DiscoveryProbe™ FDA-approved Drug Library
Catalog No.
L1021
2320 approved drugs and API from pharmacopoeia
Featured Products
DiscoveryProbe™ FDA-approved drug library includes 2320 approved drugs and API from pharmacopoeia for high throughput screening (HTS) and high content screening (HCS). All drugs were from approved institutions such as FDA, EMA, HMA, CFDA, PMDA, or pharmacopoeia such as USP, BP, EP, JP, Ph.Int, etc. The bioactivity and safety of these drugs were confirmed in vitro or in vivo. So, it can be used to find new targets for old drugs.
- 1. Yan Guo, Boyuan Liu, et al. "2′-O-Galloylhyperin Prevents Tissue Remodeling in Thyroid Eye Disease: Prospects as a Thyrotropin Receptor Antagonist." The Journal of Clinical Endocrinology & Metabolism 02 December 2024
- 2. Fraser Hughes, Alex Cookson, et al. "HTS Library Plate Rejuvenation Using a DMSO-Rich Atmosphere." SLAS Technol. 2024 Oct 11:100204 PMID: 39396728
- 3. Sunniva Sigurdardóttir, Suélen Fernandes Silva, et al. "An automated positive selection screen in yeast provides support for boron-containing compounds as inhibitors of SARS-CoV-2 main protease." Microbiol Spectr. 2024 Aug 20:e0124924. PMID: 39162260
- 4. Haiyan Dong, Chuangyu Wen, et al. "Nilotinib boosts the efficacy of anti-PDL1 therapy in colorectal cancer by restoring the expression of MHC-I." J Transl Med. 2024 Aug 14;22(1):769 PMID: 39143573
- 5. Canrong Li, Yuguo Yi, et al. "TORSEL, a 4EBP1-based mTORC1 live-cell sensor, reveals nutrient-sensing targeting by histone deacetylase inhibitors." Cell Biosci. 2024 Jun 1;14(1):68. PMID: 38824577
- 6. Yubao Fan, Shanshan Huang, et al. "The adipose-neural axis is involved in epicardial adipose tissue-related cardiac arrhythmias." Cell Rep Med. 2024 May 21;5(5):101559 PMID: 38744275
- 7. Yuting Pan, Ying Xuan, et al. "Time-dependent proteomics and drug response in expanding cancer cells." Pharmacol Res. 2024 Jun:204:107208. PMID: 38729587
- 8. Xiaojuan Zhang, Quanbin Xu, et al. "Chandipura Viral Glycoprotein (CNV-G) Promotes Gectosome Generation and Enables Delivery of Intracellular Therapeutics." Mol Ther. 2024 May 3:S1525-0016(24)00298-3. PMID: 38702887
- 9. Xiaoyu Chen, Huilin Zhao, et al. "Two natural compounds as potential inhibitors against the Helicobacter pylori and Acinetobacter baumannii IspD enzymes." Int J Antimicrob Agents. 2024 May;63(5):107160. PMID: 38537721
- 10. Susmita Khamrui, Tetyana Dodatko, et al. "Characterization, structure and inhibition of the human succinyl-CoA:glutarate-CoA transferase, a genetic modifier of glutaric aciduria type 1." bioRxiv. 2024 Feb 7:2024.02.07.578422. PMID: 38370847
- 11. Lanqin Wu, et al. "Saracatinib inhibits necroptosis and ameliorates psoriatic inflammation by targeting MLKL." Cell Death Dis. 2024 Feb 8;15(2):122. PMID: 38331847
- 12. Soo Young Lee, et al. "5-aminosalicylic acid suppresses osteoarthritis through the OSCAR-PPARγ axis." Nat Commun. 2024 Feb 3;15(1):1024. PMID: 38310093
- 13. Siyi He, Luis Delgadillo Silva, et al. "A high-throughput screening approach to discover potential colorectal cancer chemotherapeutics: Repurposing drugs to disrupt 14-3-3 protein-BAD interactions." bioRxiv [Preprint]. 2023 Dec 15:2023.12.14.571727. PMID: 38168191
- 14. Haya Albanna, Alesia Gjoni, et al. "Activation of Adrenoceptor Alpha-2 (ADRA2A) Promotes Chemosensitization to Carboplatin in Ovarian Cancer Cell Lines." Curr Issues Mol Biol. 2023 Nov 28;45(12):9566-9578. PMID: 38132444
- 15. Annika Ullrich, Johannes Schneider, et al. "Discovery of a functionally selective serotonin 5-HT1A receptor agonist for the treatment of pain." bioRxiv. September 14, 2023.
