Biologically Active Compound Library

Life Chemicals offers its Bioactive Screening Compound Library of over 8,000 drug-like small molecules as a perfect starting point for phenotypic (cell-based) and target-based high throughput screening (HTS) drug discovery research projects.

The selected structurally diverse bioactive molecules have been tested in functional, binding and other biological assays and have confirmed bioactivity in vitro and/or in vivo against about 600 biological targets of pharmaceutical interest.

The Library has been designed on the basis of the ChEMBL database (v25) which contained:

  • 1,929,473 compound records
  • 1,592,191 compounds
  • 13,968,617 activities
  • 1,212,831 assays
  • 11,019 targets

This Bioactive Compound Collection includes enzyme inhibitors, receptor ligands, and ion channel regulators for different targets (such as kinases, GPCRs, ion channels) and activity areas (e.g., biotechnology, epigenetics, antiviral or antibacterial research).

Each entry is supplied with a link to its Compound Report Card and Bioactivity Summary. High compound purity (> 90%) is confirmed by LCMS and/or NMR analytical data.

The activity records of the presented set of bioactive compounds meet the following criteria:

  • Inhibition > 30 %
  • Ki < 10 µM
  • EC50 < 10 µM
  • CC50 < 10 µM
  • Kd < 10 µM
  • Potency < 10 µM
  • XC50 < 10 µM
  • Residual Activity < 50 %
  • AC50 < 10 µM
  • IZ > 10 mm
  • MIC < 10 µg/mL
  • MIC < 10 µM

The compound selection can be customized based on your requirements, cherry-picking is available. The Advanced Subset of highly active compounds (the selection criteria: activity values < 1 µM, inhibition > 70 %) as well as focused subsets for specific target types and therapeutic areas are available on request.

A preplated set based on this Screening Library is also offered. For more details, please, consult our Pre-plated Focused Libraries.

Please, contact us at orders@lifechemicals.com for any additional information and price quotations.

Examples of protein targets against which compounds from the Library have shown activity are provided below:

  • 3C-like protease
  • 4'-phosphopantetheinyl transferase
  • Acidic alpha-glucosidase
  • Activin receptor type-1
  • Adenosine A3 receptor
  • Aldehyde dehydrogenase 1A1
  • ALK tyrosine kinase receptor
  • AMP-activated protein kinase
  • Ataxin-2
  • ATPase family (AAA domain) protein 5
  • Beta Lactamase
  • Bone morphogenetic protein (1B,2)
  • Bromodomain (to Zn-finger) protein 2B
  • CaM kinase II delta
  • Casein kinase I (epsilon, gamma)
  • Cell division protein kinase 8
  • Chaperone activity of bc1 complex-like Citron Rho-interacting kinase
  • Cyclin-dependent kinase (1,3,3-like 4,7,9)
  • Cytochrome P450 (2C19, 2D6)
  • Death-associated protein kinase 3
  • Discoidin domain-containing receptor 2 Dual specificity mitogen-activated protein kinase (1,2,5)
  • DSP testis-specific protein kinase 1
  • DSP protein kinase CLK1
  • Enoyl Reductase
  • Ephrin type-A receptor (1-8)
  • Ephrin type-B receptor (1,2,4,6)
  • Epidermal growth factor receptor erbB1
  • Epithelial discoidin domain receptor 1
  • Eukaryotic translation initiation factor 2-alpha kinase 4
  • FAD-linked sulfhydryl oxidase ALR
  • Fibroblast growth factor receptor (1-4)
  • G protein-coupled receptor 44
  • Geminin
  • Glucagon-like peptide 1 receptor
  • Glucose-6-phosphate dehydrogenase-6- phosphogluconolactonase
  • Glycogen synthase kinase-3 beta
  • Hepatocyte growth factor HepG2
  • Histone acetyltransferase GCN5
  • Histone-lysine N-methyltransferase, H3 lysine-9 specific 3
  • Hormonally tumor-associated kinase
  • Huntingtin
  • Inhibitor of nuclear factor kappa B kinase (alpha and beta subunit)
  • Insulin receptor
  • Insulin-like growth factor I receptor
  • Interleukin-1 associated kinase (1,4)
  • Isocitrate dehydrogenase [NADP] Leukocyte tyrosine kinase
  • Luciferin 4-monooxygenase
  • Lysine-specific demethylase 4D-like
  • Macrophage colony-stimulating receptor
  • Macrophage-stimulating protein receptor
  • MAP kinase (p38, signal-integ.2, MNK1)
  • Methionine aminopeptidase 2
  • Methionyl-tRNA synthetase, putative
  • Misshapen-like kinase 1
  • Mitogen-activated protein kinase ( 1-6, 15)
  • Mixed lineage kinase 7
  • Monoamine oxidase (A,B)
  • M-phase phosphoprotein 8
  • Mycobacterium bovis BCG
  • Myosin light chain kinase member 4
  • Myosin-IIIB
  • Nerve growth factor receptor Trk-A
  • Neuropeptide S receptor
  • Niemann-Pick C1 protein
  • Nonstructural protein 1
  • Paired box protein Pax-8-Phosphatidylinositol-4-phosphate 5-kinase type-1 alpha
  • Phosphorylase kinase gamma (1,2)
  • Platelet-derived growth factor (alpha,beta)
  • Proto-oncogene tyrosine kinase MER
  • Ras-related protein Rab-9A
  • Receptor-interacting serine/threonine-protein kinase 4
  • Rho-associated protein kinase 2
  • Ribosomal protein S6 kinase alpha (1,2,6)
  • Sentrin-specific protease (6-8)
  • Serine/threonine-protein kinase (10,11,16, 2,32A,33,35,AKT2,Aurora-C,Chk1,Chk2,DCLK2,GAK,MRCK beta/gamma, MRCK-A,PAK 4,PIM3,PLK4,R3,RIPK2, SBK1,SIK1,SIK2,SIK3,SRPK2,TNNI3K,
  • tousled-like 2,kinase ULK3,IRE1)
  • Serotonin transporter
  • Short transient receptor channel 4
  • Sigma opioid receptor
  • Solute carrier organic anion transporter family member (1B1,1B3)
  • Sphingomyelin phosphodiesterase
  • SPS1/STE20-related protein kinase YSK4
  • Stem cell growth factor receptor
  • Survival motor neuron protein
  • Thioredoxin reductase (type1, glutathione)
  • Thymidine phosphorylase
  • TRAF2- and NCK-interacting kinase
  • Tubulin (alpha, beta)
  • Tyrosine kinase non-receptor protein 2
  • Tyrosine-protein kinase receptor (FLT3,
  • RET, Tie-1, TYRO3, UFO, rbB-2, erbB-4, erbB-3)
  • Tyrosine-protein kinase (ABL,ABL2, BLK,BRK,BTK,CSK,FGR,FRK,FYN,
  • HCK,JAK3,LCK,Lyn,SRC,Srms,TIE-2,
  • TXK,YES)
  • Uncharacterized aarF protein kinase 4
  • Vascular endothelial growth factor (1-3)
  • Voltage-gated T-type calcium channel alpha-1H subunit
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