Drug discovery is a highly complex and multidisciplinary process with many branches and possibilities, which typically start with the identification of suitable drug targets. Such targets are biomolecules, most of which are proteins, such as receptors, enzymes or ion channels. In the process of validating a target, it is necessary to determine the relevance of the target to the disease under study and that the adjustment of the target can lead to effective treatment. The initial steps for target validation are usually performed in vitro and in animal models, and the final validation can only be performed in human clinical trials.

Modulators acting on targets can be agonists or antagonists in the case of receptors, activators or inhibitors of enzymes, and openers or blockers of ion channels. Active compounds that demonstrate dose-dependent target modulation are called lead compounds. The phase of lead compound identification starts with the design and development of suitable assay to monitor the target under study. In general, lead compounds continue to be optimized for their efficacy and selectivity, as well as their physicochemical properties, and their pharmacokinetics and safety are evaluated before they become candidates. The late phase of the drug discovery process are human clinical trials.

High Throughput Screening AssaysThe Process of Drug Research and Development

High-Throughput Screening (HTS)

High-Throughput Screening (HTS) is a standard method for drug discovery in the pharmaceutical industry and has been widely used in the past decades. HTS is basically a process of screening a large number of active modulators against selected and specific targets. The drug discovery potential of HTS is enormous, when coupled to different types of libraries, including combinatorial chemistry, genomics, protein, and peptide libraries. The screening attrition rate in drug discovery protocols suggests that one marketable drug emerges from approximately one million screened compounds. The primary goal of the HTS assay is to accelerate drug discovery by screening large compound libraries to reduce the costs of drug development.

Product Range

Amerigo Scientific offers high throughput screening (HTS) assays for validated drug targets. The assays are in 96-well or 384-well plate format for tests of inhibition or IC50 measurement of compounds against the specific drug target proteins and enzymes. The validated drug targets include human proteins for anti-cancer and proteins from bacterial, viral and bacterial phage for anti-infection.

HTS Assays for Anticancer Drug Targets

Cancer is one of the biggest threats to human life in the world. The development of novel anticancer drugs is critical for patients with cancer who have no drugs to treat, as well as for reducing the financial burden on patients and prolonging their lives. According to the mechanism of action, anticancer drugs can be divided into angiogenesis inhibitors, DNA intercalators, DNA synthesis inhibitors, transcription regulators, enzyme inhibitors, etc. In clinical use, some of the anticancer agents that target DNA are often used in combination with drugs with other mechanisms of action to improve the survival rate of cancer patients.

Amerigo Scientific offers HTS assays kits for screening potential anticancer compounds that act the following validated targets:

Target Product Name CAT. No.
Human DNA Polymerase Alpha Human DNA Polymerase Alpha Assay Kit HDPA100K
Human DNA Polymerase Alpha Assay Kit Plus HDPA100KE1
Human DNA Polymerase Beta Human DNA polymerase beta assay kit (enzyme not included) DPB100K
Human DNA Polymerase Beta Assay Kit Plus DPB100KE
Human DNA Polymerase Gamma Human DNA Polymerase Gamma Assay Kit DPG100K
Human DNA Polymerase Gamma Assay Kit Plus DPG100KE
Human DNA Topoisomerase I Gel-Based Human Topoisomerase I DNA relaxation Assay Kit GHRA100KE
Human topoisomerase I DNA relaxation assay HTS kit (enzyme not included) HRA1000
Human topoisomerase I DNA relaxation assay kit (enzyme not included) HRA020K
Human Topoisomerase I DNA Relaxation Assay Kit -100 HRA100K
Human Topoisomerase I DNA Relaxation Assay Kit Plus -100 HRA100KE
Human Topoisomerase I DNA Relaxation Assay Kit Plus -1000 HRA1000KE
Human DNA Topoisomerase II 96-Well Human Topo II DNA Decatenation Assay Kit Plus (enzyme included) HDD96KE
Gel-based Human Topoisomerase II DNA Decatenation Assay Kit Plus HDD100KEG
Human Topoisomerase II DNA Decatenation Assay Kit (enzyme not included) HDC020K
Human Topoisomerase II DNA Decatenation Assay Kit Plus (enzyme included) HDC020KE
Human Topoisomerase II DNA Decatenation Assay Kit Plus-100 (enzyme included) HDC100KE
Human Topoisomerase II DNA Decatenation Assay Reagent Set (enzyme not included) HDC100
Human Kinase Human Thymidylate Kinase Assay Kit Plus-500 (enzyme included) HTMK500KE
Human PARP-1 Human poly (ADP-ribose) polymerase-1 assay kit (enzyme not included) PAR100K
Human poly (ADP-ribose) polymerase-1 assay kit Plus (enzyme included) PAR100KE
Human Mitochondrial ClpP Protease Human Mitochondrial ClpP Protease Assay Kit HMP100K
Human Mitochondrial ClpP Protease Assay Kit Plus HMP100KE
Human Mitochondrial RNA Polymerase Human Mitochondrial RNA Polymerase Assay Kit MRPA100K
Human Mitochondrial RNA Polymerase Assay Kit Plus MRPA100KE

