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ChEMBL ligand: CHEMBL21156 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941] | ||||||||
ChEMBL | Inhibition of cyclin dependent kinase 2 | B | 5.48 | pIC50 | 3300 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 1219-1223 [PMID:11934592] |
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 Fibroblast growth factor receptor 2 | B | 6.03 | pIC50 | 940 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 1219-1223 [PMID:11934592] |
inhibitor of nuclear factor kappa B kinase subunit beta/Inhibitor of nuclear factor kappa B kinase beta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1991] [GtoPdb: 2039] [UniProtKB: O14920] | ||||||||
ChEMBL | Inhibition of I-kappa-B kinase 2 | B | 6.52 | pIC50 | 300 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 1219-1223 [PMID:11934592] |
maternal embryonic leucine zipper kinase/Maternal embryonic leucine zipper kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4578] [GtoPdb: 2102] [UniProtKB: Q14680] | ||||||||
ChEMBL | Inhibition of His6-tagged MELK catalytic domain (1 to 340 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) cells using Bcl-GL as substrate measured after 30 mins in presence of [gamma32P]ATP by liquid scintillation counting method | B | 6.48 | pIC50 | 330 | nM | IC50 | Bioorg Med Chem (2017) 25: 2609-2616 [PMID:28351607] |
platelet derived growth factor receptor beta/platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095189] [GtoPdb: 1804, 1803] [UniProtKB: P09619, P16234] | ||||||||
ChEMBL | Inhibition of Platelet-derived growth factor receptor | B | 5.83 | pIC50 | 1490 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 1219-1223 [PMID:11934592] |
mPGES1/Prostaglandin E synthase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5658] [GtoPdb: 1377] [UniProtKB: O14684] | ||||||||
ChEMBL | Inhibition of mPGES-1 in IL-1beta-stimulated human A549 cell microsomal membranes assessed as reduction in PGE2 formation incubated for 15 mins using PGH2 substrate by RP-HPLC method | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem (2015) 23: 4839-4845 [PMID:26088337] |
protein kinase C alpha/Protein kinase C alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL299] [GtoPdb: 1482] [UniProtKB: P17252] | ||||||||
ChEMBL | Inhibition of protein kinase C alpha | B | 5.92 | pIC50 | 1200 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 1219-1223 [PMID:11934592] |
Raf-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase RAF in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1906] [GtoPdb: 2184] [UniProtKB: P04049] | ||||||||
ChEMBL | Inhibition of protein kinase Raf | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 1219-1223 [PMID:11934592] |
C-terminal Src kinase/Tyrosine-protein kinase CSK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2634] [GtoPdb: 1994] [UniProtKB: P41240] | ||||||||
ChEMBL | Inhibition of Tyrosine-protein kinase CSK | B | 5.68 | pIC50 | 2100 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 1219-1223 [PMID:11934592] |
FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FYN in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241] | ||||||||
ChEMBL | Inhibition of protein kinase Fyn | B | 6.3 | pIC50 | 500 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 1219-1223 [PMID:11934592] |
HCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase HCK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3234] [GtoPdb: 2032] [UniProtKB: P08631] | ||||||||
ChEMBL | Inhibition of protein kinase Hck | B | 5.11 | pIC50 | 7700 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 1219-1223 [PMID:11934592] |
Janus kinase 1/Tyrosine-protein kinase JAK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458] | ||||||||
ChEMBL | Inhibition of JAK1 (unknown origin) using 1 mM of ATP and Tyr6 peptide by Z'-LYTE kinase assay | B | 6.22 | pIC50 | 600 | nM | IC50 | J Med Chem (2015) 58: 7596-7602 [PMID:26351728] |
ChEMBL | Inhibition of JAK1 | B | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (2008) 51: 7015-7019 [PMID:18844338] |
ChEMBL | Inhibition of JAK1 (unknown origin) using 87 uM of ATP and Tyr6 peptide by Z'-LYTE kinase assay | B | 8.4 | pIC50 | 4 | nM | IC50 | J Med Chem (2015) 58: 7596-7602 [PMID:26351728] |
Janus kinase 1/Tyrosine-protein kinase JAK1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2968] [GtoPdb: 2047] [UniProtKB: P52332] | ||||||||
ChEMBL | Inhibition of murine Jak 1 protein kinase | B | 7.82 | pIC50 | 15 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 1219-1223 [PMID:11934592] |
