| Assay ID | Title | Year | Journal | Article |
|---|
| AID1816543 | Binding affinity to human HSP90-alpha assessed as change in heat capacity at 20 to 30 degC by isothermal titration calorimetry | 2021 | Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5
| Thermodynamic Dissection of Potency and Selectivity of Cytosolic Hsp90 Inhibitors. |
| AID1574366 | Toxicity in BALB/cA Jc1 nu/nu mouse xenografted with human NCI-H1975 cells assessed as body weight loss at 10 mg/kg, po daily for 14 days | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
| Discovery of 3-Ethyl-4-(3-isopropyl-4-(4-(1-methyl-1 H-pyrazol-4-yl)-1 H-imidazol-1-yl)-1 H-pyrazolo[3,4- b]pyridin-1-yl)benzamide (TAS-116) as a Potent, Selective, and Orally Available HSP90 Inhibitor. |
| AID1574365 | Antitumor activity against human NCI-H1975 cells xenografted in BALB/cA Jc1 nu/nu mouse assessed as tumor growth at 10 mg/kg, po daily for 14 days relative to control | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
| Discovery of 3-Ethyl-4-(3-isopropyl-4-(4-(1-methyl-1 H-pyrazol-4-yl)-1 H-imidazol-1-yl)-1 H-pyrazolo[3,4- b]pyridin-1-yl)benzamide (TAS-116) as a Potent, Selective, and Orally Available HSP90 Inhibitor. |
| AID1574364 | Inhibition of human CYP450 (unknown origin) | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
| Discovery of 3-Ethyl-4-(3-isopropyl-4-(4-(1-methyl-1 H-pyrazol-4-yl)-1 H-imidazol-1-yl)-1 H-pyrazolo[3,4- b]pyridin-1-yl)benzamide (TAS-116) as a Potent, Selective, and Orally Available HSP90 Inhibitor. |
| AID1574369 | Downregulation of phosphorylated RPS6 protein level in tumors of BALB/cA Jc1 nu/nu mouse xenografted with human NCI-H1975 cells at 10 mg/kg, po daily for 3 days measured at 12 hrs post last dose | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
| Discovery of 3-Ethyl-4-(3-isopropyl-4-(4-(1-methyl-1 H-pyrazol-4-yl)-1 H-imidazol-1-yl)-1 H-pyrazolo[3,4- b]pyridin-1-yl)benzamide (TAS-116) as a Potent, Selective, and Orally Available HSP90 Inhibitor. |
| AID1574363 | Cytotoxicity against human stromal cells | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
| Discovery of 3-Ethyl-4-(3-isopropyl-4-(4-(1-methyl-1 H-pyrazol-4-yl)-1 H-imidazol-1-yl)-1 H-pyrazolo[3,4- b]pyridin-1-yl)benzamide (TAS-116) as a Potent, Selective, and Orally Available HSP90 Inhibitor. |
| AID1574368 | Downregulation of phosphorylated AKT1/2/3 protein level in tumors of BALB/cA Jc1 nu/nu mouse xenografted with human NCI-H1975 cells at 10 mg/kg, po daily for 3 days measured at 12 hrs post last dose | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
| Discovery of 3-Ethyl-4-(3-isopropyl-4-(4-(1-methyl-1 H-pyrazol-4-yl)-1 H-imidazol-1-yl)-1 H-pyrazolo[3,4- b]pyridin-1-yl)benzamide (TAS-116) as a Potent, Selective, and Orally Available HSP90 Inhibitor. |
| AID1816534 | Binding affinity to human HSP90-beta by fluorescence polarization competitive binding assay | 2021 | Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5
| Thermodynamic Dissection of Potency and Selectivity of Cytosolic Hsp90 Inhibitors. |
| AID1574357 | Displacement of biotin-labeled geldanamycin from His-tagged HSP90alpha NTD (unknown origin) preincubated for 2 hrs followed by biotin-labeled geldanamycin addition and measured after 1 hr by AlphaScreen assay | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
| Discovery of 3-Ethyl-4-(3-isopropyl-4-(4-(1-methyl-1 H-pyrazol-4-yl)-1 H-imidazol-1-yl)-1 H-pyrazolo[3,4- b]pyridin-1-yl)benzamide (TAS-116) as a Potent, Selective, and Orally Available HSP90 Inhibitor. |
| AID1816536 | Binding affinity to TRAP1 (unknown origin) by fluorescence polarization competitive binding assay | 2021 | Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5
| Thermodynamic Dissection of Potency and Selectivity of Cytosolic Hsp90 Inhibitors. |
| AID1604474 | Inhibition of FITC-geldanamycin binding to N-terminal His-tagged recombinant human GRP94 expressed in Escherichia coli preincubated for 2 hrs followed by Geldanamycin-FITC addition and measured after 5 hrs by fluorescence polarization competitive binding | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Heat Shock Protein 90 Inhibitors: An Update on Achievements, Challenges, and Future Directions. |
| AID1574358 | Growth inhibition of human SK-BR-3 cells after 72 hrs by CellTiter-Glo assay | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
| Discovery of 3-Ethyl-4-(3-isopropyl-4-(4-(1-methyl-1 H-pyrazol-4-yl)-1 H-imidazol-1-yl)-1 H-pyrazolo[3,4- b]pyridin-1-yl)benzamide (TAS-116) as a Potent, Selective, and Orally Available HSP90 Inhibitor. |
| AID1816542 | Binding affinity to human HSP90-alpha N-terminal domain assessed as dissociation constant at 100 uM at 25 degC by isothermal titration calorimetry | 2021 | Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5
