CZ-OPENSCREEN uses different assays including biochemical (ligand binding and enzymatic activity assays) and cell-based assays (reporter, viability, apoptosis, cytotoxicity, proliferation, chemosensitivity, phenotypic and cell differentiation assays). Different readouts are available and routinely used such as luminescence, AlphaScreen, FRET/TR-FRET, HTRF, fluorescence intensity, fluorescence anisotropy, BRET, radioactivity-based scintillation and scintillation proximity assays, confocal microscopy, label-free impedance, and mass spectrometry. Most of the assays are miniaturized and are performed in 384- or 1536-well format.
                                    
                                    
                                
                                        Chemosensitive profiling
                                    
                                    
                                        Chemosensitive profiling platform for systematic chemosensitive profiling of libraries of small molecules on the panel of cell lines of various histological origins. This service provides a unique complex information to chemist users about the potential clinical value of their compound library. The collection of cell lines represents cellular models for various types of cancers and is conceived to cover the most diverse types of tissues. Furthermore, each tissue is represented by one or more cell lines, according to the frequency that this type of oncological diseases contributes to the world's total cancer mortality. Systematic profiling of compound libraries provides information about the phenotypic changes, cytotoxic and anti-proliferative properties of compounds in each cell line. The association of obtained activity profiles with genetic background and specifically accumulated mutations in respective cell lines allows to identify specific pathways/processes/receptors utilised by small molecules.
                                    
                                    
   Cell line
  
  
   Organism
  
  
   Site primary
  
  
   Type
  
  
   Classification
  
  
   Primary Cell line
  
  
   Description
  
 
       Cell line
      
      
       A-375
      
     
       Organism
      
      human
     
       Site primary
      
      skin
     
       Type
      
      cancer
     
       Classification
      
      melanoma
     
       Primary Cell line
      
      transformed
     
       Description
      
      amelanotic melanoma
     
       Cell line
      
      
       A-498
      
     
       Organism
      
      human
     
       Site primary
      
      kidney
     
       Type
      
      cancer
     
       Classification
      
      carcinoma
     
       Primary Cell line
      
      transformed
     
       Description
      
      renal carcinoma
     
       Cell line
      
      
       A-549
      
     
       Organism
      
      human
     
       Site primary
      
      lung
     
       Type
      
      cancer
     
       Classification
      
      carcinoma
     
       Primary Cell line
      
      transformed
     
       Description
      
      lung adenocarcinoma
     
       Cell line
      
      
       BJ
      
     
       Organism
      
      human
     
       Site primary
      
      skin
     
       Type
      
      normal
     
       Classification
      
      normal
     
       Primary Cell line
      
      primary
     
       Description
      
      fibroblasts
     
       Cell line
      
      
       BNL 1ME A.7R.1
      
     
       Organism
      
      mouse
     
       Site primary
      
      liver
     
       Type
      
      normal
     
       Classification
      
      normal
     
       Primary Cell line
      
      transformed
     
       Description
      
      normal hepatocytes
     
       Cell line
      
      
       BT-20
      
     
       Organism
      
      human
     
       Site primary
      
      breast
     
       Type
      
      cancer
     
       Classification
      
      carcinoma
     
       Primary Cell line
      
      transformed
     
       Description
      
      breast adenocarcinoma
     
       Cell line
      
      C17.2
     
       Organism
      
      mouse
     
       Site primary
      
      brain (cerebellum)
     