- 16. Min Zheng, Cheng Yu, et al. "ChaC1-based drug screenings identify a synergistic lethal effect of auranofin and proteasome inhibitors in hepatocellular carcinoma cells.." Research Square. 10 Aug, 2023.
- 17. Somaya A Abdel-Rahman, Katarzyna Świderek, et al. "First-in-class Small Molecule Inhibitors of ICOS/ICOSL interaction as a novel class of immunomodulators." RSC Med Chem. 2023 Aug 1;14(9):1767-1777. PMID: 37731692
- 18. Yan Guo, Hongtao Liu, et al. "Novel metallo‐β‐lactamases inhibitors restore the susceptibility of carbapenems to New Delhi metallo‐lactamase‐1 (NDM‐1)‐harbouring bacteria." Br J Pharmacol. 2024 Jan;181(1):54-69 PMID: 37539785
- 19. Xiaodan Zhu, Shasha He, et al. "Protective Effect and Mechanism of Autophagy in Endothelial Cell Injury Induced by Hyperoxia." Am J Perinatol. 2024 May;41(S 01):e2365-e2375. PMID: 37516120
- 20. Jie Zheng, Junjie Yang, et al. "CIL-ExPMRM: An Ultrasensitive Chemical Isotope Labeling Assisted Pseudo-MRM Platform to Accelerate Exposomic Suspect Screening." Environ Sci Technol. 2023 Aug 1;57(30):10962-10973. PMID: 37469223
- 21. De-Ping Wang, Fang-Ying Jiang, et al. "Crystal structure of RNA helicase from Saint Louis encephalitis virus and discovery of its inhibitors." Genes Dis. 2022 Jul 31;10(2):389-392. PMID: 37223502
- 22. Somaya A Abdel-Rahman, Ashfaq Ur Rehman, et al. "Discovery of First-in-Class Small Molecule Inhibitors of Lymphocyte Activation Gene 3 (LAG-3)." ACS Med Chem Lett. 2023 Apr 11;14(5):629-635. PMID: 37197466
- 23. Wei Yang, Xiongfei Sun, et al. "TLR8 agonist Motolimod-induced inflammatory death for treatment of acute myeloid leukemia." Biomed Pharmacother. 2023 Jul:163:114759. PMID: 37105077
- 24. Jingjing Zhang, Yingpei Jiang, et al. "Development of FRET and Stress Granule Dual-Based System to Screen for Viral 3C Protease Inhibitors." Molecules. 2023 Mar 28;28(7):3020. PMID: 37049786
- 25. Fabrizio Fierro, Lior Peri, et al. "Inhibiting a promiscuous GPCR: iterative discovery of bitter taste receptor ligands." Cell Mol Life Sci. 2023 Apr 3;80(4):114. PMID: 37012410
- 26. Zhiyu Song, Chenglong Zhao, et al. "Carbenoxolone disodium suppresses the migration of gastric cancer by targeting HDAC6." Future Med Chem. 2023 Feb;15(4):333-344. PMID: 36946221
- 27. Liuqing Chen, Meiting Chen, et al. "Ratiometric NAD+ Sensors Reveal Subcellular NAD+ Modulators." ACS Sens. 2023 Apr 28;8(4):1518-1528. PMID: 36931900
- 28. Jing Han, Shuiqing Hu, et al. "Discovery of podofilox as a potent cGAMP–STING signaling enhancer with antitumor activity." Cancer Immunol Res. 2023 May 3;11(5):583-599. PMID: 36921097
- 29. Beatrice Alexander-Howden, Li Zhang, et al. "A screen for MeCP2-TBL1 interaction inhibitors using a luminescence-based assay." Sci Rep. 2023 Mar 8;13(1):3868. PMID: 36890145
- 30. Eirini D Tseligka, Stéphanie Conzelmann, et al. "Identification of selective hepatitis delta virus ribozyme inhibitors by high-throughput screening of small molecule libraries." JHEP Rep.2022 Dec 17;5(3):100652. PMID: 36704052
- 31. Dandan Jiang, Peizhi Ma. "Canagliflozin, characterized as a HDAC6 inhibitor, inhibits gastric cancer metastasis." Front Oncol. 2022 Nov 15;12:1057455. PMID: 36457493
- 32. Elizabeth R Sharlow, Danielle C Llaneza, et al. "High content screening miniaturization and single cell imaging of mature human feeder layer-free iPSC-derived neurons." SLAS Discov. 2022 Oct 21;S2472-5552(22)13703-2. PMID: 36273809
