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TargetMol | Compound Library

Approved Drug Library

Catalog No. L1000

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.

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Catalog No. L1000

Approved Drug Library

sizeIn stock

  • 1 mg
  • 30 μL x 10 mM (in DMSO)
  • 50 μL x 10 mM (in DMSO)
  • 100 μL x 10 mM (in DMSO)
  • 250 μL x 10 mM (in DMSO)
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Product Description Product Description

  • A unique collection of 2860 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;

Advantages Introduction Advantages Introduction

High-Standard Entry Criteria

TargetMol’s Approved Drug Library is curated with stringent entry criteria to ensure that every compound in the collection is structurally well-defined and of high purity. Multiple analytical techniques—such as NMR, HPLC, and LCMS—are employed to verify compound integrity. Through a rigorous multi-step screening process, we exclude compounds with ambiguous structures (e.g., mixtures and polymers) and non-active agents such as sunscreens, contrast agents, and inorganic compounds. This helps reduce ineffective screening efforts and unnecessary resource consumption. This library includes only FDA-approved small molecule drugs. For compounds approved by other regulatory agencies (such as PMDA, EMA, and NMPA), please refer to our L4200 FDA-Approved Drug Library and L1020 EMA Approved Drug Library.

 Approved Drug Library
Drug Approval Authorities

Significant Structural Diversity

TargetMol’s Approved Drug Library exhibits remarkable structural diversity, offering substantial advantages in drug discovery. Based on MACCS fingerprint analysis, the library can be categorized into 2,205 classes, effectively covering a broad chemical space. The library includes a wide variety of compounds, ranging from simple to highly complex chemical structures. This diversity provides a wealth of possibilities for identifying lead compounds with high affinity and specificity for target proteins, significantly advancing drug innovation.

 Approved Drug Library
Library Diversity Analysis

Diverse Compound Selection

TargetMol’s Approved Drug Library is characterized by not only a high degree of chemical diversity but also broad biological representativeness. The compounds included in this library target a wide range of key signaling pathways, such as kinases, G protein-coupled receptors (GPCRs), ion channels, and epigenetic regulators. It comprehensively covers multiple therapeutic areas, including cancer, immune disorders, neurological diseases, metabolic disorders, and infectious diseases. Approximately 20% of the approved drugs in the library are natural products, comprising monomeric compounds isolated from plants, animals, and microorganisms. This library serves as an ideal resource for drug repurposing, lead optimization, and the development of new therapeutic strategies. It supports the full spectrum from basic research to translational medicine, accelerating the efficient development of innovative drugs.

 Approved Drug Library  Approved Drug Library
Pathways And Disease Types Composition
 Approved Drug Library
Types of Approved Natural Products

Regular Updates to Compound Libraries

TargetMol ensures compound libraries stay at the forefront of science by regularly updating our database to include the latest approved and marketed drugs.

Flexible Packaging Options

TargetMol provides a variety of standard packaging sizes (such as 30 μL, 50 μL, 100 μL, 250 μL, and 1 mg), and offer customized packaging solutions tailored to specific needs.

Personalized Custom Services

TargetMol offers fully customized screening services, including the design and synthesis of compound libraries. Our highly flexible service is designed to efficiently meet the unique needs of scientists and researchers.

Packaging And Storage Packaging And Storage

  • Powder or pre-dissolved DMSO solutions in 96/384 well plate with optional 2D barcode
  • Shipped with blue ice
  • This compound library is provided at a concentration of 10 mM in DMSO. A small number of compounds may be provided in different solvents or concentrations due to solubility or stability requirements. Please refer to the specific product information for details.