| Thermodynamic Dissection of Potency and Selectivity of Cytosolic Hsp90 Inhibitors. |
| AID1604472 | Inhibition of FITC-geldanamycin binding to recombinant human HSP90alpha expressed in Escherichia coli preincubated for 2 hrs followed by Geldanamycin-FITC addition and measured after 5 hrs by fluorescence polarization competitive binding assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Heat Shock Protein 90 Inhibitors: An Update on Achievements, Challenges, and Future Directions. |
| AID1604475 | Inhibition of FITC-geldanamycin binding to N-terminal His-tagged recombinant human TRAP1 (60 to 704 residues) expressed in Escherichia coli preincubated for 2 hrs followed by Geldanamycin-FITC addition and measured after 5 hrs by fluorescence polarization | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Heat Shock Protein 90 Inhibitors: An Update on Achievements, Challenges, and Future Directions. |
| AID1574370 | Downregulation of phosphorylated MAPK1/3 protein level in tumors of BALB/cA Jc1 nu/nu mouse xenografted with human NCI-H1975 cells at 10 mg/kg, po daily for 3 days measured at 12 hrs post last dose | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
| Discovery of 3-Ethyl-4-(3-isopropyl-4-(4-(1-methyl-1 H-pyrazol-4-yl)-1 H-imidazol-1-yl)-1 H-pyrazolo[3,4- b]pyridin-1-yl)benzamide (TAS-116) as a Potent, Selective, and Orally Available HSP90 Inhibitor. |
| AID1574367 | Downregulation of EGFR protein level in tumors of BALB/cA Jc1 nu/nu mouse xenografted with human NCI-H1975 cells at 10 mg/kg, po daily for 3 days measured at 12 hrs post last dose | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
| Discovery of 3-Ethyl-4-(3-isopropyl-4-(4-(1-methyl-1 H-pyrazol-4-yl)-1 H-imidazol-1-yl)-1 H-pyrazolo[3,4- b]pyridin-1-yl)benzamide (TAS-116) as a Potent, Selective, and Orally Available HSP90 Inhibitor. |
| AID1604473 | Inhibition of FITC-geldanamycin binding to recombinant human HSP90beta expressed in Escherichia coli preincubated for 2 hrs followed by Geldanamycin-FITC addition and measured after 5 hrs by fluorescence polarization competitive binding assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Heat Shock Protein 90 Inhibitors: An Update on Achievements, Challenges, and Future Directions. |
| AID1574362 | AUC (0 to 6 hrs) in Balb/cA mouse at 50 mg/kg, po by LC-MS/MS analysis | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
| Discovery of 3-Ethyl-4-(3-isopropyl-4-(4-(1-methyl-1 H-pyrazol-4-yl)-1 H-imidazol-1-yl)-1 H-pyrazolo[3,4- b]pyridin-1-yl)benzamide (TAS-116) as a Potent, Selective, and Orally Available HSP90 Inhibitor. |
| AID1816535 | Binding affinity to GRP94 (unknown origin) by fluorescence polarization competitive binding assay | 2021 | Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5
| Thermodynamic Dissection of Potency and Selectivity of Cytosolic Hsp90 Inhibitors. |
| AID1816533 | Inhibition of FITC-GDA binding to human HSP90-alpha incubated for 2 hrs followed by FITC-GDA addition and measured after 5 hrs by fluorescence polarization competitive binding assay | 2021 | Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5
| Thermodynamic Dissection of Potency and Selectivity of Cytosolic Hsp90 Inhibitors. |
| AID1574359 | 1-octanol/aqueous buffer partition coefficient, log D of the compound at pH 7.4 by HPLC method | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
| Discovery of 3-Ethyl-4-(3-isopropyl-4-(4-(1-methyl-1 H-pyrazol-4-yl)-1 H-imidazol-1-yl)-1 H-pyrazolo[3,4- b]pyridin-1-yl)benzamide (TAS-116) as a Potent, Selective, and Orally Available HSP90 Inhibitor. |
| AID1574361 | Solubility of the compound in pH 7.4 solution by chromatography method | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
| Discovery of 3-Ethyl-4-(3-isopropyl-4-(4-(1-methyl-1 H-pyrazol-4-yl)-1 H-imidazol-1-yl)-1 H-pyrazolo[3,4- b]pyridin-1-yl)benzamide (TAS-116) as a Potent, Selective, and Orally Available HSP90 Inhibitor. |
| 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. |
| AID1347412 | qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| 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. |
| AID1347414 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Secondary screen by immunofluorescence | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| 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. |
| AID1347415 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: tertiary screen by RT-qPCR | 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. |
| 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. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |