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TargetMol | Compound Library

Kinase Inhibitor Library

Catalog No. L1600

In biochemistry, a kinase is an enzyme that catalyzes the transfer of phosphate groups from high-energy, phosphate-donating molecules (ATP) to specific substrates. This process is known as phosphorylation. The protein kinases make up the majority of all kinases and are widely studied. A protein kinase modifies other molecules, mostly proteins, by phosphorylation to regulate the majority of cellular pathways, especially those involved in signal transduction. Various other kinases act on small molecules such as lipids, carbohydrates, amino acids, and nucleotides, either for signaling or to prime them for metabolic pathways.

TargetMol's Kinase Inhibitor Library, containing 2930 kinase inhibitors/regulators , can be used for research in chemical genomics, pharmacological study, and drug screening for related diseases.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

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Catalog No. L1600

Kinase Inhibitor 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 2930 kinase inhibitors for high throughput screening and high content screening for drug discovery in kinase related diseases;
  • Bioactivity and safety confirmed by pre-clinical research and clinical trials, and some of them are approved by FDA;
  • Targets include MAPK, PI3K, JAK, STAT, CDK, MEK, Insulin/IGF receptors, CaM Kinease II, PKA, JNK, PKC, RAF, EGFR, SAPK, GSK, MLCK, Src-family, IKK, PDGFR, VEGFR, etc;
  • Detailed compound information with structure, target, activity, IC50 value, and biological activity description;
  • 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

The TargetMol’s Kinase Inhibitor Library is built on strict entry criteria to ensure that every compound in the library possesses a well-defined structure and high purity, verified through multiple analytical techniques such as NMR, HPLC, and LC-MS. Through a multi-tiered screening process, we effectively eliminate mixtures, polymers, and other compounds with ambiguous structures.

Significant Structural Diversity

The TargetMol’s Kinase Inhibitor Library features remarkable structural diversity, offering significant advantages in drug discovery. Based on an 85% MACCS fingerprint similarity threshold, the library can be categorized into 2,389 clusters, effectively covering a broad chemical space. The compounds in the library range from simple to highly complex chemical structures, providing a wide array of possibilities for identifying lead compounds with high affinity and specificity for target proteins. This diversity greatly enhances the potential for drug innovation. Whether targeting traditional drug targets or emerging, more challenging ones, the Kinase Inhibitor Library offers a rich source of candidate compounds to accelerate the drug development process.

 Kinase Inhibitor Library
Library Diversity Analysis

Excellent Drug-Like Properties

68% of the compounds in TargetMol’s Kinase Inhibitor Library comply with Lipinski’s Rule of Five (Ro5), indicating favorable bioavailability and permeability.

 Kinase Inhibitor Library  Kinase Inhibitor Library
 Kinase Inhibitor Library  Kinase Inhibitor Library
 Kinase Inhibitor Library  Kinase Inhibitor Library

Multidimensional Pharmacokinetic Analysis

A comprehensive evaluation of TargetMol's Kinase Inhibitor Library was conducted, systematically analyzing three key pharmacological parameters: blood-brain barrier permeability, cardiotoxicity (HERG K+ channel blockade), and oral absorption properties.

 Kinase Inhibitor Library  Kinase Inhibitor Library  Kinase Inhibitor Library

Extensive Target Coverage

Protein kinases, as key regulators of intracellular signaling pathways, play crucial roles in the pathophysiology of various diseases and have become one of the most prominent targets in 21st-century drug development. As of June 2025, the FDA has approved 88 protein kinase inhibitors, covering more than twenty different kinases. The human kinome consists of over 500 protein kinases, with more than 85% implicated in at least one disease or developmental disorder. Nevertheless, for the majority of protein kinases, no effective inhibitors have yet advanced to the clinical stage, leaving substantial room for exploration in kinase inhibitor development. Kinase inhibitors are especially critical in the development of anticancer therapies. Many types of cancer are associated with the abnormal activation of specific kinases, which promote tumor progression by regulating key processes such as cell proliferation, apoptosis, and angiogenesis. Inhibitors designed to target specific kinases can not only effectively block cancer cell growth but also show tremendous potential in preclinical research and early-stage clinical trials.

 Kinase Inhibitor Library  Kinase Inhibitor Library
Status of driver kinases in therapeutic development (Fleuren, E., Zhang, L., Wu, J. et al. The kinome 'at large' in cancer. Nat Rev Cancer 16, 83–98 (2016).)

TargetMol's kinase inhibitor library encompasses inhibitors targeting a wide range of key kinase family members, including AGC, CAMK, CK1, CMGC, Other, STE, Tyrosine Kinase (TK), Tyrosine Kinase-Like (TKL), and Atypical groups. This comprehensive collection covers approximately 300 kinases across the human kinome. The extensive target coverage empowers researchers to more effectively identify and develop selective inhibitors, helping to overcome challenges associated with kinase structural similarity and selectivity. This feature is crucial for accelerating the discovery of therapeutic strategies for cancer as well as other debilitating diseases, such as autoimmune disorders, diabetes, and neurological diseases.

 Kinase Inhibitor Library

Regular Database Updates

We regularly update our database to ensure that our compound libraries include the latest compounds, keeping your research at the forefront of scientific discovery.

Flexible Packaging Options

We offer a variety of standard packaging sizes (such as 30μL, 50μL, 100μL, 250μL, 1 mg), and can provide customized packaging solutions tailored to your specific needs.

