CS / EN
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.
Viability/proliferation assays
ATP, Redox, 3H-Thy
Apoptosis/Cell death
Caspase 3/7, Annexin V
Cytotoxicity/Necrosis
LDH, protease
Ca2+ mobilization (FLIPR)
GPCRs, Ion channels
Cell cycle analysis
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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
HL-60
Organism
human
Site primary
blood
Type
cancer
Classification
leukemia
Primary Cell line
transformed
Description
acute myeloid leukaemia
Cell line
K562
Organism
human
Site primary
blood
Type
cancer
Classification
leukemia
Primary Cell line
transformed
Description
chronic myelogenous leukemia
Cell line
U-937
Organism
human
Site primary
blood
Type
cancer
Classification
lymphoma
Primary Cell line
transformed
Description
histiocytic lymphoma
Cell line
U2OS
Organism
human
Site primary
bone
Type
cancer
Classification
sarcoma
Primary Cell line
transformed
Description
osteosarcoma
Cell line
BT-20
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
SK-BR-3
Organism
human
Site primary
breast
Type
cancer
Classification
carcinoma
Primary Cell line
transformed
Description
breast adenocarcinoma
Cell line
T47D
Organism
human
Site primary
breast
Type
cancer
Classification
carcinoma
Primary Cell line
transformed
Description
breast adenocarcinoma
Cell line
D283 Med
Organism
human
Site primary
brain
Type
cancer
Classification
blastoma
Primary Cell line
transformed
Description
medulloblastoma
Cell line
HCT116
Organism
human
Site primary
colon
Type
cancer
Classification
carcinoma
Primary Cell line
transformed
Description
colorectal adenocarcinoma
Cell line
HT-29
Organism
human
Site primary
colon
Type
cancer
Classification
carcinoma
Primary Cell line
transformed
Description
colorectal adenocarcinoma
Cell line
LS174T
Organism
human
Site primary
colon
Type
cancer
Classification
carcinoma
Primary Cell line
transformed
Description
colorectal adenocarcinoma
Cell line
RKO
Organism
human
Site primary
colon
Type
cancer
Classification
carcinoma
Primary Cell line
transformed
Description
colorectal adenocarcinoma
Cell line
SW480
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
BNL 1ME A.7R.1
Organism
mouse
Site primary
liver
Type
normal
Classification
normal
Primary Cell line
transformed
Description
normal hepatocytes
Cell line
Hep G2
Organism
human
Site primary
liver
Type
cancer
Classification
carcinoma
Primary Cell line
transformed
Description
hepatocellular carcinoma
Cell line
RD
Organism
human
Site primary
muscle
Type
cancer
Classification
sarcoma
Primary Cell line
transformed
Description
rhabdomyosarcoma
Cell line
SJCRH30
Organism
human
Site primary
muscle
Type
cancer
Classification
sarcoma
Primary Cell line
transformed
Description
rhabdomyosarcoma
Cell line
Caov-3
Organism
human
Site primary
ovary
Type
cancer
Classification
carcinoma
Primary Cell line
transformed
Description
ovarian adenocarcinoma
Cell line
SK-OV-3
Organism
human
Site primary
ovary
Type
cancer
Classification
carcinoma
Primary Cell line
transformed
Description
ovarian adenocarcinoma
Cell line
DU 145
Organism
human
Site primary
prostate
Type
cancer
Classification
carcinoma
Primary Cell line
transformed
Description
prostate adenocarcinoma
Cell line
LNCaP
Organism
human
Site primary
prostate
Type
cancer
Classification
carcinoma
Primary Cell line
transformed
Description
prostate adenocarcinoma
Cell line
PC-3
Organism
human
Site primary
prostate
Type
cancer
Classification
carcinoma
Primary Cell line
transformed
Description
prostate adenocarcinoma
Cell line
BJ
Organism
human
Site primary
skin
Type
normal
Classification
normal
Primary Cell line
primary
Description
fibroblasts
Cell line
Caco-2
Organism
human
Site primary
colon
Type
cancer
Classification
carcinoma
Primary Cell line
transformed
Description
colorectal adenocarcinoma
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
NCI-H460
Organism
human
Site primary
lung
Type
cancer
Classification
carcinoma
Primary Cell line
transformed
Description
large cell lung carcinoma
Cell line
SK-MEL-5
Organism
human
Site primary
skin
Type
cancer
Classification
melanoma
Primary Cell line
transformed
Description
malignant melanoma
Cell line
Caki-1
Organism
human
Site primary
kidney
Type
cancer
Classification
carcinoma
Primary Cell line
transformed
Description
clear cell carcinoma
Cell line
U-138 MG
Organism
human
Site primary
brain
Type
cancer
Classification
glioblastoma
Primary Cell line
transformed
Description
astrocytoma
Cell line
SW 1088
Organism
human
Site primary
brain
Type
cancer
Classification
glioblastoma
Primary Cell line
transformed
Description
astrocytoma
Cell line
HT29-MTX-E12
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
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
JAR
Organism
human
Site primary
placenta
Type
cancer
Classification
carcinoma
Primary Cell line
transformed
Description
Choriocarcinoma
Cell line
HuH7
Organism
human
Site primary
liver
Type
cancer
Classification
carcinoma
Primary Cell line
Description
liver carcinoma
Cell line
SK-HEP-1
Organism
human
Site primary
liver
Type
cancer
Classification
carcinoma
Primary Cell line
Description
liver 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
Chemical libraries (or compound collections/sets) are one of the essential components for research areas of chemical biology and medicinal chemistry. Chemical libraries are collections of small organic compounds, usable in drug discovery and other industrial processes.
