Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
ChEMBL ligand: CHEMBL2158866 |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
---|---|---|---|---|---|---|---|---|
cyclin dependent kinase 1/Cyclin-dependent kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL308] [GtoPdb: 1961] [UniProtKB: P06493] | ||||||||
ChEMBL | Inhibition of CDK1 | B | 4.49 | pIC50 | 32000 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 6636-6641 [PMID:23021994] |
cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941] | ||||||||
ChEMBL | Inhibition of CDK2 | B | 5.15 | pIC50 | 7100 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 6636-6641 [PMID:23021994] |
glycogen synthase kinase 3 alpha/Glycogen synthase kinase-3 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2850] [GtoPdb: 2029] [UniProtKB: P49840] | ||||||||
ChEMBL | Inhibition of GSK3alpha | B | 6.59 | pIC50 | 260 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 6636-6641 [PMID:23021994] |
glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841] | ||||||||
ChEMBL | Inhibition of GSK3beta | B | 6.48 | pIC50 | 330 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 6636-6641 [PMID:23021994] |
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/PI3-kinase p110-alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4005] [GtoPdb: 2153] [UniProtKB: P42336] | ||||||||
ChEMBL | Inhibition of PI3Kalpha using diC8-tagged PIP2 as substrate after 30 to 60 mins by TAMRA-based fluorescence polarization assay | B | 7.04 | pIC50 | 92 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 6636-6641 [PMID:23021994] |
GtoPdb | - | - | 7.04 | pIC50 | 92 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 6636-41 [PMID:23021994] |
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma/PI3-kinase p110-gamma subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3267] [GtoPdb: 2156] [UniProtKB: P48736] | ||||||||
GtoPdb | - | - | 7.22 | pIC50 | 60 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 6636-41 [PMID:23021994] |
ChEMBL | Inhibition of PI3Kgamma using diC8-tagged PIP2 as substrate after 30 to 60 mins by TAMRA-based fluorescence polarization assay | B | 7.22 | pIC50 | 60 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 6636-6641 [PMID:23021994] |
mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2842] [GtoPdb: 2109] [UniProtKB: P42345] | ||||||||
GtoPdb | - | - | 7.3 | pIC50 | 50 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 6636-41 [PMID:23021994] |
ChEMBL | Inhibition of mTOR | B | 7.3 | pIC50 | 50 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 6636-6641 [PMID:23021994] |
SMG1 nonsense mediated mRNA decay associated PI3K related kinase/Serine/threonine-protein kinase SMG1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795195] [GtoPdb: 2201] [UniProtKB: Q96Q15] | ||||||||
ChEMBL | Inhibition of human recombinant SMG1 expressed in HEK293 cells using GST-tagged p53 as substrate after 1 hr by DELFIA assay | B | 9.96 | pIC50 | 0.11 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 6636-6641 [PMID:23021994] |
GtoPdb | - | - | 9.96 | pIC50 | 0.11 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 6636-41 [PMID:23021994] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]