified geldanamycin analogues. |
AID395892 | Binding affinity to Hsp90 in human SKBR3 cells | 2009 | Bioorganic & medicinal chemistry, Mar-15, Volume: 17, Issue:6
| Discovery and development of heat shock protein 90 inhibitors. |
AID266548 | Inhibition of human SKBR3 cell growth | 2006 | Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15
| Design, synthesis, and biological evaluation of hydroquinone derivatives of 17-amino-17-demethoxygeldanamycin as potent, water-soluble inhibitors of Hsp90. |
AID394603 | Cytotoxicity against human MCF7 cells after 72 hrs | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
| Potent non-benzoquinone ansamycin heat shock protein 90 inhibitors from genetic engineering of Streptomyces hygroscopicus. |
AID394598 | Binding affinity to human recombinant Hsp90alpha N-terminal domain by scintillation proximity assay | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
| Potent non-benzoquinone ansamycin heat shock protein 90 inhibitors from genetic engineering of Streptomyces hygroscopicus. |
AID1212925 | Metabolic stability in human liver microsomes at 5 uM by liquid chromatography-tandem mass spectrometry | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
| In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes. |
AID444597 | Hepatic clearance in human liver microsomes measured per million cells | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Dihydroxyphenylisoindoline amides as orally bioavailable inhibitors of the heat shock protein 90 (hsp90) molecular chaperone. |
AID327963 | Inhibition of TNF-alpha-induced NF-kappaB activation in human HeLa cells | 2008 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
| Hypoxia-inducible factor-1 and nuclear factor-kappaB inhibitory meroterpene analogues of bakuchiol, a constituent of the seeds of Psoralea corylifolia. |
AID465321 | Toxicity in iv dosed dog assessed as maximum tolerated dose | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Heat shock protein 90: inhibitors in clinical trials. |
AID394604 | Cytotoxicity against NQ01-deficient human MDA468 cells after 72 hrs | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
| Potent non-benzoquinone ansamycin heat shock protein 90 inhibitors from genetic engineering of Streptomyces hygroscopicus. |
AID344857 | Cytotoxicity against human A2058 cells by MTT assay | 2008 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23
| Dihydroxylphenyl amides as inhibitors of the Hsp90 molecular chaperone. |
AID291918 | Viability of human Hep3B cells under normoxic conditions after 24 hrs by MTT assay | 2007 | Journal of natural products, Jul, Volume: 70, Issue:7
| Abietane diterpenes from Salvia miltiorrhiza inhibit the activation of hypoxia-inducible factor-1. |
AID1076811 | Antiproliferative activity against human SKBR3 cells assessed as inhibition of cell viability after 48 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
| Synthesis and evaluation of a novel class Hsp90 inhibitors containing 1-phenylpiperazine scaffold. |
AID1076810 | Antiproliferative activity against human HCT116 cells assessed as inhibition of cell viability after 48 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
| Synthesis and evaluation of a novel class Hsp90 inhibitors containing 1-phenylpiperazine scaffold. |
AID1127400 | Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay | 2014 | European journal of medicinal chemistry, May-22, Volume: 79 | Identification and optimization of novel Hsp90 inhibitors with tetrahydropyrido[4,3-d]pyrimidines core through shape-based screening. |
AID394605 | Cytotoxicity against NQ01-deficient human NCI-H596 cells after 72 hrs | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
| Potent non-benzoquinone ansamycin heat shock protein 90 inhibitors from genetic engineering of Streptomyces hygroscopicus. |
AID1127401 | Antiproliferative activity against human A231 cells after 48 hrs by MTT assay | 2014 | European journal of medicinal chemistry, May-22, Volume: 79 | Identification and optimization of novel Hsp90 inhibitors with tetrahydropyrido[4,3-d]pyrimidines core through shape-based screening. |
AID1885316 | Inhibition of KDM5A (unknown origin) measured by AlphaScreen assay | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
| Recent Advances with KDM4 Inhibitors and Potential Applications. |
AID506585 | Inhibition of HSP90-mediated proliferation of human NCI-H526 cells at 1 uM after 96 hrs by sulforhodamine B assay | 2007 | Nature chemical biology, Aug, Volume: 3, Issue:8
| Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer. |
AID1625290 | Inhibition of Hsp90 in human SKBR3 cells | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
| Development of Heat Shock Protein (Hsp90) Inhibitors To Combat Resistance to Tyrosine Kinase Inhibitors through Hsp90-Kinase Interactions. |
AID327961 | Inhibition of hypoxia-induced HIF1 activation in human AGS cells by reporter gene assay | 2008 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
| Hypoxia-inducible factor-1 and nuclear factor-kappaB inhibitory meroterpene analogues of bakuchiol, a constituent of the seeds of Psoralea corylifolia. |
AID1212926 | Terminal half life in human | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
| In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes. |
AID344856 | Inhibition of Hsp90 in human A2058 cells assessed as Akt degradation | 2008 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23
| Dihydroxylphenyl amides as inhibitors of the Hsp90 molecular chaperone. |
AID715287 | Inhibition of Hsp90 in human COLO205 cells xenografted in mouse assessed as Her2 degradation at 100 mg/kg administered QD for 2 days measured 8 hrs post-last dose | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
| Discovery of XL888: a novel tropane-derived small molecule inhibitor of HSP90. |
AID1212959 | Drug metabolism assessed as human recombinant CYP3A5-mediated (4E,6Z,8S,9S,10E,12S,13R,14S,16R)-19-(2-(dimethylamino)ethylamino)-13-hydroxy-10-(hydroxymethyl)-8,14-dimethoxy-4,12,16-trimethyl-3,20,22-trioxo-2-azabicyclo[16.3.1]docosa-1(21),4,6,10,18-penta | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
| In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes. |
AID1212974 | Drug metabolism in human liver microsomes assessed as 1 uM CYP3A inhibitor ketoconazole-mediated inhibition of (4E,6Z,8S,9S,10E,12S,13R,14S,16R)-19-(2-(dimethylamino)-1-hydroxyethylamino)-13-hydroxy-8,14-dimethoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-a | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
| In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes. |
AID266550 | Degradation of Her2 in SKBR3 cells | 2006 | Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15
| Design, synthesis, and biological evaluation of hydroquinone derivatives of 17-amino-17-demethoxygeldanamycin as potent, water-soluble inhibitors of Hsp90. |
AID1212960 | Drug metabolism assessed as human recombinant CYP3A5-mediated (4E,6Z,8S,9S,10E,12S,13R,14S,16R)-19-(2-(dimethylamino)-1-hydroxyethylamino)-13-hydroxy-8,14-dimethoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-azabicyclo[16.3.1]docosa-1(21),4,6,10,18-pentaen-9 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
| In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes. |
AID394600 | Cytotoxicity against human SKBR3 cells after 72 hrs | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
| Potent non-benzoquinone ansamycin heat shock protein 90 inhibitors from genetic engineering of Streptomyces hygroscopicus. |
AID1212969 | Drug metabolism assessed as human recombinant CYP2B6-mediated oxidative metabolism at 1 uM by liquid chromatography-tandem mass spectrometry | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
| In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes. |
AID266553 | Upregulation of Hsp70 in SKOV3 cells | 2006 | Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15
| Design, synthesis, and biological evaluation of hydroquinone derivatives of 17-amino-17-demethoxygeldanamycin as potent, water-soluble inhibitors of Hsp90. |
AID465320 | Toxicity in iv dosed rat assessed as maximum tolerated dose | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Heat shock protein 90: inhibitors in clinical trials. |
AID1212975 | Drug metabolism in human liver microsomes assessed as 1 uM CYP3A inhibitor ketoconazole-mediated inhibition of (4E,6Z,8S,9S,10E,12S,13R,14S,16R)-19-(2-(dimethylamino)ethylamino)-13,14-dihydroxy-8-methoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-azabicyclo[ | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
| In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes. |
AID1212961 | Drug metabolism assessed as human recombinant CYP3A5-mediated (4E,6Z,8S,9S,10E,12S,13R,14S,16R)-19-(2-(dimethylamino)ethylamino)-13,14-dihydroxy-8-methoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-azabicyclo[16.3.1]docosa-1(21),4,6,10,18-pentaen-9-yl carbam | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
