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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 2975 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
COX
Histamine Receptor
DNA/RNA Synthesis
Potassium Channel
Antifungal
Calcium Channel
Sodium Channel
ROS
HIV Protease
NF-κB
Cytochromes P450
Glucocorticoid Receptor
SARS-CoV
Topoisomerase
Estrogen/progestogen Receptor
Reactive Oxygen Species
Virus Protease
Influenza Virus
PDE
Ferroptosis
GABA Receptor
RAAS
EGFR
VEGFR
Interleukin
Estrogen Receptor/ERR
Serotonin Transporter
Akt
TNF
HSV
Mitophagy
iGluR
Dehydrogenase
Prostaglandin Receptor
Microtubule Associated
Cholinesterase (ChE)
HCV Protease
PPAR
c-Kit
Nucleoside Antimetabolite/Analog
ERK
PDGFR
p38 MAPK
Proteasome
HBV
Progesterone Receptor
ribosome
Reverse Transcriptase
Norepinephrine
Caspase
Angiotensin-converting Enzyme (ACE)
NO Synthase
Carbonic Anhydrase
JAK
Drug Metabolite
HDAC
Antifection
MMP
FGFR
c-Met/HGFR
MAO
Androgen Receptor
Opioid Receptor
Monoamine Oxidase
ATPase
STAT
TRP/TRPV Channel
Proton pump
DNA Alkylator/Crosslinker
PI3K
TLR
Bcr-Abl
HIF/HIF Prolyl-Hydroxylase
FLT
JNK
Bcl-2 Family
mTOR
Mitochondrial Metabolism
DPP-4
Adenosine Receptor
Thrombin
P-gp
Tyrosine Kinases
AMPK
CDK
Nrf2
NMDAR
Beta Amyloid
MRP
Src
Anti-infection
Transferase
IL Receptor
ALK
PKC
Amino Acids and Derivatives
Ras
Phosphatase
Wnt/beta-catenin
HMG-CoA Reductase
Thyroid hormone receptor(THR)
Raf
MEK
HSP
PARP
Antifolate
GNRH Receptor
Serine Protease
SGLT
c-RET
Lipoxygenase
Retinoid Receptor
ROS Kinase
DHFR
Phospholipase
Tyrosinase
Trk receptor
Reductase
GluR
GSK-3
CFTR
Sigma receptor
Glutathione Peroxidase
Antioxidant
ADC Cytotoxin
Factor Xa
HER
DNA gyrase
IκB/IKK
ABC Transporter
Endothelin Receptor
Antiviral
S1P Receptor
P2X Receptor
CaMK
Neurokinin receptor
ROCK
NADPH
Histone Methyltransferase
P2Y Receptor
Chloride channel
PKA
HIF
DNA Alkylation
Kras
glycosidase
DNA Methyltransferase
LPL Receptor
Guanylate cyclase
FXR
MDM-2/p53
Hedgehog/Smoothened
Leukotriene Receptor
Monoamine Transporter
GPCR
TAM Receptor
Aromatase
Vitamin
Cysteine Protease
GPCR19
Integrin
DNA
Xanthine Oxidase
Complement System
Necroptosis
Na-K-Cl cotransporter
Isocitrate Dehydrogenase (IDH)
PGE Synthase
Vasopressin Receptor
Hydroxylase
Glucosidase
Gamma-secretase
NOD-like Receptor (NLR)
CaSR
Molecular Glues
IGF-1R
UGT
Fatty Acid Synthase
Melatonin Receptor
Somatostatin
Decarboxylase
FKBP
Neprilysin
Aminopeptidase
Annexin A
OAT
Serine/threonin kinase
Cell wall
Arginase
NOD
FAK
Thrombopoietin Receptor
Aryl Hydrocarbon Receptor
Gap Junction Protein
AhR
Smo
Melanocortin Receptor
Oxytocin Receptor
TGF-beta/Smad
Histone Demethylase
c-Fms
NOS
MT Receptor
Ligand for E3 Ligase
MAPK
BTK
IRE1
Lipase
Telomerase
Free radical scavengers
Adenosine Deaminase
Mucin
Imidazoline Receptor
Syk
Immunology/Inflammation related
RANKL/RANK
PERK
GST
CCR
IFNAR
Aurora Kinase
MicroRNA
CGRP Receptor
Lipid
PAK
Cannabinoid Receptor
LDL
Cholecystokinin Receptor
CXCR
ASBT
Sirtuin
Cuproptosis
MTP
IKZF
PLK
PAFR
Rho
Glutathione reductase
Ligands for Target Protein for PROTAC
CSF-1R
GRK
TOPK
GHSR
Amylase
Platelet aggregation
ATG
IRAK
ATP Citrate Lyase
Phosphorylase
Monocarboxylate transporter
FOXO
Integrase
FAAH
Protease-activated Receptor
Beta-Secretase
LDLR
NR4A
GluCls
Na+/Ca2+ Exchanger
Acyltransferase
PD-1/PD-L1
GlyT
Photosensitizer
LTR
Ephrin Receptor
Tie-2
CRM1
YAP
RSV
BCRP
ROR
PROTAC Linker
NADPH-oxidase
Casein Kinase
S6 Kinase
DUB
Mdm2
OCT
Prolyl Endopeptidase (PREP)
ASK
NPC1L1
Aquaporin
transporter
Survivin
MTH1
RIP kinase
p62
Epigenetic Reader Domain
CRISPR/Cas9
Adiponectin Receptor
Advanced Glycation End Products
IDO
Indoleamine 2,3-Dioxygenase (IDO)
Huntingtin
Taste receptor
PTEN
Hydrogenase
CETP
Liver X Receptor
Epoxide Hydrolase
Dynamin
E1/E2/E3 Enzyme
Arp2/3 Complex
gp120/CD4
cAMP
BACE
Glucagon Receptor
DNA-PK
Myosin
STING
Urea Transporter
HCAR
HCN Channel
PAD
Chk
Hck
MIF
c-Myc
Pyroptosis
PKM
RAR/RXR
p53
ATM/ATR
Wee1
Hexokinase
IAP
PDK
PAI-1
OXPHOS
VDA
CRFR
Ferroportin
PGC-1α

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