PP1 analog II [Ligand Id: 6028] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL573578
  • Calmodulin-domain protein kinase 1 in Toxoplasma gondii [ChEMBL: CHEMBL1781862] [UniProtKB: Q9BJF5]
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  • calcium/calmodulin-dependent protein kinase II alpha subunit/CaM kinase II alpha in Human [ChEMBL: CHEMBL4147] [GtoPdb: 1555] [UniProtKB: Q9UQM7]
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  • protein kinase, cAMP-dependent, catalytic, alpha subunit/cAMP-dependent protein kinase alpha-catalytic subunit in Human [ChEMBL: CHEMBL4101] [GtoPdb: 1476] [UniProtKB: P17612]
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  • mitogen-activated protein kinase 8/c-Jun N-terminal kinase 1 in Human [ChEMBL: CHEMBL2276] [GtoPdb: 1496] [UniProtKB: P45983]
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  • cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
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  • protein kinase D1/Protein kinase C mu in Human [ChEMBL: CHEMBL3863] [GtoPdb: 1489] [UniProtKB: Q15139]
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  • protein kinase D3/Protein kinase C nu in Human [ChEMBL: CHEMBL2595] [GtoPdb: 2174] [UniProtKB: O94806]
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  • protein kinase D2/Serine/threonine-protein kinase D2 in Human [ChEMBL: CHEMBL4900] [GtoPdb: 2173] [UniProtKB: Q9BZL6]
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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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  • 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 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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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Calmodulin-domain protein kinase 1 in Toxoplasma gondii (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1781862] [UniProtKB: Q9BJF5]
ChEMBL Inhibition of Toxoplasma gondii recombinant N-terminal hexahistidine tagged CDPK1 expressed in Escherichia coli using syntide-2 as substrate after 90 mins by luminescence based scintillation counter B 7.51 pIC50 31 nM IC50 ACS Med Chem Lett (2010) 1: 331-335 [PMID:21116453]
calcium/calmodulin-dependent protein kinase II alpha subunit/CaM kinase II alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4147] [GtoPdb: 1555] [UniProtKB: Q9UQM7]
ChEMBL Inhibition of CAMK2 F89G mutant B 8.1 pIC50 8 nM IC50 Nat Chem Biol (2005) 1: 130-142 [PMID:16408016]
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 PKA in the presence of 20uM ATP B 6.3 pIC50 500 nM IC50 Biochem J (2007) 408: 297-315 [PMID:17850214]
mitogen-activated protein kinase 8/c-Jun N-terminal kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2276] [GtoPdb: 1496] [UniProtKB: P45983]
ChEMBL Inhibition of JNK-M108A in the presence of 20uM ATP B 6.6 pIC50 250 nM IC50 Biochem J (2007) 408: 297-315 [PMID:17850214]
ChEMBL Inhibition of JNK-M108G in the presence of 20uM ATP B 6.85 pIC50 140 nM IC50 Biochem J (2007) 408: 297-315 [PMID:17850214]
cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
ChEMBL Inhibition of wild type CDK2 B 4.54 pIC50 29000 nM IC50 Nat Chem Biol (2005) 1: 130-142 [PMID:16408016]
ChEMBL Inhibition of CDK2 F80G mutant B 8.3 pIC50 5 nM IC50 Nat Chem Biol (2005) 1: 130-142 [PMID:16408016]
protein kinase D1/Protein kinase C mu in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3863] [GtoPdb: 1489] [UniProtKB: Q15139]
ChEMBL Inhibition of recombinant FLAG-tagged PKD1 (unknown origin) expressed in HEK293T cells using Syntide-2 as substrate measured after 15 mins by ADP-Glo assay B 5.99 pIC50 1013 nM IC50 Eur J Med Chem (2020) 205: 112638-112638 [PMID:32835918]
ChEMBL Inhibition of PKD1 in the presence of 50uM ATP B 6.6 pIC50 250 nM IC50 Biochem J (2007) 408: 297-315 [PMID:17850214]
protein kinase D3/Protein kinase C nu in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2595] [GtoPdb: 2174] [UniProtKB: O94806]
ChEMBL Inhibition of recombinant FLAG-tagged PKD3 (unknown origin) expressed in HEK293T cells using Syntide-2 as substrate measured after 15 mins by ADP-Glo assay B 6.21 pIC50 616 nM IC50 Eur J Med Chem (2020) 205: 112638-112638 [PMID:32835918]
protein kinase D2/Serine/threonine-protein kinase D2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4900] [GtoPdb: 2173] [UniProtKB: Q9BZL6]
ChEMBL Inhibition of recombinant FLAG-tagged PKD2 (unknown origin) expressed in HEK293T cells using Syntide-2 as substrate measured after 15 mins by ADP-Glo assay B 6.1 pIC50 786 nM IC50 Eur J Med Chem (2020) 205: 112638-112638 [PMID:32835918]
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 6.89 pIC50 130 nM IC50 Biochem J (2007) 408: 297-315 [PMID:17850214]
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 wild type c-Abl B 5.47 pIC50 3400 nM IC50 Nat Chem Biol (2005) 1: 130-142 [PMID:16408016]
ChEMBL Inhibition of c-Abl T315A mutant B 6.92 pIC50 120 nM IC50 Nat Chem Biol (2005) 1: 130-142 [PMID:16408016]
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 6.29 pIC50 510 nM IC50 Biochem J (2007) 408: 297-315 [PMID:17850214]
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 wild type c-Fyn B 6 pIC50 1000 nM IC50 Nat Chem Biol (2005) 1: 130-142 [PMID:16408016]
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 6.34 pIC50 460 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 6.21 pIC50 620 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]