| In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes. |
AID1625300 | Cytotoxicity against HGF-induced erlotinib-resistant human Ma1 cells assessed as inhibition of cell growth after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
| Development of Heat Shock Protein (Hsp90) Inhibitors To Combat Resistance to Tyrosine Kinase Inhibitors through Hsp90-Kinase Interactions. |
AID485532 | Inhibition of hypoxia-induced VEGF protein secretion in human Hep3B cells after 16 hrs by ELISA | 2010 | Journal of natural products, Jun-25, Volume: 73, Issue:6
| An isoaurone and other constituents from Trichosanthes kirilowii seeds inhibit hypoxia-inducible factor-1 and nuclear factor-kappaB. |
AID344858 | Inhibition of Hsp90 in human A2058 cells | 2008 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23
| Dihydroxylphenyl amides as inhibitors of the Hsp90 molecular chaperone. |
AID1212956 | Drug metabolism in human liver microsomes assessed as (4E,6Z,8S,9S,10E,12S,13R,14S,16R)-19-(2-(dimethylamino)ethylamino)-8,13-dihydroxy-14-methoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-azabicyclo[16.3.1]docosa-1(21),4,6,10,18-pentaen-9-yl carbamate form | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
| In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes. |
AID1127395 | Inhibition of HSP90 (unknown origin)-mediated ATPase activity at 40 uM after 3 hrs by malachite green assay relative to control | 2014 | European journal of medicinal chemistry, May-22, Volume: 79 | Identification and optimization of novel Hsp90 inhibitors with tetrahydropyrido[4,3-d]pyrimidines core through shape-based screening. |
AID1127397 | Displacement of FITC-geldanamycin from HSP90 (unknown origin) after 30 mins by fluorescence polarization assay | 2014 | European journal of medicinal chemistry, May-22, Volume: 79 | Identification and optimization of novel Hsp90 inhibitors with tetrahydropyrido[4,3-d]pyrimidines core through shape-based screening. |
AID1212927 | Total clearance in human | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
| In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes. |
AID1076813 | Inhibition of full-length Hsp90-ATPase activity (unknown origin) assessed as inhibition of ATP hydrolysis by spectrophotometry | 2014 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
| Synthesis and evaluation of a novel class Hsp90 inhibitors containing 1-phenylpiperazine scaffold. |
AID1632347 | Inhibition of 6x-His tagged human recombinant full length Hsp90alpha ATPase preincubated for 0.5 hrs followed by ATP addition measured after 30 mins by HTRF assay | 2016 | Bioorganic & medicinal chemistry, 10-01, Volume: 24, Issue:19
| Structure-activity relationship of Garcinia xanthones analogues: Potent Hsp90 inhibitors with cytotoxicity and antiangiogenesis activity. |
AID350574 | Cytotoxicity against human CCRF-CEM cells after 72 hrs by celltiter-96 aqueous one solution assay | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Potent cytotoxic C-11 modified geldanamycin analogues. |
AID1212962 | Drug metabolism assessed as human recombinant CYP3A5-mediated (4E,6Z,8S,9S,10E,12S,13R,14S,16R)-19-(2-(dimethylamino)ethylamino)-13-hydroxy-8,14-dimethoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-azabicyclo[16.3.1]docosa-1(21),4,6,10,18-pentaen-9-yl carbam | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
| In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes. |
AID596788 | Displacement of [3H]-(R)-2-(5-chloro-2,4-dihydroxybenzoyl)-N-ethylisoindoline-1-carboxamide from human his(6)-tagged HSP90alpha after 30 mins by scintillation proximity assay | 2011 | Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
| Optimization of potent, selective, and orally bioavailable pyrrolodinopyrimidine-containing inhibitors of heat shock protein 90. Identification of development candidate 2-amino-4-{4-chloro-2-[2-(4-fluoro-1H-pyrazol-1-yl)ethoxy]-6-methylphenyl}-N-(2,2-difl |
AID394601 | Cytotoxicity against human SKOV3 cells after 72 hrs | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
| Potent non-benzoquinone ansamycin heat shock protein 90 inhibitors from genetic engineering of Streptomyces hygroscopicus. |
AID266546 | Inhibition of BODIPY-AG binding to human HSP90 | 2006 | Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15
| Design, synthesis, and biological evaluation of hydroquinone derivatives of 17-amino-17-demethoxygeldanamycin as potent, water-soluble inhibitors of Hsp90. |
AID266547 | Inhibition of BODIPY-AG binding to dog Grp94 | 2006 | Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15
| Design, synthesis, and biological evaluation of hydroquinone derivatives of 17-amino-17-demethoxygeldanamycin as potent, water-soluble inhibitors of Hsp90. |
AID394602 | Cytotoxicity against human HCT116 cells after 72 hrs | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
| Potent non-benzoquinone ansamycin heat shock protein 90 inhibitors from genetic engineering of Streptomyces hygroscopicus. |
AID1127396 | Inhibition of full-length HSP90 (unknown origin) expressed in Escherichia coli assessed as inhibition of ATPase activity after 3 hrs by spectrophotometric analysis | 2014 | European journal of medicinal chemistry, May-22, Volume: 79 | Identification and optimization of novel Hsp90 inhibitors with tetrahydropyrido[4,3-d]pyrimidines core through shape-based screening. |
AID344855 | Cytotoxicity against human MDA-MB-231 cells by MTT assay | 2008 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23
| Dihydroxylphenyl amides as inhibitors of the Hsp90 molecular chaperone. |
AID422512 | Inhibition of hypoxia-induced VEGF protein secretion in human Hep3B cells after 16 hrs by ELISA | 2009 | Journal of natural products, Jan, Volume: 72, Issue:1
| Hypoxia-inducible factor-1 inhibitory benzofurans and chalcone-derived diels-alder adducts from Morus species. |
AID1451199 | Cytotoxicity against mouse primary hepatocytes assessed as reduction in cell viability at 5 to 20 uM after 24 hrs by MTT assay | 2017 | Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
| Paralog Specificity Determines Subcellular Distribution, Action Mechanism, and Anticancer Activity of TRAP1 Inhibitors. |
AID1451185 | Inhibition of HSP90 in human HeLa cells assessed as induction of Akt degradation at 10 uM after 6 hrs by Western blot method | 2017 | Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
| Paralog Specificity Determines Subcellular Distribution, Action Mechanism, and Anticancer Activity of TRAP1 Inhibitors. |
AID1212937 | Drug metabolism in human liver microsomes assessed as (4E,6Z,8S,9S,10E,12S,13R,14S,16R)-19-(2-(dimethylamino)ethylamino)-13,14-dihydroxy-8-methoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-azabicyclo[16.3.1]docosa-1(21),4,6,10,18-pentaen-9-yl carbamate form | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
| In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes. |
AID1212970 | Drug metabolism assessed as human recombinant CYP2C9-mediated oxidative metabolism at 1 uM by liquid chromatography-tandem mass spectrometry | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
| In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes. |
AID715289 | Inhibition of Hsp90 in human COLO205 cells xenografted in mouse assessed as Raf1 degradation at 100 mg/kg administered QD for 2 days measured 8 hrs post-last dose | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
| Discovery of XL888: a novel tropane-derived small molecule inhibitor of HSP90. |
AID291914 | Inhibition of HIF1 activation in human AGS cells assessed as inhibition of hypoxia-induced luciferase expression after 16 hrs by reporter assay | 2007 | Journal of natural products, Jul, Volume: 70, Issue:7
| Abietane diterpenes from Salvia miltiorrhiza inhibit the activation of hypoxia-inducible factor-1. |
AID1212928 | Drug metabolism in human liver microsomes assessed as stability after 2 hrs relative to control by liquid chromatography-tandem mass spectrometry | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
| In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes. |
AID1212953 | Drug metabolism in human liver microsomes assessed as (4E,6Z,8S,9S,10E,12S,13R,14S,16R)-19-(2-(dimethylamino)-1-hydroxyethylamino)-13-hydroxy-8,14-dimethoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-azabicyclo[16.3.1]docosa-1(21),4,6,10,18-pentaen-9-yl carb | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
| In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes. |
AID255773 | Cytotoxicity against SKBr3 cells | 2005 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 15, Issue:22
| Structure-based design of 7-carbamate analogs of geldanamycin. |
AID350567 | Cytotoxicity against human SKBR3 cells after 72 hrs by celltiter-glo assay | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Potent cytotoxic C-11 modified geldanamycin analogues. |