For the selection of new compounds, we employ advanced cheminformatic tools. High degree of chemical diversity is one of the fundamental requirements for chemical library used in high throughput screening (HTS). Conversely, we sort and compile the compounds with similar properties (structural, physicochemical, pharmacological, etc.) into smaller, focused sub-libraries also called subsets. By utilizing such specialized subsets, higher economic and time efficiency of the biological activity testing can be achieved.
Our sample collection grows dynamically, and almost every day the sample count is expanding. The highest possible quality of the individual samples in the library is essential for providing reliable and reproducible screening results. Compound integrity in time is assured by optimal storage conditions (-20 °C, nitrogen atmosphere) and gentle handling conditions (limiting freeze-thaw cycles, limited exposure to atmospheric environment, protection of light-sensitive samples from daylight, etc.). Identity of the chemical samples is assured by following strict rules for registration and handling, which contain a series of security checkpoints to prevent unwanted sample confusion.
For more information on Compound management at CZ-OS, please visit section: Equipment/Compound Management
174,884
DIVERSITY SETS
9,173
BIOACTIVES
7,152
INDUSTRIAL
4,695
ACADEMIC
2,738
NATURAL PRODUCTS
DIVERSITY SETS
~174,448 compounds
wide coverage of chemical space custom compiled sets of chemicals lead-like and drug-like compounds IP-free
ChemBridge Diverse set
25K
Enamine Diverse set
45K
NCI Diversity II
1.4K
EU-OS ECBL Diversity set
99K
BIOACTIVES
9,173 compounds
curated set of tool compounds, chemical probes, and drugs including precompiled commercial libraries from Sigma, Prestwick and Cayman Chemical (prostagnadins and fatty acids)
CZ-OPENSCREEN bioactive set
2.6K
EU-OPENSCREEN bioactive set
2.4K
COMMERCIAL SETS
4.1K
OTHER
~15,000 compounds
proprietary chemical substances donated by academic/commercial research groups commercially inaccessible chemistry
Academic chemistry collection
4.7K
Industrial chemistry collection
7.1K
Natural Products and Extracts
2.8K
3
Compound management
Compound management
Storage
1
2x asmStore (Hamilton)
Module stores, picks, and compiles individual microtube racks/microplates in a temperature controlled, nitrogen environment.
2
asmServer (Hamilton)
Input/output module for asmStore modules. Provides an environmentally controlled storage buffer of up to 40 microtube racks or microplates.
4
Readers & dispensers
Device
Type
Plate types
Parameters
Type
Multimode reader
Plate types
96/384/1536
Parameters
Filter based: fluorescence intensity inc. FRET, time-resolved fluorescence, luminescence, absorbance, fluorescence polarization, AlphaScreen/AlphaLISA
Type
Multimode reader
Plate types
96/384/1536
Parameters
Filter based: fluorescence intensity, time-resolved fluorescence, luminescence, absorbance, fluorescence polarization, AlphaLISA/AlphaScreen
Type
Multimode reader
Plate types
96/384
Parameters
Monochromator based: label-free EPIC technology (Corning), fluorescence intensity, absorbance
Type
Multimode reader
Plate types
24/96/384, tubes
Parameters
12-detectors: Radiometry, luminescence
Type
Multimode reader
Plate types
384
Parameters
Fluorescence (FLIPR assays, FRET), luminescence (BRET)
Type
Microscope
Plate types
96/384/1536, slides
Parameters
Confocal-based, Dual spinning disk (Nipkow), 4x sCMOS camera, Lasers: 405 nm, 445 nm, 488 nm, 561 nm, 640 nm and 365 nm UV light source; Objectives: 4x, 10x, 20x, 40x, 60x magnification.
Type
Microscope
Plate types
96/384/1536, slides
Parameters
Filter-based. Fluorescence, brightfield and digital phase contrast images. Confocal and wide-field.
Type
Label-free
Plate types
384/1536
Parameters
Acoustic Ejection Mass Spectrometry (AEMS) system, Acoustic droplet ejection, SCIEX Triple Quad 6500+ mass spectrometer
Type
Label-free
Plate types
384
Parameters
Impedance-based. High-throughput Instrument uses biosensors to continuously monitor cell proliferation, morphology change, and attachment quality with a label-free protocol
Type
Label-free
Plate types
96
Parameters
Impedance-based. Instrument uses biosensors to continuously monitor cell proliferation, morphology change, and attachment quality with a label-free protocol
Type
Liquid handling
Plate types
384/1536
Parameters
Acoustic Liquid Handler for a High-throughput assays. Volumes from 2.5 nl
Type
Liquid handling
Plate types
96/384/1536
Parameters
Multipurpose dispenser. Possible to dispense as many as 12 different reagents simultaneously by utilizing 96 independently controlled outputs. Dispense any volume, of any reagent, into any well.
Type
Liquid handling
Plate types
96/384/1536
Parameters
Modular dispensor with 8 individually controllable channels.
Type
Liquid handling
Plate types
96/384/1536
Parameters
A Reagent Dispenser with precise dispensing over a 0.5 to 2500μL range
Type
Liquid handling
Plate types
96/384
Parameters
An automated liquid handling workstations for flexible automated sample preparation. 384-well pipetting head, Pintool (25nl)
Type
Liquid handling
Plate types
96/384/1536
Parameters
Centrifugation technology for removing liquids.
Type
Liquid handling
Plate types
384
Parameters
Automated Microplate Washer