SU11274 [Ligand Id: 5057] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL261641 (SU-11274)
  • cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin E1 in Human [ChEMBL: CHEMBL1907605] [GtoPdb: 1973] [UniProtKB: P24864P24941]
  • This target only has 1 pki data point
  • 6.31
1 CHEMBL261641_lig_chart_1 Cyclin-dependent kinase 2/cyclin E1 Human
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  • MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581]
  • Hepatocyte growth factor receptor in Dog [ChEMBL: CHEMBL2046265] [UniProtKB: Q75ZY9]
  • This target only has 0 pki data point
  • 0
2 CHEMBL261641_lig_chart_2 Hepatocyte growth factor receptor HumanDog
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  • Plasmodium falciparum [ChEMBL: CHEMBL364]
  • This target only has 0 pki data point
  • 0
3 CHEMBL261641_lig_chart_3 Plasmodium falciparum Plasmodium falciparum
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  • protein tyrosine kinase 2 beta/Protein tyrosine kinase 2 beta in Human [ChEMBL: CHEMBL5469] [GtoPdb: 2181] [UniProtKB: Q14289]
  • This target only has 1 pki data point
  • 7.98
4 CHEMBL261641_lig_chart_4 Protein tyrosine kinase 2 beta Human
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  • zeta chain of T cell receptor associated protein kinase 70/Tyrosine-protein kinase ZAP-70 in Human [ChEMBL: CHEMBL2803] [GtoPdb: 2285] [UniProtKB: P43403]
  • This target only has 1 pki data point
  • 5
5 CHEMBL261641_lig_chart_5 Tyrosine-protein kinase ZAP-70 Human
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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: P24864P24941]
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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]