ChEMBL | Inhibition of mouse JAK1 | B | 7.82 | pIC50 | 15 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674] | ||||||||
ChEMBL | Inhibition of JAK2 (unknown origin) using 1 mM of ATP and Tyr6 peptide by Z'-LYTE kinase assay | B | 5.85 | pIC50 | 1400 | nM | IC50 | J Med Chem (2015) 58: 7596-7602 [PMID:26351728] |
GtoPdb | - | - | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 1219-23 [PMID:11934592] |
ChEMBL | Inhibition of protein kinase Jak 2 | B | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 1219-1223 [PMID:11934592] |
ChEMBL | Inhibition of JAK2 | B | 9 | pIC50 | 1 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
ChEMBL | Inhibition of JAK2 | B | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (2008) 51: 7015-7019 [PMID:18844338] |
ChEMBL | Inhibition of JAK2 (unknown origin) using 35 uM of ATP and Tyr6 peptide by Z'-LYTE kinase assay | B | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (2015) 58: 7596-7602 [PMID:26351728] |
Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333] | ||||||||
ChEMBL | Inhibition of JAK3 (unknown origin) using 1 mM of ATP and Tyr6 peptide by Z'-LYTE kinase assay | B | 6.05 | pIC50 | 900 | nM | IC50 | J Med Chem (2015) 58: 7596-7602 [PMID:26351728] |
ChEMBL | Inhibition of JAK3 (unknown origin) using 16 uM of ATP and Tyr6 peptide by Z'-LYTE kinase assay | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2015) 58: 7596-7602 [PMID:26351728] |
GtoPdb | - | - | 8.3 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 1219-23 [PMID:11934592] |
ChEMBL | Inhibition of protein kinase Jak 3 | B | 8.3 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 1219-1223 [PMID:11934592] |
ChEMBL | Inhibition of JAK3 | B | 8.3 | pIC50 | 5 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
ChEMBL | Inhibition of JAK3 | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2008) 51: 7015-7019 [PMID:18844338] |
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 p56 Lck tyrosine kinase | B | 5.1 | pIC50 | >8000 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 1219-1223 [PMID:11934592] |
ChEMBL | Inhibition of p56 Lck tyrosine kinase | B | 5.1 | pIC50 | >8000 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 1219-1223 [PMID:11934592] |
SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931] | ||||||||
ChEMBL | Inhibition of Src protein tyrosine kinase | B | 5.1 | pIC50 | >8000 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 1219-1223 [PMID:11934592] |
TEK receptor tyrosine kinase/Tyrosine-protein kinase TIE-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4128] [GtoPdb: 1842] [UniProtKB: Q02763] | ||||||||
ChEMBL | Inhibition of Tek kinase | B | 4.62 | pIC50 | 24000 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 1219-1223 [PMID:11934592] |
tyrosine kinase 2/Tyrosine-protein kinase TYK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3553] [GtoPdb: 2269] [UniProtKB: P29597] | ||||||||
ChEMBL | Inhibition of Tyk2 (unknown origin) using 1 mM of ATP and Tyr3 peptide by Z'-LYTE kinase assay | B | 5.77 | pIC50 | 1700 | nM | IC50 | J Med Chem (2015) 58: 7596-7602 [PMID:26351728] |
ChEMBL | Inhibition of Tyk2 (unknown origin) using 25 uM of ATP and Tyr3 peptide by Z'-LYTE kinase assay | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2015) 58: 7596-7602 [PMID:26351728] |
GtoPdb | - | - | 9 | pIC50 | 1 | nM | IC50 | Proc Natl Acad Sci USA (2007) 104: 20523-8 [PMID:18077363] |
ChEMBL | Inhibition of Tyrosine kinase 2 kinase | B | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 1219-1223 [PMID:11934592] |
ChEMBL | Inhibition of Tyk2 | B | 9 | pIC50 | 1 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
ChEMBL | Inhibition of TYK2 | B | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (2008) 51: 7015-7019 [PMID:18844338] |
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 Vascular endothelial growth factor receptor 1 | B | 5.82 | pIC50 | 1520 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 1219-1223 [PMID:11934592] |
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 Vascular endothelial growth factor receptor 2 | B | 5.85 | pIC50 | 1400 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 1219-1223 [PMID:11934592] |
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 Vascular endothelial growth factor receptor 3 | B | 6.16 | pIC50 | 690 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 1219-1223 [PMID:11934592] |
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]