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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
  • 10 μL x 10 mM (in DMSO)
  • 20 μL x 10 mM (in DMSO)
  • 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 3170 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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Library Customization | TargetMol Library Composition

Antibacterial
Apoptosis
Antibiotic
Autophagy
Endogenous Metabolite
Adrenergic Receptor
5-HT Receptor
AChR
Parasite
Dopamine Receptor
Histamine Receptor
COX
DNA/RNA Synthesis
Potassium Channel
Antifungal
Sodium Channel
Calcium Channel
HIV Protease
ROS
NF-κB
Glucocorticoid Receptor
SARS-CoV
Cytochromes P450
Topoisomerase
Estrogen/progestogen Receptor
Reactive Oxygen Species
Influenza Virus
Virus Protease
PDE
Ferroptosis
EGFR
GABA Receptor
RAAS
VEGFR
Estrogen Receptor/ERR
Interleukin
Serotonin Transporter
TNF
iGluR
HSV
Akt
HCV Protease
Prostaglandin Receptor
Dehydrogenase
PPAR
c-Kit
Mitophagy
Microtubule Associated
Nucleoside Antimetabolite/Analog
ERK
Cholinesterase (ChE)
Proteasome
PDGFR
p38 MAPK
HBV
Reverse Transcriptase
Norepinephrine
Progesterone Receptor
ribosome
Caspase
JAK
c-Met/HGFR
Carbonic Anhydrase
Opioid Receptor
Angiotensin-converting Enzyme (ACE)
Androgen Receptor
ATPase
Antifection
HDAC
NO Synthase
TRP/TRPV Channel
MAO
Drug Metabolite
STAT
PI3K
MMP
FGFR
Proton pump
Bcr-Abl
CDK
Mitochondrial Metabolism
DPP-4
TLR
Monoamine Oxidase
Bcl-2 Family
Ras
HIF/HIF Prolyl-Hydroxylase
DNA Alkylator/Crosslinker
JNK
mTOR
Beta Amyloid
Anti-infection
Thrombin
Adenosine Receptor
Phosphatase
FLT
Src
Tyrosine Kinases
PKC
NMDAR
P-gp
Nrf2
ALK
AMPK
HMG-CoA Reductase
Transferase
Amino Acids and Derivatives
MRP
Wnt/beta-catenin
IL Receptor
MEK
GNRH Receptor
Raf
HSP
Thyroid hormone receptor(THR)
Antioxidant
PARP
Antifolate
Antiviral
GluR
Phospholipase
Sigma receptor
ROS Kinase
DHFR
Serine Protease
DNA gyrase
Lipoxygenase
SGLT
Trk receptor
Retinoid Receptor
c-RET
Tyrosinase
CFTR
Histone Methyltransferase
ADC Cytotoxin
Reductase
Glutathione Peroxidase
GSK-3
ABC Transporter
Endothelin Receptor
Factor Xa
PKA
ROCK
DNA Alkylation
CaMK
IκB/IKK
Kras
Neurokinin receptor
HER
Chloride channel
P2Y Receptor
Leukotriene Receptor
P2X Receptor
S1P Receptor
GPCR
Integrin
LPL Receptor
NADPH
FXR
Monoamine Transporter
Hedgehog/Smoothened
Vasopressin Receptor
glycosidase
Hydroxylase
HIF
Complement System
MDM-2/p53
DNA Methyltransferase
Necroptosis
Cysteine Protease
Vitamin
Na-K-Cl cotransporter
Glucosidase
Guanylate cyclase
Isocitrate Dehydrogenase (IDH)
Fatty Acid Synthase
Xanthine Oxidase
IGF-1R
DNA
PGE Synthase
GPCR19
Aromatase
Melanocortin Receptor
TAM Receptor
Melatonin Receptor
CaSR
UGT
Gamma-secretase
MT Receptor
Molecular Glues
MAPK
OAT
Neprilysin
c-Fms
CGRP Receptor
Gap Junction Protein
NOD
NOD-like Receptor (NLR)
ASBT
Arginase
Cell wall
Histone Demethylase
Serine/threonin kinase
Aryl Hydrocarbon Receptor
Annexin A
Smo
Ligands for E3 Ligase
Somatostatin
Aurora Kinase
Thrombopoietin Receptor
TGF-beta/Smad
Aminopeptidase
Sirtuin
FKBP
Oxytocin Receptor
FAK
AhR
BTK
MicroRNA
NOS
LTR
IFNAR
PERK
Lipase
TOPK
Rho
RANKL/RANK
Immunology/Inflammation related
IRE1
Adenylate cyclase
LDL
PAK
CCR
CXCR
Epigenetic Reader Domain
Mucin
Telomerase
Free radical scavengers
Decarboxylase
RSV
GST
Adenosine Deaminase
Cuproptosis
Cannabinoid Receptor
Syk
Imidazoline Receptor
MTP
IKZF
Monocarboxylate transporter
ROR
CRM1
Ligands for Target Protein for PROTAC
YAP
Na+/Ca2+ Exchanger
Tie-2
Cholecystokinin Receptor
Photosensitizer
ATG
Cell Cycle Arrest
NR4A
LDLR
Amylase
CSF-1R
Myosin
PAFR
GRK
Glucagon Receptor
Phosphorylase
Hexokinase
Integrase
PROTAC Linker
FAAH
ATP Citrate Lyase
Lipid
BCRP
Beta-Secretase
Glutathione reductase
Acyltransferase
Ephrin Receptor
transporter
GluCls
GHSR
FOXO
PLK
Platelet aggregation
IRAK
Protease-activated Receptor
p53
PD-1/PD-L1
Advanced Glycation End Products
Mdm2
Taste receptor
NPC1L1
Hydrogenase
RAR/RXR
DNA-PK
Dynamin
BACE
CETP
gp120/CD4
MIF
VDA
OCT
c-Myc
Liver X Receptor
Glucokinase
IDO
IAP
Prolyl Endopeptidase (PREP)
E1/E2/E3 Enzyme
RIP kinase
Adiponectin Receptor
MTH1
Arp2/3 Complex
GlyT
HCN Channel
Bradykinin Receptor
ACK1
HCAR
PTEN
Chk
PAD
Epoxide Hydrolase
cAMP
DUB
Indoleamine 2,3-Dioxygenase (IDO)
Wee1
OXPHOS
Huntingtin
PSMA
Survivin
STING
Urea Transporter
ASK
CRFR
PAI-1
Pyroptosis
Casein Kinase
ATM/ATR
p62
CRISPR/Cas9
PDK
Aquaporin
NADPH-oxidase
S6 Kinase
PKM
Ferroportin
Drug-Linker Conjugates for ADC
PGC-1α

Keywords