ZM-306416 [Ligand Id: 8245] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL150315 (CB-676475)
  • EPH receptor B2/Ephrin type-B receptor 2 in Human [ChEMBL: CHEMBL3290] [GtoPdb: 1831] [UniProtKB: P29323]
There should be some charts here, you may need to enable JavaScript!
  • fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362]
There should be some charts here, you may need to enable JavaScript!
  • fms related receptor tyrosine kinase 1/Vascular endothelial growth factor receptor 1 in Human [ChEMBL: CHEMBL1868] [GtoPdb: 1812] [UniProtKB: P17948]
There should be some charts here, you may need to enable JavaScript!
  • kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
There should be some charts here, you may need to enable JavaScript!
  • epidermal growth factor receptor in Human [GtoPdb: 1797] [UniProtKB: P00533]
There should be some charts here, you may need to enable JavaScript!
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 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]