MLP Probes
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Probe Target and Type: |
Tumor Hsp90 Inhibitor |
Assay Center: | Ray Dingledine, Emory Chemical Biology Discovery Center |
Chemistry Center: | Ray Dingledine, Emory Chemical Biology Discovery Center |
Assay Provider: | Gabriela Chiosis, Memorial Sloan-Kettering |
Specific Aim: |
To identify novel tumor Hsp90 inhibitors with potential for use in cancer therapy and in the treatment of neurodegenerative diseases. |
IC50/EC50: | 1,000 nM |
AntiTarget and Selectivity: | Unavailable (see probe report for details) |
Chemical Probe (Pubchem Id): | 24724290 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | 15296636+17942784+18571929 |
Probe Report: | Click to Download |
Date Submitted: | 4/14/2008 |
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Probe Target and Type: |
DNA-polymerase III (polymerase core enzme) inhibitor |
Assay Center: | Chris Austin, NIH Chemical Genomics Center(NCGC) |
Chemistry Center: | Chris Austin, NIH Chemical Genomics Center(NCGC) |
Assay Provider: | Charles McHenry, U. Colorado |
Specific Aim: |
1. Transfer and run the HTS assay for the DNA polymerase III Holoenzyme (Pol III HE) from the representative Gram (-) model organism E. coli. 2. Prioritize compounds identified via HTS of the MLSCN library for further chemical optimization and development. |
IC50/EC50: | 37 nM |
AntiTarget and Selectivity: | Unavailable (see probe report for details) |
Chemical Probe (Pubchem Id): | 11113162 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | Unavailable (see probe report for details) |
Probe Report: | Click to Download |
Date Submitted: | 4/2/2008 |
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Probe Target and Type: |
qHTS Assay for Disrupters of an Hsp90 Co-Chaperone Interaction |
Assay Center: | Chris Austin, NIH Chemical Genomics Center(NCGC) |
Chemistry Center: | Chris Austin, NIH Chemical Genomics Center(NCGC) |
Assay Provider: | Fang Yi, Yale |
Specific Aim: | |
IC50/EC50: | 1,150 nM |
AntiTarget and Selectivity: | Unavailable (see probe report for details) |
Chemical Probe (Pubchem Id): | 26753499 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | Unavailable (see probe report for details) |
Probe Report: | Click to Download |
Date Submitted: | 4/2/2008 |
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Probe Target and Type: |
DNA Primase Inihibitor |
Assay Center: | Chris Austin, NIH Chemical Genomics Center(NCGC) |
Chemistry Center: | Chris Austin, NIH Chemical Genomics Center(NCGC) |
Assay Provider: | Charles McHenry, U. Colorado |
Specific Aim: |
1. Transfer and run the HTS assay for the DNA polymerase III Holoenzyme (Pol III HE) from the representative Gram (-) model organism E. coli. 2. Prioritize compounds identified via HTS of the MLSCN library for further chemical optimization and development. |
IC50/EC50: | 30,000 nM |
AntiTarget and Selectivity: | Polymerase Core: 277 [9] |
Chemical Probe (Pubchem Id): | 11111487 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | Unavailable (see probe report for details) |
Probe Report: | Click to Download |
Date Submitted: | 4/2/2008 |
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Probe Target and Type: |
Ikappa-B-alpha stabilizers in a human lymphoma cell line |
Assay Center: | Chris Austin, NIH Chemical Genomics Center(NCGC) |
Chemistry Center: | Chris Austin, NIH Chemical Genomics Center(NCGC) |
Assay Provider: | Douglas Auld, NCGC |
Specific Aim: | |
IC50/EC50: | 2600 nM |
AntiTarget and Selectivity: | Cytoxicity [non-toxic 57 uM after 4 hrs] |
Chemical Probe (Pubchem Id): | 857745 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | 18024113+17355202 |
Probe Report: | Click to Download |
Date Submitted: | 4/2/2008 |
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Probe Target and Type: |
Splicing modulators at the Beta Globin locus |
Assay Center: | Chris Austin, NIH Chemical Genomics Center(NCGC) |
Chemistry Center: | Chris Austin, NIH Chemical Genomics Center(NCGC) |
Assay Provider: | Ryszard Kole, UNC |
Specific Aim: |
Identify small-molecule modulators of Beta-Globin splicing by high throughput screening of chemical libraries. |
IC50/EC50: | 500 nM |
AntiTarget and Selectivity: | Unavailable (see probe report for details) |
Chemical Probe (Pubchem Id): | 11110741 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | Unavailable (see probe report for details) |
Probe Report: | Click to Download |
Date Submitted: | 4/2/2008 |
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Probe Target and Type: |
Tau Filament Binding |
Assay Center: | Chris Austin, NIH Chemical Genomics Center(NCGC) |
Chemistry Center: | Chris Austin, NIH Chemical Genomics Center(NCGC) |
Assay Provider: | Jeff Kuret, Ohio State U. |
Specific Aim: |
Identify ligands capable of binding amyloidgenic tau conformations with high affinity. |
IC50/EC50: | 2,700 nM |
AntiTarget and Selectivity: | Alpha-synuclein [2.4-fold] |
Chemical Probe (Pubchem Id): | 862054 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | 17761424 |
Probe Report: | Click to Download |
Date Submitted: | 4/2/2008 |
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Probe Target and Type: |
Epigenetic Modulators |
Assay Center: | Chris Austin, NIH Chemical Genomics Center(NCGC) |
Chemistry Center: | Chris Austin, NIH Chemical Genomics Center(NCGC) |
Assay Provider: | Elizabeth Martinez, U. Texas SW MC |
Specific Aim: |
Identify small-molecule modulators of cellular epigenetic pathways |
IC50/EC50: | 5,000 nM |
AntiTarget and Selectivity: | AP1 signaling assay [?7 (Inactive @ 38 uM)] |
Chemical Probe (Pubchem Id): | 26755514 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | 18211814 |
Probe Report: | Click to Download |
Date Submitted: | 4/2/2008 |
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Probe Target and Type: |
Epigenetic Modulators |
Assay Center: | Chris Austin, NIH Chemical Genomics Center(NCGC) |
Chemistry Center: | Chris Austin, NIH Chemical Genomics Center(NCGC) |
Assay Provider: | Elizabeth Martinez, U. Texas SW MC |
Specific Aim: |
Identify small-molecule modulators of cellular epigenetic pathways |
IC50/EC50: | 8,900 nM |
AntiTarget and Selectivity: | AP1 signaling assay [?4 (Inactive @ 38 uM)] |
Chemical Probe (Pubchem Id): | 26752291 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | 18211814 |
Probe Report: | Click to Download |
Date Submitted: | 4/2/2008 |