- 33. Xianglian Zhou, Yuting Pan, et al. "Tideglusib Inhibits Pif1 Helicase of Bacteroides sp. via an Irreversible and Cys-380-Dependent Mechanism." ACS Omega. 2022 Aug 25;7(35):31289-31298. PMID: 36092604
- 34. Jhin Jieh Lim, Lissa Hooi, et al. "Rational drug combination design in patient-derived avatars reveals effective inhibition of hepatocellular carcinoma with proteasome and CDK inhibitors." J Exp Clin Cancer Res. 2022 Aug 15;41(1):249. PMID: 35971164
- 35. Youjie Yin, Peng Ma, et al. "The CRTC-CREB axis functions as a transcriptional sensor to protect against proteotoxic stress in Drosophila." Cell Death Dis. 2022 Aug 6;13(8):688 PMID: 35933423
- 36. Babak Andi, Desigan Kumaran, et al. "Hepatitis C virus NS3/4A inhibitors and other drug‑like compounds as covalent binders of SARS‑CoV‑2 main protease." Sci Rep. 2022 Jul 16;12(1):12197 PMID: 35842458
- 37. Can Cui, Yuting Pan, et al. "Eltrombopag binds SDC4 directly and enhances MAPK signaling and macropinocytosis in cancer cells." American Journal of Cancer Research, 15 Jun 2022, 12(6):2697-2710. PMID: 35812066
- 38. Yubao Fan, Shanshan Huang, et al. "The adipose-neural axis is critically involved in cardiac arrhythmias." bioRxiv. June 13, 2022.
- 39. David Pladevall-Morera, María Castejón-Griñán, et al. "ATRX-Deficient High-Grade Glioma Cells Exhibit Increased Sensitivity to RTK and PDGFR Inhibitors." Cancers (Basel) 2022 Mar 31;14(7):1790. PMID: 35406561
- 40. Jian Guo, Sam Shen, et al. "JPA: Joint Metabolic Feature Extraction Increases the Depth of Chemical Coverage for LC-MS-Based Metabolomics and Exposomics." Metabolites. 2022 Feb 26;12(3):212. PMID: 35323655
- 41. Shiu-Wan Chan, Talha Shafi, et al. "Kite-Shaped Molecules Block SARS-CoV-2 Cell Entry at a Post-Attachment Step." Viruses.2021 Nov 19;13(11):2306. PMID: 34835112
- 42. Narmeen S Rashid, Nicole S Hairr, et al. "Identification of nuclear export inhibitor-based combination therapies in preclinical models of triple-negative breast cancer." Transl Oncol.2021 Dec;14(12):101235. PMID: 34628286
- 43. Yunxia Xu, Ke Chen, et al. "Repurposing clinically approved drugs for COVID-19 treatment targeting SARS-CoV-2 papain-like protease." Int J Biol Macromol2021 Oct 1;188:137-146. PMID: 34364941
- 44. Jing Nan, Shaoran Zhang, et al. "Discovery of Novel GMPS Inhibitors of Candidatus Liberibacter Asiaticus by Structure Based Design and Enzyme Kinetic." Biology (Basel).20212021 Jun 28;10(7):594. PMID: 34203217
- 45. Yan Ling Ng, Cyrill Kafi Salim, et al. "Drug repurposing for COVID-19: Approaches, challenges and promising candidates." Pharmacol Ther.2021 Dec;228:107930. PMID: 34174275
- 46. Xianglian Zhou, Yuting Pan, et al. "Tanshinones induce tumor cell apoptosis via directly targeting FHIT." Sci Rep. 2021 Jun 9;11(1):12217. PMID: 34108553
- 47. Alon Ben David, Eran Diamant, et al. "Identification of SARS-CoV-2 Receptor Binding Inhibitors by In Vitro Screening of Drug Libraries." Molecules.20202021 May 27;26(11):3213. PMID: 34072087
- 48. James M. Havrilla, Cong Liu, et al. "PhenCards: a data resource linking human phenotype information to biomedical knowledge." Genome Med. 2021 May 25;13(1):91. PMID: 34034817
- 49. Peizhi Ma, Gang Jia, et al. "Monobenzone, a Novel and Potent KDM1A Inhibitor, Suppresses Migration of Gastric Cancer Cells." Front Pharmacol. 2021 Apr 15;12:640949. PMID: 33935733
