PP2 [Ligand Id: 9404] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL406845 (AG-1879) |
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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 | 7.39 | pIC50 | 41 | nM | IC50 | Biochem J (2007) 408: 297-315 [PMID:17850214] |
| EPH receptor B2/Ephrin type-B receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3290] [GtoPdb: 1831] [UniProtKB: P29323] | ||||||||
| ChEMBL | Equilibrium binding constant for EPH receptor B2 | B | 4.44 | pKd | 36500 | nM | Kd | J Med Chem (2005) 48: 3221-3230 [PMID:15857128] |
| ChEMBL | Inhibition of EPH receptor B2 using ELISA | B | 4.28 | pIC50 | 52000 | nM | IC50 | J Med Chem (2005) 48: 3221-3230 [PMID:15857128] |
| 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 | 5 | pKi | >10000 | nM | Ki | ACS Med Chem Lett (2012) 3: 383-386 [PMID:24900482] |
| ChEMBL | Inhibition of EGFR | B | 6.32 | pIC50 | 480 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
| mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539] | ||||||||
| ChEMBL | Inhibition of p38 alpha (unknown origin) using Ser/Thr 15 as substrate incubated for 1 hr in presence of ATP by Z'-Lyte assay | B | 5.37 | pIC50 | 4230 | nM | IC50 | Eur J Med Chem (2021) 215: 113277-113277 [PMID:33601311] |
| 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 | 7.72 | pIC50 | 19 | 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 | Binding affinity to human recombinant Abl by cell free assay | B | 6.3 | pKi | 500 | nM | Ki | J Med Chem (2008) 51: 1252-1259 [PMID:18257513] |
| 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 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 | - | - | 8.3 | pIC50 | 5 | nM | IC50 | J Biol Chem (1996) 271: 695-701 [PMID:8557675] |
| HCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase HCK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3234] [GtoPdb: 2032] [UniProtKB: P08631] | ||||||||
| ChEMBL | Inhibition of Hck | B | 8.3 | pIC50 | 5 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
| 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 | 9.1 | pKi | 0.79 | nM | Ki | ACS Med Chem Lett (2012) 3: 383-386 [PMID:24900482] |
| ChEMBL | Inhibition of p56 Lck tyrosine kinase in Jurkat cells where p56lck autophosphorylation is inhibited. | B | 8.4 | pIC50 | 4 | nM | IC50 | Bioorg Med Chem Lett (1997) 7: 417-420 |
| ChEMBL | Inhibition of p56lck autophosphorylation | B | 8.4 | pIC50 | 4 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
| GtoPdb | - | - | 8.4 | pIC50 | 4 | nM | IC50 | J Biol Chem (1996) 271: 695-701 [PMID:8557675] |
| 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 | 7.51 | pIC50 | 31 | 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 | 7.44 | pIC50 | 36 | 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 | Inhibitory activity against Src in cell free assay | B | 6.3 | pKi | 500 | nM | Ki | J Med Chem (2006) 49: 1549-1561 [PMID:16509573] |
| ChEMBL | Inhibition of human recombinant Src | B | 6.3 | pKi | 500 | nM | Ki | J Med Chem (2007) 50: 5579-5588 [PMID:17929792] |
| ChEMBL | Inhibition of GST-tagged c-Src preincubated for 30 mins measured after 60 mins | B | 5.55 | pIC50 | 2800 | nM | IC50 | Bioorg Med Chem (2012) 20: 6821-6830 [PMID:23098606] |
| ChEMBL | Inhibition of c-Src after 60 mins | B | 5.55 | pIC50 | 2800 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 449-452 [PMID:21084189] |
| ChEMBL | Inhibition of GST-fussed c-SRC after 30 mins | B | 5.55 | pIC50 | 2800 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1342-1346 [PMID:21300544] |
| ChEMBL | Inhibition of His6-tagged c-Src kinase domain using AEEEIYGEFEAKKKK as substrate pre-incubated for 10 mins before substrate addition measured after 30 mins by Transcreener ADP2 FI Assay | B | 6.3 | pIC50 | 500 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 410-414 [PMID:22119472] |
| ChEMBL | Inhibition of 6xHis-tagged Src catalytic domain (unknown origin) expressed in Escherichia coli using AEEEIYGEFEAKKKK as substrate incubated for 10 mins prior to substrate addition measured after 30 mins by fluorescence intensity assay | B | 6.3 | pIC50 | 500 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 3230-3234 [PMID:23602444] |
| ChEMBL | Inhibition cSRC | B | 7.3 | pIC50 | 50 | nM | IC50 | Bioorg Med Chem (2010) 18: 4615-4624 [PMID:20570525] |
| ChEMBL | Inhibition of Src (unknown origin) using Src-family kinase bisamide rhodamine 110 peptide substrate after 1 hr by fluorescence assay | B | 9.3 | pIC50 | 0.5 | nM | IC50 | Eur J Med Chem (2018) 157: 503-526 [PMID:30114661] |
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]