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Probe Target and Type: |
Epigenetic Modulators |
Assay Center: | Chris Austin, NIH Chemical Genomics Center(NCGC) |
Chemistry Center: | Chris Austin, NIH Chemical Genomics Center(NCGC) |
Assay Provider: | Elizabeth Martinez, U. Texas SW MC |
Specific Aim: |
Identify small-molecule modulators of cellular epigenetic pathways |
IC50/EC50: | 7,900 nM |
AntiTarget and Selectivity: | AP1 signaling assay [?5 (Inactive @ 38 uM)] |
Chemical Probe (Pubchem Id): | 17389072 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | 18211814 |
Probe Report: | Click to Download |
Date Submitted: | 4/2/2008 |
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Probe Target and Type: |
Agonists of the Thyroid Stimulating Hormone Receptor |
Assay Center: | Chris Austin, NIH Chemical Genomics Center(NCGC) |
Chemistry Center: | Chris Austin, NIH Chemical Genomics Center(NCGC) |
Assay Provider: | Marvin Gershengorn, NIH/NIDDK |
Specific Aim: |
Identify small-molecule agonists of the Thyroid Stimulating Hormone Receptor. |
IC50/EC50: | 11,500 nM |
AntiTarget and Selectivity: | FSHR, LHCGR [Inactive @100 uM] |
Chemical Probe (Pubchem Id): | 3714076 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | 18216391 |
Probe Report: | Click to Download |
Date Submitted: | 4/2/2008 |
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Probe Target and Type: |
Inhibitor of the Mevalonate Pathway in Streptococcus pneumoniae 1: Inhibitors of Mevalonate Kinase (MK) |
Assay Center: | Gary Piazza, Southern Research Molecular Libraries Screening Center |
Chemistry Center: | Gary Piazza, Southern Research Molecular Libraries Screening Center |
Assay Provider: | Thomas Leyh, Albert Einstein COM |
Specific Aim: |
To identify specific probes that inhibit the MK enzyme, the first of three enzymes in the mevalonate pathway of S. pneumoniae. |
IC50/EC50: | 510 nM |
AntiTarget and Selectivity: | Diphosphomevalonate decarboxylase (DPMDC) [Inactive] |
Chemical Probe (Pubchem Id): | 26701727 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | Unavailable (see probe report for details) |
Probe Report: | Click to Download |
Date Submitted: | 4/1/2008 |
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Probe Target and Type: |
Pantothenate Synthetase (PanC) Inhibitor |
Assay Center: | Gary Piazza, Southern Research Molecular Libraries Screening Center |
Chemistry Center: | Gary Piazza, Southern Research Molecular Libraries Screening Center |
Assay Provider: | Lucile White, SRI |
Specific Aim: |
To identify specific probes that inhibit the Mycobacterium tuberculosis pantothenate synthetase enzyme for X-ray crystallographic studies |
IC50/EC50: | 60 nM |
AntiTarget and Selectivity: | In Vitro Inhibition of M. tuberculosis [Inactive] |
Chemical Probe (Pubchem Id): | 26736112 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | Unavailable (see probe report for details) |
Probe Report: | Click to Download |
Date Submitted: | 4/1/2008 |
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Probe Target and Type: |
S1P1 Antagonist |
Assay Center: | Hugh Rosen, The Scripps Research Institute Molecular Libraries Screening Center |
Chemistry Center: | Hugh Rosen, The Scripps Research Institute Molecular Libraries Screening Center |
Assay Provider: | Germana Sanna, Scripps |
Specific Aim: |
Identify compounds which provide insight into the molecular mechanism of S1P biological function. |
IC50/EC50: | nM |
AntiTarget and Selectivity: | Unavailable (see probe report for details) |
Chemical Probe (Pubchem Id): | 24257742 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | Unavailable (see probe report for details) |
Probe Report: | Click to Download |
Date Submitted: | 3/30/2008 |
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Probe Target and Type: |
High Throughput Fluorescence Polarization Screen for Bcl-B Phenotypic Converters |
Assay Center: | John Reed, San Diego Center for Chemical Genomics |
Chemistry Center: | John Reed, San Diego Center for Chemical Genomics |
Assay Provider: | John Reed, Burnham |
Specific Aim: |
To identify small molecule chemical probes that bind to Bcl-B within its TR3-binding site. |
IC50/EC50: | 5600 nM |
AntiTarget and Selectivity: | BH-3/Bcl-B or Bcl-2; TR3/Bcl-B or Bcl-2; ATP-Hsp70 binding [ All >100] |
Chemical Probe (Pubchem Id): | 17457047 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | Unavailable (see probe report for details) |
Probe Report: | Click to Download |
Date Submitted: | 3/24/2008 |
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Probe Target and Type: |
Autoinducing pheromone (AIP)-dependent bacterial quorum sensing: AIP binding target |
Assay Center: | Larry Sklar, New Mexico Molecular Libraries Screening Center |
Chemistry Center: | Larry Sklar, New Mexico Molecular Libraries Screening Center |
Assay Provider: | Hattie Gresham, UNM |
Specific Aim: |
1. To screen libraries of small molecules in a high throughput fluorescence-based screening assay to identify compounds capable of suppressing pheromone-dependent activation of the promoter for a global regulator of Staphylococcus aureus virulence, RNAIII. 2. To confirm that the compounds that inhibit RNAIII promoter activation also inhibit expression of the virulence genes that are regulated by RNAIII. |
IC50/EC50: | 150 nM |
AntiTarget and Selectivity: | Bacterial Viability Assay [No detectable effects in short and long cultures] |
Chemical Probe (Pubchem Id): | 24424558 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | Unavailable (see probe report for details) |
Probe Report: | Click to Download |
Date Submitted: | 3/14/2008 |
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Probe Target and Type: |
Autoinducing pheromone (AIP)-dependent bacterial quorum sensing of S. aureus Agr3 agr locus genotype: target downstream of AIP binding |
Assay Center: | Larry Sklar, New Mexico Molecular Libraries Screening Center |
Chemistry Center: | Larry Sklar, New Mexico Molecular Libraries Screening Center |
Assay Provider: | Hattie Gresham, UNM |
Specific Aim: |
1. To screen libraries of small molecules in a high throughput fluorescence-based screening assay to identify compounds capable of suppressing pheromone-dependent activation of the promoter for a global regulator of Staphylococcus aureus virulence, RNAIII. 2. To confirm that the compounds that inhibit RNAIII promoter activation also inhibit expression of the virulence genes that are regulated by RNAIII. |
