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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 |
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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] |
ChEMBL | Inhibition of FYN (unknown origin) | B | 8.3 | pIC50 | 5 | nM | IC50 | RSC Med Chem (2022) 13: 1008-1028 [PMID:36324498] |
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] |
ChEMBL | Inhibition of LCK (unknown origin) | B | 8.4 | pIC50 | 4 | nM | IC50 | RSC Med Chem (2022) 13: 1008-1028 [PMID:36324498] |
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 | Binding affinity to chicken 6-His tagged c-Src expressed in Escherichia coli Bl21 (DE3) assessed as dissociation constant | B | 6.53 | pKd | 296 | nM | Kd | Eur J Med Chem (2021) 216: 113318-113318 [PMID:33730624] |
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 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]