- 50. Lesley-Anne Pearson, Charlotte J Green, et al. "Development of a High-Throughput Screening Assay to Identify Inhibitors of the SARS-CoV-2 Guanine-N7-Methyltransferase Using RapidFire Mass Spectrometry." SLAS Discov.2021 Jul;26(6):749-756. PMID: 33724070
- 51. Adam Pickard, Ben C Calverley, et al. "Discovery of re-purposed drugs that slow SARS-CoV-2 replication in human cells." bioRxiv. 2021 Mar 10;2021.01.31.428851. PMID: 33564760
- 52. Gur D, Chitlaru T, Mamroud E, et al. "Screening of an FDA-Approved Library for Novel Drugs against Y. pestis." Antibiotics (Basel). 2021 Jan 3;10(1):40. PMID: 33401634
- 53. Moore JA, Meakin M, et al. "Effects of Caspofungin, Tolcapone, and Other FDA-Approved Medications on MRSA Susceptibility to Vancomycin." J Glob Antimicrob Resist. 2020;S2213-7165(20)30078-3. PMID: 32247076
- 54. Turner TH, Alzubi MA, et al. "Identification of synergistic drug combinations using breast cancer patient-derived xenografts." Sci Rep. 2020 Jan 30;10(1):1493. PMID: 32001757
- 55. Yang JJ, Han Y, et al. "Streamlined MRM method transfer between instruments assisted with HRMS matching and retention-time prediction." Anal Chim Acta. 2020;1100:88–96. PMID: 31987156
Catalog No. | Product Name | Summary | Targets | CAS Number | Smiles |
A3298 | Cetirizine | Antihistamine | Neuroscience|Histamine Receptor | 83881-51-0 | C1CN(CCN1CCOCC(=O)O)C(C2=CC=CC=C2)C3=CC=C(C=C3)Cl |
A3789 | Salmeterol xinafoate | β2-adrenergic receptor agonist | GPCR/G protein|Adrenergic Receptor | 94749-08-3 | C1=CC=C(C=C1)CCCCOCCCCCCNCC(C2=CC(=C(C=C2)O)CO)O.C1=CC=C2C(=C1)C=CC(=C2O)C(=O)O |
A4363 | Fluvastatin Sodium | HMG-CoA reductase inhibitor | Metabolism|HMG-CoA Reductase | 93957-55-2 | CC(C)N1C2=CC=CC=C2C(=C1C=CC(CC(CC(=O)[O-])O)O)C3=CC=C(C=C3)F.[Na+] |
A4370 | Moclobemide (Ro 111163) | Reversible inhibitor of MAO-A | Metabolism|MAO | 71320-77-9 | C1COCCN1CCNC(=O)C2=CC=C(C=C2)Cl |
A8252 | Nintedanib(BIBF 1120) | VEGFR/PDGFR/FGFR inhibitor | Tyrosine Kinase/Adaptors|PDGFR | 928326-83-4 | CN1CCN(CC1)CC(=O)N(C)C2=CC=C(C=C2)NC(=C3C4=C(C=C(C=C4)C(=O)OC)NC3=O)C5=CC=CC=C5 |
B1792 | Montelukast Sodium | Leukotriene receptor antagonist | GPCR/G protein|CysLT1 receptor | 151767-02-1 | CC(C)(C1=CC=CC=C1CCC(C2=CC=CC(=C2)C=CC3=NC4=C(C=CC(=C4)Cl)C=C3)SCC5(CC5)CC(=O)[O-])O.[Na+] |
N1674 | Piperine | MAPK inhibitor | Natural Products | 94-62-2 | C1CCN(CC1)C(=O)C=CC=CC2=CC3=C(C=C2)OCO3 |
N1707 | Coumarin | Precursor in chemical reaction | Natural Products | 91-64-5 | C1=CC=C2C(=C1)C=CC(=O)O2 |
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Form | Pre-dissolved DMSO solutions | Stability | Solution: -20°C for 12 months, -80°C for 24 months |
Packaging | 96-well Microplate format with peelable foil seal; 96-well DeepWell format with peelable foil seal and EVA cap (100 μL/well, 10 mM DMSO); 96-well rack with Matrix 2D Barcoded ScrewTop Storage tubes (250 μL or 100 μL/well, 10 mM DMSO). |
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Shipping Condition | Evaluation sample solution: ship with blue ice All other available size: ship with RT, or blue ice upon request |
1. Barrows NJ, Campos RK, Powell ST, et al. A Screen of FDA-Approved Drugs for Inhibitors of Zika Virus Infection. Cell Host Microbe. 2016 Jul 27. pii: S1931-3128(16)30303-1.