IC50/EC50: | 150 nM |
AntiTarget and Selectivity: | Bacterial Viability Assay [No detectable effects in short and long cultures] |
Chemical Probe (Pubchem Id): | 4246674 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | Unavailable (see probe report for details) |
Probe Report: | Click to Download |
Date Submitted: | 3/14/2008 |
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Probe Target and Type: |
Formylpeptide Receptor (FPR) Antagonist |
Assay Center: | Larry Sklar, New Mexico Molecular Libraries Screening Center |
Chemistry Center: | Larry Sklar, New Mexico Molecular Libraries Screening Center |
Assay Provider: | Bruce Edwards, UNM |
Specific Aim: | |
IC50/EC50: | 95 nM |
AntiTarget and Selectivity: | FPRL-1 [119] |
Chemical Probe (Pubchem Id): | 24428139 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | Unavailable (see probe report for details) |
Probe Report: | Click to Download |
Date Submitted: | 3/14/2008 |
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Probe Target and Type: |
Formylpeptide Receptor-Like 1 (FPRL-1) Antagonist |
Assay Center: | Larry Sklar, New Mexico Molecular Libraries Screening Center |
Chemistry Center: | Larry Sklar, New Mexico Molecular Libraries Screening Center |
Assay Provider: | Bruce Edwards, UNM |
Specific Aim: | |
IC50/EC50: | 3100 nM |
AntiTarget and Selectivity: | FPR [21] |
Chemical Probe (Pubchem Id): | 24702504 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | Unavailable (see probe report for details) |
Probe Report: | Click to Download |
Date Submitted: | 3/14/2008 |
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Probe Target and Type: |
Competitive inhibitor of lingand binding for G protein-coupled receptor 30 (GPR30) |
Assay Center: | Larry Sklar, New Mexico Molecular Libraries Screening Center |
Chemistry Center: | Larry Sklar, New Mexico Molecular Libraries Screening Center |
Assay Provider: | Eric Prossnitz, UNM |
Specific Aim: |
To identify small molecule ligands specific for GPR30 or the classical estrogen receptors (ER? and ER?). |
IC50/EC50: | 7 nM |
AntiTarget and Selectivity: | Era; ERb [no significant binding to ER alpha or beta] |
Chemical Probe (Pubchem Id): | 48409542 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | Unavailable (see probe report for details) |
Probe Report: | Click to Download |
Date Submitted: | 3/14/2008 |
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Probe Target and Type: |
Competitive inhibitor of lingand binding for G protein-coupled receptor 30 (GPR30) |
Assay Center: | Larry Sklar, New Mexico Molecular Libraries Screening Center |
Chemistry Center: | Larry Sklar, New Mexico Molecular Libraries Screening Center |
Assay Provider: | Eric Prossnitz, UNM |
Specific Aim: |
To identify small molecule ligands specific for GPR30 or the classical estrogen receptors (ER? and ER?). |
IC50/EC50: | 20 nM |
AntiTarget and Selectivity: | Era; ERb [no significant binding to ER alpha or beta] |
Chemical Probe (Pubchem Id): | 48409616 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | Unavailable (see probe report for details) |
Probe Report: | Click to Download |
Date Submitted: | 3/14/2008 |
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Probe Target and Type: |
Activator of Prostate Cell Differentiation |
Assay Center: | Larry Sklar, New Mexico Molecular Libraries Screening Center |
Chemistry Center: | Larry Sklar, New Mexico Molecular Libraries Screening Center |
Assay Provider: | Todd Thompson, UNM |
Specific Aim: |
1. To screen for small molecules that modulate prostate cell differentiation, using HyperCyt® high throughput (HT) flow cytometry. 2. To counter-screen active compounds identified in the primary and confirmatory screens in LNCaP cells in a similar dose response assay using PC-3 cells to identify small molecules that induce intracellular granularity in an androgen-independent manner. |
IC50/EC50: | 300 nM |
AntiTarget and Selectivity: | Androgen Independent Phenotypic Response [N/A] |
Chemical Probe (Pubchem Id): | 4246202 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | Unavailable (see probe report for details) |
Probe Report: | Click to Download |
Date Submitted: | 3/14/2008 |
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Probe Target and Type: |
Ruthenium-based TrkA Inhibitor |
Assay Center: | Scott Diamond, Penn Center for Molecular Discovery |
Chemistry Center: | Scott Diamond, Penn Center for Molecular Discovery |
Assay Provider: | Scott Diamond, Penn |
Specific Aim: |
To design potent, specific, and novel Ruthenium-based small-molecule inhibitors of the protein kinase TrkA. |
IC50/EC50: | 30 nM |
AntiTarget and Selectivity: | Unavailable (see probe report for details) |
Chemical Probe (Pubchem Id): | 49649811 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | Unavailable (see probe report for details) |
Probe Report: | Click to Download |
Date Submitted: | 3/13/2008 |
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Probe Target and Type: |
Aggregation and Clearance of Huntingtin Inclusions: Huntington’s Disease Assay |
Assay Center: | Jim Rothman, MLSCN Center at Columbia University |
Chemistry Center: | Jim Rothman, MLSCN Center at Columbia University |
Assay Provider: | Ai Yamamoto, Columbia |
Specific Aim: | |
IC50/EC50: | nM |
AntiTarget and Selectivity: | Unavailable (see probe report for details) |
Chemical Probe (Pubchem Id): | Unavailable (see probe report for details) |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | Unavailable (see probe report for details) |
Probe Report: | Click to Download |
Date Submitted: | 3/12/2008 |
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Probe Target and Type: |
Protein Kinase D Inhibitor |
Assay Center: | John Lazo, University of Pittsburgh Molecular Screening Center |
Chemistry Center: | John Lazo, University of Pittsburgh Molecular Screening Center |
Assay Provider: | Q. Jane Wang, Pittsburgh |
Specific Aim: |
To identify small molecule inhibitors of PKD |
IC50/EC50: | 264 nM |
AntiTarget and Selectivity: | AKT; CDK7; PLK1 [> 50-fold] |
Chemical Probe (Pubchem Id): | 4242787 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | 17546004 |
Probe Report: | Click to Download |
Date Submitted: | 3/10/2008 |
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Probe Target and Type: |
Inhibitors of the Polo box domain of Human Polo-like kinase 1 |
