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Approved Drug Library

Catalog No. L1000
  Library Compound List   Excel SDF

Traditional de novo drug discovery and development involves an HTS campaign for de novo candidate hits and requires highly specialized screening facilities and compound libraries containing several million compounds. It is a time consuming and expensive process. As the regulation for drug safety and efficacy is increasingly getting complex, the cost of developing new drugs is keeping skyrocket. Drug repositioning, also known as old drugs for new uses, is an effective strategy to find new indications for existing drugs and has recently drawn attention and has led to several blockbuster drugs because of its high efficiency and low-cost. High-content screens, new biomarkers, noninvasive imaging techniques, and advanced in bioinformatics have created new opportunities for pursuing novel indications for approved compounds.

Approved drugs all have known and well-characterized bioactivities, safety and bioavailability – properties which could dramatically accelerate drug development and optimization. Hits from this set will provide a significant head start in any drug optimization program.

In addition, a growing number of compounds have been identified from this library that can functionally replace reprogramming transcription factors, enhance efficiency of iPSC generation and accelerate the reprogramming process by single use or a combination of several molecules.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Compound Libraries | TargetMol
Pack Size
1 mg
30 μL * 10 mM (in DMSO)
50 μL * 10 mM (in DMSO)
100 μL * 10 mM (in DMSO)
250 μL * 10 mM (in DMSO)
If the above compound libraries do not match your needs,
please contact our compound library specialist for a customized compound library at inquiry@targetmol.com
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Product Description

  • A unique collection of 2863 approved drugs for high throughput screening (HTS) and high content screening (HCS);
  • All compounds collected in this library are drugs approved by Food and Drug Administration (FDA), the European Medicine Agency (EMA), or National Medical Products Administration (NMPA), etc;
  • An effective tool for discovering new with old drugs and new drug target identification;
  • Covers various research areas, such as Cancer, Cardiovascular disease, GPCR/G protein, Neuroscience, Membrane Transporter/Ion Channel, Microbiology & Virology, Immunology/Inflammation, Tyrosine Kinase/Adaptors, etc.
  • More detailed compound information with structure, target, activity, IC50 value, and brief introduction;
  • Structurally diverse, medicinally active, and cell permeable;
  • NMR and HPLC validated to ensure high purity and quality;

Library Customization

Targetmol Compound Libraries can be highly customized! Learn More

Packaging And Storage

  • Powder or pre-dissolved DMSO solutions in 96/384 well plate with optional 2D barcode
  • Shipped with blue ice
Request Library Compound List (L1000)