AID1127398 | Antiproliferative activity against human SKBR3 cells after 48 hrs by MTT assay | 2014 | European journal of medicinal chemistry, May-22, Volume: 79 | Identification and optimization of novel Hsp90 inhibitors with tetrahydropyrido[4,3-d]pyrimidines core through shape-based screening. |
AID1212957 | Drug metabolism in human liver microsomes assessed as (4E,6Z,8S,9S,10E,12R,13R,14S,16R)-19-(2-(dimethylamino)-1-hydroxyethylamino)-13-hydroxy-12,16-bis(hydroxymethyl)-8,14-dimethoxy-4,10-dimethyl-3,20,22-trioxo-2-azabicyclo[16.3.1]docosa-1(21),4,6,10,18-p | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
| In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes. |
AID1212955 | Drug metabolism in human liver microsomes assessed as (4E,6Z,8S,9S,10E,12S,13R,14S,16R)-19-(2-(dimethylamino)ethylamino)-13,14-dihydroxy-8-methoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-azabicyclo[16.3.1]docosa-1(21),4,6,10,18-pentaen-9-yl carbamate form | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
| In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes. |
AID485530 | Inhibition of hypoxia-induced HIF1alpha protein accumulation in human Hep3B cells treated for 30 mins measured after 12 hrs by Western blot analysis | 2010 | Journal of natural products, Jun-25, Volume: 73, Issue:6
| An isoaurone and other constituents from Trichosanthes kirilowii seeds inhibit hypoxia-inducible factor-1 and nuclear factor-kappaB. |
AID1451184 | Inhibition of HSP90 in human HeLa cells assessed as induction of chk1 degradation at 10 uM after 6 hrs by Western blot method | 2017 | Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
| Paralog Specificity Determines Subcellular Distribution, Action Mechanism, and Anticancer Activity of TRAP1 Inhibitors. |
AID699452 | Inhibition of luciferase activity in human LN229-Lux cells at 2.5 to 10 uM incubated for 1 hr under normoxia followed by 24 hrs under hypoxia by reporter gene assay | 2012 | Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15
| Design and in vitro activities of N-alkyl-N-[(8-R-2,2-dimethyl-2H-chromen-6-yl)methyl]heteroarylsulfonamides, novel, small-molecule hypoxia inducible factor-1 pathway inhibitors and anticancer agents. |
AID266549 | Inhibition of human SKOV3 cell growth | 2006 | Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15
| Design, synthesis, and biological evaluation of hydroquinone derivatives of 17-amino-17-demethoxygeldanamycin as potent, water-soluble inhibitors of Hsp90. |
AID422513 | Inhibition of hypoxia-induced HIF1 activation in human Hep3B cells by pGL3-HRE-luciferase reporter gene assay | 2009 | Journal of natural products, Jan, Volume: 72, Issue:1
| Hypoxia-inducible factor-1 inhibitory benzofurans and chalcone-derived diels-alder adducts from Morus species. |
AID1451187 | Inhibition of HSP90 in human PC3 cells assessed as induction of chk1 degradation at 10 uM after 6 hrs by Western blot method | 2017 | Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
| Paralog Specificity Determines Subcellular Distribution, Action Mechanism, and Anticancer Activity of TRAP1 Inhibitors. |
AID596787 | Inhibition of human HSP90 in human NCI-H1299 cells assessed as Akt degradation after 24 hrs by luminex assay | 2011 | Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
| Optimization of potent, selective, and orally bioavailable pyrrolodinopyrimidine-containing inhibitors of heat shock protein 90. Identification of development candidate 2-amino-4-{4-chloro-2-[2-(4-fluoro-1H-pyrazol-1-yl)ethoxy]-6-methylphenyl}-N-(2,2-difl |
AID1212973 | Drug metabolism in human liver microsomes assessed as 1 uM CYP3A inhibitor ketoconazole-mediated inhibition of (4E,6Z,8S,9S,10E,12S,13R,14S,16R)-19-(2-(dimethylamino)ethylamino)-13-hydroxy-10-(hydroxymethyl)-8,14-dimethoxy-4,12,16-trimethyl-3,20,22-trioxo | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
| In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes. |
AID1127399 | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay | 2014 | European journal of medicinal chemistry, May-22, Volume: 79 | Identification and optimization of novel Hsp90 inhibitors with tetrahydropyrido[4,3-d]pyrimidines core through shape-based screening. |
AID506584 | Binding affinity to HSP90 in human NCI-H526 cells at 1 uM after 24 hrs by fluorescence polarization assay | 2007 | Nature chemical biology, Aug, Volume: 3, Issue:8
| Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer. |