Assay Center: | John Lazo, University of Pittsburgh Molecular Screening Center |
Chemistry Center: | John Lazo, University of Pittsburgh Molecular Screening Center |
Assay Provider: | Michael Yaffe, MIT |
Specific Aim: |
1. Screen MLSCN compound libraries for inhibitors of the polo box domain of polo-like kinase-1 (Plk-1-PBD) using a high throughput-ready fluorescence polarization (FP) assay. 2. Follow up primary screen of PBD inhibitors with secondary biochemical and cell based assays to confirm hits. |
IC50/EC50: | 13280 nM |
AntiTarget and Selectivity: | Redox Cycling [] |
Chemical Probe (Pubchem Id): | 47212999 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | Unavailable (see probe report for details) |
Probe Report: | Click to Download |
Date Submitted: | 3/7/2008 |
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Probe Target and Type: |
Inhibitor of anti-apoptotic protein Bfl-1 |
Assay Center: | John Reed, San Diego Center for Chemical Genomics |
Chemistry Center: | John Reed, San Diego Center for Chemical Genomics |
Assay Provider: | John Reed, Burnham |
Specific Aim: |
To identify chemical probes of Bfl-1 through a fluorescence polarization assay (FPA) using FITC-Bid BH3 peptide. |
IC50/EC50: | 2600 and 1800 nM |
AntiTarget and Selectivity: | Bcl-B; Bcl-2; 4 Bcl family members [All >100] |
Chemical Probe (Pubchem Id): | 26514105 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | Unavailable (see probe report for details) |
Probe Report: | Click to Download |
Date Submitted: | 1/10/2008 |
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Probe Target and Type: |
Inhibitor of anti-apoptotic protein Bfl-1 |
Assay Center: | John Reed, San Diego Center for Chemical Genomics |
Chemistry Center: | John Reed, San Diego Center for Chemical Genomics |
Assay Provider: | John Reed, Burnham |
Specific Aim: |
To identify chemical probes of Bfl-1 through a fluorescence polarization assay (FPA) using FITC-Bid BH3 peptide. |
IC50/EC50: | 460 and 570 nM |
AntiTarget and Selectivity: | Bcl-B; Bcl-2; 4 Bcl family members [All >100] |
Chemical Probe (Pubchem Id): | 3962106 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | Unavailable (see probe report for details) |
Probe Report: | Click to Download |
Date Submitted: | 1/10/2008 |
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Probe Target and Type: |
EphA4 Receptor Antagonists for Nervous System Repair |
Assay Center: | John Reed, San Diego Center for Chemical Genomics |
Chemistry Center: | John Reed, San Diego Center for Chemical Genomics |
Assay Provider: | Elena Pasquale, Burnham |
Specific Aim: |
To identify small molecule antagonists that inhibit the binding of EphA4 to the KYL peptide which interacts with high affinity to the ephrin-binding site of EphA4. |
IC50/EC50: | 2100 nM |
AntiTarget and Selectivity: | EphB4; Alk Phos [EphB4 >50; Alk Phos > 1000] |
Chemical Probe (Pubchem Id): | 17465980 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | Unavailable (see probe report for details) |
Probe Report: | Click to Download |
Date Submitted: | 1/10/2008 |
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Probe Target and Type: |
Chemical Inhibitors of ER Stress |
Assay Center: | John Reed, San Diego Center for Chemical Genomics |
Chemistry Center: | John Reed, San Diego Center for Chemical Genomics |
Assay Provider: | John Reed, Burnham |
Specific Aim: |
To identify compounds that selectively inhibit cell death induced by endoplasmic reticulum (ER) stress in mammalian cells. |
IC50/EC50: | 8,800 nM |
AntiTarget and Selectivity: | apoptosis induced by TNF/chx; staurosporine or VP16 up to 100 uM [>50 for all cell death pathways] |
Chemical Probe (Pubchem Id): | 17464539 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | Unavailable (see probe report for details) |
Probe Report: | Click to Download |
Date Submitted: | 1/10/2008 |
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Probe Target and Type: |
Tissue-nonspecific Alkaline Phosphatase (TNAP) |
Assay Center: | John Reed, San Diego Center for Chemical Genomics |
Chemistry Center: | John Reed, San Diego Center for Chemical Genomics |
Assay Provider: | Jose Luis Millan, Burnham |
Specific Aim: |
To identify novel highly potent and selective inhibitors of TNAP which to date have not been available. |
IC50/EC50: | 5 nM |
AntiTarget and Selectivity: | PLAP (690); GAPDH [PLAP > 10; GAPDH >10;] |
Chemical Probe (Pubchem Id): | 48410135 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | Unavailable (see probe report for details) |
Probe Report: | Click to Download |
Date Submitted: | 1/10/2008 |
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Probe Target and Type: |
Intestinal alkaline phosphatase (IAP-L) Inhibitor |
Assay Center: | John Reed, San Diego Center for Chemical Genomics |
Chemistry Center: | John Reed, San Diego Center for Chemical Genomics |
Assay Provider: | Jose Luis Millan, Burnham |
Specific Aim: |
To identify inhibitors of intestinal alkaline phosphatase (IAP) that show selectivity for the target over the other alkaline phosphatase isozymes (PLAP, TNAP). |
IC50/EC50: | 122 nM |
AntiTarget and Selectivity: | IAP-C; TNAP-L(518); TNAP-C(614); PLAP-L(690) [IAP-C 11.3; TNAP-L 6.5X; TNAP-C > 1000X; PLAP-L 34.3X] |
Chemical Probe (Pubchem Id): | 46493464 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | Unavailable (see probe report for details) |
Probe Report: | Click to Download |
Date Submitted: | 1/10/2008 |
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Probe Target and Type: |
Human Cathepsin L Inhibitor |
Assay Center: | Scott Diamond, Penn Center for Molecular Discovery |
Chemistry Center: | Scott Diamond, Penn Center for Molecular Discovery |
Assay Provider: | Scott Diamond, Penn |
Specific Aim: |
To perform a high throughput screen of the NIH Molecular Libraries Small Molecule Repository (MLSMR) to identify novel, potent, and selective inhibitors of human cathepsin L. |
IC50/EC50: | 6.9 nM |
AntiTarget and Selectivity: | Cathepsin B; Non-toxic to zebrafish at 100 ?M; Inhibits SARS-CoV pseudotype infection with IC50 = ~200 nM; Inhibits Ebola virus pseudotype infection with IC50 = ~200 nM. [725] |
Chemical Probe (Pubchem Id): | 46493575 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | Unavailable (see probe report for details) |
Probe Report: | Click to Download |
Date Submitted: | 1/7/2008 |
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Probe Target and Type: |