Customized Services

To support researchers in achieving their specific research goals, we provide fully customized screening services, including the design and synthesis of tailored compound libraries and personalized project screening. Our highly flexible service model is designed to efficiently meet the unique needs of scientific research and accelerate groundbreaking discoveries.

Packaging And Storage | TargetMol Packaging And Storage

  • Powder or pre-dissolved DMSO solutions in 96/384 well plate with optional 2D barcode
  • Shipped with blue ice

Library Customization | TargetMol Library Customization

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Targetmol Compound Libraries
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Library Customization | TargetMol Library Composition

Apoptosis
Autophagy
CDK
PI3K
EGFR
VEGFR
JAK
p38 MAPK
mTOR
Akt
ERK
Src
FLT
PKC
PDGFR
AMPK
FGFR
GSK-3
Raf
NF-κB
c-Kit
Bcr-Abl
c-Met/HGFR
ALK
MAPK
JNK
Aurora Kinase
Tyrosine Kinases
ROCK
PKA
MEK
Casein Kinase
IκB/IKK
RIP kinase
Endogenous Metabolite
IGF-1R
Antibacterial
Serine/threonin kinase
Glucosidase
c-RET
FAK
DNA-PK
TAM Receptor
CaMK
Trk receptor
ATM/ATR
S6 Kinase
Glucokinase
PERK
TGF-beta/Smad
TNF
STAT
PLK
c-Fms
Syk
Pim
Chk
Parasite
ROR
Caspase
HER
IRAK
DYRK
Wnt/beta-catenin
BTK
COX
LRRK2
PDK
Ras
Mitophagy
IL Receptor
Influenza Virus
Potassium Channel
Antibiotic
HIV Protease
PAK
Phosphatase
IRE1
Tyrosinase
ROS Kinase
PROTACs
Calcium Channel
Ephrin Receptor
Bcl-2 Family
Reactive Oxygen Species
DNA/RNA Synthesis
PI4K
Ferroptosis
PPAR
ROS
Epigenetic Reader Domain
MMP
AChR
Dehydrogenase
S1P Receptor
Antifungal
Adrenergic Receptor
CSF-1R
PDE
GRK
Cytochromes P450
MNK
Beta Amyloid
5-HT Receptor
Discoidin Domain Receptor (DDR)
Antiviral
SGK
Microtubule Associated
MLK
Serine Protease
LIM Kinase
HSV
HDAC
Sodium Channel
Kinesin
PKM
Adenosine Receptor
AAK1
Wee1
SARS-CoV
Nrf2
NO Synthase
Antioxidant
Tie-2
Virus Protease
PARP
PYK2
SIK
Topoisomerase
Mitochondrial Metabolism
Antifection
Cholinesterase (ChE)
Lipoxygenase
Interleukin
Histone Methyltransferase
HCV Protease
Histamine Receptor
Rho
Drug Metabolite
MELK
DAPK
NOS
Dopamine Receptor
Integrin
LPL Receptor
TOPK
Hck
TRP/TRPV Channel
LDL
ACK1
P-gp
TLR
transporter
ASK
Hippo pathway
ATPase
Carbonic Anhydrase
Estrogen/progestogen Receptor
MAO
Myosin
Hexokinase
DNA Alkylation
Prostaglandin Receptor
Sirtuin
Carboxypeptidase
Cannabinoid Receptor
p53
GPCR
Transferase
Ligands for Target Protein for PROTAC
YAP
BACE
IFNAR
NADPH
Estrogen Receptor/ERR
HBV
Cholecystokinin Receptor
Aryl Hydrocarbon Receptor
E1/E2/E3 Enzyme
Haspin Kinase
Molecular Glues
GluR
Indoleamine 2,3-Dioxygenase (IDO)
HSP
PAI-1
Phospholipase
HIF/HIF Prolyl-Hydroxylase
FOXO3
Chloride channel
MyD88
Histone Demethylase
RAAS
gp120/CD4
Glutathione Peroxidase
GTPase
Serotonin Transporter
Nucleoside Antimetabolite/Analog
FXR
Amylase
Gamma-secretase
Monoamine Transporter
PTEN
DUB
BCRP
Beta-Secretase
Reverse Transcriptase
CRISPR/Cas9
HIF
Anti-infection
ADC Cytotoxin
IKZF
Kras
Apelin receptor
Proteasome
Proton pump
NPC1L1
RAR/RXR
DHFR
Necroptosis
Melatonin Receptor
MRP
Antifolate
Cell Cycle Arrest
Liver X Receptor
NAMPT
Stemness kinase
Immunology/Inflammation related
iGluR
Glucagon Receptor
P2X Receptor
NMDAR
Opioid Receptor
Fatty Acid Synthase
Bombesin Receptor
Hedgehog/Smoothened
FAAH
PAD
cAMP
Thrombopoietin Receptor
Norepinephrine
DNA
ATP Citrate Lyase
Lipid
PGE Synthase
Acyltransferase
Porcupine
STING
Histone Acetyltransferase
Decarboxylase
cGAS
RSV
Retinoid Receptor
Ligand for E3 Ligase
Protease
Aromatase
GABA Receptor
RXFP receptor
Fer/FerT kinase
Gap Junction Protein
BMI-1
NADPH-oxidase
NOD
MAP3K
Sigma receptor
Protease-activated Receptor
p97
AhR
PD-1/PD-L1
Monoamine Oxidase