SU11652 [Ligand Id: 6043] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL13485 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| epidermal growth factor receptor/Epidermal growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] | ||||||||
| ChEMBL | Inhibition of epidermal growth factor receptor (EGF-R) | B | 4.7 | pIC50 | >20000 | nM | IC50 | J Med Chem (2003) 46: 1116-1119 [PMID:12646019] |
| ChEMBL | Inhibition of EGFR | B | 4.7 | pIC50 | >20000 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
| ChEMBL | Inhibition of EGFR | B | 5.52 | pIC50 | 3000 | nM | IC50 | J Biol Chem (2007) 282: 6833-6842 [PMID:17197699] |
| fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362] | ||||||||
| ChEMBL | Inhibition of Fibroblast growth factor receptor 1 | B | 6.77 | pIC50 | 170 | nM | IC50 | J Med Chem (2003) 46: 1116-1119 [PMID:12646019] |
| ChEMBL | Inhibition of FGFR1 | B | 6.77 | pIC50 | 170 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
| GtoPdb | - | - | 6.77 | pIC50 | 170 | nM | IC50 | J Med Chem (2003) 46: 1116-9 [PMID:12646019] |
| KIT proto-oncogene, receptor tyrosine kinase/Mast/stem cell growth factor receptor Kit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721] | ||||||||
| GtoPdb | - | - | 8 | pIC50 | 10 | nM | IC50 | Proc Natl Acad Sci USA (2007) 104: 20523-8 [PMID:18077363] |
| ChEMBL | Inhibition of c-kit | B | 8 | pIC50 | 10 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
| maternal embryonic leucine zipper kinase/Maternal embryonic leucine zipper kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4578] [GtoPdb: 2102] [UniProtKB: Q14680] | ||||||||
| ChEMBL | Inhibition of His6-tagged MELK catalytic domain (1 to 340 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) cells using Bcl-GL as substrate measured after 30 mins in presence of [gamma32P]ATP by liquid scintillation counting method | B | 6.12 | pIC50 | 760 | nM | IC50 | Bioorg Med Chem (2017) 25: 2609-2616 [PMID:28351607] |
| ChEMBL | MELK Inhibitor Library Screening assay: MELK and its substrate, Bcl-G were both recombinantly expressed and purified for use in screening assays (See Methods). 752 compounds from an in-house curated inhibitor library were subjected to a p81-based kinase assay. 10 nM MELK 340 and 10 μM Bcl-GL in kinase assay buffer (50 mM HEPES pH 7.5, 100 mM KCl, 0.1 mM EDTA, 0.1 mM EGTA, 10 mM MgCl2, 10 μg/mL BSA) with 10 mM DTT were added to either 10 μM or 1 μM inhibitor aliquoted into 96 well plates (final 1% DMSO). The mixture was incubated at room temperature for 30 minutes prior to initiation of the assay with 40 μM γ-32P-ATP (100-1000 CPM/pmol). 40 μL aliquots were spotted onto a p81 96 well filter plate (Unifilter, Whatman), quenched, and washed with 75 mM O-phosphoric acid 8 times, followed by a final wash with acetone for drying. Wells were then filled with scintillation fluid, sealed, and quantified using a MicroBeta TriLux liquid scintillation counter (PerkinElmer). Each inhibitor plate was assayed in duplicate, with at least 4 wells without MELK to establish background and at least 4 wells without inhibitor as a negative control. All readings were corrected for background signal based on the average counts from the wells without enzyme. Percent inhibition, defined as [100−(CPM+inhibitor/average CPM of positive controls)*100], was determined first at 10 μM inhibitor. The top 50 inhibitors were then re-screened in duplicate at 1 μM. | B | 6.12 | pIC50 | 760 | nM | IC50 | US-10981896-B2. Indolinone derivatives as inhibitors of maternal embryonic leucine zipper kinase (2021) |
| platelet derived growth factor receptor beta/platelet derived growth factor receptor alpha in Human [GtoPdb: 1804, 1803] [UniProtKB: P09619, P16234] | ||||||||
| GtoPdb | - | - | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2003) 46: 1116-9 [PMID:12646019] |
| platelet derived growth factor receptor beta/platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor in Mouse (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096980] [GtoPdb: 1804, 1803] [UniProtKB: P05622, P26618] | ||||||||
| ChEMBL | Inhibition of Platelet-derived growth factor induced 3T3 cell proliferation | F | 7 | pIC50 | 100 | nM | IC50 | J Med Chem (2003) 46: 1116-1119 [PMID:12646019] |
| ChEMBL | Inhibition of PDGF-induced BrdU incorporation in 3T3 cells | F | 7.15 | pIC50 | <70 | nM | IC50 | J Med Chem (2003) 46: 1116-1119 [PMID:12646019] |
| platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1913] [GtoPdb: 1804] [UniProtKB: P09619] | ||||||||
| ChEMBL | Inhibition of PDGFRbeta | B | 5.52 | pIC50 | 3000 | nM | IC50 | J Biol Chem (2007) 282: 6833-6842 [PMID:17197699] |
| GtoPdb | - | - | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2003) 46: 1116-9 [PMID:12646019] |
| ChEMBL | Inhibition of Platelet-derived growth factor receptor beta (PDGF-Rbeta) | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2003) 46: 1116-1119 [PMID:12646019] |
| ChEMBL | Inhibition of PDGFRbeta | B | 8.52 | pIC50 | 3 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
| NIMA related kinase 2/Serine/threonine-protein kinase Nek2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3835] [GtoPdb: 2117] [UniProtKB: P51955] | ||||||||
| ChEMBL | Inhibition of human recombinant Nek2 T175A mutant by coupled pyruvate kinase/lactate dehydrogenase assay | B | 5.1 | pIC50 | 8000 | nM | IC50 | J Biol Chem (2007) 282: 6833-6842 [PMID:17197699] |
| kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968] | ||||||||
| ChEMBL | Inhibition of VEGFR2 | B | 5.52 | pIC50 | 3000 | nM | IC50 | J Biol Chem (2007) 282: 6833-6842 [PMID:17197699] |
| ChEMBL | Inhibition of Vascular endothelial growth factor receptor 2 | B | 7.57 | pIC50 | 27 | nM | IC50 | J Med Chem (2003) 46: 1116-1119 [PMID:12646019] |
| ChEMBL | Inhibition of VEGFR2 | B | 7.57 | pIC50 | 27 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
| GtoPdb | - | - | 7.57 | pIC50 | 27 | nM | IC50 | J Med Chem (2003) 46: 1116-9 [PMID:12646019] |
ChEMBL data shown on this page come from version 36:
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]