AID350575 | Cytotoxicity against human paclitaxel-resistant CCRF-CEM cells after 72 hrs by celltiter-96 aqueous one solution assay | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Potent cytotoxic C-11 modified geldanamycin analogues. |
AID1212963 | Drug metabolism assessed as human recombinant CYP3A5-mediated (4E,6Z,8S,9S,10E,12R,13R,14S,16R)-19-(2-(dimethylamino)-1-hydroxyethylamino)-13-hydroxy-12,16-bis(hydroxymethyl)-8,14-dimethoxy-4,10-dimethyl-3,20,22-trioxo-2-azabicyclo[16.3.1]docosa-1(21),4,6 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
| In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes. |
AID350572 | Cytotoxicity against human SKOV3 cells after 72 hrs by celltiter-glo assay | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Potent cytotoxic C-11 modified geldanamycin analogues. |
AID1212954 | Drug metabolism in human liver microsomes assessed as (4E,6Z,8S,9S,10E,12S,13R,14S,16R)-19-(2-(dimethylamino)ethylamino)-13-hydroxy-10-(hydroxymethyl)-8,14-dimethoxy-4,12,16-trimethyl-3,20,22-trioxo-2-azabicyclo[16.3.1]docosa-1(21),4,6,10,18-pentaen-9-yl | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
| In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes. |
AID1451186 | Inhibition of HSP90 in human HeLa cells assessed as induction of HSP70 protein expression at 10 uM after 6 hrs by Western blot method | 2017 | Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
| Paralog Specificity Determines Subcellular Distribution, Action Mechanism, and Anticancer Activity of TRAP1 Inhibitors. |
AID1170900 | Reduction in oxygen consumption rate in human NCI-H1299 cells incubated for 12 hrs | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
| Discovery and optimization of 4,5-diarylisoxazoles as potent dual inhibitors of pyruvate dehydrogenase kinase and heat shock protein 90. |
AID1451189 | Inhibition of HSP90 in human PC3 cells assessed as induction of HSP70 protein expression at 10 uM after 6 hrs by Western blot method | 2017 | Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
| Paralog Specificity Determines Subcellular Distribution, Action Mechanism, and Anticancer Activity of TRAP1 Inhibitors. |
AID580563 | Antiviral activity against Hepatitis C virus genotype 1b Con1 infected in human HuH7 cells assessed as GAPDH RNA or 18S rRNA level after 3 days by qRT-PCR analysis | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
| Selection and characterization of hepatitis C virus replicons dually resistant to the polymerase and protease inhibitors HCV-796 and boceprevir (SCH 503034). |
AID350568 | Binding affinity to human recombinant HSP90 | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Potent cytotoxic C-11 modified geldanamycin analogues. |
AID266551 | Degradation of Her2 in SKOV3 cells | 2006 | Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15
| Design, synthesis, and biological evaluation of hydroquinone derivatives of 17-amino-17-demethoxygeldanamycin as potent, water-soluble inhibitors of Hsp90. |
AID1212976 | Drug metabolism in human liver microsomes assessed as 1 uM CYP3A inhibitor ketoconazole-mediated inhibition of (4E,6Z,8S,9S,10E,12S,13R,14S,16R)-19-(2-(dimethylamino)ethylamino)-8,13-dihydroxy-14-methoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-azabicyclo[ | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
| In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes. |
AID444594 | Displacement of [3H]pGA from His-tagged Hsp90 by scintillation proximity assay | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Dihydroxyphenylisoindoline amides as orally bioavailable inhibitors of the heat shock protein 90 (hsp90) molecular chaperone. |
AID394593 | Cytotoxicity against human SKBR3 cells after 72 hrs in presence of NQO1 inhibitor dicoumarol | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
| Potent non-benzoquinone ansamycin heat shock protein 90 inhibitors from genetic engineering of Streptomyces hygroscopicus. |
AID344853 | Inhibition of Hsp90 in human MDA-MB-231 cells assessed as Akt degradation | 2008 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23
| Dihydroxylphenyl amides as inhibitors of the Hsp90 molecular chaperone. |
AID1076812 | Antiproliferative activity against human MCF7 cells assessed as inhibition of cell viability after 48 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
| Synthesis and evaluation of a novel class Hsp90 inhibitors containing 1-phenylpiperazine scaffold. |
AID344854 | Inhibition of Hsp90 in human MDA-MB-231 cells assessed as her2 degradation | 2008 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23
