FMK [Ligand Id: 9358] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL515414
  • EPH receptor A2/Ephrin type-A receptor 2 in Human [ChEMBL: CHEMBL2068] [GtoPdb: 1822] [UniProtKB: P29317]
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  • ribosomal protein S6 kinase B1/Ribosomal protein S6 kinase 1 in Human [ChEMBL: CHEMBL4501] [GtoPdb: 1525] [UniProtKB: P23443]
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  • ribosomal protein S6 kinase A3/Ribosomal protein S6 kinase alpha 3 in Human [ChEMBL: CHEMBL2345] [GtoPdb: 1528] [UniProtKB: P51812]
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  • Transitional endoplasmic reticulum ATPase in Human [ChEMBL: CHEMBL1075145] [UniProtKB: P55072]
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  • FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FYN in Human [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241]
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  • LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Mouse [ChEMBL: CHEMBL2480] [GtoPdb: 2053] [UniProtKB: P06240]
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  • Tyrosine-protein kinase SRC in Chicken [ChEMBL: CHEMBL3655] [UniProtKB: P00523]
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  • YES proto-oncogene 1, Src family tyrosine kinase/Tyrosine-protein kinase YES in Human [ChEMBL: CHEMBL2073] [GtoPdb: 2284] [UniProtKB: P07947]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 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 33:

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]