       Type
      
      normal
     
       Classification
      
      normal
     
       Primary Cell line
      
      immortalized
     
       Description
      
      neural progenitor or stem-like cells
     
       Cell line
      
      
       Caco-2
      
     
       Organism
      
      human
     
       Site primary
      
      colon
     
       Type
      
      cancer
     
       Classification
      
      carcinoma
     
       Primary Cell line
      
      transformed
     
       Description
      
      colorectal adenocarcinoma
     
       Cell line
      
      
       Caki-1
      
     
       Organism
      
      human
     
       Site primary
      
      kidney
     
       Type
      
      cancer
     
       Classification
      
      carcinoma
     
       Primary Cell line
      
      transformed
     
       Description
      
      clear cell carcinoma
     
       Cell line
      
      
       Caov-3
      
     
       Organism
      
      human
     
       Site primary
      
      ovary
     
       Type
      
      cancer
     
       Classification
      
      carcinoma
     
       Primary Cell line
      
      transformed
     
       Description
      
      ovarian adenocarcinoma
     
       Cell line
      
      
       D283 Med
      
     
       Organism
      
      human
     
       Site primary
      
      brain
     
       Type
      
      cancer
     
       Classification
      
      blastoma
     
       Primary Cell line
      
      transformed
     
       Description
      
      medulloblastoma
     
       Cell line
      
      
       DU 145
      
     
       Organism
      
      human
     
       Site primary
      
      prostate
     
       Type
      
      cancer
     
       Classification
      
      carcinoma
     
       Primary Cell line
      
      transformed
     
       Description
      
      prostate adenocarcinoma
     
       Cell line
      
      
       HCT116
      
     
       Organism
      
      human
     
       Site primary
      
      colon
     
       Type
      
      cancer
     
       Classification
      
      carcinoma
     
       Primary Cell line
      
      transformed
     
       Description
      
      colorectal adenocarcinoma
     
       Cell line
      
      
       HEK-293
      
     
       Organism
      
      human
     
       Site primary
      
      kidney
     
       Type
      
      normal
     
       Classification
      
      normal
     
       Primary Cell line
      
      normal, immortalized
     
       Description
      
      embryonic kidney cells
     
       Cell line
      
      HEK-293T
     
       Organism
      
      human
     
       Site primary
      
      kidney
     
       Type
      
      normal
     
       Classification
      
      normal
     
       Primary Cell line
      
      normal, immortalized
     
       Description
      
      embryonic kidney cells
     
       Cell line
      
      Hep G2
     
       Organism
      
      human
     
       Site primary
      
      liver
     
       Type
      
      cancer
     
       Classification
      
      carcinoma
     
       Primary Cell line
      
      transformed
     
       Description
      
      hepatocellular carcinoma
     
       Cell line
      
      
       HL-60
      
     
       Organism
      
      human
     
       Site primary
      
      blood
     
       Type
      
      cancer
     
       Classification
      
      leukemia
     
       Primary Cell line
      
      transformed
     
       Description
      
      acute myeloid leukaemia
     
       Cell line
      
      
       HT-29
      
     
       Organism
      
      human
     
       Site primary
      
      colon
     
       Type
      
      cancer
     
       Classification
      
      carcinoma
     
       Primary Cell line
      
      transformed
     
       Description
      
      colorectal adenocarcinoma
     
       Cell line
      
      HT29-MTX-E12
     
       Organism
      
      human
     
       Site primary
      
      colon
     
       Type
      
      cancer
     
       Classification
      
      carcinoma
     
       Primary Cell line
      
      transformed
     
       Description
      
      colorectal adenocarcinoma
     
       Cell line
      
      HuH7
     
       Organism
      
      human
     
       Site primary
      
      liver
     
       Type
      
      cancer
     
       Classification
      
      carcinoma
     
       Primary Cell line
      
     
       Description
      
      liver carcinoma
     
       Cell line
      
      JAR
     
       Organism
      
      human
     
       Site primary
      
      placenta
     
       Type
      
      cancer
     
       Classification
      
      carcinoma
     
       Primary Cell line
      
