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ChEMBL ligand: CHEMBL505896 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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protein kinase, cAMP-dependent, catalytic, alpha subunit/cAMP-dependent protein kinase alpha-catalytic subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4101] [GtoPdb: 1476] [UniProtKB: P17612] | ||||||||
ChEMBL | Inhibition of PKAalpha | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2008) 51: 5766-5779 [PMID:18763753] |
mitogen-activated protein kinase 9/c-Jun N-terminal kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4179] [GtoPdb: 1497] [UniProtKB: P45984] | ||||||||
ChEMBL | Inhibition of JNK2 | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2008) 51: 5766-5779 [PMID:18763753] |
cyclin dependent kinase 5/Cyclin-dependent kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4036] [GtoPdb: 1977] [UniProtKB: Q00535] | ||||||||
ChEMBL | Inhibition of CDK5 | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2008) 51: 5766-5779 [PMID:18763753] |
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] | ||||||||
ChEMBL | Inhibition of EGFR | B | 5.77 | pIC50 | 1700 | nM | IC50 | J Med Chem (2008) 51: 5766-5779 [PMID:18763753] |
fibroblast growth factor receptor 2/Fibroblast growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4142] [GtoPdb: 1809] [UniProtKB: P21802] | ||||||||
ChEMBL | Inhibition of FGFRK2 | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2008) 51: 5766-5779 [PMID:18763753] |
MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581] | ||||||||
ChEMBL | Inhibition of cMet by HTRF assay | B | 8.05 | pKi | 8.9 | nM | Ki | J Med Chem (2008) 51: 5766-5779 [PMID:18763753] |
ChEMBL | Inhibition of human c-MET | B | 7.77 | pIC50 | 17 | nM | IC50 | Eur J Med Chem (2011) 46: 3675-3680 [PMID:21641696] |
GtoPdb | - | - | 7.77 | pIC50 | 17 | nM | IC50 | J Biol Chem (2008) 283: 2675-83 [PMID:18055465] |
ChEMBL | Inhibition of c-Met by HTRF assay | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2008) 51: 2879-2882 [PMID:18426196] |
ChEMBL | Inhibition of wild type GST-tagged c-Met kinase domain (1058 to 1365) (unknown origin) expressed in Sf9 cells by HTRF assay | B | 8.05 | pIC50 | 8.9 | nM | IC50 | Bioorg Med Chem (2013) 21: 2843-2855 [PMID:23628470] |
ChEMBL | Inhibition of c-Met (unknown origin) | B | 8.05 | pIC50 | 8.9 | nM | IC50 | Eur J Med Chem (2013) 64: 62-73 [PMID:23644189] |
ChEMBL | Inhibition of c-Met (unknown origin) | B | 8.05 | pIC50 | 8.9 | nM | IC50 | Eur J Med Chem (2014) 83: 581-593 [PMID:24996144] |
colony stimulating factor 1 receptor/Macrophage colony stimulating factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1844] [GtoPdb: 1806] [UniProtKB: P07333] | ||||||||
ChEMBL | Inhibition of cFMS kinase | B | 7.43 | pIC50 | 37 | nM | IC50 | J Med Chem (2008) 51: 5766-5779 [PMID:18763753] |
macrophage stimulating 1 receptor/Macrophage-stimulating protein receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2689] [GtoPdb: 1816] [UniProtKB: Q04912] | ||||||||
ChEMBL | Inhibition of phosphorylated RON | B | 6.71 | pKi | 195 | nM | Ki | J Med Chem (2008) 51: 5766-5779 [PMID:18763753] |
mitogen-activated protein kinase 3/MAP kinase ERK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3385] [GtoPdb: 1494] [UniProtKB: P27361] | ||||||||
ChEMBL | Inhibition of ERK1 | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2008) 51: 5766-5779 [PMID:18763753] |
ribosomal protein S6 kinase B1/Ribosomal protein S6 kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4501] [GtoPdb: 1525] [UniProtKB: P23443] | ||||||||
ChEMBL | Inhibition of P70S6 | B | 5 | pIC50 | 10000 | nM | IC50 | J Med Chem (2008) 51: 5766-5779 [PMID:18763753] |
ribosomal protein S6 kinase A5/Ribosomal protein S6 kinase alpha 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4237] [GtoPdb: 1523] [UniProtKB: O75582] | ||||||||
ChEMBL | Inhibition of MSK1 | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2008) 51: 5766-5779 [PMID:18763753] |
AKT serine/threonine kinase 1/Serine/threonine-protein kinase AKT in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749] | ||||||||
ChEMBL | Inhibition of PKBalpha | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2008) 51: 5766-5779 [PMID:18763753] |
aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965] | ||||||||
ChEMBL | Inhibition of Aurora2 | B | 6.94 | pIC50 | 116 | nM | IC50 | J Med Chem (2008) 51: 5766-5779 [PMID:18763753] |
Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309] | ||||||||
ChEMBL | Inhibition of PIM1 kinase | B | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2008) 51: 5766-5779 [PMID:18763753] |
Pim-2 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523] [GtoPdb: 2159] [UniProtKB: Q9P1W9] | ||||||||
ChEMBL | Inhibition of PIM2 kinase | B | 4.6 | pIC50 | >25000 | nM | IC50 | J Med Chem (2008) 51: 5766-5779 [PMID:18763753] |
Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187] | ||||||||
ChEMBL | Inhibition of BTK | B | 7.72 | pIC50 | 19 | nM | IC50 | J Med Chem (2008) 51: 5766-5779 [PMID:18763753] |
Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674] | ||||||||
ChEMBL | Inhibition of JAK2 | B | 4.6 | pIC50 | >25000 | nM | IC50 | J Med Chem (2008) 51: 5766-5779 [PMID:18763753] |
Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333] | ||||||||
ChEMBL | Inhibition of JAK3 | B | 5.08 | pIC50 | >8300 | nM | IC50 | J Med Chem (2008) 51: 5766-5779 [PMID:18763753] |
LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239] | ||||||||
ChEMBL | Inhibition of LCK | B | 8.1 | pIC50 | 8 | nM | IC50 | J Med Chem (2008) 51: 5766-5779 [PMID:18763753] |
TEK receptor tyrosine kinase/Tyrosine-protein kinase TIE-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4128] [GtoPdb: 1842] [UniProtKB: Q02763] | ||||||||
ChEMBL | Inhibition of Tie2 kinase | B | 6.55 | pIC50 | 285 | nM | IC50 | J Med Chem (2008) 51: 5766-5779 [PMID:18763753] |
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 ZAP70 | B | 5.27 | pIC50 | >5400 | nM | IC50 | J Med Chem (2008) 51: 5766-5779 [PMID:18763753] |
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 Flt1 kinase | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2008) 51: 5766-5779 [PMID:18763753] |
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 phosphorylated KDR by HTRF assay | B | 6.37 | pKi | 422 | nM | Ki | J Med Chem (2008) 51: 5766-5779 [PMID:18763753] |
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 kinase | B | 6.92 | pIC50 | 120 | nM | IC50 | J Med Chem (2008) 51: 5766-5779 [PMID:18763753] |
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]