MLPCN Introduction
Small molecules, often with molecular weights of 500 or below, have proven to be extremely important to researchers to explore function at the molecular, cellular, and in vivo level. Such molecules have also been proven to be valuable for treating diseases, and most medicines marketed today are from this class. A key challenge is to identify small molecules effective at modulating a given biological process or disease state.
The Molecular Libraries Roadmap, through one of its components, the Molecular Libraries Probe Production Centers Network (MLPCN), offered biomedical researchers access to the large-scale screening capacity, along with medicinal chemistry and informatics necessary to identify chemical probes to study the functions of genes, cells, and biochemical pathways.
NIH anticipated that these projects will facilitate the development of new drugs, by providing early stage chemical compounds that will enable researchers in the public and private sectors to validate new drug targets, which could then move into the drug-development pipeline. This is particularly true for rare diseases, which may not be attractive for development by the private sector.
UF Scripps Biomedical Research became part of the University of Florida’s academic health center in April of 2022. Previously, we were a branch of Scripps Research, also known as The Scripps Research Institute.
The Scripps Research Institute was awarded more than $80 million by the National Institutes of Health to greatly expand the work of The Scripps Research Institute Molecular Screening Center, further strengthening the collaborative efforts of teams of scientists at the La Jolla, California and Jupiter, Florida campuses. The six-year grant was the largest ever awarded to Scripps Research at the time.
The Scripps Research Institute Molecular Screening Center used Lead Identification’s high throughput robotics to screen discoveries made in laboratories in La Jolla and Jupiter, as well as other research institutions, against various biological targets. The goal was to uncover “proof-of-concept molecules” that could be useful in developing new treatments for a large number of human diseases.
The Scripps center was one of only four such large centers nationwide. Together with five smaller specialized centers, they comprised the Molecular Libraries Production Centers Network, a part of the NIH’s strategic funding plan, the Roadmap Initiative.
Please reference the table below to view all the public domain campaigns screened at UF Scripps. Filter drop down menus can be used to isolate areas of interest in the table. Use the “Clear Filters” button to regenerate all available campaigns. By clicking on the column name, lists can be sorted ascending/descending alphabetically. By clicking on the arrow on the right side of the column names, columns can be added/removed. Also, columns can be manually resized. To view available BioAssay Summaries on the PubChem website, please click on the relevant PubChem Summary AID number in the PubChem column.
The High-Throughput Molecular Screening Center screened over 150 assays as part of the MLPCN initiative, encompassing a broad and large variety of targets using numerous different detection technologies and assay formats during this time. A breakdown of public domain HTS campaign types by category can be found in the specific categories of: Target Class, Assay Type, HTS Class and Cell Line.
Probe Reports
To view all probe reports generated as part of Lead Identification’s MLPCN efforts, please click HERE.
MLPCN Pipeline
A table containing all the public domain campaigns screened at the High-Throughput Molecular Screening Center can be found below.
Target Class | Target Subclass/Family | Assay Type | HTS Class | Target/Pharm | PubChem |
Tissue | Human Blood (T Cell) | Viability | Mammalian Cell | Jurkat Cytox | 1673 |
Transferase | Kinase | Enzymatic | Biochemical | FAK INH | 1802 |
Transferase | Kinase | Enzymatic | Biochemical | JNK3 INH | 746 |
Transferase | Kinase | Enzymatic | Biochemical | PKA INH | 524 |
Transferase | Kinase | Enzymatic | Biochemical | ROCK2 INH | 604 |
