PP1 analog II [Ligand Id: 6028] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL573578 |
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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 12/Cyclin-dependent kinase 12 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3559692] [GtoPdb: 1965] [UniProtKB: Q9NYV4] | ||||||||
| ChEMBL | Inhibition of CDK12 (unknown origin) | B | 7 | pIC50 | 100 | nM | IC50 | Eur J Med Chem (2022) 240: 114603-114603 [PMID:35868123] |
| 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 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]