Publications Cited TargetMol Libraries

1. Nature. 2020, 582: 289-293. 2. Nucleic Acids Research. 2021. 3. Nature Communications. 2023, 14(1): 7574. 4. Protein & Cell. 2021, 12(11): 877-888. 5. Nature Communications. 2021, 12(1): 1-12. 6. Cell Reports. 2022: 111117. 7. Cancer Letters. 2022: 216011. 8. Cell Death & Disease. 2023, 14(1): 11. 9. Cell & Bioscience. 2022, 12(1): 1-17.
10. Cell Reports. 2022, 39(1): 110643. 11. Pharmacological Research. 2021: 105860. 12. Acta Pharmacologica Sinica. 2023: 1-14. 13. Elife. 2021, 10: e63810. 14. Mbio. 2021, 12(1): e02754-20. 15. European Journal of Medicinal Chemistry. 2023: 115893. 16. Elife. 2021, 10: e67381. 17. Communications Biology. 2022, 5(1): 1-13. 18. Molecular Cancer Therapeutics. 2018 Feb;17(2):419-431. 19. Computational and Structural Biotechnology Journal. 2022. 20. iScience. 2023. 21. Frontiers in chemistry. 2022, 10. 22. Bioorganic Chemistry. 2022: 106191. 23. Frontiers in Cellular and Infection Microbiology. 2021: 1280. 24. Bioorganic Chemistry. 2020. 25. Scientific Reports. 2022, 12(1): 1-16. 26. Methods. 2022, 205: 247-262. 27. Cancer Science. 2021, 112(11): 4722. 28. Cognitive computation. 2021 Feb 2;1-13. 29. Antiviral Research. 2020, 174: 104701. 30. Toxicology and Applied Pharmacology. 2023: 116792. 31. Virology. 2022. 32. Investigational New Drugs. 2019 May 14: 1-10. 33. Acta Biochimica et Biophysica Sinica. 2021. 34. Structural Chemistry. 2022: 1-13. 35. Chinese Medical Journal. 2020, 133(9): 1051-1056. 36. Interdisciplinary Sciences, Computational Life Sciences. 2020, 12: 368-376. 37. Researchsquare. 2023. 38. BVS. 2020. 39. Journal of Southern Medical University. 2022, 42(4): 554-560. 40. Journal of Southern Medical University. 2021, 41(12): 1835-1842. 41. Strategies to Overcome Superbug Invasions. 2021: 269-287. 42. bioRxiv. 2020. 43. Research square. 2020. 44. Researchsquare. 2020. 45. Cell Stem Cell. 2022 Apr 29(4) 545–558. 46. Science Bulletin. 2022. 47. Science Translational Medicine. 2022, 14(656): eabn3231. 48. Science Advances. 2023, 9(9): eade3760. 49. Nature Biotechnology. 2021, 39(11): 1444-1452. 50. Nature Communications. 2022, 13(1): 1-15.. 51. Nature Communications. 2023, 14(1): 1020.. 52. Nature Communications. 2023, 14(1): 2756.. 53. Blood. 2021, 137(11): 1478-1490. 54. Advanced Science. 2020, 7(16): 2000925. 55. Angewandte Chemie. 2021. 56. Acta Pharmaceutica Sinica B. 2022. 57. Bone Research. 2023, 11(1): 54. 58. Pharmacology & Therapeutics. (2021): 107930. 59. Journal of Cell Biology. 2022, 221(5): e202112024. 60. Tan Q, Wu D, Lin Y, et al.Identifying eleven new ferroptosis inhibitors as neuroprotective agents from FDA-approved drugs.Bioorganic Chemistry.2024: 107261. 61. Duo L, Chen Y, Liu Q, et al.Discovery of Novel SOS1 Inhibitors Using Machine Learning.RSC Medicinal Chemistry.2024 62. Zou X, Yin J, Lei Q, et al.Bosutinib Laden Three-Dimensional Printed Zein Scaffolds Promote Osteogenesis.ACS Applied Polymer Materials.2024 63. Wang C, Ji Y, Huo X, et al.Discovery of Salifungin as a Repurposed Antibiotic against Methicillin-Resistant Staphylococcus aureus with Limited Resistance Development.ACS Infectious Diseases.2024
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Library Composition

