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ChEMBL ligand: CHEMBL515414 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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EPH receptor A2/Ephrin type-A receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2068] [GtoPdb: 1822] [UniProtKB: P29317] | ||||||||
ChEMBL | Inhibition of Eph-A2 in the presence of 50uM ATP | B | 6.12 | pIC50 | 760 | nM | IC50 | Biochem J (2007) 408: 297-315 [PMID:17850214] |
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 S6K1 in the presence of 20uM ATP | B | 6.02 | pIC50 | 950 | nM | IC50 | Biochem J (2007) 408: 297-315 [PMID:17850214] |
ribosomal protein S6 kinase A3/Ribosomal protein S6 kinase alpha 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2345] [GtoPdb: 1528] [UniProtKB: P51812] | ||||||||
ChEMBL | Inhibition of RSK2 C-terminal kinase domain expressed in Escherichia coli preincubated for 30 mins | B | 4.82 | pIC50 | 15000 | nM | IC50 | Science (2005) 308: 1318-1321 [PMID:15919995] |
GtoPdb | - | - | 7.82 | pIC50 | 15 | nM | IC50 | Nat Chem Biol (2007) 3: 156-60 [PMID:17259979] |
ChEMBL | Inhibition of His6-tagged RSK2 C-terminal domian expressed in Escherichia coli after 30 mins | B | 7.82 | pIC50 | 15 | nM | IC50 | Nat Chem Biol (2007) 3: 156-160 [PMID:17259979] |
ChEMBL | Inhibition of RSK2 after 60 mins | B | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (2011) 54: 3564-3574 [PMID:21488662] |
ChEMBL | Inhibition of RSK2 transfected in HEK293 cells | B | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (2012) 55: 6243-6262 [PMID:22621397] |
ChEMBL | Inhibition of His6x-tagged RSK2 C-terminal domain (unknown origin) expressed in Escherichia coli | B | 7.82 | pIC50 | 15 | nM | IC50 | Bioorg Med Chem (2013) 21: 1724-1734 [PMID:23434140] |
ChEMBL | Inhibition of RSK2 (unknown origin) | B | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (2021) 64: 13572-13587 [PMID:34496560] |
ChEMBL | Inhibition of wild type RSK2 (unknown origin) | B | 7.82 | pIC50 | 15 | nM | IC50 | Eur J Med Chem (2023) 251: 115229-115229 [PMID:36898330] |
ChEMBL | Inhibition of PMA-stimulated RSK2 phosphorylation in HEK293 cells after 1 hr by Western blotting analysis | B | 6.82 | pEC50 | 150 | nM | EC50 | Nat Chem Biol (2007) 3: 156-160 [PMID:17259979] |
Transitional endoplasmic reticulum ATPase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075145] [UniProtKB: P55072] | ||||||||
ChEMBL | Inhibition of p97 in human HeLa cells assessed as reduction in proteasomal turnover of p97-dependent reporter substrate UbG76V-GFP incubated for 120 mins by luciferase reporter gene assay | B | 4.33 | pIC50 | 47000 | nM | IC50 | Eur J Med Chem (2021) 213: 113148-113148 [PMID:33476933] |
ChEMBL | Inhibition of His6-tagged p97 (unknown origin) expressed in Escherichia coli BL21 (DE3) assessed as reduction in ATPase activity measured after 60 mins by biomol green reagent based assay | B | 4.52 | pIC50 | >30000 | nM | IC50 | Eur J Med Chem (2021) 213: 113148-113148 [PMID:33476933] |
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 FYN Val285Cys mutant expressed in Escherichia coli | B | 9 | pIC50 | 1 | nM | IC50 | Science (2005) 308: 1318-1321 [PMID:15919995] |
LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2480] [GtoPdb: 2053] [UniProtKB: P06240] | ||||||||
ChEMBL | Inhibition of Lck in the presence of 50uM ATP | B | 6.12 | pIC50 | 750 | nM | IC50 | Biochem J (2007) 408: 297-315 [PMID:17850214] |
Tyrosine-protein kinase SRC in Chicken (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3655] [UniProtKB: P00523] | ||||||||
ChEMBL | Inhibition of Src in the presence of 50uM ATP | B | 6.25 | pIC50 | 560 | nM | IC50 | Biochem J (2007) 408: 297-315 [PMID:17850214] |
YES proto-oncogene 1, Src family tyrosine kinase/Tyrosine-protein kinase YES in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073] [GtoPdb: 2284] [UniProtKB: P07947] | ||||||||
ChEMBL | Inhibition of Yes in the presence of 20uM ATP | B | 6.29 | pIC50 | 510 | nM | IC50 | Biochem J (2007) 408: 297-315 [PMID:17850214] |
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]