HTS Assays for Antiviral Drug Targets

Viruses are submicroscopic infectious agents with either DNA or RNA as the genetic material and cause a variety of diseases in humans, animals, and plants. A virus must infect a host cell to replicate itself using the components of the host cell and then new viruses are release from the host cell. Virus infection process includes six steps, namely virus attachment, invasion, uncoating, replication, assembly, and release.

Antiviral drugs are one class of medication specifically used to treat viral infections by inhibiting the development of target pathogens rather than destroying them. With emerging new viruses in the current situation, it is increasingly important to develop drugs to treat or prevent them. Antiviral drugs generally target specific regions of the virus and specific phases of the virus life cycle. The modern antiviral drug design aims at identifying viral proteins or their parts. The antivirus targets should not resemble any human proteins to reduce any side-effects and should be common among many strains of viruses.

Amerigo Scientific offers HTS assays kits for screening potential antiviral compounds that act on specific virus proteins or enzymes:


HTS Assays for Antibacterial Drug Targets

Antibacterial drugs are known to either block key biochemical pathways or to interfere with cellular structures, leading to either growth inhibition or bacterial death. Cellular processes interfered by the widely used antibiotics can be grouped into six target categories: bacterial cell wall biosynthesis, bacterial cell membranes, bacterial protein biosynthesis, DNA replication and repair, RNA synthesis, and folate biosynthesis. The distinct cellular constituents as antibacterial targets include enzymes, enzyme substrates, RNA, DNA, membranes, etc. It is estimated that more than validated 40 targets have been developed for antimicrobial drugs on the market.

Amerigo Scientific offers HTS assays kits for screening potential antibacterial compounds that target the following validated targets:

Target Product Name CAT. No.
Bacterial DNA Topoisomerase I DNA Topoisomerase I Assay Kit (enzyme not included) DRA020K
DNA Topoisomerase I assay reagent Set for HTS (enzyme not included) DRA1000
E. coli DNA Topoisomerase I Assay Kit Plus (E. coli Topo I included) DRA020KE
E. coli DNA Topoisomerase I Assay Kit Plus-100 (enzyme included) DRA100KE
Gel-Based E. coli Topoisomerase I DNA relaxation Assay Kit GDRA100KE
96-Well E. coli Topo I DNA Decatenation Assay Kit Plus (enzyme included) T1DD-96KE
Bacterial DNA Gyrase DNA Topoisomerase II (Gyrase) Assay Kit (enzyme not included) DSA020K
96-well E. coli Gyrase DNA Cleavage Assay Kit Plus (enzyme included) T2C96KE
96-Well E. coli gyrase DNA Decatenation Assay Kit Plus (enzyme included) T2DD-96KE
E. coli DNA Topoisomerase II (Gyrase) Assay Kit Plus (E. coli gyrase included) DSA020KE
E. coli DNA Topoisomerase II (Gyrase) Assay Kit Plus-100 (enzyme included) DSA100KE
E. coli gyrase ATPase assay Kit Plus (enzyme included) T2A-100KE
Gel-based E. coli DNA Topoisomerase II (Gyrase) Assay Kit Plus-100 (for 100 assays) GDSA100KE
Quinolone-resistant E. coli Gyrase Mutant D87G Assay kit Plus-100 D87G100KE
Quinolone-resistant E. coli Gyrase Mutant S83W Assay kit Plus-100 S83W100KE
P. aeruginosa Gyrase ATPase assay Kit Plus (enzyme included) T2A-100KP
P. aeruginosa Gyrase DNA Supercoiling Assay Kit Plus (enzyme included) DSA100KP
S. aureus gyrase ATPase assay Kit Plus (enzyme included) T2A-100KS
S. aureus Gyrase DNA Supercoiling Assay Kit Plus (enzyme included) DSA020KSE
S. aureus Gyrase DNA Supercoiling Assay Plus-100 DSA100KSE
96-Well S. aureus gyrase DNA Decatenation Assay Kit Plus (enzyme included) T2DD-96KS
Bacterial DNA Topoisomerase IV E. coli DNA Topoisomerase IV Assay Kit Plus (E. coli Topo IV included) DDC020KE
E. coli DNA Topoisomerase IV Assay Kit Plus-100 (enzyme included) DDC100KE
Gel-Based E. coli Topoisomerase IV DNA Decatenation Assay Kit Plus GDDA100KE
P. aeruginosa Topoisomerase IV ATPase Assay Kit Plus (enzyme included) T4A-100KP
S. aureus Topoisomerase IV ATPase Assay Kit Plus (enzyme included) T4A-100KS
96-well E. coli Topo IV DNA Cleavage Assay Kit Plus T4C96KE
96-Well E. coli Topo IV DNA Decatenation Assay Kit Plus (enzyme included) EDD96KE
E. coli Topo IV ATPase Assay Kit Plus (enzyme included) T4A-100KE
E. coli Topo IV DNA Relaxation Assay Kit Plus (enzyme included) T4RA-100KE
P. aeruginosa Topo IV DNA Relaxation Assay Kit Plus (enzyme included) T4RA-100KP
96-Well P. aeruginosa Topo IV DNA Decatenation Assay Kit Plus (enzyme included) PDD96KE
S. aureus Topo IV DNA Relaxation Assay Kit Plus (enzyme included) T4RA-100KS
96-well S. aureus Topo IV DNA Cleavage Assay Kit Plus (enzyme included) T4C96KS
96-Well S. aureus Topo IV DNA Decatenation Assay Kit Plus (enzyme included) SDD96KE
S. pneumoniae Topo IV ATPase Assay Kit Plus (enzyme included) T4A-100KN
S. pneumoniae Topo IV DNA Relaxation Assay Kit Plus (enzyme included) T4RA-100KN
96-Well S. pneumoniae Topo IV DNA Decatenation Assay Kit Plus (enzyme included) NDD96KE
Bacterial DNA Polymerase DNA polymerase Assay Kit (enzyme not included) DPA100K
E. coli DNA polymerase Assay Kit Plus (E. coli DNA pol III alpha subunit included) DPA100KE
H influenzae DNA Polymerase Assay Kit Plus (enzyme included) DPA100KH
S. pneumoniae DNA Polymerase Assay Kit Plus (enzyme included) DPA100KN
Bacterial RNA Polymerase Bacterial RNA Polymerase Pyrophosphate Assay Kit (enzyme not included) RPAP100K
E. coli RNA polymerase Assay Kit (enzyme not included) RPA100K
E. coli RNA polymerase Assay Kit Plus (E. coli RNA polymerase included) RPA100KE
E. coli RNA Polymerase Assay Pyrophosphate Kit Plus (enzyme included) RPAP100KE
S. aureus RNA polymerase assay kit (enzyme not included) RPA-100KS
S. aureus RNA polymerase assay kit Plus (enzyme included) RPA-100KSE
S. aureus RNA Polymerase Assay Pyrophosphate Kit Plus RPAP100KSE
E. coli Polynucleotide Phosphorylase (PNPase) Assay Kit PNP100K
