semaxanib [Ligand Id: 5056] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL276711 (NSC-696819, Semaxanib, Semaxinib, SU005416, Su-5416, SU-5416, SU5416) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73] | ||||||||
| ChEMBL | Inhibition of ALK using FL-Peptide 13, 5-FAM-KKSRGDYMTMQIG-CONH2 substrate after 60 mins by mobility shift assay | B | 5.74 | pIC50 | 1810 | nM | IC50 | Bioorg Med Chem (2011) 19: 3086-3095 [PMID:21515061] |
| ChEMBL | Inhibition of ALK by ELISA-based kinase assay | B | 5.92 | pIC50 | 1200 | nM | IC50 | Bioorg Med Chem (2010) 18: 1482-1496 [PMID:20117004] |
| cyclin dependent kinase 1/Cyclin-dependent kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL308] [GtoPdb: 1961] [UniProtKB: P06493] | ||||||||
| ChEMBL | In vitro inhibition of Cyclin-dependent kinase 1 (CDK-1) expressed in baculovirus | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2002) 45: 5687-5693 [PMID:12477352] |
| epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] | ||||||||
| ChEMBL | Inhibition of epidermal growth factor receptor (EGF-R) | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2003) 46: 1116-1119 [PMID:12646019] |
| ChEMBL | Inhibitory activity against Epidermal growth factor receptor | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1999) 42: 5120-5130 [PMID:10602697] |
| ChEMBL | Concentration required to achieve 50% inhibition of tyrosine phosphorylation on human Epidermal growth factor receptor (EGF RTK). | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1998) 41: 2588-2603 [PMID:9651163] |
| ChEMBL | Inhibition of EGFR (unknown origin) after 20 mins by scintillation counting | B | 4 | pIC50 | >100000 | nM | IC50 | J Nat Prod (2013) 76: 715-719 [PMID:23414235] |
| ChEMBL | Evaluated for inhibitory activity towards tyrosine kinase Epidermal growth factor receptor | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2000) 43: 2655-2663 [PMID:10893303] |
| ChEMBL | Inhibitory activity against ligand-dependent EGF cell proliferation | F | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (1999) 42: 5120-5130 [PMID:10602697] |
| ChEMBL | In vitro inhibition of Epidermal growth factor receptor (HER-1,ErbB) expressed in baculovirus | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2002) 45: 5687-5693 [PMID:12477352] |
| 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 | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2003) 46: 1116-1119 [PMID:12646019] |
| ChEMBL | Inhibitory activity of compound against FGF induced cell proliferation | F | 4.3 | pIC50 | 50000 | nM | IC50 | J Med Chem (1999) 42: 5120-5130 [PMID:10602697] |
| ChEMBL | In vitro inhibition of Fibroblast growth factor receptor expressed in baculovirus | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2002) 45: 5687-5693 [PMID:12477352] |
| ChEMBL | Evaluated for inhibitory activity towards Fibroblast growth factor receptor 1 | B | 5.15 | pIC50 | 7080 | nM | IC50 | J Med Chem (2000) 43: 2655-2663 [PMID:10893303] |
| ChEMBL | Inhibitory activity against Fibroblast growth factor receptor 1 | B | 5.15 | pIC50 | 7080 | nM | IC50 | J Med Chem (1999) 42: 5120-5130 [PMID:10602697] |
| ChEMBL | In vitro inhibition of Fibroblast growth factor receptor 1 expressed in baculovirus | B | 5.38 | pIC50 | 4200 | nM | IC50 | J Med Chem (2002) 45: 5687-5693 [PMID:12477352] |
| Insulin-like growth factor I receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069] | ||||||||
