SU11274 [Ligand Id: 5057] activity data from GtoPdb and ChEMBL
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: CHEMBL261641 (SU-11274) |
|---|
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 2/Cyclin-dependent kinase 2/cyclin E1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907605] [GtoPdb: 1973] [UniProtKB: P24864, P24941] | ||||||||
| ChEMBL | Inhibition of human recombinant CDK2/CycE using HHASPRK as substrate by ESI-MS analysis | B | 6.31 | pKi | 489.78 | nM | Ki | J Med Chem (2012) 55: 1926-1939 [PMID:22289061] |
| MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581] | ||||||||
| ChEMBL | Inhibition of Met-mediated tumorigenesis in HGF-stimulated human HepG2 cells assessed as impairment in anchorage-independent growth by soft agar growth assay | B | 5.81 | pIC50 | 1561 | nM | IC50 | Eur J Med Chem (2012) 47: 239-254 [PMID:22138308] |
| ChEMBL | Inhibition of Met-mediated tumorigenesis in HGF-stimulated human GTL16 cells assessed as impairment in anchorage-independent growth by soft agar growth assay | B | 6.64 | pIC50 | 228 | nM | IC50 | Eur J Med Chem (2012) 47: 239-254 [PMID:22138308] |
| ChEMBL | Inhibition of Met-mediated scattering in HGF-stimulated human MDCK cells pre-incubated overnight prior to HGF stimulation for 24 hrs measured after 24 to 48 hrs | B | 6.82 | pIC50 | 152 | nM | IC50 | Eur J Med Chem (2012) 47: 239-254 [PMID:22138308] |
| ChEMBL | Inhibition of human c-MET | B | 7.7 | pIC50 | 20 | nM | IC50 | Eur J Med Chem (2011) 46: 3675-3680 [PMID:21641696] |
| ChEMBL | Inhibition of Met kinase | B | 7.7 | pIC50 | 20 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
| ChEMBL | Inhibition of purified recombinant c-Met after 60 mins by ELISA | B | 7.85 | pIC50 | 14 | nM | IC50 | J Med Chem (2011) 54: 2127-2142 [PMID:21405128] |
| GtoPdb | Assay used a GST fusion with the cytoplasmic domain of human Met. | - | 8 | pIC50 | 10 | nM | IC50 | Mol Cancer Ther (2003) 2: 1085-92 [PMID:14617781] |
| ChEMBL | Inhibition of human recombinant c-MET kinase in A549 cells assessed as inhibition of HGF-induced cell growth | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2011) 54: 6342-6363 [PMID:21812414] |
| Hepatocyte growth factor receptor in Dog (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2046265] [UniProtKB: Q75ZY9] | ||||||||
| ChEMBL | Inhibition of Met-triggered cell scattering in HGF-stimulated MDCK cells preincubated for overnight before HGF challenge measured after 24 to 48 hrs | B | 6.7 | pIC50 | 200 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4693-4696 [PMID:22738633] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antimalarial activity against Plasmodium falciparum W2mef trophozoite form by hoechst 33342-thiazole orange stain based flow cytometry assay | F | 6.21 | pIC50 | 620 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 5452-5457 [PMID:19666223] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum W2mef assessed as DNA positive erythrocytes by hoechst 33342-thiazole orange stain based flow cytometry assay | F | 6.49 | pIC50 | 320 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 5452-5457 [PMID:19666223] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum W2mef schizont form by hoechst 33342-thiazole orange stain based flow cytometry assay | F | 6.5 | pIC50 | 317 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 5452-5457 [PMID:19666223] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum W2mef ring form by hoechst 33342-thiazole orange stain based flow cytometry assay | F | 6.64 | pIC50 | 228 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 5452-5457 [PMID:19666223] |
| protein tyrosine kinase 2 beta/Protein tyrosine kinase 2 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5469] [GtoPdb: 2181] [UniProtKB: Q14289] | ||||||||
| ChEMBL | Inhibition of human recombinant PYK2 by ESI-MS analysis | B | 7.98 | pKi | 10.47 | nM | Ki | J Med Chem (2012) 55: 1926-1939 [PMID:22289061] |
| zeta chain of T cell receptor associated protein kinase 70/Tyrosine-protein kinase ZAP-70 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2803] [GtoPdb: 2285] [UniProtKB: P43403] | ||||||||
| ChEMBL | Inhibition of human recombinant ZAP70 using EEEEYEEEE as substrate by ESI-MS analysis | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2012) 55: 1926-1939 [PMID:22289061] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
