PP1 [Ligand Id: 8836] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL306380
  • casein kinase 1 delta/Casein kinase I delta in Human [ChEMBL: CHEMBL2828] [GtoPdb: 1997] [UniProtKB: P48730]
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  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
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  • mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
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  • platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor alpha in Human [ChEMBL: CHEMBL2007] [GtoPdb: 1803] [UniProtKB: P16234]
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  • mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Human [ChEMBL: CHEMBL2842] [GtoPdb: 2109] [UniProtKB: P42345]
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  • receptor interacting serine/threonine kinase 2/Serine/threonine-protein kinase RIPK2 in Human [ChEMBL: CHEMBL5014] [GtoPdb: 2190] [UniProtKB: O43353]
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  • KIT proto-oncogene, receptor tyrosine kinase/Stem cell growth factor receptor in Human [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721]
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  • ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
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  • C-terminal Src kinase/Tyrosine-protein kinase CSK in Human [ChEMBL: CHEMBL2634] [GtoPdb: 1994] [UniProtKB: P41240]
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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 Human [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
  • LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Mouse [ChEMBL: CHEMBL2480] [GtoPdb: 2053] [UniProtKB: P06240]
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  • ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
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  • Tyrosine-protein kinase SRC in Chicken [ChEMBL: CHEMBL3655] [UniProtKB: P00523]
  • SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
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  • TEK receptor tyrosine kinase/Tyrosine-protein kinase TIE-2 in Human [ChEMBL: CHEMBL4128] [GtoPdb: 1842] [UniProtKB: Q02763]
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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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  • kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
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  • WNK lysine deficient protein kinase 1 in Human [GtoPdb: 2280] [UniProtKB: Q9H4A3]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
casein kinase 1 delta/Casein kinase I delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2828] [GtoPdb: 1997] [UniProtKB: P48730]
ChEMBL Inhibition of CK1delta in the presence of 20uM ATP B 6.77 pIC50 170 nM IC50 Biochem. J. (2007) 408: 297-315 [PMID:17850214]
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 6.7 pKi 199.53 nM Ki ACS Med. Chem. Lett. (2012) 3: 383-386 [PMID:24900482]
GtoPdb - - 6.6 pIC50 250 nM IC50 J Biol Chem (1996) 271: 695-701 [PMID:8557675]
mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
ChEMBL Inhibition of p38alpha active form expressed in Escherichia coli BL21(DE3) cells by HTRF assay B 5.55 pIC50 2800 nM IC50 J. Med. Chem. (2010) 53: 357-367 [PMID:19928858]
ChEMBL Displacement of N,N'-(2,2'-(3,3'-disulfanediylbis(2,5-dioxopyrrolidine-3,1-diyl))bis(ethane-2,1-diyl))bis(2-(3-(3-tert-butyl-5-(3-naphthalen-1-ylureido)-1H-pyrazol-1-yl)phenylamino)acetamide) from inactive form of p38alpha expressed in Escherichia coli BL21(DE3) cells by enzyme fragment complementation assay B 6 pIC50 1000 nM IC50 J. Med. Chem. (2010) 53: 357-367 [PMID:19928858]
GtoPdb - - 6.19 pIC50 640 nM IC50 Biochem J (2003) 371: 199-204 [PMID:12534346]
platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2007] [GtoPdb: 1803] [UniProtKB: P16234]
ChEMBL Inhibition of human PDGFRalpha using poly[Glu,Tyr]4:1 as substrate in presence of [gamma-33P]ATP B 6.18 pIC50 657 nM IC50 J. Med. Chem. (2016) 59: 4697-4710 [PMID:27115835]
mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2842] [GtoPdb: 2109] [UniProtKB: P42345]
ChEMBL Inhibition of human mTOR using poly[Glu,Tyr]4:1 as substrate in presence of [gamma-33P]ATP B 5.03 pIC50 9318 nM IC50 J. Med. Chem. (2016) 59: 4697-4710 [PMID:27115835]
