Targeted-Oncology

Product Name: Format/SizeDescriptionsDownload
Targeted Oncology Library6728 compounds
For cherry-picking
Update: 2016-11
The file contains all available Targeted-Oncology compounds selected from our Signature & BioDesign Libraries. For more information, please download >>>sdf-icon
SL#029
IDH inhibitors - Cancer Metabolism
80 compounds
Pre-Plated Set
Release: 2016
Identified pharmacophore features of known IDH inhibitors and a subsequent search across the ASINEX corporate collection has revealed several quinolone-based analogs available at ASINEX. With these compounds as a starting point, ASINEX has applied its medicinal chemistry expertise in creating an array of novel small molecules potentially interesting for IDH-related research.
Structures are available,"click here"and downlaod "File#1 (1/5) Signature Libraries.
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SL#043
State1(T) inhibitors of activated Ras
80 compounds
Pre-Plated Set
Release: 2016
ASINEX has identified several rigid analogs of BPA that are able to coordinate with Metal(II) ions and can therefore be exploited as chemical probes for Ras-related research.
Structures are available,"click here"and downlaod "File#1 (1/5) Signature Libraries.
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SL#053
Katanin inhibitors
80 compounds
Pre-Plated Set
Release: 2016
2D similarity search through ASINEX’s compound collection identified several close analogs of known katanin inhibitors that could be interesting for katanin-related research and MTA drug discovery.
Structures are available,"click here"and downlaod "File#1 (1/5) Signature Libraries.
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SL#066
Inhibitors of miсroRNA-21
80 compounds
Pre-Plated Set
Release: 2017
Small molecules that can bind directly to microRNA-21 (miR-21) have been suggested as a promising new therapy for the treatment of cancer. Screening a large library of drug-like small molecules has identified several chemotypes that bind to the pre-miR-21 hairpin with high selectivity against other oligonucleotides. The most potent hit molecules share the common 1-amino-3-(9H-carbazol-9-yl)propan-2-ol scaffold which can be considered a privileged fragment. 80 molecules containing this privileged fragment were included in this library.
Structures are available,"click here"and downlaod "File#1 (1/5) Signature Libraries.
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SL#071
Taxol pharmacophore chemical probes
80 compounds
Pre-Plated Set
Release: 2017
Structures are available,"click here"and downlaod "File#1 (1/5) Signature Libraries.
SL#085
Tubulin Inhibitors    
80 compounds
Pre-Plated Set
Release: 2018
Structures are available,"click here"and downlaod "File#1 (1/5) Signature Libraries.
SL#087
elF4A3 inhibitors  
80 compounds
Pre-Plated Set
Release: 2018
Structures are available,"click here"and downlaod "File#1 (1/5) Signature Libraries.

 