| Dihydroxylphenyl amides as inhibitors of the Hsp90 molecular chaperone. |
AID499473 | Binding affinity to Hsp90 N-terminal ATPase domain by isothermal titration calorimetry assay | 2010 | Journal of medicinal chemistry, Aug-26, Volume: 53, Issue:16
| Discovery of (2,4-dihydroxy-5-isopropylphenyl)-[5-(4-methylpiperazin-1-ylmethyl)-1,3-dihydroisoindol-2-yl]methanone (AT13387), a novel inhibitor of the molecular chaperone Hsp90 by fragment based drug design. |
AID1885314 | Inhibition of KDM4B (unknown origin) measured by AlphaScreen assay | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
| Recent Advances with KDM4 Inhibitors and Potential Applications. |
AID1451188 | Inhibition of HSP90 in human PC3 cells assessed as induction of Akt degradation at 10 uM after 6 hrs by Western blot method | 2017 | Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
| Paralog Specificity Determines Subcellular Distribution, Action Mechanism, and Anticancer Activity of TRAP1 Inhibitors. |
AID291915 | Inhibition of HIF1 activation in human Hep3B cells assessed as inhibition of hypoxia-induced luciferase expression after 16 hrs by reporter assay | 2007 | Journal of natural products, Jul, Volume: 70, Issue:7
| Abietane diterpenes from Salvia miltiorrhiza inhibit the activation of hypoxia-inducible factor-1. |
AID465282 | Chemical stability assessed as half life | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Heat shock protein 90: inhibitors in clinical trials. |
AID394592 | Cytotoxicity against human MCF7 cells after 72 hrs in presence of NQO1 inhibitor dicoumarol | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
| Potent non-benzoquinone ansamycin heat shock protein 90 inhibitors from genetic engineering of Streptomyces hygroscopicus. |
AID327962 | Cytotoxicity against human AGS cells by MTT assay | 2008 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
| Hypoxia-inducible factor-1 and nuclear factor-kappaB inhibitory meroterpene analogues of bakuchiol, a constituent of the seeds of Psoralea corylifolia. |
AID1625299 | Cytotoxicity against HGF-induced erlotinib-resistant human PC9 cells assessed as inhibition of cell growth after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
| Development of Heat Shock Protein (Hsp90) Inhibitors To Combat Resistance to Tyrosine Kinase Inhibitors through Hsp90-Kinase Interactions. |
AID394599 | Binding affinity to human recombinant Hsp90alpha N-terminal domain by isothermal titration calorimetry | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
| Potent non-benzoquinone ansamycin heat shock protein 90 inhibitors from genetic engineering of Streptomyces hygroscopicus. |
AID1212977 | Drug metabolism in human liver microsomes assessed as 1 uM CYP3A inhibitor ketoconazole-mediated inhibition of (4E,6Z,8S,9S,10E,12R,13R,14S,16R)-19-(2-(dimethylamino)-1-hydroxyethylamino)-13-hydroxy-12,16-bis(hydroxymethyl)-8,14-dimethoxy-4,10-dimethyl-3, | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
| In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes. |
AID266552 | Upregulation of Hsp70 in SKBR3 cells | 2006 | Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15
| Design, synthesis, and biological evaluation of hydroquinone derivatives of 17-amino-17-demethoxygeldanamycin as potent, water-soluble inhibitors of Hsp90. |
AID596978 | Toxicity in human A2058 cells xenografted po dosed nu/nu athymic mouse | 2011 | Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
| Optimization of potent, selective, and orally bioavailable pyrrolodinopyrimidine-containing inhibitors of heat shock protein 90. Identification of development candidate 2-amino-4-{4-chloro-2-[2-(4-fluoro-1H-pyrazol-1-yl)ethoxy]-6-methylphenyl}-N-(2,2-difl |
AID1212971 | Drug metabolism assessed as human recombinant CYP2E1-mediated oxidative metabolism at 1 uM by liquid chromatography-tandem mass spectrometry | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
| In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes. |
AID580560 | Antiviral activity against Hepatitis C virus genotype 1b Con1 infected in human HuH7 cells assessed as GAPDH RNA or 18S rRNA level after 3 days selected with 40 nM HCV-796 and 800 nM boceprevir by qRT-PCR analysis relative to control | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
| Selection and characterization of hepatitis C virus replicons dually resistant to the polymerase and protease inhibitors HCV-796 and boceprevir (SCH 503034). |