N-(quinolin-8-yl)benzenesulfonamides as Agents Capable of Down-Regulating NF?B Activity within Two Separate High-Throughput Screens of NF?B Activation |
Assay Center: | Jim Rothman, MLSCN Center at Columbia University |
Chemistry Center: | Jim Rothman, MLSCN Center at Columbia University |
Assay Provider: | Thomas Mayer, Columbia |
Specific Aim: |
To identify specific compounds that inhibit signaling mediated by NF?B after stimulation of human umbilical vein endothelial cells (HUVEC) by TNFalpha |
IC50/EC50: | nM |
AntiTarget and Selectivity: | Unavailable (see probe report for details) |
Chemical Probe (Pubchem Id): | Unavailable (see probe report for details) |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | Unavailable (see probe report for details) |
Probe Report: | Click to Download |
Date Submitted: | 12/21/2007 |
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Probe Target and Type: |
Matrix Metalloproteinase-8 (MMP-8) Inhibitor |
Assay Center: | Hugh Rosen, The Scripps Research Institute Molecular Libraries Screening Center |
Chemistry Center: | Hugh Rosen, The Scripps Research Institute Molecular Libraries Screening Center |
Assay Provider: | Gregg Fields, Florida Atlantic U. |
Specific Aim: |
To identify selective chemical inhibitors of MMP-8 |
IC50/EC50: | 2100 nM |
AntiTarget and Selectivity: | MMP-13; MMP-9 [Inactive] |
Chemical Probe (Pubchem Id): | 842343 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | 18364257+18358729 |
Probe Report: | Click to Download |
Date Submitted: | 12/20/2007 |
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Probe Target and Type: |
Matrix Metalloproteinase-13 (MMP-13) Inhibitor |
Assay Center: | Hugh Rosen, The Scripps Research Institute Molecular Libraries Screening Center |
Chemistry Center: | Hugh Rosen, The Scripps Research Institute Molecular Libraries Screening Center |
Assay Provider: | Gregg Fields, Florida Atlantic U. |
Specific Aim: |
To identify selective chemical inhibitors of MMP-13 |
IC50/EC50: | 3400 nM |
AntiTarget and Selectivity: | MMP-8; MMP-9 [Inactive] |
Chemical Probe (Pubchem Id): | 4257091 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | 18364257+18358729 |
Probe Report: | Click to Download |
Date Submitted: | 12/19/2007 |
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Probe Target and Type: |
Matrix Metalloproteinase-13 (MMP-13) Inhibitor |
Assay Center: | Hugh Rosen, The Scripps Research Institute Molecular Libraries Screening Center |
Chemistry Center: | Hugh Rosen, The Scripps Research Institute Molecular Libraries Screening Center |
Assay Provider: | Gregg Fields, Florida Atlantic U. |
Specific Aim: |
To identify selective chemical inhibitors of MMP-13 |
IC50/EC50: | 4300 nM |
AntiTarget and Selectivity: | MMP-8; MMP-9 [Inactive] |
Chemical Probe (Pubchem Id): | 7974872 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | 18364257+18358729 |
Probe Report: | Click to Download |
Date Submitted: | 12/19/2007 |
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Probe Target and Type: |
Sphingosine-1-phosphate receptor 2 (S1P2) Agonist |
Assay Center: | Hugh Rosen, The Scripps Research Institute Molecular Libraries Screening Center |
Chemistry Center: | Hugh Rosen, The Scripps Research Institute Molecular Libraries Screening Center |
Assay Provider: | Germana Sanna, Scripps |
Specific Aim: |
To identify specific agonists of the S1P2 receptor |
IC50/EC50: | 720 nM |
AntiTarget and Selectivity: | S1P1; S1P3 [Inactive] |
Chemical Probe (Pubchem Id): | 46371210 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | Unavailable (see probe report for details) |
Probe Report: | Click to Download |
Date Submitted: | 12/14/2007 |
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Probe Target and Type: |
Phosphodiesterase 4 (PDE4) Inhibitor in the cyclic response element-binding proteins (CREB) pathway |
Assay Center: | Chris Austin, NIH Chemical Genomics Center(NCGC) |
Chemistry Center: | Chris Austin, NIH Chemical Genomics Center(NCGC) |
Assay Provider: | Marshall Nirenberg, NIH/NHLBI |
Specific Aim: | |
IC50/EC50: | 30 nM |
AntiTarget and Selectivity: | Selected PDE isoforms [Inactive against other isoforms] |
Chemical Probe (Pubchem Id): | 29217043 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | 18243697 |
Probe Report: | Click to Download |
Date Submitted: | 12/10/2007 |
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Probe Target and Type: |
Chemical inhibitors of antigen receptor-induced NF-?B |
Assay Center: | John Reed, San Diego Center for Chemical Genomics |
Chemistry Center: | John Reed, San Diego Center for Chemical Genomics |
Assay Provider: | John Reed, Burnham |
Specific Aim: |
To identify compounds that selectively inhibit one of the several known pathways that lead to NF-kB activation in mammalian cells. |
IC50/EC50: | 70 nM |
AntiTarget and Selectivity: | NFkB by TNF induction; NLR agonists; TLR4; cIAP/MALT [all > 100] |
Chemical Probe (Pubchem Id): | 17450324 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | Unavailable (see probe report for details) |
Probe Report: | Click to Download |
Date Submitted: | 12/10/2007 |
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Probe Target and Type: |
Tissue-nonspecific Alkaline Phosphatase (TNAP) |
Assay Center: | John Reed, San Diego Center for Chemical Genomics |
Chemistry Center: | John Reed, San Diego Center for Chemical Genomics |
Assay Provider: | Jose Luis Millan, Burnham |
Specific Aim: |
To identify novel highly potent and selective inhibitors of TNAP which to date have not been available. |
IC50/EC50: | 193 nM |
AntiTarget and Selectivity: | PLAP-L (690); IAP (1017) [ PLAP-L >100; IAP >100] |
Chemical Probe (Pubchem Id): | 26514170 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | Unavailable (see probe report for details) |
Probe Report: | Click to Download |
Date Submitted: | 12/8/2007 |
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Probe Target and Type: |
High Throughput Screening Campaign to Identify Inhibitors of MMP-8 |
Assay Center: | Hugh Rosen, The Scripps Research Institute Molecular Libraries Screening Center |
Chemistry Center: | Hugh Rosen, The Scripps Research Institute Molecular Libraries Screening Center |
Assay Provider: | Gregg Fields, Florida Atlantic U. |
Specific Aim: |
To identify selective exosite/active site inhibitors of A Disintegrin and metalloproteinase with thrombospondin motifs-4 (ADAMTS-4) |
IC50/EC50: | nM |