| ChEMBL | Concentration required to achieve 50% inhibition of tyrosine phosphorylation on human Insulin-like growth factor I receptor | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1998) 41: 2588-2603 [PMID:9651163] |
| ChEMBL | In vitro inhibition of Insulin-like growth factor I receptor expressed in baculovirus | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2002) 45: 5687-5693 [PMID:12477352] |
| colony stimulating factor 1 receptor/Macrophage colony stimulating factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1844] [GtoPdb: 1806] [UniProtKB: P07333] | ||||||||
| ChEMBL | In vitro inhibition of Colony stimulating factor 1 receptor (CSF-1R) expressed in baculovirus | B | 7.08 | pIC50 | 84 | nM | IC50 | J Med Chem (2002) 45: 5687-5693 [PMID:12477352] |
| macrophage stimulating 1 receptor/Macrophage-stimulating protein receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2689] [GtoPdb: 1816] [UniProtKB: Q04912] | ||||||||
| ChEMBL | In vitro inhibition of Met proto-oncogene tyrosine kinase (c-Met) expressed in baculovirus | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2002) 45: 5687-5693 [PMID:12477352] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay | F | 5.1 | pIC50 | 7943.28 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| platelet derived growth factor receptor beta/platelet derived growth factor receptor alpha in Human [GtoPdb: 1804, 1803] [UniProtKB: P09619, P16234] | ||||||||
| GtoPdb | - | - | 6.17 | pIC50 | 680 | nM | IC50 | J Med Chem (2000) 43: 2310-23 [PMID:10882357] |
| 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 | 4.69 | pIC50 | 20300 | nM | IC50 | J Med Chem (2003) 46: 1116-1119 [PMID:12646019] |
| ChEMBL | Inhibitory activity against Platelet-derived growth factor receptor (PDGF-R) in NIH3T3 mouse fibroblast cells | B | 4.69 | pIC50 | 20260 | nM | IC50 | J Med Chem (1999) 42: 5120-5130 [PMID:10602697] |
| ChEMBL | Inhibition of PDGF-induced BrdU incorporation in 3T3 cells | F | 5.39 | pIC50 | 4050 | nM | IC50 | J Med Chem (2003) 46: 1116-1119 [PMID:12646019] |
| platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2007] [GtoPdb: 1803] [UniProtKB: P16234] | ||||||||
| ChEMBL | Inhibition of PDGFR-alpha (unknown origin) after 20 mins by scintillation counting | B | 6.7 | pIC50 | 200 | nM | IC50 | J Nat Prod (2013) 76: 715-719 [PMID:23414235] |
| 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 | In vitro inhibition of Platelet-derived growth factor receptor beta expressed in baculovirus | B | 4.42 | pIC50 | 37900 | nM | IC50 | J Med Chem (2002) 45: 5687-5693 [PMID:12477352] |
| ChEMBL | Inhibition of Platelet-derived growth factor receptor beta (PDGF-Rbeta) | B | 4.64 | pIC50 | 22900 | nM | IC50 | J Med Chem (2003) 46: 1116-1119 [PMID:12646019] |
| ChEMBL | Test concentration required to achieve 50% inhibition of tyrosine phosphorylation on human Platelet-derived growth factor receptor beta (PDGF RTK). | B | 4.69 | pIC50 | 20260 | nM | IC50 | J Med Chem (1998) 41: 2588-2603 [PMID:9651163] |
| ChEMBL | Inhibitory activity against Platelet-derived growth factor receptor beta | B | 4.98 | pIC50 | 10500 | nM | IC50 | J Med Chem (1999) 42: 5120-5130 [PMID:10602697] |
| ChEMBL | Evaluated for inhibitory activity towards tyrosine kinase PDGF-Rbeta | B | 5 | pIC50 | 10100 | nM | IC50 | J Med Chem (2000) 43: 2655-2663 [PMID:10893303] |
