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] |
| BLK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase BLK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2250] [GtoPdb: 1940] [UniProtKB: P51451] | ||||||||
| ChEMBL | Inhibition of N-terminal GST tagged BLK (1 to 505 end residues) (unknown origin) expressed in Sf21insect cells by time resolved fluorescence based assay | B | 6.84 | pIC50 | 144 | nM | IC50 | Eur J Med Chem (2023) 256: 115460-115460 [PMID:37163946] |
| ChEMBL | Induction of ubiquitin proteasomal system dependent BLK degradation in human Ramos cells measured after 12 hrs by Western blot analysis | B | 7.52 | pEC50 | >30 | nM | EC50 | Eur J Med Chem (2023) 256: 115460-115460 [PMID:37163946] |
| 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] |
| ChEMBL | Inhibition of FYN (unknown origin) | B | 8.22 | pIC50 | 6 | nM | IC50 | RSC Med Chem (2022) 13: 1008-1028 [PMID:36324498] |
| 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 |
| ChEMBL | Inhibition of LCK (unknown origin) | B | 8.3 | pIC50 | 5 | nM | IC50 | RSC Med Chem (2022) 13: 1008-1028 [PMID:36324498] |
| 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 src (unknown origin) | B | 6.77 | pIC50 | 170 | nM | IC50 | J Med Chem (2021) 64: 10581-10605 [PMID:34313432] |
| 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 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]
