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

Keywords