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

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ChEMBL ligand: CHEMBL150315 (CB-676475)
  • EPH receptor B2/Ephrin type-B receptor 2 in Human [ChEMBL: CHEMBL3290] [GtoPdb: 1831] [UniProtKB: P29323]
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  • fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362]
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  • fms related receptor tyrosine kinase 1/Vascular endothelial growth factor receptor 1 in Human [ChEMBL: CHEMBL1868] [GtoPdb: 1812] [UniProtKB: P17948]
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  • kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
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  • epidermal growth factor receptor in Human [GtoPdb: 1797] [UniProtKB: P00533]
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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 32:

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]