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] |
| ChEMBL | Inhibition of FLT3 (unknown origin) | B | 6.8 | pIC50 | 160 | nM | IC50 | Bioorg Med Chem (2023) 90: 117367-117367 [PMID:37348260] |
| 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 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]