AntiTarget and Selectivity: | Unavailable (see probe report for details) |
Chemical Probe (Pubchem Id): | 24278620 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | Unavailable (see probe report for details) |
Probe Report: | Click to Download |
Date Submitted: | 12/7/2007 |
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Probe Target and Type: |
AmpC beta-lactamase Non-Covalent Inhibitor |
Assay Center: | Chris Austin, NIH Chemical Genomics Center(NCGC) |
Chemistry Center: | Chris Austin, NIH Chemical Genomics Center(NCGC) |
Assay Provider: | Brian Shoichet, UCSF |
Specific Aim: |
To identify novel inhibitors (both covalent and non-covalent) of the AmpC B-lactamase enzyme class. |
IC50/EC50: | 8000 nM |
AntiTarget and Selectivity: | Unavailable (see probe report for details) |
Chemical Probe (Pubchem Id): | 26740854 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | 18333608+17447748 |
Probe Report: | Click to Download |
Date Submitted: | 12/6/2007 |
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Probe Target and Type: |
AmpC beta-lactamase Covalent Inhibitor |
Assay Center: | Chris Austin, NIH Chemical Genomics Center(NCGC) |
Chemistry Center: | Chris Austin, NIH Chemical Genomics Center(NCGC) |
Assay Provider: | Brian Shoichet, UCSF |
Specific Aim: |
To identify novel inhibitors (both covalent and non-covalent) of the AmpC B-lactamase enzyme class. |
IC50/EC50: | 66 nM |
AntiTarget and Selectivity: | Cruzain; Chymotrypsin; Malate Dehydrogenase [410 ; <1 ;.600] |
Chemical Probe (Pubchem Id): | 864201 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | 18333608+17447748 |
Probe Report: | Click to Download |
Date Submitted: | 12/6/2007 |
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Probe Target and Type: |
Human Cathepsin L Inhibitor |
Assay Center: | Scott Diamond, Penn Center for Molecular Discovery |
Chemistry Center: | Scott Diamond, Penn Center for Molecular Discovery |
Assay Provider: | Scott Diamond, Penn |
Specific Aim: |
To perform a high throughput screen of the NIH Molecular Libraries Small Molecule Repository (MLSMR) to identify novel, potent, and selective inhibitors of human cathepsin L. |
IC50/EC50: | 56 nM |
AntiTarget and Selectivity: | Cathepsin B [45] |
Chemical Probe (Pubchem Id): | 26681509 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | Unavailable (see probe report for details) |
Probe Report: | Click to Download |
Date Submitted: | 12/5/2007 |
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Probe Target and Type: |
Inhibitors of the NS2B-NS3 Proteinase of West Nile Virus |
Assay Center: | John Lazo, University of Pittsburgh Molecular Screening Center |
Chemistry Center: | John Lazo, University of Pittsburgh Molecular Screening Center |
Assay Provider: | Alex Strongin, Burnham |
Specific Aim: |
Identify drug-like small molecule inhibitors of the NS3 West Nile virus protease by high throughput screening of chemical libraries. |
IC50/EC50: | 183 nM |
AntiTarget and Selectivity: | Cathepsin Cysteine Proteases [] |
Chemical Probe (Pubchem Id): | 852843 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | 18181690 |
Probe Report: | Click to Download |
Date Submitted: | 12/5/2007 |
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Probe Target and Type: |
12-kDa FK506-binding protein (FKBP12) Activator |
Assay Center: | John Reed, San Diego Center for Chemical Genomics |
Chemistry Center: | John Reed, San Diego Center for Chemical Genomics |
Assay Provider: | Maurizio Pellechia, Burnham |
Specific Aim: |
Identify novel chemical probes that target FKBP12 |
IC50/EC50: | 200 (Kd) nM |
AntiTarget and Selectivity: | T-Cell activation (immunosupression) [>100 ] |
Chemical Probe (Pubchem Id): | 26679186 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | 18038971 |
Probe Report: | Click to Download |
Date Submitted: | 11/1/2007 |
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Probe Target and Type: |
Toll-Like Receptor 4-MyD88 Signaling Inhibitor |
Assay Center: | Hugh Rosen, The Scripps Research Institute Molecular Libraries Screening Center |
Chemistry Center: | Hugh Rosen, The Scripps Research Institute Molecular Libraries Screening Center |
Assay Provider: | Peter Tobias, Scripps |
Specific Aim: |
To identify inhibitors of TLR4 signaling |
IC50/EC50: | 370 nM |
AntiTarget and Selectivity: | Beta-lactamase [Inactive] |
Chemical Probe (Pubchem Id): | 26543390 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | 17615244 |
Probe Report: | Click to Download |
Date Submitted: | 10/29/2007 |
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Probe Target and Type: |
Measles Virus Inhibitor |
Assay Center: | Ray Dingledine, Emory Chemical Biology Discovery Center |
Chemistry Center: | Ray Dingledine, Emory Chemical Biology Discovery Center |
Assay Provider: | Richard Plemper, Emory |
Specific Aim: |
1. To identify novel MV-specific probes through high throughput screening (HTS) of the MLSCN library. 2. To counterscreen putative probes in independent assays and rank confirmed hits by active concentration and cytotoxicit. 3. To determine the specificity of selected probes and assess their mechanisms of antiviral activity |
IC50/EC50: | 3.8 nM |
AntiTarget and Selectivity: | cell toxicity [>16,500] |
Chemical Probe (Pubchem Id): | 24769845 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | 18529043+17643302+17470652 |
Probe Report: | Click to Download |
Date Submitted: | 10/26/2007 |
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Probe Target and Type: |
High-Throughput Screening Campaign to Identify Inhibitors of SF-1 |
Assay Center: | Hugh Rosen, The Scripps Research Institute Molecular Libraries Screening Center |
Chemistry Center: | Hugh Rosen, The Scripps Research Institute Molecular Libraries Screening Center |
Assay Provider: | Xiaolin Li, Orphagen Pharmaceuticals |
Specific Aim: |
To identify selective cell-permeable inhibitors of the steroidogenic factor 1 |
IC50/EC50: | 603 nM |
AntiTarget and Selectivity: | RAR-related Orphan Receptor A (RORA) [Inactive] |
Chemical Probe (Pubchem Id): | 46499798 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | 18334597+18374567 |
Probe Report: | Click to Download |
Date Submitted: | 10/22/2007 |
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Probe Target and Type: |
High-Throughput Screening Campaign to Identify Inhibitors of SF-1 |
Assay Center: | Hugh Rosen, The Scripps Research Institute Molecular Libraries Screening Center |
