PP1 [Ligand Id: 8836] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL306380 |
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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 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]