Antibacterial (408)
Antibiotic (379)
Autophagy (341)
Endogenous Metabolite (257)
Apoptosis (252)
5-HT Receptor (167)
Adrenergic Receptor (162)
AChR (140)
COX (120)
Dopamine Receptor (112)
Histamine Receptor (109)
Parasite (93)
Antifungal (92)
HIV Protease (87)
Sodium Channel (82)
DNA/RNA Synthesis (81)
Calcium Channel (80)
Potassium Channel (75)
Topoisomerase (54)
Glucocorticoid Receptor (54)
Estrogen/progestogen Receptor (48)
Ferroptosis (47)
PDE (45)
Influenza Virus (44)
P450 (44)
SARS-CoV (43)
RAAS (40)
NF-κB (38)
Reactive Oxygen Species (38)
EGFR (37)
GABA Receptor (35)
Dehydrogenase (34)
VEGFR (33)
ribosome (32)
Mitophagy (32)
c-Kit (31)
HCV Protease (30)
Nucleoside Antimetabolite/Analog (30)
Serotonin Transporter (30)
PPAR (29)
Prostaglandin Receptor (28)
PDGFR (28)
AChE (28)
Estrogen Receptor/ERR (27)
HSV (26)
Reverse Transcriptase (26)
Norepinephrine (25)
Microtubule Associated (25)
Proteasome (24)
Progesterone Receptor (23)
Antifection (22)
HBV (22)
MAO (22)
Proton pump (22)
ATPase (21)
DNA Alkylator/Crosslinker (21)
iGluR (20)
Androgen Receptor (19)
Carbonic Anhydrase (19)
JAK (19)
FLT (18)
Virus Protease (18)
HDAC (18)
Thrombin (17)
Opioid Receptor (16)
TNF (16)
ROS (16)
FGFR (16)
Monoamine Oxidase (16)
Bcr-Abl (15)
Tyrosine Kinases (15)
Adenosine Receptor (15)
DPP-4 (15)
NMDAR (14)
TRP/TRPV Channel (14)
Phosphatase (14)
MRP (14)
Transferase (14)
c-Met/HGFR (14)
Src (14)
PKC (13)
Antifolate (13)
HIF/HIF Prolyl-Hydroxylase (13)
Drug Metabolite (12)
Retinoid Receptor (12)
Raf (12)
CDK (12)
SGLT (11)
HMG-CoA Reductase (11)
ALK (11)
Phospholipase (11)
IL Receptor (11)
GluR (11)
P-gp (11)
DNA gyrase (11)
Thyroid hormone receptor(THR) (11)
Amino Acids and Derivatives (11)
DHFR (10)
CaMK (10)
MMP (10)
c-RET (10)
PARP (10)
Lipoxygenase (9)
Antioxidant (9)
PI3K (9)
Factor Xa (9)
ABC (9)
AMPK (9)
Interleukin (9)
BTK (9)
Mitochondrial Metabolism (9)
DNA Alkylation (9)
mTOR (8)
CAT (8)
NO Synthase (8)
Antiviral (8)
P2Y Receptor (8)
Tyrosinase (8)
GPR (7)
CFTR (7)
STAT (7)
HER (7)
Beta Amyloid (7)
PKA (7)
Monoamine Transporter (7)
Chloride channel (7)
Nrf2 (7)
MEK (7)
Trk receptor (7)
TAM Receptor (7)
S1P Receptor (7)
Neurokinin receptor (7)
DNA Methyltransferase (7)
Glutathione Peroxidase (6)
LPL Receptor (6)
ERK (6)
Endothelin Receptor (6)
ROCK (6)
Vasopressin Receptor (6)
DNA (6)
Hedgehog/Smoothened (6)
Aromatase (6)
NADPH (6)
Serine Protease (6)
BCL (6)
P2X Receptor (6)
Histone Methyltransferase (6)
CaSR (5)
HIF (5)
Ras (5)
Akt (5)
Cysteine Protease (5)
Anti-infection (5)
Reductase (5)
TLR (5)
Xanthine Oxidase (5)
Fatty Acid Synthase (5)
Wnt/beta-catenin (5)
FXR (5)
Integrin (5)
GNRH Receptor (5)
Caspase (5)
Hydroxylase (5)
ROS Kinase (5)
Sigma receptor (5)
Guanylate cyclase (5)
PGE Synthase (4)
p38 MAPK (4)
Lipid (4)
NOS (4)
Ligand for E3 Ligase (4)
AhR (4)
Decarboxylase (4)
NOD (4)
GPCR19 (4)
Imidazoline Receptor (4)
IκB/IKK (4)
HSP (4)
cholecystokinin (4)
Neprilysin (4)
Oxytocin Receptor (4)
Aryl Hydrocarbon Receptor (4)
UGT (4)
Molecular Glues (4)
GSK-3 (4)
Leukotriene Receptor (4)
Melatonin Receptor (4)
Annexin A (4)
MT Receptor (4)
Serine/threonin kinase (4)
Smo (4)
Aminopeptidase (3)
Free radical scavengers (3)
Na-K-Cl cotransporter (3)
Glucosidase (3)
Histone Demethylase (3)
Adenosine deaminase (3)
Complement System (3)
Isocitrate Dehydrogenase (IDH) (3)
GST (3)
CCR (3)
TOPK (3)
Arginase (3)
Cannabinoid Receptor (3)
LTR (3)
PAK (3)
LDL (3)
TGF-beta/Smad (3)
Cell wall (3)
NOD-like Receptor (NLR) (3)
Gamma-secretase (3)
IGF-1R (3)
Glutathione reductase (3)
Syk (3)
Gap Junction Protein (3)
GlyT (2)
Melanocortin Receptor (2)
PKM (2)
Phosphorylase (2)
IRE1 (2)
Monocarboxylate transporter (2)
FAK (2)
Protease-activated Receptor (2)
CRM1 (2)
GHSR (2)
ROR (2)
Ligands for Target Protein for PROTAC (2)
Hexokinase (2)
PLK (2)
CGRP Receptor (2)
Rho (2)
Integrase (2)
c-Fms (2)
RSV (2)
CETP (2)
Beta-Secretase (2)
MAPK (2)
Acyltransferase (2)
OAT (2)
Thrombopoietin Receptor (2)
Aurora Kinase (2)
Ephrin Receptor (2)
GluCls (2)
IFNAR (2)
YAP (2)
CXCR (2)
Somatostatin (1)
S6 Kinase (1)
MTH1 (1)
Liver X Receptor (1)
PAFR (1)
CRISPR/Cas9 (1)
Taste receptor (1)
JNK (1)
Adiponectin receptor (1)
Mdm2 (1)
advanced glycation end products (1)
RAR/RXR  (1)
Bradykinin Receptor (1)
ATP Citrate Lyase (1)
Myosin (1)
DUB (1)
Lipase (1)
p53 (1)
PD-1/PD-L1 (1)
Telomerase (1)
CSF-1R (1)
IAP (1)
Immunology/Inflammation related (1)
FAAH (1)
Na+/Ca2+ Exchanger (1)
Aquaporin (1)
ACK (1)
Chk (1)
Pyroptosis (1)
Dynamin (1)
OX Receptor (1)
DNA-PK (1)
PAD (1)
Histone Acetyltransferase (1)
Angiotensin-converting Enzyme (ACE) (1)
Sirtuin (1)
Epoxide Hydrolase (1)
STING (1)
NADPH-oxidase (1)
Hydrogenase (1)
cAMP (1)
Indoleamine 2,3-Dioxygenase (IDO) (1)
Platelet aggregation (1)
Epigenetic Reader Domain (1)
VDA (1)
NPC1L1 (1)
Glucagon Receptor (1)
PROTAC Linker (1)
GRK (1)
BACE (1)