Receptor | GPCR | Reporter Gene | Mammalian Cell | 5HT1A AG | 567 |
Receptor | GPCR | Reporter Gene | Mammalian Cell | 5HT1A ANT | 612 |
Receptor | GPCR | Reporter Gene | Mammalian Cell | 5HT1E AG | 1676 |
Receptor | GPCR | Reporter Gene | Mammalian Cell | 5HT1E ANT | 1675 |
Receptor | GPCR | Reporter Gene | Mammalian Cell | S1P1 AG | 449 |
Receptor | GPCR | Reporter Gene | Mammalian Cell | S1P1 ANT | – |
Receptor | GPCR | Reporter Gene | Mammalian Cell | S1P2 AG | 729 |
Receptor | GPCR | Reporter Gene | Mammalian Cell | S1P2 ANT | 1657 |
Receptor | GPCR | Reporter Gene | Mammalian Cell | S1P3 AG | 373 |
Receptor | GPCR | Reporter Gene | Mammalian Cell | S1P3 ANT | 1820 |
Factor | Transcription Factor | Reporter Gene | Mammalian Cell | NFkB INH | 1664 |
Receptor | Nuclear Receptor | Reporter Gene | Mammalian Cell | RAR INH | – |
Receptor | Nuclear Receptor | Reporter Gene | Mammalian Cell | RORA / ACT | 1954 |
Receptor | Nuclear Receptor | Reporter Gene | Mammalian Cell | RORA / INH | 1901 |
Receptor | Nuclear Receptor | Reporter Gene | Mammalian Cell | SF-1 ACT | 1951 |
Receptor | Nuclear Receptor | Reporter Gene | Mammalian Cell | SF-1 INH | 1844 |
Hydrolase | Aggrecanase | Enzymatic | Biochemical | ADAMTS4 INH | – |
Virus | HIV | Protein-RNA | Biochemical | HIV Rev-RRE INH | 1667 |
Hydrolase | Matrix Metalloproteinase | Enzymatic | Biochemical | MMP-13 INH | 1931 |
Hydrolase | Matrix Metalloproteinase (Collagenase) | Enzymatic | Biochemical | MMP-8 | – |
Hydrolase | Glucosidase | Enzymatic | Biochemical | β-gluc ENH | 1670 |
Receptor | Receptor Tyrosine Kinase | Protein-Protein | Biochemical | EphB4 INH | 1669 |
Receptor | Nuclear Receptor | Protein-Protein | Biochemical | PPARg/ Src1 AG | 1808 |
Receptor | Nuclear Receptor | Protein-Protein | Biochemical | PPARg/ Src2 AG | 1810 |
Receptor | Nuclear Receptor | Protein-Protein | Biochemical | PPARg/ Src3 AG | 1812 |
Factor | Transcription Factor | Reporter Gene | Mammalian Cell | STAT-1 INH | 1803 |
Factor | Transcription Factor | Reporter Gene | Mammalian Cell | STAT-1 ACT | 1804 |
Factor | Transcription Factor | Reporter Gene | Mammalian Cell | STAT-3 ACT | 1805 |
Factor | Transcription Factor | Reporter Gene | Mammalian Cell | STAT-3 INH | 1806 |
– | – | – | – | STAT-5 INH | – |
Receptor | GPCR | Complementation | Mammalian Cell | Mu-Delta IAG | 504368 |
Receptor | GPCR | Complementation | Mammalian Cell | Mu-Delta AG | 504355 |
Receptor | Toll-like receptor | Complementation | Mammalian Cell | TLR4 INH | 1953 |
Receptor | GPCR | Reporter Gene | Mammalian Cell | GalR2 AG | 1671 |
Receptor | GPCR | Reporter Gene | Mammalian Cell | GalR2 ANT | 1668 |
Chaperone | monomeric chaperone | Reporter Gene | Mammalian Cell | Hsp70 ACT | 1203 |
Hydrolase | Matrix Metalloproteinase | Enzymatic | Mammalian Cell | IDE ACT | 493124 |
Hydrolase | Matrix Metalloproteinase | Enzymatic | Mammalian Cell | IDE INH | 434984 |
Receptor | GPCR | Second Messenger | Mammalian Cell | NPY-Y1 ANT | 1040 |
Receptor | GPCR | Second Messenger | Mammalian Cell | NPY-Y1 POT | 1304 |
Receptor | GPCR | Second Messenger | Mammalian Cell | NPY-Y2 ANT | 1791 |
Receptor | GPCR | Second Messenger | Mammalian Cell | NPY-Y2 POT | 1359 |
Transferase | Kinase | Enzymatic | Mammalian Cell | PERK (ISR) INH | 1842 |
Transferase | Kinase | Reporter Gene | Mammalian Cell | Wee1 Degr INH | 1807 |
Chaperone | Dimeric Chaperone | Protein Renaturation | Biochemical | Hsp90 INH | 1831 |
Hydrolase | Peptidase | Enzymatic | Biochemical | M1 INH | 434966 |
Hydrolase | Peptidase | Enzymatic | Biochemical | M17 INH | 434965 |
Channel | Ion Channel | Second Messenger | Mammalian Cell | TRPML3 AG | 1809 |
Channel | Ion Channel | Second Messenger | Mammalian Cell | TRPN1 AG | 1424 |
Transferase | Kinase | Viability | Mammalian Cell | Jak2 INH | 1797 |
Tissue | Mouse Blood (B Cell) | Viability | Mammalian Cell | BAF3 Cytox | 1486 |
Hydrolase | Proteinase | Enzymatic | Biochemical | Cathepsin L | 1906 |
Tissue | Rat Intestinal Epthelium | Viability | Mammalian Cell | IEC-6 Cell Line | 2201 |
Factor | Transcription Factor | Reporter Gene | Mammalian Cell | KLF5 INH | 1858 |