      transformed
     
       Description
      
      Choriocarcinoma
     
       Cell line
      
      
       K562
      
     
       Organism
      
      human
     
       Site primary
      
      blood
     
       Type
      
      cancer
     
       Classification
      
      leukemia
     
       Primary Cell line
      
      transformed
     
       Description
      
      chronic myelogenous leukemia
     
       Cell line
      
      
       LNCaP
      
     
       Organism
      
      human
     
       Site primary
      
      prostate
     
       Type
      
      cancer
     
       Classification
      
      carcinoma
     
       Primary Cell line
      
      transformed
     
       Description
      
      prostate adenocarcinoma
     
       Cell line
      
      
       LS 174T
      
     
       Organism
      
      human
     
       Site primary
      
      colon
     
       Type
      
      cancer
     
       Classification
      
      carcinoma
     
       Primary Cell line
      
      transformed
     
       Description
      
      colorectal adenocarcinoma
     
       Cell line
      
      
       MCF7
      
     
       Organism
      
      human
     
       Site primary
      
      breast
     
       Type
      
      cancer
     
       Classification
      
      carcinoma
     
       Primary Cell line
      
      transformed
     
       Description
      
      breast adenocarcinoma
     
       Cell line
      
      
       MDA-MB-231
      
     
       Organism
      
      human
     
       Site primary
      
      breast
     
       Type
      
      cancer
     
       Classification
      
      carcinoma
     
       Primary Cell line
      
      transformed
     
       Description
      
      breast adenocarcinoma
     
       Cell line
      
      
       NCI-H460
      
     
       Organism
      
      human
     
       Site primary
      
      lung
     
       Type
      
      cancer
     
       Classification
      
      carcinoma
     
       Primary Cell line
      
      transformed
     
       Description
      
      large cell lung carcinoma
     
       Cell line
      
      ONS-76
     
       Organism
      
      human
     
       Site primary
      
      brain
     
       Type
      
      cancer
     
       Classification
      
      blastoma
     
       Primary Cell line
      
     
       Description
      
      medulloblastoma
     
       Cell line
      
      
       PC-3
      
     
       Organism
      
      human
     
       Site primary
      
      prostate
     
       Type
      
      cancer
     
       Classification
      
      carcinoma
     
       Primary Cell line
      
      transformed
     
       Description
      
      prostate adenocarcinoma
     
       Cell line
      
      RAW 264.7
     
       Organism
      
      mouse
     
       Site primary
      
      macrophage
     
       Type
      
      ascites
     
       Classification
      
      leukemia
     
       Primary Cell line
      
      transformed
     
       Description
      
      tumor induced by Abelson murine leukemia virus
     
       Cell line
      
      
       RD
      
     
       Organism
      
      human
     
       Site primary
      
      muscle
     
       Type
      
      cancer
     
       Classification
      
      sarcoma
     
       Primary Cell line
      
      transformed
     
       Description
      
      rhabdomyosarcoma
     
       Cell line
      
      
       RKO
      
     
       Organism
      
      human
     
       Site primary
      
      colon
     
       Type
      
      cancer
     
       Classification
      
      carcinoma
     
       Primary Cell line
      
      transformed
     
       Description
      
      colorectal adenocarcinoma
     
       Cell line
      
      
       SJCRH30
      
     
       Organism
      
      human
     
       Site primary
      
      muscle
     
       Type
      
      cancer
     
       Classification
      
      sarcoma
     
       Primary Cell line
      
      transformed
     
       Description
      
      rhabdomyosarcoma
     
       Cell line
      
      
       SK-BR-3
      
     
       Organism
      
      human
     
       Site primary
      
      breast
     
       Type
      
      cancer
     
       Classification
      
      carcinoma
     
       Primary Cell line
      
      transformed
     
       Description
      
      breast adenocarcinoma
     
       Cell line
      
      SK-HEP-1
     
       Organism
      
      human
     
       Site primary
      
      liver
     
       Type
      
      cancer
     
       Classification
      
      carcinoma
     
       Primary Cell line
      
     
       Description
      
      liver adenocarcinoma
     
       Cell line
      
      
