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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 2960 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
Antifungal
Potassium Channel
Calcium Channel
Sodium Channel
ROS
HIV Protease
NF-κB
Cytochromes P450
Glucocorticoid Receptor
SARS-CoV
Topoisomerase
Estrogen/progestogen Receptor
Reactive Oxygen Species
Influenza Virus
Virus Protease
PDE
Ferroptosis
GABA Receptor
EGFR
VEGFR
RAAS
Interleukin
Estrogen Receptor/ERR
Serotonin Transporter
Akt
Dehydrogenase
TNF
HSV
Mitophagy
Prostaglandin Receptor
iGluR
PPAR
HCV Protease
Microtubule Associated
c-Kit
ERK
Nucleoside Antimetabolite/Analog
Cholinesterase (ChE)
PDGFR
Proteasome
p38 MAPK
HBV
ribosome
Progesterone Receptor
Reverse Transcriptase
Norepinephrine
Caspase
NO Synthase
Angiotensin-converting Enzyme (ACE)
Drug Metabolite
Antifection
Carbonic Anhydrase
HDAC
JAK
MMP
Opioid Receptor
Androgen Receptor
FGFR
Monoamine Oxidase
c-Met/HGFR
MAO
ATPase
Proton pump
STAT
TRP/TRPV Channel
PI3K
DNA Alkylator/Crosslinker
TLR
Bcl-2 Family
DPP-4
HIF/HIF Prolyl-Hydroxylase
Bcr-Abl
FLT
mTOR
JNK
Mitochondrial Metabolism
P-gp
Adenosine Receptor
NMDAR
Nrf2
Beta Amyloid
Anti-infection
Thrombin
Src
Tyrosine Kinases
CDK
AMPK
MRP
HMG-CoA Reductase
Transferase
Amino Acids and Derivatives
IL Receptor
Ras
Phosphatase
PKC
ALK
Wnt/beta-catenin
Thyroid hormone receptor(THR)
Raf
MEK
GNRH Receptor
Antifolate
PARP
HSP
Serine Protease
Trk receptor
Retinoid Receptor
Tyrosinase
SGLT
Lipoxygenase
ROS Kinase
DHFR
GSK-3
Phospholipase
c-RET
Glutathione Peroxidase
GluR
Sigma receptor
CFTR
Reductase
ADC Cytotoxin
DNA gyrase
CaMK
Antiviral
Factor Xa
Antioxidant
ABC Transporter
HER
DNA Alkylation
Endothelin Receptor
IκB/IKK
P2Y Receptor
S1P Receptor
Chloride channel
Histone Methyltransferase
NADPH
ROCK
HIF
PKA
Neurokinin receptor
Leukotriene Receptor
Guanylate cyclase
LPL Receptor
P2X Receptor
DNA Methyltransferase
GPCR
MDM-2/p53
Monoamine Transporter
glycosidase
Kras
Hedgehog/Smoothened
GPCR19
Complement System
Cysteine Protease
FXR
Xanthine Oxidase
PGE Synthase
Necroptosis
Na-K-Cl cotransporter
Isocitrate Dehydrogenase (IDH)
Vasopressin Receptor
Aromatase
Vitamin
DNA
Hydroxylase
Integrin
Glucosidase
TAM Receptor
Gamma-secretase
Melatonin Receptor
UGT
Fatty Acid Synthase
Molecular Glues
NOD-like Receptor (NLR)
CaSR
IGF-1R
MAPK
OAT
c-Fms
NOS
Serine/threonin kinase
Aryl Hydrocarbon Receptor
FKBP
Somatostatin
Aurora Kinase
Thrombopoietin Receptor
Aminopeptidase
FAK
Cell wall
Annexin A
MT Receptor
AhR
Arginase
Melanocortin Receptor
Gap Junction Protein
NOD
Histone Demethylase
Smo
TGF-beta/Smad
Decarboxylase
Neprilysin
Ligand for E3 Ligase
BTK
MicroRNA
Lipase
Immunology/Inflammation related
Syk
IRE1
LDL
CXCR
Free radical scavengers
CGRP Receptor
Cannabinoid Receptor
ASBT
Mucin
Cuproptosis
IFNAR
RANKL/RANK
Telomerase
Lipid
PAK
GST
Oxytocin Receptor
PERK
CCR
Sirtuin
Imidazoline Receptor
Cholecystokinin Receptor
Adenosine Deaminase
MTP
IKZF
ROR
Ligands for Target Protein for PROTAC
PAFR
RSV
PLK
Monocarboxylate transporter
Amylase
GluCls
CRM1
GlyT
BCRP
Protease-activated Receptor
YAP
Phosphorylase
Na+/Ca2+ Exchanger
Photosensitizer
Rho
Ephrin Receptor
GHSR
Platelet aggregation
IRAK
PD-1/PD-L1
LTR
ATG
NR4A
PROTAC Linker
FAAH
ATP Citrate Lyase
Tie-2
TOPK
LDLR
CSF-1R
Integrase
Beta-Secretase
Glutathione reductase
Acyltransferase
FOXO
Dynamin
MTH1
Glucagon Receptor
Hexokinase
HCAR
Chk
DUB
RAR/RXR
Prolyl Endopeptidase (PREP)
PTEN
Epoxide Hydrolase
OXPHOS
Huntingtin
STING
Pyroptosis
NADPH-oxidase
p53
PKM
MIF
RIP kinase
PAD
Indoleamine 2,3-Dioxygenase (IDO)
Wee1
Survivin
Urea Transporter
ASK
Aquaporin
Advanced Glycation End Products
BACE
CETP
OCT
Hck
IDO
GRK
Arp2/3 Complex
transporter
PDK
S6 Kinase
Mdm2
gp120/CD4
c-Myc
Liver X Receptor
HCN Channel
cAMP
CRFR
PAI-1
Hydrogenase
VDA
IAP
E1/E2/E3 Enzyme
Adiponectin Receptor
Casein Kinase
p62
CRISPR/Cas9
Taste receptor
NPC1L1
DNA-PK
Myosin
Epigenetic Reader Domain
ATM/ATR
Ferroportin
PGC-1α

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