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 unique biological targets of pharmaceutical interest.
Our biologically relevant compound collection includes enzyme inhibitors, receptor ligands, and ion channel regulators for different molecular targets (such as kinases, GPCRs, ion channels) and activity areas (e.g., biotechnology, epigenetics, antiviral or antibacterial research). It is aimed for screening against complex biological targets, unclassified proteins and enzymes.
The compound selection can be customized based on your requirements, cherry picking is available.
Please, contact us at orders@lifechemicals.com for any additional information and price quotations.
For a pre plated set based on this Screening Library, please explore our Pre-plated Focused Libraries.
Compound Selection
The Screening 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 annotated activities
- 1,212,831 assays
- 11,019 targets
Initial dataset was curated automatically and manually, data clustered. 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.
Activity Profiling
The target activity records of the presented set of bioactive compounds meet the following criteria:
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The Advanced Screening 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.
Target profiling
Therapeutically irrelevant entities were removed. Examples of protein targets against which compounds from the Library have shown activity are provided below:
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
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