       SK-MEL-5
      
     
       Organism
      
      human
     
       Site primary
      
      skin
     
       Type
      
      cancer
     
       Classification
      
      melanoma
     
       Primary Cell line
      
      transformed
     
       Description
      
      malignant melanoma
     
       Cell line
      
      
       SK-OV-3
      
     
       Organism
      
      human
     
       Site primary
      
      ovary
     
       Type
      
      cancer
     
       Classification
      
      carcinoma
     
       Primary Cell line
      
      transformed
     
       Description
      
      ovarian adenocarcinoma
     
       Cell line
      
      
       SW 1088
      
     
       Organism
      
      human
     
       Site primary
      
      brain
     
       Type
      
      cancer
     
       Classification
      
      glioblastoma
     
       Primary Cell line
      
      transformed
     
       Description
      
      astrocytoma
     
       Cell line
      
      
       SW480
      
     
       Organism
      
      human
     
       Site primary
      
      colon
     
       Type
      
      cancer
     
       Classification
      
      carcinoma
     
       Primary Cell line
      
      transformed
     
       Description
      
      colorectal adenocarcinoma
     
       Cell line
      
      THP-1
     
       Organism
      
      human
     
       Site primary
      
      monocyte
     
       Type
      
      cancer
     
       Classification
      
      leukemia
     
       Primary Cell line
      
      transformed
     
       Description
      
      Acute monocytic leukemia
     
       Cell line
      
      
       U-138 MG
      
     
       Organism
      
      human
     
       Site primary
      
      brain
     
       Type
      
      cancer
     
       Classification
      
      glioblastoma
     
       Primary Cell line
      
      transformed
     
       Description
      
      astrocytoma
     
       Cell line
      
      
       U2OS
      
     
       Organism
      
      human
     
       Site primary
      
      bone
     
       Type
      
      cancer
     
       Classification
      
      sarcoma
     
       Primary Cell line
      
      transformed
     
       Description
      
      osteosarcoma
     
       Cell line
      
      
       U-937
      
     
       Organism
      
      human
     
       Site primary
      
      blood
     
       Type
      
      cancer
     
       Classification
      
      lymphoma
     
       Primary Cell line
      
      transformed
     
       Description
      
      histiocytic lymphoma
     
       Cell line
      
      
       ZR-75-1
      
     
       Organism
      
      human
     
       Site primary
      
      breast
     
       Type
      
      cancer
     
       Classification
      
      carcinoma
     
       Primary Cell line
      
      transformed
     
       Description
      
      breast adenocarcinoma
     
                                        ReceptorX platform 
                                    
The platform consists of different panels of biochemical and cell-based assays and represents exclusive asset of the infrastructure, accessible to large scientific community from both academia and industry. The core of the platform consists of selective and sensitive clonal reporter cell lines for individual nuclear receptors employing multiple reporter luciferase enzymes. The platform is built as a complex multi-level system of different assay types allowing for profiling of large compound libraries with exceptionally low rate of false positives as well as for detailed selectivity studies of small focused chemical libraries providing highly biologically relevant information about compound activities.
    
    
        Nuclear receptors:
        
            ERα, ERβ, AR, PR, GR, MR, ERRγ, FXR, LXRα, LXRβ, PPARα, PPARβ, PPARγ, PXR, CAR, TRα, TRβ
            RARα, RARβ, RARγ, VDR, RXRα, RXRβ, RXRγ, RORα, RORβ, RORγ, NURR1, SF-1, LRH-1, NGFI-B
        
    
        
            Link to individual receptors at Guide to Pharmacology
        
    
        
    
        PathWAY platform            
    
The platform is based on cell-based luciferase reporter cell lines that are used to identify regulators (agonists/antagonists) of various signaling pathways: e.g. Wnt pathway (GO:0016055, R-HSA-195721), hypoxia pathway (GO:0071456, R-HSA-12341740), Shh pathway (GO:0007224), calcineurin/NF-AT signaling (GO:003317300), cAMP signaling (GO:0019933), NFkB signaling (GO:0007249), IL-6 signaling (GO:0070102), p53/DNA damage response (GO:0006976).
    For more information on assay development see 
    The Assay Gudiance Manual from NIH

 
                             
                             
                             
                             
                            