| ChEMBL | Inhibitory activity of compound against PDGF induced cell proliferation | F | 5.34 | pIC50 | 4540 | nM | IC50 | J Med Chem (1999) 42: 5120-5130 [PMID:10602697] |
| ChEMBL | Inhibition of PDGFRbeta in human SF539 cells by phosphotyrosine ELISA | B | 5.62 | pIC50 | 2400 | nM | IC50 | Bioorg Med Chem (2009) 17: 7324-7336 [PMID:19748785] |
| ChEMBL | In vitro inhibition of Platelet-derived growth factor receptor beta expressed in baculovirus | B | 5.65 | pIC50 | 2220 | nM | IC50 | J Med Chem (2002) 45: 5687-5693 [PMID:12477352] |
| ChEMBL | Inhibition of Platelet-derived growth factor receptor beta | B | 6.17 | pIC50 | 680 | nM | IC50 | J Med Chem (2000) 43: 2310-2323 [PMID:10882357] |
| GtoPdb | - | - | 6.17 | pIC50 | 680 | nM | IC50 | J Med Chem (2000) 43: 2310-23 [PMID:10882357] |
| ChEMBL | Inhibition of PDGFR-beta (unknown origin) after 20 mins by scintillation counting | B | 6.4 | pIC50 | 400 | nM | IC50 | J Nat Prod (2013) 76: 715-719 [PMID:23414235] |
| ChEMBL | Inhibition of PDGFRbeta | B | 7.17 | pIC50 | 68 | nM | IC50 | Nat Chem Biol (2006) 2: 265-273 [PMID:16565716] |
| ChEMBL | Inhibition of PDGFRb (unknown origin) | B | 7.17 | pIC50 | 68 | nM | IC50 | Medchemcomm (2014) 5: 1829-1833 |
| erb-b2 receptor tyrosine kinase 2/Receptor protein-tyrosine kinase erbB-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1824] [GtoPdb: 2019] [UniProtKB: P04626] | ||||||||
| ChEMBL | Concentration required to achieve 50% inhibition of tyrosine phosphorylation on human Her-2 receptor tyrosine kinase (HER-2 RTK) | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1998) 41: 2588-2603 [PMID:9651163] |
| KIT proto-oncogene, receptor tyrosine kinase/Stem cell growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721] | ||||||||
| ChEMBL | In vitro inhibition of Mast/stem cell growth factor receptor (c-Kit kinase) expressed in baculovirus | B | 6.18 | pIC50 | 660 | nM | IC50 | J Med Chem (2002) 45: 5687-5693 [PMID:12477352] |
| ChEMBL | Inhibition of Proto-oncogene tyrosine-kinase c-Kit | B | 6.4 | pIC50 | 400 | nM | IC50 | J Med Chem (2000) 43: 2310-2323 [PMID:10882357] |
| GtoPdb | - | - | 6.4 | pIC50 | 400 | nM | IC50 | J Med Chem (2000) 43: 2310-23 [PMID:10882357] |
| ChEMBL | In vitro inhibition of Mast/stem cell growth factor receptor (c-Kit kinase) expressed in baculovirus | B | 7.46 | pIC50 | 35 | nM | IC50 | J Med Chem (2002) 45: 5687-5693 [PMID:12477352] |
| ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519] | ||||||||
| ChEMBL | Inhibition of ABL by ELISA-based kinase assay | B | 4.96 | pIC50 | 11000 | nM | IC50 | Bioorg Med Chem (2010) 18: 1482-1496 [PMID:20117004] |
| ChEMBL | In vitro inhibition of c-Abl tyrosine kinase expressed in baculovirus | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2002) 45: 5687-5693 [PMID:12477352] |
| fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888] | ||||||||
| ChEMBL | Inhibition of FLT3 by ELISA-based kinase assay | B | 6.8 | pIC50 | 160 | nM | IC50 | Bioorg Med Chem (2010) 18: 1482-1496 [PMID:20117004] |
| ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949] | ||||||||
| ChEMBL | Inhibition of human recombinant His-tagged RET expressed in Sf9 insect cells | B | 6.77 | pIC50 | 170 | nM | IC50 | Bioorg Med Chem (2010) 18: 1482-1496 [PMID:20117004] |
| SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931] | ||||||||
| ChEMBL | Evaluated for inhibitory activity towards p60 c-Src tyrosine kinase | B | 4.79 | pIC50 | 16400 | nM | IC50 | J Med Chem (2000) 43: 2655-2663 [PMID:10893303] |
| ChEMBL | In vitro inhibition of c-SRC kinase expressed in baculovirus | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2002) 45: 5687-5693 [PMID:12477352] |
| TEK receptor tyrosine kinase/Tyrosine-protein kinase TIE-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4128] [GtoPdb: 1842] [UniProtKB: Q02763] | ||||||||
| ChEMBL | In vitro inhibition of Tyrosine protein kinase receptor TIE-2 (Tek) expressed in baculovirus | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2002) 45: 5687-5693 [PMID:12477352] |
| 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 GST-fused ZAP-70 expressed in Sf9 cells | B | 4.68 | pIC50 | 20700 | nM | IC50 | Eur J Med Chem (2009) 44: 4793-4800 [PMID:19674816] |
| fms related receptor tyrosine kinase 1/Vascular endothelial growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1868] [GtoPdb: 1812] [UniProtKB: P17948] | ||||||||
| ChEMBL | Inhibition of GST-Flt1 kinase domain (unknown origin) expressed in baculovirus infected Sf9 cells after 20 mins by scintillation counting | B | 5.52 | pIC50 | 3000 | nM | IC50 | J Nat Prod (2013) 76: 715-719 [PMID:23414235] |
| ChEMBL | In vitro inhibition of Vascular endothelial growth factor receptor 1 (VEGFR-1) expressed in baculovirus | B | 7.37 | pIC50 | 43 | nM | IC50 | J Med Chem (2002) 45: 5687-5693 [PMID:12477352] |
| ChEMBL | Inhibition of VEGFR1 (unknown origin) | B | 7.37 | pIC50 | 43 | nM | IC50 | Medchemcomm (2014) 5: 1829-1833 |
| ChEMBL | Inhibition of VEGF-receptor 1, Flt-1 | B | 8.1 | pIC50 | 8 | nM | IC50 | J Med Chem (2000) 43: 2310-2323 [PMID:10882357] |
| GtoPdb | - | - | 8.1 | pIC50 | 8 | nM | IC50 | J Med Chem (2000) 43: 2310-23 [PMID:10882357] |
| fms related receptor tyrosine kinase 1/Vascular endothelial growth factor receptor 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3516] [GtoPdb: 1812] [UniProtKB: P35969] | ||||||||
| ChEMBL | Concentration required to achieve 50% inhibition of tyrosine phosphorylation on murine VEGF receptor (FLK-1 RTK). | B | 5.98 | pIC50 | 1040 | nM | IC50 | J Med Chem (1998) 41: 2588-2603 [PMID:9651163] |
| 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 in human U251 cells by phosphotyrosine cell-based ELISA | B | 4.89 | pIC50 | 12900 | nM | IC50 | J Med Chem (2010) 53: 1563-1578 [PMID:20092323] |
| ChEMBL | Inhibition of recombinant human KDR incubated for 1 hr using Tyr1 substrate by fluorimetry based Z'-LYTE-Tyr1 Peptide assay | B | 4.89 | pIC50 | 12900 | nM | IC50 | ACS Med Chem Lett (2019) 10: 457-462 [PMID:30996779] |
| ChEMBL | Inhibition Assay: Inhibition of various kinase enzyme. | B | 4.89 | pIC50 | 12900 | nM | IC50 | US-9422297-B2. Tricyclic compounds having cytostatic and/or cytotoxic activity and methods of use thereof (2016) |
| ChEMBL | Inhibition Assay: Inhibition of various kinase enzyme. | B | 4.89 | pIC50 | 12900 | nM | IC50 | US-9422297-B2. Tricyclic compounds having cytostatic and/or cytotoxic activity and methods of use thereof (2016) |
| ChEMBL | Inhibition of human KDR incubated for 50 mins by omnia tyr peptide 8 substrate based fluorescence assay | B | 4.89 | pIC50 | 12900 | nM | IC50 | Eur J Med Chem (2015) 103: 29-43 [PMID:26318056] |
| ChEMBL | Inhibition of VEGFR2 in human U251 cells pretreated for 60 mins measured after 1 hr by ELISA | B | 4.89 | pIC50 | 12900 | nM | IC50 | Bioorg Med Chem (2012) 20: 4217-4225 [PMID:22739090] |
| ChEMBL | Inhibition of VEGFR2 expressed in human A431 cells | B | 4.89 | pIC50 | 12900 | nM | IC50 | Bioorg Med Chem (2010) 18: 5261-5273 [PMID:20558072] |
| ChEMBL | Inhibition of VEGFR2 tyrosine kinase activity in VEGF-stimulated human U251 cells after 60 mins by ELISA | B | 4.92 | pIC50 | 12000 | nM | IC50 | Bioorg Med Chem (2012) 20: 910-914 [PMID:22204741] |
| ChEMBL | Inhibition of VEGFR2 phosphorylation in human U251 cells after 10 mins by FLISA | B | 4.92 | pIC50 | 12000 | nM | IC50 | Bioorg Med Chem (2010) 18: 3575-3587 [PMID:20403700] |
| ChEMBL | Inhibition of VEGFR2 in human U251 cells assessed as inhibition of VEGF-induced tyrosine phosphorylation incubated for 60 mins prior to VEGF-activation measured 10 mins by ELISA | B | 4.92 | pIC50 | 12000 | nM | IC50 | Bioorg Med Chem (2013) 21: 1857-1864 [PMID:23434139] |
| ChEMBL | Inhibition of VEGF-induced VEGFR2 phosphorylation in human U251 cells overexpressing Flk-1 pretreated for 60 mins prior to VEGF addition measured after 10 mins by phosphotyrosine ELISA cytoblot analysis | B | 4.92 | pIC50 | 12000 | nM | IC50 | Bioorg Med Chem (2013) 21: 1312-1323 [PMID:23375090] |
| ChEMBL | Inhibition of VEGF-induced VEGFR2 phosphorylation in human U251 cells preincubated for 60 mins followed by VEGF induction measured after 10 mins by ELISA | B | 4.92 | pIC50 | 12000 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 1602-1607 [PMID:28258797] |
| ChEMBL | Inhibition of VEGFR2 expressed in human tumor cells | B | 4.97 | pIC50 | 10600 | nM | IC50 | Bioorg Med Chem (2008) 16: 5514-5528 [PMID:18467105] |
| ChEMBL | Inhibition Assay: Inhibition of various kinase enzyme. | B | 4.97 | pIC50 | 10600 | nM | IC50 | US-9422297-B2. Tricyclic compounds having cytostatic and/or cytotoxic activity and methods of use thereof (2016) |
| ChEMBL | Inhibition of VEGFR2 | B | 4.97 | pIC50 | 10600 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 3177-3181 [PMID:20403693] |
| ChEMBL | Inhibition of VEGF-induced VEGFR2 autophosphorylation in human U251 cells incubated for 60 mins prior to VEGF-induction measured after 10 mins by phosphotyrosine ELISA | B | 5.61 | pIC50 | 2430 | nM | IC50 | Bioorg Med Chem (2012) 20: 2444-2454 [PMID:22370340] |
| ChEMBL | In vitro inhibition of Vascular endothelial growth factor receptor 2 (VEGFR-2) expressed in baculovirus | B | 5.89 | pIC50 | 1300 | nM | IC50 | J Med Chem (2002) 45: 5687-5693 [PMID:12477352] |
| ChEMBL | Inhibition of Vascular endothelial growth factor receptor 2 | B | 5.91 | pIC50 | 1230 | nM | IC50 | J Med Chem (2003) 46: 1116-1119 [PMID:12646019] |
| ChEMBL | Inhibition of KDR (unknown origin) after 20 mins by scintillation counting | B | 6 | pIC50 | 1000 | nM | IC50 | J Nat Prod (2013) 76: 715-719 [PMID:23414235] |
| ChEMBL | Inhibition of VEGFR induced autophosphorylation of human Vascular endothelial growth factor receptor 2 (VEGFR2) transfected in CHO cells | B | 6.05 | pIC50 | 884 | nM | IC50 | J Med Chem (2002) 45: 5687-5693 [PMID:12477352] |
| ChEMBL | Inhibitory activity against Vascular endothelial growth factor receptor 2 | B | 6.15 | pIC50 | 700 | nM | IC50 | J Med Chem (1999) 42: 5120-5130 [PMID:10602697] |
| ChEMBL | Evaluated for inhibitory activity towards tyrosine kinase Vascular endothelial growth factor receptor 2 | B | 6.15 | pIC50 | 700 | nM | IC50 | J Med Chem (2000) 43: 2655-2663 [PMID:10893303] |
| ChEMBL | In vitro inhibition of KDR | B | 6.64 | pIC50 | 230 | nM | IC50 | J Med Chem (2005) 48: 5412-5414 [PMID:16107139] |
| ChEMBL | In vitro inhibition of Vascular endothelial growth factor receptor 2 (VEGFR-2) | B | 6.66 | pIC50 | 220 | nM | IC50 | J Med Chem (2002) 45: 5687-5693 [PMID:12477352] |
| ChEMBL | Inhibition of VEGFR2 | B | 6.66 | pIC50 | 220 | nM | IC50 | Nat Chem Biol (2006) 2: 265-273 [PMID:16565716] |
| ChEMBL | Inhibition of VEGFR2 (unknown origin) | B | 6.66 | pIC50 | 220 | nM | IC50 | Medchemcomm (2014) 5: 1829-1833 |
| ChEMBL | Inhibition of KDR | B | 6.7 | pIC50 | 200 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 2126-2133 [PMID:17306530] |
| ChEMBL | Inhibition of Vascular endothelial growth factor receptor 2 (KDR) | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2000) 43: 2310-2323 [PMID:10882357] |
| GtoPdb | - | - | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2000) 43: 2310-23 [PMID:10882357] |
| ChEMBL | Inhibition of FLK1 | B | 6.96 | pIC50 | 110 | nM | IC50 | Bioorg Med Chem (2009) 17: 7732-7742 [PMID:19822433] |
| ChEMBL | Inhibitory activity of compound against VEGF induced cell proliferation | F | 7.4 | pIC50 | 40 | nM | IC50 | J Med Chem (1999) 42: 5120-5130 [PMID:10602697] |
| ChEMBL | Inhibition of VEGFR2 in human U251 cells compound pretreated for 60 min before VEGF stimulation for 10 mins by phosphotyrosine ELISA cytoblot method | B | 7.89 | pIC50 | 12.9 | nM | IC50 | Bioorg Med Chem (2015) 23: 2408-2423 [PMID:25882519] |
| ChEMBL | Inhibition of VEGFR2 in human U251 cells by phosphotyrosine ELISA assay | B | 7.89 | pIC50 | 12.9 | nM | IC50 | Bioorg Med Chem (2014) 22: 3753-3772 [PMID:24890652] |
| ChEMBL | Inhibition of VEGFR2 in human U251 cells by phosphotyrosine ELISA | B | 7.89 | pIC50 | 12.9 | nM | IC50 | ACS Med Chem Lett (2014) 5: 480-484 [PMID:24900865] |
| ChEMBL | Inhibition of VEGF-induced VEGFR2 activation in human U251 cells pretreated for 60 mins followed by VEGF addition and measured after 10 mins by ELISA | B | 7.89 | pIC50 | 12.9 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 3085-3093 [PMID:30098869] |
| ChEMBL | Inhibition of VEGFR-2 in human U251 cells assessed as reduction in VEGF induced phosphorylation preincubated for 60 mins followed by VEGF addition measured after 10 mins by ELISA method | B | 7.89 | pIC50 | 12.9 | nM | IC50 | Bioorg Med Chem (2017) 25: 545-556 [PMID:27894589] |
| kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3337] [GtoPdb: 1813] [UniProtKB: P35918] | ||||||||
| ChEMBL | Inhibitory activity against Vascular endothelial growth factor receptor 2 (VEGF-R2) in NIH3T3 mouse fibroblast cells | B | 5.98 | pIC50 | 1040 | nM | IC50 | J Med Chem (1999) 42: 5120-5130 [PMID:10602697] |
| fms related receptor tyrosine kinase 4/Vascular endothelial growth factor receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1955] [GtoPdb: 1814] [UniProtKB: P35916] | ||||||||
| ChEMBL | Inhibition of Flt4 (unknown origin) after 20 mins by scintillation counting | B | 6.3 | pIC50 | 500 | nM | IC50 | J Nat Prod (2013) 76: 715-719 [PMID:23414235] |
| ChEMBL | In vitro inhibition of Vascular endothelial growth factor receptor 3 [VEGFR-3(Flt-4)] expressed in baculovirus | B | 7.3 | pIC50 | 50 | nM | IC50 | J Med Chem (2002) 45: 5687-5693 [PMID:12477352] |
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]