receptor interacting serine/threonine kinase 2/Serine/threonine-protein kinase RIPK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5014] [GtoPdb: 2190] [UniProtKB: O43353]
ChEMBL Inhibition of RIP2 in the presence of 100uM ATP B 7.59 pIC50 26 nM IC50 Biochem. J. (2007) 408: 297-315 [PMID:17850214]
KIT proto-oncogene, receptor tyrosine kinase/Stem cell growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721]
ChEMBL Inhibition of human KIT using poly[Glu,Tyr]4:1 as substrate in presence of [gamma-33P]ATP B 5.88 pIC50 1318 nM IC50 J. Med. Chem. (2016) 59: 4697-4710 [PMID:27115835]
ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
ChEMBL Inhibition of human ABL using EAIYAAPFAKKK as substrate in presence of [gamma-33P]ATP B 6.83 pIC50 147 nM IC50 J. Med. Chem. (2016) 59: 4697-4710 [PMID:27115835]
C-terminal Src kinase/Tyrosine-protein kinase CSK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2634] [GtoPdb: 1994] [UniProtKB: P41240]
ChEMBL Inhibition of CSK in the presence of 20uM ATP B 6.19 pIC50 640 nM IC50 Biochem. J. (2007) 408: 297-315 [PMID:17850214]
GtoPdb - - 6.28 pIC50 520 nM IC50 Biochem J (2003) 371: 199-204 [PMID:12534346]
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 human FYN using poly[Glu,Tyr]4:1 as substrate in presence of [gamma-33P]ATP B 7.57 pIC50 27 nM IC50 J. Med. Chem. (2016) 59: 4697-4710 [PMID:27115835]
ChEMBL Inhibition of FYN (unknown origin) by cell culture based assay B 8 pIC50 10 nM IC50 Eur J Med Chem (2017) 142: 229-243 [PMID:28814374]
GtoPdb - - 8.22 pIC50 6 nM IC50 J Biol Chem (1996) 271: 695-701 [PMID:8557675]
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 7.2 pKi 63.1 nM Ki ACS Med. Chem. Lett. (2012) 3: 383-386 [PMID:24900482]
ChEMBL Inhibition of p56 Lck tyrosine kinase catalytic domain at 5 uM ATP B 6.6 pIC50 250 nM IC50 Bioorg. Med. Chem. Lett. (2000) 10: 2167-2170 [PMID:11012021]
ChEMBL Inhibition of p56 Lck tyrosine kinase at 5 uM ATP B 6.82 pIC50 151 nM IC50 Bioorg. Med. Chem. Lett. (2000) 10: 2167-2170 [PMID:11012021]
GtoPdb - - 8.3 pIC50 5 nM IC50 J Biol Chem (1996) 271: 695-701 [PMID:8557675]
ChEMBL Inhibition of p56 Lck tyrosine kinase in Jurkat cells where p56lck autophosphorylation is inhibited. B 8.3 pIC50 5 nM IC50 Bioorg. Med. Chem. Lett. (1997) 7: 417-420
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 7.4 pIC50 40 nM IC50 Biochem. J. (2007) 408: 297-315 [PMID:17850214]
ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
ChEMBL Inhibition of human RET using poly[Glu,Tyr]4:1 as substrate in presence of [gamma-33P]ATP B 7.96 pIC50 11 nM IC50 J. Med. Chem. (2016) 59: 4697-4710 [PMID:27115835]
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 7.28 pIC50 53 nM IC50 Biochem. J. (2007) 408: 297-315 [PMID:17850214]
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 at 5 mM ATP B 6.77 pIC50 170 nM IC50 Bioorg. Med. Chem. Lett. (2000) 10: 2167-2170 [PMID:11012021]
ChEMBL Inhibition of C-terminal His-tagged full length human SRC expressed in insect cells preincubated for 20 mins using poly[Glu,Tyr]4:1 as substrate measured after 5 to 120 mins in presence of [gamma-33P]ATP by Kinome assay B 7.77 pIC50 17 nM IC50 J. Med. Chem. (2016) 59: 4697-4710 [PMID:27115835]
ChEMBL Inhibition of GST-tagged human recombinant c-src using biotinylated peptide as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by microplate reader analysis B 8.3 pIC50 5 nM IC50 MedChemComm (2015) 6: 1518-1534
TEK receptor tyrosine kinase/Tyrosine-protein kinase TIE-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4128] [GtoPdb: 1842] [UniProtKB: Q02763]
ChEMBL Inhibition of tie-2 at 5 uM ATP B 5.15 pIC50 7000 nM IC50 Bioorg. Med. Chem. Lett. (2000) 10: 2167-2170 [PMID:11012021]
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 human YES using poly[Glu,Tyr]4:1 as substrate in presence of [gamma-33P] ATP B 7.44 pIC50 36 nM IC50 J. Med. Chem. (2016) 59: 4697-4710 [PMID:27115835]
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 at 5 uM ATP B 5.8 pIC50 1600 nM IC50 Bioorg. Med. Chem. Lett. (2000) 10: 2167-2170 [PMID:11012021]
WNK lysine deficient protein kinase 1 in Human [GtoPdb: 2280] [UniProtKB: Q9H4A3]
GtoPdb - - 4.9 pKi 12700 nM Ki Biochemistry (2009) 48: 10255-66 [PMID:19739668]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]