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) |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
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 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]