Hydrolase | Aminopeptidase | Enzymatic | Biochemical | M18AAP INH | 1855 |
Lipid Protein | Lipid Droplet Scaffold Protein and Coactivator Protein | Complementation | Biochemical | Abhd-Mldp Binding | 493241 |
Lipid Protein | Lipid Droplet Scaffold Protein and Coactivator Protein | Complementation | Biochemical | Abhd-Plin Binding | 493057 |
Factor | Transcription Factor | Reporter Gene | Mammalian Cell | AHR AG | 2804 |
Receptor | GPCR | Second Messenger | Mammalian Cell | GPR7 ANT | 1880 |
Transferase | Phosphotransferase | Enzymatic | Biochemical | TPT1 INH | 1963 |
RNA Binding Protein | STAR | Protein-RNA | Biochemical | GLD-1 INH | 2290 |
Hydrolase | Beta-lactamase | Enzymatic | Biochemical | IMP-1 INH | 2715 |
Receptor | Notch | Viability | Mammalian Cell | Notch AG | 434983 |
Hydrolase | Beta-lactamase | Enzymatic | Biochemical | VIM-2 INH | 1854 |
Hydrolase | Protease | Enzymatic | Biochemical | 3CLpro INH | 1859 |
DNA | hairpin oligonucleotide | DNA Binding | Biochemical | FID INH | 1845 |
Oxidoreductase | Transferase | Protein-Activity Probe | Biochemical | GSTO1-1 INH | 2175 |
Virus | HIV | Protein-Protein | Biochemical | HCV Core INH | 1911 |
Oxidoreductase | Oxidase | Enzymatic | Mammalian Cell | Nox-1 INH | 1796 |
Hydrolase | Helicase | Enzymatic | Biochemical | NS3 Helicase INH | 1830 |
Transferase | ATPase | Enzymatic | Biochemical | P97 INH | 1794 |
Virus | Nuclear Antigen | Protein-DNA | Biochemical | EBNA-1 INH | 1955 |
Virus | Nuclear Antigen | Protein-DNA | Biochemical | ZTA INH | 2234 |
Receptor | GPCR | Second Messenger | Mammalian Cell | V1R AG | 2797 |
Hydrolase | Esterase | Protein-Activity Probe | Biochemical | LYPLA1 | 2202 |
Hydrolase | Esterase | Protein-Activity Probe | Biochemical | LYPLA2 | 2203 |
Receptor | GPCR | Second Messenger | Mammalian Cell | OTR AG | 2482 |
Receptor | GPCR | Second Messenger | Mammalian Cell | OTR POT | 2481 |
Hydrolase | Esterase | Protein-Activity Probe | Biochemical | PME-1 | 2143 |
Hydrolase | Phosphatase | Enzymatic | Biochemical | PP1 INH | 2235 |
Hydrolase | Phosphatase | Enzymatic | Biochemical | PP5 INH | 2034 |
Hydrolase | Peptidase | Protein-Activity Probe | Biochemical | FAM108B INH | 2200 |
Mitochondrial Protein | Bcl-2 | Protein-Protein | Biochemical | Mcl-1 INH | 2090 |
Mitochondrial Protein | Bcl-2 | Protein-Protein | Biochemical | Bcl-xL INH | 2144 |
Receptor | Nuclear Receptor | Protein-Protein | Biochemical | NR2E3 AG | 2325 |
Hydrolase | Esterase | Protein-Activity Probe | Biochemical | RBBP9 INH | 1790 |
Receptor | GPCR | Reporter Gene | Mammalian Cell | S1P4 AG | 1801 |
Receptor | GPCR | Reporter Gene | Mammalian Cell | S1P4 ANT | 1853 |
Receptor | GPCR | Second Messenger | Mammalian Cell | CHO ANT | 463079 |
Receptor | GPCR | Second Messenger | Mammalian Cell | Orexin 1 ANT | 435008 |
Receptor | GPCR | Second Messenger | Mammalian Cell | OX1R ANT | 485270 |
Hydrolase | Deiminase | Protein-Activity Probe | Biochemical | Pad4 INH | 463083 |
Hydrolase | Peptidase | Protein-Activity Probe | Biochemical | PREPL INH | 2760 |
Hydrolase | Protease | Protein-Activity Probe | Biochemical | Rv3671c INH | 2652 |
Hydrolase | Helicase and/or Nuclease | Viability | Bacterial Cell | AddAB INH | 449731 |
Tissue | E. coli | Viability | Bacterial Cell | E. coli Cytox | 449728 |
Hydrolase | Lipase | Enzymatic | Biochemical | Dagl INH | 504420 |
Hydrolase | Esterase | Protein-Activity Probe | Biochemical | pPAFAH INH | 463092 |
Hydrolase | Esterase | Protein-Activity Probe | Biochemical | PAFAH1b2 INH | 492971 |
Hydrolase | Esterase | Protein-Activity Probe | Biochemical | PAFAH1b3 INH | 492979 |
Hydrolase | Esterase | Protein-Activity Probe | Biochemical | PAFAH2 INH | 492969 |
Hydrolase | Caspase | Enzymatic | Biochemical | Procaspase3 ACT | 463197 |
Hydrolase | Caspase | Enzymatic | Biochemical | Procaspase7 ACT | 463210 |
Myofilament | Troponin/Tropomysin/Actin | Protein Conformation | Biochemical | RTF INH | 504337 |
Myofilament | Troponin/Tropomysin/Actin | Protein Conformation | Biochemical | RTF ACT | 493018 |
Receptor | Nuclear Receptor | Reporter Gene | Mammalian Cell | LRH1 IAG | 488781 |