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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
Autophagy
Apoptosis
Endogenous Metabolite
5-HT Receptor
Adrenergic Receptor
AChR
COX
Dopamine Receptor
Histamine Receptor
Parasite
Antifungal
HIV Protease
Sodium Channel
Potassium Channel
Calcium Channel
DNA/RNA Synthesis
Glucocorticoid Receptor
Estrogen/progestogen Receptor
Topoisomerase
SARS-CoV
Cytochromes P450
PDE
Ferroptosis
RAAS
Influenza Virus
EGFR
NF-κB
VEGFR
GABA Receptor
Reactive Oxygen Species
c-Kit
Dehydrogenase
Estrogen Receptor/ERR
HCV Protease
Mitophagy
PDGFR
Serotonin Transporter
Nucleoside Antimetabolite/Analog
PPAR
ribosome
Microtubule Associated
Cholinesterase (ChE)
Norepinephrine
HSV
Prostaglandin Receptor
Reverse Transcriptase
Progesterone Receptor
Proteasome
ATPase
MAO
Antifection
HBV
HDAC
iGluR
Androgen Receptor
Carbonic Anhydrase
FGFR
JAK
Bcr-Abl
DNA Alkylator/Crosslinker
DPP-4
FLT
Opioid Receptor
Proton pump
Src
Virus Protease
HMG-CoA Reductase
MRP
ROS
Thrombin
TRP/TRPV Channel
Adenosine Receptor
c-Met/HGFR
Monoamine Oxidase
TNF
Tyrosine Kinases
HIF/HIF Prolyl-Hydroxylase
Transferase
ALK
NMDAR
Raf
AMPK
Drug Metabolite
IL Receptor
MMP
Phosphatase
PKC
Thyroid hormone receptor(THR)
Antifolate
CDK
c-RET
Interleukin
Lipoxygenase
Mitochondrial Metabolism
PARP
Retinoid Receptor
SGLT
DHFR
PI3K
Amino Acids and Derivatives
Antioxidant
Antiviral
DNA Alkylation
Endothelin Receptor
Factor Xa
GluR
MEK
P-gp
Phospholipase
STAT
ABC Transporter
ADC Cytotoxin
DNA gyrase
HSP
Monoamine Transporter
NO Synthase
P2Y Receptor
ROCK
S1P Receptor
Serine Protease
Tyrosinase
Beta Amyloid
CaMK
CFTR
DNA Methyltransferase
HER
HIF
Histone Methyltransferase
mTOR
NADPH
Nrf2
PKA
TLR
Trk receptor
Aromatase
Caspase
Chloride channel
DNA
FXR
Glutathione Peroxidase
GNRH Receptor
Guanylate cyclase
Hedgehog/Smoothened
Hydroxylase
Integrin
LPL Receptor
Neurokinin receptor
P2X Receptor
Reductase
ROS Kinase
Sigma receptor
TAM Receptor
Vasopressin Receptor
Bcl-2 Family
Cysteine Protease
ERK
Fatty Acid Synthase
GPCR
GPCR19
PGE Synthase
Xanthine Oxidase
AhR
Akt
Annexin A
Anti-infection
Aryl Hydrocarbon Receptor
Cell wall
c-Fms
CGRP Receptor
Decarboxylase
FAK
Gap Junction Protein
GSK-3
Isocitrate Dehydrogenase (IDH)
IκB/IKK
Leukotriene Receptor
Ligand for E3 Ligase
Melatonin Receptor
Molecular Glues
MT Receptor
Neprilysin
NOD
NOS
Smo
UGT
Wnt/beta-catenin
Adenosine Deaminase
Aminopeptidase
Arginase
Cannabinoid Receptor
CaSR
CCR
Complement System
CXCR
Free radical scavengers
Gamma-secretase
Glucosidase
Histone Demethylase
IGF-1R
Imidazoline Receptor
LDL
Lipid
MicroRNA
Na-K-Cl cotransporter
NOD-like Receptor (NLR)
OAT
Oxytocin Receptor
p38 MAPK
PAK
Serine/threonin kinase
Syk
TGF-beta/Smad
BTK
Vitamin
Acyltransferase
Aurora Kinase
Beta-Secretase
CETP
Cholecystokinin Receptor
CRM1
CSF-1R
Ephrin Receptor
GHSR
GluCls
Glutathione reductase
GlyT
GST
Hexokinase
IFNAR
Integrase
IRE1
Kras
Ligands for Target Protein for PROTAC
LTR
MAPK
Melanocortin Receptor
Monocarboxylate transporter
Na+/Ca2+ Exchanger
PLK
Protease-activated Receptor
Ras
Rho
ROR
RSV
Thrombopoietin Receptor
TOPK
YAP
ACK1
Adiponectin Receptor
Advanced Glycation End Products
Angiotensin-converting Enzyme (ACE)
Aquaporin
ATP Citrate Lyase
BACE
cAMP
Chk
CRFR
CRISPR/Cas9
DNA-PK
DUB
Dynamin
Epigenetic Reader Domain
Epoxide Hydrolase
FAAH
Glucagon Receptor
gp120/CD4
GRK
Hck
HCN Channel
Hydrogenase
IAP
Immunology/Inflammation related
Indoleamine 2,3-Dioxygenase (IDO)
Lipase
Liver X Receptor
Mdm2
MTH1
Mucin
Myosin
NADPH-oxidase
NPC1L1
p53
PAD
PAFR
PD-1/PD-L1
PDK
Phosphorylase
PKM
Platelet aggregation
PROTAC Linker
Pyroptosis
S6 Kinase
Sirtuin
Somatostatin
STING
Taste receptor
Telomerase
VDA