E. coli Polynucleotide Phosphorylase (PNPase) Assay Kit Plus PNP100KE
Pyrophosphate Assay Reagent for RNAP (enzyme not included) PPA1000
Bacterial DNA Helicase E. coli DNA Helicase ATPase assay Kit Plus-100 DNAB100KE
E. coli DNA Helicase ATPase assay Kit Plus-500 DNAB500KE
H. influenzae DNA Helicase ATPase assay Kit Plus-100 DNAB100KH
H. influenzae DNA Helicase ATPase assay Kit Plus-500 DNAB500KH
P. aeruginosa DNA Helicase ATPase assay Kit Plus-100 DNAB100KP
P. aeruginosa DNA Helicase ATPase assay Kit Plus-500 DNAB500KP
S. aureus DNA Helicase ATPase assay Kit Plus-100 DNAB100KS
S. aureus DNA Helicase ATPase assay Kit Plus-500 DNAB500KS
S. pneumoniae DNA Helicase ATPase assay Kit Plus-100 DNAB100KN
S. pneumoniae DNA Helicase ATPase assay Kit Plus-500 DNAB500KN
Bacterial DNA Primase E. coli DNA Primase Assay Kit (enzyme not included) EGA100K
E. coli DNA Primase Assay Kit Plus (E. coli primase-helicase included) EGA100KE
H. influenzae DNA Primase Assay Kit (enzyme not included) HGA100K
H. influenzae DNA Primase Assay Kit Plus (enzyme included) HGA100KE
S. aureus DNA Primase Assay Kit (enzyme not included) AGA100K
S. aureus DNA Primase Assay Kit Plus (enzyme included) AGA100KE
S. pneumonia DNA Primase Assay Kit (enzyme not included) PGA100K
S. pneumonia DNA Primase Assay Kit Plus (enzyme included) PGA100KE
Bacterial DNA Ligase NAD-dependent DNA Ligase Assay Kit (enzyme not included) NLA100K
E. coli NAD+-dependent DNA ligase assay kit Plus (E. coli ligase included) NLA100KE
Bacterial Kinase E. coli Guanylate Kinase Assay Kit Plus GMK100KE
E. coli Guanylate Kinase Assay Kit Plus-500 GMK500KE
E. coli NAD+ Kinase Assay Kit Plus NADK100KE
E. coli NAD+ Kinase Assay Kit Plus-500 NADK500KE
E. coli Thymidylate Kinase Assay Kit Plus (enzyme included) TMK100KE
E. coli Thymidylate Kinase Assay Kit Plus-500 (enzyme included) TMK500KE
E. coli UMP Kinase Assay Kit Plus UMK100KE
E. coli UMP Kinase Assay Kit Plus-500 UMK500KE
S. pneumoniae Guanylate kinase Assay Kit Plus-500 GMK500KN
Bacterial Beta Lactamase Beta Lactamase Assay Kit LAC100K
E. coli Beta Lactamase Assay Kit Plus LAC100KE
Bacterial GlmU E. coli GlmU Assay Kit Plus-100 GLU100KE
E. coli GlmU Assay Kit Plus-500 GLU500KE
Bacterial IspD E. coli IspD Assay Kit Plus-100 ISPD100KE
E. coli IspD Assay Kit Plus-500 ISPD500KE
P. aeruginosa IspD Assay Kit Plus-100 ISPD100KP
P. aeruginosa IspD Assay Kit Plus-500 ISPD500KP
Bacterial PncB S. aureus PncB Assay Kit Plus-100 PNCB100KS
S. aureus PncB Assay Kit Plus-500 PNCB500KS
S. pneumoniae PncB Assay Kit Plus-100 PNCB100KN
S. pneumoniae PncB Assay Kit Plus-500 PNCB500KN
Bacterial Biotin Protein Ligase E. coli Biotin Protein Ligase Assay Kit Plus-100 BPL100KE
E. coli Biotin Protein Ligase Assay Kit Plus-500 BPL500KE
ClpP Protease M. Tuberculosis ClpP Protease Assay Kit TBP100K
M. Tuberculosis ClpP Protease Assay Kit Plus TBP100KE
Bacterial Ddl E. coli D-Alanine: D-Alanine Ligase Assay Kit Plus-100 DDA100KE
E. coli D-Alanine: D-Alanine Ligase Assay Kit Plus-500 DDA500KE
Bacterial Cell Wall Synthesis E. coli MurA Assay Kit Plus-100 MURA100KE
E. coli MurA Assay Kit Plus-500 MURA500KE
E. coli MurC Assay Kit Plus-100 MURC100KE
E. coli MurC Assay Kit Plus-500 MURC500KE
E. coli MurD Assay Kit Plus-100 MURD100KE
E. coli MurD Assay Kit Plus-500 MURD500KE
E. coli MurE Assay Kit Plus-100 MURE100KE
E. coli MurE Assay Kit Plus-500 MURE500KE
E. coli MurF Assay Kit Plus-100 MURF100KE
E. coli MurF Assay Kit Plus-500 MURF500KE
P. aeruginosa MurD Assay Kit Plus-100 MURD100KP
P. aeruginosa MurF Assay Kit Plus-100 MURF100KP
S. aureus MurD - for 100 assays MURD-100SA
S. aureus MurD Assay Kit Plus-100 MURD100KS
S. aureus MurF Assay Kit Plus-100 MURF100KS
S. pneumoniae MurC Assay Kit Plus-100 MURC100KN
S. pneumoniae MurC Assay Kit Plus-500 MURC500KN
S. pneumoniae MurF Assay Kit Plus-100 MURF100KN

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