Library Information Sample

Empty 1000025-07-9 1000413-72-8 229005-80-5 1000787-75-6 946387-07-1 1000998-59-3 1175526-27-8 1001288-58-9 1001350-96-4 1001404-83-6 Empty
Vadadustat TAK875 TAK-779 Tegobuvir RN-1734 BMS-687453 AM211 FT011 BMS754807 AAI101
Empty 1001625-82-6 1001645-58-4 1001753-24-7 1001908-89-9 1002304-34-8 1002-84-2 100291-86-9 100299-08-9 10030-52-1 10040-45-6 Empty
RPW-24 SRT1720 hydrochloride INH6 SRT 2183 AMG208 Pentadecanoic acid Apiopaeonoside Pemirolast potassium L-Anserine nitrate salt Sodium Picosulfate
Empty 100427-26-7 1004316-88-4 10045-45-1 100462-37-1 1004990-28-6 100-51-6 1005-24-9 1005264-47-0 1005334-57-5 1005342-46-0 Empty
Lercanidipine Cobicistat 1-Ethyl-2-benzimidazolinone ROSIRIDIN PF-AKT400 Benzyl alcohol 1-Methylnicotinamide chloride MX69 CVT-10216 LCL161
Empty 1005491-05-3 100-55-0 1005504-62-0 1005883-72-6 100643-71-8 1007207-67-1 10075-50-0 1007647-73-5 100784-20-1 10083-24-6 Empty
Tirasemtiv Roniacol Rg3039 Z433927330 Desloratadine CH5132799 5-Bromoindole Smurf1-IN-A01 Halosulfuron-methyl Piceatannol
Empty 100872-83-1 100874-08-6 1009119-64-5 1009119-65-6 100929-71-3 1009298-09-2 1009298-59-2 100929-99-5 1009734-33-1 10097-84-4 Empty
ML346 SB 4 Daclatasvir Daclatasvir dihydrochloride NADPH (tetracyclohexanamine) AZD8055 Vistusertib PAβN dihydrochloride HZ1157 Rotundine
Empty 1009816-48-1 1009817-63-3 1009820-21-6 100986-85-4 101001-34-7 1010411-21-8 1010-60-2 1011244-68-0 1011301-27-1 1011529-10-4 Empty
Thiamet G B-AP15 Silmitasertib Levofloxacin Pamicogrel GSK369796 Dihydrochloride 2-Chloronaphthoquinone TFAP Tenovin3 Azvudine
Empty 101152-94-7 101155-02-6 1011557-82-6 1011-74-1 101-20-2 1012054-59-9 101-21-3 101-26-8 101303-98-4 1013101-36-4 Empty
Milnacipran hydrochloride BW-A78U Tenovin-6 DL-Normetanephrine hydrochloride Triclocarban CUDC101 Chlorpropham Mestinon Zacopride hydrochloride PF04691502
Empty 101-31-5 1013-69-0 1013750-77-0 1013753-99-5 10138-52-0 1013920-15-4 1013937-63-7 1014691-61-2 101477-54-7 101494-95-5 Empty
L-Hyoscyamine Noreugenin ML-030 BC-1382 Gadolinium chloride Vorolanib VTP-27999 TFA GSK0660 Lomerizine hydrochloride 8-CHLOROQUINAZOLIN-4(1H)-ONE
TargetMol