SU11274 [Ligand Id: 5057] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL261641 (SU-11274) |
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| 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 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]