AID1212936 | Drug metabolism in human liver microsomes assessed as (4E,6Z,8S,9S,10E,12S,13R,14S,16R)-19-(2-(dimethylamino)ethylamino)-13-hydroxy-10-(hydroxymethyl)-8,14-dimethoxy-4,12,16-trimethyl-3,20,22-trioxo-2-azabicyclo[16.3.1]docosa-1(21),4,6,10,18-pentaen-9-yl | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
| In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes. |
AID1451198 | Cytotoxicity against human corneal cells assessed as reduction in cell viability at 5 to 20 uM after 24 hrs by MTT assay | 2017 | Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
| Paralog Specificity Determines Subcellular Distribution, Action Mechanism, and Anticancer Activity of TRAP1 Inhibitors. |
AID580561 | Antiviral activity against Hepatitis C virus genotype 1b Con1 infected in human HuH7 cells assessed as GAPDH RNA or 18S rRNA level after 3 days selected with 40 nM HCV-796 and 800 nM boceprevir by qRT-PCR analysis | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
| Selection and characterization of hepatitis C virus replicons dually resistant to the polymerase and protease inhibitors HCV-796 and boceprevir (SCH 503034). |
AID1885315 | Inhibition of KDM4C (unknown origin) measured by AlphaScreen assay | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
| Recent Advances with KDM4 Inhibitors and Potential Applications. |
AID291916 | Viability of human AGS cells under normoxic conditions after 24 hrs by MTT assay | 2007 | Journal of natural products, Jul, Volume: 70, Issue:7
| Abietane diterpenes from Salvia miltiorrhiza inhibit the activation of hypoxia-inducible factor-1. |
AID350573 | Cytotoxicity against human A549 cells after 72 hrs by celltiter-glo assay | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Potent cytotoxic C-11 modified geldanamycin analogues. |
AID254267 | Binding affinity for human heat shock protein 90 in scintillation proximity assay | 2005 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 15, Issue:22
| Structure-based design of 7-carbamate analogs of geldanamycin. |
AID596793 | Intrinsic clearance in human liver microsomes at 1 uM after 45 mins by LC MS/MS analysis | 2011 | Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
| Optimization of potent, selective, and orally bioavailable pyrrolodinopyrimidine-containing inhibitors of heat shock protein 90. Identification of development candidate 2-amino-4-{4-chloro-2-[2-(4-fluoro-1H-pyrazol-1-yl)ethoxy]-6-methylphenyl}-N-(2,2-difl |
AID444595 | Inhibition of Hsp90 in human H1299 assessed as degradation of Hsp90 client protein Akt | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Dihydroxyphenylisoindoline amides as orally bioavailable inhibitors of the heat shock protein 90 (hsp90) molecular chaperone. |
AID422511 | Inhibition of hypoxia-induced HIF1alpha protein accumulation in human Hep3B cells treated for 30 mins measured after 12 hrs by Western blot analysis | 2009 | Journal of natural products, Jan, Volume: 72, Issue:1
| Hypoxia-inducible factor-1 inhibitory benzofurans and chalcone-derived diels-alder adducts from Morus species. |
AID1885317 | Inhibition of KDM6B (unknown origin) measured by AlphaScreen assay | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
| Recent Advances with KDM4 Inhibitors and Potential Applications. |
AID596980 | Antitumor activity against human A2058 cells xenografted in nu/nu athymic mouse model assessed as inhibition of tumor growth at 10 mg/kg, ip bid for 14 days | 2011 | Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
| Optimization of potent, selective, and orally bioavailable pyrrolodinopyrimidine-containing inhibitors of heat shock protein 90. Identification of development candidate 2-amino-4-{4-chloro-2-[2-(4-fluoro-1H-pyrazol-1-yl)ethoxy]-6-methylphenyl}-N-(2,2-difl |
AID327964 | Cytotoxicity against human HeLa cells by MTT assay | 2008 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
| Hypoxia-inducible factor-1 and nuclear factor-kappaB inhibitory meroterpene analogues of bakuchiol, a constituent of the seeds of Psoralea corylifolia. |
AID499474 | Cytotoxicity against human HCT116 cells by Alamar blue assay | 2010 | Journal of medicinal chemistry, Aug-26, Volume: 53, Issue:16
| Discovery of (2,4-dihydroxy-5-isopropylphenyl)-[5-(4-methylpiperazin-1-ylmethyl)-1,3-dihydroisoindol-2-yl]methanone (AT13387), a novel inhibitor of the molecular chaperone Hsp90 by fragment based drug design. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |