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ChEMBL ligand: CHEMBL150315 (CB-676475) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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EPH receptor B2/Ephrin type-B receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3290] [GtoPdb: 1831] [UniProtKB: P29323] | ||||||||
ChEMBL | Equilibrium binding constant for EPH receptor B2 | B | 5.21 | pKd | 6200 | nM | Kd | J. Med. Chem. (2005) 48: 3221-3230 [PMID:15857128] |
ChEMBL | Inhibition of EPH receptor B2 using ELISA | B | 5.07 | pIC50 | 8500 | nM | IC50 | J. Med. Chem. (2005) 48: 3221-3230 [PMID:15857128] |
fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362] | ||||||||
ChEMBL | FGFR-1 (FTK) inhibitory activity at 2 uM of ATP in vitro. | B | 5.15 | pIC50 | 7000 | nM | IC50 | J. Med. Chem. (1999) 42: 5369-5389 [PMID:10639280] |
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 VEGFR1 | B | 4.75 | pIC50 | 17700 | nM | IC50 | Bioorg. Med. Chem. Lett. (2010) 20: 3177-3181 [PMID:20403693] |
ChEMBL | Inhibition of VEGFR1 expressed in human tumor cells | B | 4.75 | pIC50 | 17700 | nM | IC50 | Bioorg. Med. Chem. (2008) 16: 5514-5528 [PMID:18467105] |
ChEMBL | Inhibition of VEGF-induced VEGFR1 autophosphorylation in human A498 cells incubated for 60 mins prior to VEGF-induction measured after 10 mins by phosphotyrosine ELISA | B | 4.75 | pIC50 | 17700 | nM | IC50 | Bioorg. Med. Chem. (2012) 20: 2444-2454 [PMID:22370340] |
ChEMBL | Inhibition of VEGFR1 tyrosine kinase activity in VEGF-stimulated human A498 cells after 60 mins by ELISA | B | 4.85 | pIC50 | 14100 | nM | IC50 | Bioorg. Med. Chem. (2012) 20: 910-914 [PMID:22204741] |
ChEMBL | Inhibition of VEGF-induced VEGFR1 phosphorylation in human A498 cells overexpressing Flt-1 pretreated for 60 mins prior to VEGF addition measured after 10 mins by phosphotyrosine ELISA cytoblot analysis | B | 4.85 | pIC50 | 14100 | nM | IC50 | Bioorg. Med. Chem. (2013) 21: 1312-1323 [PMID:23375090] |
ChEMBL | Inhibition of VEGFR1 in human A498 cells by phosphotyrosine cell-based ELISA | B | 4.85 | pIC50 | 14100 | nM | IC50 | J. Med. Chem. (2010) 53: 1563-1578 [PMID:20092323] |
ChEMBL | Inhibition of VEGFR1 phosphorylation in human A498 cells after 10 mins by FLISA | B | 4.85 | pIC50 | 14100 | nM | IC50 | Bioorg. Med. Chem. (2010) 18: 3575-3587 [PMID:20403700] |
ChEMBL | Inhibitory activity against flt kinase | B | 5.7 | pIC50 | 2000 | nM | IC50 | Bioorg. Med. Chem. Lett. (2006) 16: 129-133 [PMID:16216503] |
ChEMBL | In vitro vascular endothelial growth factor receptor 1 inhibitory activity at 2 uM of ATP. | B | 5.7 | pIC50 | 2000 | nM | IC50 | J. Med. Chem. (1999) 42: 5369-5389 [PMID:10639280] |
GtoPdb | - | - | 6.48 | pIC50 | 330 | nM | IC50 |
J Biomol Screen (2012) 17: 885-99 [PMID:22573732]; J Med Chem (1999) 42: 5369-89 [PMID:10639280] |
kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968] | ||||||||
ChEMBL | Inhibitory activity against VEGFR2 kinase | B | 5.82 | pIC50 | 1500 | nM | IC50 | Bioorg. Med. Chem. Lett. (2006) 16: 129-133 [PMID:16216503] |
GtoPdb | - | - | 7 | pIC50 | 100 | nM | IC50 | J Med Chem (1999) 42: 5369-89 [PMID:10639280] |
ChEMBL | Vascular endothelial growth factor receptor 2 inhibitory activity at 2 uM of ATP in vitro. | B | 7 | pIC50 | 100 | nM | IC50 | J. Med. Chem. (1999) 42: 5369-5389 [PMID:10639280] |
epidermal growth factor receptor in Human [GtoPdb: 1797] [UniProtKB: P00533] | ||||||||
GtoPdb | - | - | 8 | pIC50 | 10 | nM | IC50 | J Biomol Screen (2012) 17: 885-99 [PMID:22573732] |
ChEMBL data shown on this page come from version 31:
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]