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Antibacterial
Antibiotic
Apoptosis
Autophagy
Endogenous Metabolite
Adrenergic Receptor
5-HT Receptor
AChR
Parasite
Dopamine Receptor
COX
Histamine Receptor
Potassium Channel
Antifungal
Sodium Channel
DNA/RNA Synthesis
HIV Protease
Calcium Channel
Glucocorticoid Receptor
Cytochromes P450
SARS-CoV
Topoisomerase
Estrogen/progestogen Receptor
Reactive Oxygen Species
NF-κB
Virus Protease
Influenza Virus
Ferroptosis
PDE
RAAS
VEGFR
EGFR
Estrogen Receptor/ERR
Serotonin Transporter
GABA Receptor
Dehydrogenase
Mitophagy
HCV Protease
c-Kit
Cholinesterase (ChE)
Microtubule Associated
PPAR
Nucleoside Antimetabolite/Analog
PDGFR
HSV
Prostaglandin Receptor
ribosome
iGluR
HBV
Norepinephrine
Interleukin
Reverse Transcriptase
Proteasome
Progesterone Receptor
TNF
ATPase
MAO
Angiotensin-converting Enzyme (ACE)
FGFR
Proton pump
Antifection
JAK
HDAC
Drug Metabolite
Monoamine Oxidase
Carbonic Anhydrase
MMP
Androgen Receptor
c-Met/HGFR
DNA Alkylator/Crosslinker
TRP/TRPV Channel
Bcr-Abl
Opioid Receptor
DPP-4
FLT
HIF/HIF Prolyl-Hydroxylase
Src
p38 MAPK
Caspase
ROS
Akt
Bcl-2 Family
Anti-infection
PI3K
Adenosine Receptor
MRP
Tyrosine Kinases
CDK
Mitochondrial Metabolism
HMG-CoA Reductase
Thrombin
Transferase
AMPK
Phosphatase
ERK
Raf
NMDAR
P-gp
ALK
STAT
NO Synthase
Thyroid hormone receptor(THR)
Amino Acids and Derivatives
PARP
PKC
IL Receptor
HSP
Nrf2
Antifolate
Lipoxygenase
SGLT
Retinoid Receptor
Phospholipase
c-RET
DHFR
Serine Protease
mTOR
MEK
Ras
ROS Kinase
ADC Cytotoxin
Antioxidant
JNK
Factor Xa
DNA Alkylation
Endothelin Receptor
GluR
Antiviral
Beta Amyloid
P2Y Receptor
ROCK
DNA gyrase
ABC Transporter
Monoamine Transporter
CaMK
TLR
IκB/IKK
HIF
Sigma receptor
Tyrosinase
CFTR
S1P Receptor
GPCR
Histone Methyltransferase
LPL Receptor
NADPH
Glutathione Peroxidase
PKA
Leukotriene Receptor
FXR
Trk receptor
MDM-2/p53
DNA Methyltransferase
HER
Chloride channel
Integrin
Reductase
GSK-3
GNRH Receptor
Wnt/beta-catenin
Cysteine Protease
P2X Receptor
Glucosidase
Guanylate cyclase
Isocitrate Dehydrogenase (IDH)
Hedgehog/Smoothened
Vasopressin Receptor
Xanthine Oxidase
DNA
PGE Synthase
GPCR19
Kras
Aromatase
Hydroxylase
Neurokinin receptor
TAM Receptor
Melatonin Receptor
Gamma-secretase
Molecular Glues
Fatty Acid Synthase
Complement System
NOS
Cell wall
CaSR
Serine/threonin kinase
Vitamin
Aryl Hydrocarbon Receptor
Annexin A
UGT
MT Receptor
Na-K-Cl cotransporter
Smo
Aurora Kinase
Thrombopoietin Receptor
IGF-1R
TGF-beta/Smad
OAT
Aminopeptidase
Decarboxylase
Neprilysin
FKBP
Ligand for E3 Ligase
c-Fms
Gap Junction Protein
NOD
FAK
AhR
NOD-like Receptor (NLR)
MicroRNA
ASBT
Arginase
Histone Demethylase
Cholecystokinin Receptor
LDL
BTK
PAK
CCR
CXCR
Mucin
Telomerase
Lipid
MAPK
Free radical scavengers
Sirtuin
GST
Oxytocin Receptor
Adenosine Deaminase
CGRP Receptor
Cuproptosis
Cannabinoid Receptor
Syk
Imidazoline Receptor
IKZF
Monocarboxylate transporter
ROR
MTP
CRM1
Ligands for Target Protein for PROTAC
YAP
LTR
Na+/Ca2+ Exchanger
IFNAR
Necroptosis
Tie-2
TOPK
Photosensitizer
Rho
NR4A
CSF-1R
Immunology/Inflammation related
IRE1
GlyT
Hexokinase
Integrase
FAAH
ATP Citrate Lyase
Beta-Secretase
Glutathione reductase
Acyltransferase
Ephrin Receptor
GluCls
RSV
Melanocortin Receptor
GHSR
PLK
Protease-activated Receptor
PD-1/PD-L1
Advanced Glycation End Products
Mdm2
Taste receptor
NPC1L1
Hydrogenase
RAR/RXR
DNA-PK
Dynamin
BACE
Lipase
gp120/CD4
MIF
VDA
OCT
c-Myc
Hck
ATG
Liver X Receptor
IDO
IAP
Prolyl Endopeptidase (PREP)
Myosin
E1/E2/E3 Enzyme
Adiponectin Receptor
PAFR
MTH1
GRK
Glucagon Receptor
Phosphorylase
Arp2/3 Complex
PROTAC Linker
HCN Channel
HCAR
PTEN
Somatostatin
Chk
PAD
Epoxide Hydrolase
cAMP
Epigenetic Reader Domain
DUB
Indoleamine 2,3-Dioxygenase (IDO)
BCRP
OXPHOS
Survivin
STING
CRFR
Pyroptosis
Casein Kinase
p62
CRISPR/Cas9
PDK
Aquaporin
Platelet aggregation
NADPH-oxidase
S6 Kinase
p53
PKM

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