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Product Name: Format/SizeDescriptionsDownload
SL#003
Wnt/β-catenin Pathway Inhibitors
80 compounds
Pre-Plated Set
Release: 2016
ASINEX has screened 21000 small molecules in a luciferase reporter assay using the colorectal cancer cell lines, SW620 (APC mutation) and HCT116 (GSK3b mutation). Selected primary hits were optimized to yield an array of active compounds showing EC50 0.1-5 uM. The most promising compounds down regulate the expression of the key WNT oncogenes: DKK, cycD, CD44.
Structures are available,"click here"and downlaod "File#1 (1/5) Signature Libraries.
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SL#001
Mcl-1 Apoptosis
80 compounds
Pre-Plated Set
Release: 2016
ASINEX has developed several acylsulfonamide derivatives with Mcl-1 binding potency and improved physico-chemical characteristics.
Structures are available,"click here"and downlaod "File#1 (1/5) Signature Libraries.
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SL#002
Bcl-xL Apoptosis
80 compounds
Pre-Plated Set
Release: 2016
ASINEX has identified dihydrobenzofurane as a functional a-helix mimetic displaying uM Bcl-xL binding affinity determined by a fluorescence polarization assay.
Structures are available,"click here"and downlaod "File#1 (1/5) Signature Libraries.
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SL#011
MDM2-p53 (α-Helix mimetics)
80 compounds
Pre-Plated Set
Release: 2016
ASINEX has performed in-silico analyses of common structural futures of known MDM2 antagonists to build up a predictive pharmacophore model [1]. Several ɑ-helix mimetic scaffolds were selected as p53 backbone mimetics and p53 binding epitope mimetics [2,3]. The in vitro potency of compounds was confirmed in a fluorescence polarization assay, with the IC50s ranging from 1 to 10 µM.
Structures are available,"click here"and downlaod "File#1 (1/5) Signature Libraries.
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Product Name: Format/SizeDescriptionsDownload
Immuno-Oncology Library11346 compounds
For cherry-picking
Update: 2016-11
The file contains all available Immuno-Oncology compounds selected from our Signature & BioDesign Libraries. For more information, please download >>>sdf-icon pdf-icon
SL#021
IDO1 inhibitors
80 compounds
Pre-Plated Set
Release: 2016
By utilizing a combination of scaffold hopping and structure-based design strategies ASINEX has developed a library of small molecules for IDO1 drug discovery. Selected compounds have shown significant IDO1 inhibitory activity in vitro as measured in the enzymatic biochemical assays.
Structures are available,"click here"and downlaod "File#1 (1/5) Signature Libraries.
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SL#026
IRAK4 inhibitors
80 compounds
Pre-Plated Set
Release: 2016
ASINEX has created a series of IRAK4-oriented compounds by combining the IRAK4 hinge binding motif with proprietary natural product-like fragments. Several compounds from this library were screened against IRAK4 kinase in vitro and showed sub-uM IC50. Sunitinib was also included in the library as a reference compound.
Structures are available,"click here"and downlaod "File#1 (1/5) Signature Libraries.
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SL#033
PD1/PD-L1 inhibitors
80 compounds
Pre-Plated Set
Release: 2016
ASINEX has designed a set of novel small molecule probes that can be used for exploration of PD-1/PD-L1 signaling pathway.
Structures are available,"click here"and downlaod "File#1 (1/5) Signature Libraries.
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Phenotypic Screening Sets: Format/SizeDescriptionsDownload
Phenotypic Pre-Plated Set14320 compounds
Pre-Plated Set
Amount: 0.01-2.0 mg
Update: 2017-03
ASINEX has created a diverse set of molecules by applying strict physico-chemical and structural descriptors to ensure good solubility and permeability properties. For more information, please download >>>sdf-icon pdf-icon
SL#004
Oncology Phenotypic Screening-1
(Non-Macrocycle)
80 compounds / set
Pre-Plated Set
Release: 2016
ASINEX's oncology-oriented phenotypic library includes compounds based on several scaffolds with proven cytotoxicity (sub-µM EC50 in MTT assay) against a number of cancer cell lines: MV-411 (acute monocytic leukemia), HCT-116 (human colon cancer), MCF-7 (human breast adenocarcinoma‎), A-172 (Human glioblastoma), COLO-320 (colorectal adenocarcinoma), U-937 (histiocytic lymphoma), A-375 (malignant melanoma), BXPC-3 (pancreas adenocarcinoma), U118-MG (malignant glioma), and LN-229 (glioblastoma). Some active compounds were screened in a biochemical assay showing nM level of IC50 against several kinases: Aurora A, Haspin, VEGFR, EGFR, PDGFR.
Structures are available,"click here"and downlaod "File#1 (1/5) Signature Libraries.
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SL#023
Oncology Phenotypic Screening-2
(Colon Cancer/Non-Macrocycle)
80 compounds / set
Pre-Plated Set
Release: 2016
ASINEX has evaluated the susceptibility of several colon cancer cell lines (HCT-116, SW-620, COLO-320, RKO) to a diverse array of small molecules and identified a series of related compounds that kill cancer cells at sub-µM concentrations with limited off target effect on healthy cells (human fibroblasts). Additional screening in a cell-based luciferase reporter assay of Wnt signaling has provided preliminary evidence of Wnt-dependent mechanism of action.
Structures are available,"click here"and downlaod "File#1 (1/5) Signature Libraries.
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SL#035
Oncology Phenotypic Screening-3
(Macrocycles)
80 compounds / set
Pre-Plated Set
Release: 2016
ASINEX has evaluated the susceptibility of several cancer cell lines (i.e. RKO, HCT116, Molt-4, Rs4-11, U937, A549, H1568, H23, PANC1, A2780) to an array of peptidic and non-peptidic macrocycles and identified a series of compounds that kill cancer cells at µM concentrations.
Structures are available,"click here"and downlaod "File#1 (1/5) Signature Libraries.
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Please click here for List of all Signature Libraries.

 

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