Abstract
We interrogated a FDA-approved chemicals library for their ability to block infection of human HuH-7 cells by a newly isolated ZIKV strain (ZIKV MEX_I_7). In our in vitro screening assay, more than 20 out of 774 tested compounds reduced ZIKV infection. Then these compounds were further validated for inhibition of ZIKV infection in human neural, cervical and placental stem cell lines, as well as primary human amnion cells. We found that others that had no previously known antiviral activity (e.g., daptomycin) and anti-flaviviral drugs (e.g., bortezomib and mycophenolic acid) were identified as inhibitors of ZIKV infection. There were several drugs that reduced ZIKV infection across multiple cell types, which could be tested in clinical studies of ZIKV infection and provided small molecules to study ZIKV pathogenesis.
Abstract
We interrogated a FDA-approved chemicals library for their ability to block infection of human HuH-7 cells by a newly isolated ZIKV strain (ZIKV MEX_I_7). In our in vitro screening assay, more than 20 out of 774 tested compounds reduced ZIKV infection. Then these compounds were further validated for inhibition of ZIKV infection in human neural, cervical and placental stem cell lines, as well as primary human amnion cells. We found that others that had no previously known antiviral activity (e.g., daptomycin) and anti-flaviviral drugs (e.g., bortezomib and mycophenolic acid) were identified as inhibitors of ZIKV infection. There were several drugs that reduced ZIKV infection across multiple cell types, which could be tested in clinical studies of ZIKV infection and provided small molecules to study ZIKV pathogenesis.
2. Stavrovskaya IG, Narayanan MV, Zhang W, et al. Clinically approved heterocyclics act on a mitochondrial target and reduce stroke-induced pathology. J Exp Med. 2004 Jul 19;200(2):211-22.
Abstract
Mitochondria are a major checkpoint in several pathways leading to neuronal cell death and the mitochondrial permeability transition (mPT) may be critical in stroke-related injury. In order to prove this hypothesis, 1,040 FDA-approved drugs and other bioactive compounds were tested as potential mPT inhibitors. We found that 28 structurally related drugs, including tricyclic antipsychotics and antidepressants, capable of delaying the mPT. Clinically achievable doses of promethazine inhibited mPT and were protective in both in vitro and mouse models of stroke. Also, promethazine protected primary neuronal cultures subjected to oxygen-glucose deprivation and reduced neurological impairment and infarct size in mice subjected to middle cerebral artery occlusion/reperfusion. These results provided a class of safe, tolerable drugs for stroke and neurodegeneration and also provided new tools for understanding mitochondrial roles in neuronal cell death.
Abstract
Mitochondria are a major checkpoint in several pathways leading to neuronal cell death and the mitochondrial permeability transition (mPT) may be critical in stroke-related injury. In order to prove this hypothesis, 1,040 FDA-approved drugs and other bioactive compounds were tested as potential mPT inhibitors. We found that 28 structurally related drugs, including tricyclic antipsychotics and antidepressants, capable of delaying the mPT. Clinically achievable doses of promethazine inhibited mPT and were protective in both in vitro and mouse models of stroke. Also, promethazine protected primary neuronal cultures subjected to oxygen-glucose deprivation and reduced neurological impairment and infarct size in mice subjected to middle cerebral artery occlusion/reperfusion. These results provided a class of safe, tolerable drugs for stroke and neurodegeneration and also provided new tools for understanding mitochondrial roles in neuronal cell death.