Chemistry Center: | Hugh Rosen, The Scripps Research Institute Molecular Libraries Screening Center |
Assay Provider: | Xiaolin Li, Orphagen Pharmaceuticals |
Specific Aim: |
To identify modular, chemically tractable, selective, and cell-permeable inverse agonists of the nuclear receptor RAR. |
IC50/EC50: | 195 nM |
AntiTarget and Selectivity: | RAR-related Orphan Receptor A (RORA) [Inactive] |
Chemical Probe (Pubchem Id): | 46499846 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | 18334597+18374567 |
Probe Report: | Click to Download |
Date Submitted: | 10/22/2007 |
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Probe Target and Type: |
High-Throughput Screening Campaign to Identify Inhibitors of SF-1 |
Assay Center: | Hugh Rosen, The Scripps Research Institute Molecular Libraries Screening Center |
Chemistry Center: | Hugh Rosen, The Scripps Research Institute Molecular Libraries Screening Center |
Assay Provider: | Xiaolin Li, Orphagen Pharmaceuticals |
Specific Aim: |
To identify selective cell-permeable inhibitors of the steroidogenic factor 1 (orphan nuclear receptor NR5A1) |
IC50/EC50: | 200 nM |
AntiTarget and Selectivity: | RAR-related Orphan Receptor A (RORA) [Inactive] |
Chemical Probe (Pubchem Id): | 46499821 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | 18334597+18374567 |
Probe Report: | Click to Download |
Date Submitted: | 10/22/2007 |
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Probe Target and Type: |
HIV-1 Reverse Transcriptase Associated Ribonuclease H (Rnase H) Inhibitor |
Assay Center: | John Lazo, University of Pittsburgh Molecular Screening Center |
Chemistry Center: | John Lazo, University of Pittsburgh Molecular Screening Center |
Assay Provider: | Michael Parniak, Pittsburgh |
Specific Aim: | |
IC50/EC50: | 31 nM |
AntiTarget and Selectivity: | Unavailable (see probe report for details) |
Chemical Probe (Pubchem Id): | 863762 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | Unavailable (see probe report for details) |
Probe Report: | Click to Download |
Date Submitted: | 10/20/2007 |
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Probe Target and Type: |
Zebrafish Angiogenesis Inhibitor |
Assay Center: | Ray Dingledine, Emory Chemical Biology Discovery Center |
Chemistry Center: | Ray Dingledine, Emory Chemical Biology Discovery Center |
Assay Provider: | Eric Sandberg, Zygogen Inc |
Specific Aim: |
To discover novel angiogenesis inhibitors using live zebrafish embryos. |
IC50/EC50: | 310 nM |
AntiTarget and Selectivity: | cell toxicity (HUVECs) [28] |
Chemical Probe (Pubchem Id): | 17405181 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | 18056466 |
Probe Report: | Click to Download |
Date Submitted: | 9/20/2007 |
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Probe Target and Type: |
Rho Kinase II Inhibitor |
Assay Center: | Hugh Rosen, The Scripps Research Institute Molecular Libraries Screening Center |
Chemistry Center: | Hugh Rosen, The Scripps Research Institute Molecular Libraries Screening Center |
Assay Provider: | Philip LaGrasso, Scripps |
Specific Aim: |
To find potent inhibitors for Rho-Kinase. “Kinase-Glo”, an ATP depletion assay was used to find inhibitors that are specific to the ATP binding site. |
IC50/EC50: | 80 nM |
AntiTarget and Selectivity: | PKA [Inactive] |
Chemical Probe (Pubchem Id): | 26657388 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | 17368019+18227223 |
Probe Report: | Click to Download |
Date Submitted: | 8/23/2007 |
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Probe Target and Type: |
CREB signaling pathway: CRE potentiator |
Assay Center: | Chris Austin, NIH Chemical Genomics Center(NCGC) |
Chemistry Center: | Chris Austin, NIH Chemical Genomics Center(NCGC) |
Assay Provider: | Marshall Nirenberg, NIH/NHLBI |
Specific Aim: |
Identify small molecular potentiators of the CREB pathway for memory and cognitive disorders using quantitative high throughput screening (qHTS). |
IC50/EC50: | 79 nM |
AntiTarget and Selectivity: | Unavailable (see probe report for details) |
Chemical Probe (Pubchem Id): | 863038 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | 18243697 |
Probe Report: | Click to Download |
Date Submitted: | 6/5/2007 |
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Probe Target and Type: |
Molecule Modulators: Voltage-Dependent Potassium (RMI) |
Assay Center: | David Weaver, Vanderbilt Screening Center for GPCRs, Ion Channels & Transporters |
Chemistry Center: | David Weaver, Vanderbilt Screening Center for GPCRs, Ion Channels & Transporters |
Assay Provider: | Ming Zhou, Columbia |
Specific Aim: |
To identify small molecule modulators of KvBeta that are cell permeable and have a Km sufficient for in vitro cellular physiology assays. |
IC50/EC50: | 30 nM |
AntiTarget and Selectivity: | Unavailable (see probe report for details) |
Chemical Probe (Pubchem Id): | 856002 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | Unavailable (see probe report for details) |
Probe Report: | Click to Download |
Date Submitted: | 6/1/2007 |
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Probe Target and Type: |
Allosteric Modulators of the M1 Muscarinic Receptor - Antagonist |
Assay Center: | David Weaver, Vanderbilt Screening Center for GPCRs, Ion Channels & Transporters |
Chemistry Center: | David Weaver, Vanderbilt Screening Center for GPCRs, Ion Channels & Transporters |
Assay Provider: | Jeff Conn, Vanderbilt |
Specific Aim: |
To identify small molecule modulators of M1 muscarinic receptor that are cell permeable, exhibit micromolar potency, and show greater than 10 fold selectivity over other muscarinic family members M2, M3, M4 and M5. |
IC50/EC50: | 1200 nM |
AntiTarget and Selectivity: | Unavailable (see probe report for details) |
Chemical Probe (Pubchem Id): | 4248988 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | Unavailable (see probe report for details) |
Probe Report: | Click to Download |
Date Submitted: | 6/1/2007 |
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Probe Target and Type: |
Sphingosine-1-phosphate receptor 1 (S1P1) Agonist |
Assay Center: | Hugh Rosen, The Scripps Research Institute Molecular Libraries Screening Center |
Chemistry Center: | Hugh Rosen, The Scripps Research Institute Molecular Libraries Screening Center |
Assay Provider: | Germana Sanna, Scripps |
Specific Aim: |
Identify compounds which provide insight into the molecular mechanism of S1P biological function. |
IC50/EC50: | 226 nM |
AntiTarget and Selectivity: | S1P3 [Inactive] |
Chemical Probe (Pubchem Id): | 4258673 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | 15975516+16342326+18091583 |
Probe Report: | Click to Download |
Date Submitted: | 2/1/2007 |
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Probe Target and Type: |
Sphingosine-1-phosphate receptor 3 (S1P3) Agonist |
Assay Center: | Hugh Rosen, The Scripps Research Institute Molecular Libraries Screening Center |
Chemistry Center: | Hugh Rosen, The Scripps Research Institute Molecular Libraries Screening Center |
Assay Provider: | Germana Sanna, Scripps |
Specific Aim: |
Identify compounds which provide insight into the molecular mechanism of S1P biological function. |
IC50/EC50: | 6630 nM |
AntiTarget and Selectivity: | S1P1 [Inactive] |
Chemical Probe (Pubchem Id): | 7977380 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | 15975516+16342326+18091583 |
Probe Report: | Click to Download |
Date Submitted: | 2/1/2007 |
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Probe Target and Type: |
Sphingosine-1-phosphate receptor 3 (S1P3) Agonist |
Assay Center: | Hugh Rosen, The Scripps Research Institute Molecular Libraries Screening Center |
Chemistry Center: | Hugh Rosen, The Scripps Research Institute Molecular Libraries Screening Center |
Assay Provider: | Germana Sanna, Scripps |
Specific Aim: |
Identify compounds which provide insight into the molecular mechanism of S1P biological function. |
IC50/EC50: | 4280 nM |
AntiTarget and Selectivity: | S1P1 [Inactive] |
Chemical Probe (Pubchem Id): | 864271 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | 15975516+16342326+18091583 |
Probe Report: | Click to Download |
Date Submitted: | 2/1/2007 |
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Probe Target and Type: |
Sphingosine-1-phosphate receptor 3 (S1P3) Agonist |
Assay Center: | Hugh Rosen, The Scripps Research Institute Molecular Libraries Screening Center |
Chemistry Center: | Hugh Rosen, The Scripps Research Institute Molecular Libraries Screening Center |
Assay Provider: | Germana Sanna, Scripps |
Specific Aim: |
Identify compounds which provide insight into the molecular mechanism of S1P biological function. |
IC50/EC50: | 2700 nM |
AntiTarget and Selectivity: | S1P1 [Inactive] |
Chemical Probe (Pubchem Id): | 7967985 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | 15975516+16342326+18091583 |
Probe Report: | Click to Download |
Date Submitted: | 2/1/2007 |
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Probe Target and Type: |
Sphingosine-1-phosphate receptor 3 (S1P3) Agonist |
Assay Center: | Hugh Rosen, The Scripps Research Institute Molecular Libraries Screening Center |
Chemistry Center: | Hugh Rosen, The Scripps Research Institute Molecular Libraries Screening Center |
Assay Provider: | Germana Sanna, Scripps |
Specific Aim: |
Identify compounds which provide insight into the molecular mechanism of S1P biological function. |
IC50/EC50: | 2340 nM |
AntiTarget and Selectivity: | S1P1 [Inactive] |
Chemical Probe (Pubchem Id): | 3714904 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | 15975516+16342326+18091583 |
Probe Report: | Click to Download |
Date Submitted: | 2/1/2007 |
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Probe Target and Type: |
Glucocerebrosidase Inhibitor (Chemotype 3) |
Assay Center: | Chris Austin, NIH Chemical Genomics Center(NCGC) |
Chemistry Center: | Chris Austin, NIH Chemical Genomics Center(NCGC) |
Assay Provider: | Wei Zheng, NCGC |
Specific Aim: | |
IC50/EC50: | 330 nM |
AntiTarget and Selectivity: | Rice alpha glucosidase; Human alpha galactosidase [Inactive @ 77 uM] |
Chemical Probe (Pubchem Id): | 49645689 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | 17827006+17670938 |
Probe Report: | Click to Download |
Date Submitted: | 2/1/2007 |
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Probe Target and Type: |
Glucocerebrosidase Inhibitor (Chemotype 2) |
Assay Center: | Chris Austin, NIH Chemical Genomics Center(NCGC) |
Chemistry Center: | Chris Austin, NIH Chemical Genomics Center(NCGC) |
Assay Provider: | Wei Zheng, NCGC |
Specific Aim: | |
IC50/EC50: | 74 nM |
AntiTarget and Selectivity: | Rice alpha glucosidase; Human alpha galactosidase [Inactive @ 77 uM] |
Chemical Probe (Pubchem Id): | 4264637 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | 17827006+17670938 |
Probe Report: | Click to Download |
Date Submitted: | 2/1/2007 |
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Probe Target and Type: |
Glucocerebrosidase Inhibitor (Chemotype 1) |
Assay Center: | Chris Austin, NIH Chemical Genomics Center(NCGC) |
Chemistry Center: | Chris Austin, NIH Chemical Genomics Center(NCGC) |
Assay Provider: | Wei Zheng, NCGC |
Specific Aim: | |
IC50/EC50: | 35 nM |
AntiTarget and Selectivity: | Rice alpha glucosidase; Human alpha galactosidase [Inactive @ 77 uM] |
Chemical Probe (Pubchem Id): | 26753329 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | 17827006+17670938 |
Probe Report: | Click to Download |
Date Submitted: | 2/1/2007 |
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Probe Target and Type: |
Inhibitor of Schistosoma Mansoni Redox Cascade |
Assay Center: | Chris Austin, NIH Chemical Genomics Center(NCGC) |
Chemistry Center: | Chris Austin, NIH Chemical Genomics Center(NCGC) |
Assay Provider: | David Williams, Illinois State U. |
Specific Aim: | |
IC50/EC50: | 25 nM |
AntiTarget and Selectivity: | human GR [Inactive @ 50 uM] |
Chemical Probe (Pubchem Id): | 11111612 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | 18345010+18235848 |
Probe Report: | Click to Download |
Date Submitted: | 12/20/2006 |
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Probe Target and Type: |
Inhibitor of Bacillus stearothermophilus Pyruvate Kinase |
Assay Center: | Chris Austin, NIH Chemical Genomics Center(NCGC) |
Chemistry Center: | Chris Austin, NIH Chemical Genomics Center(NCGC) |
Assay Provider: | Douglas Auld, NCGC |
Specific Aim: | |
IC50/EC50: | 250 nM |
AntiTarget and Selectivity: | Human PK; Leishmania Mexicana PK [Inactive at 57uM] |
Chemical Probe (Pubchem Id): | 862236 |
Pubchem Summary BioAssay ID: | Unavailable (see probe report for details) |
Publications (PubMed Ids): | 16864780 |
Probe Report: | Click to Download |
Date Submitted: | 10/1/2006 |
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