AG1478 [Ligand Id: 4862] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL7917 (AG-1478) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Alpha-ketoglutarate-dependent dioxygenase FTO in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2331065] [UniProtKB: Q9C0B1] | ||||||||
| ChEMBL | Inhibition of FTO (unknown origin) demethylation activity using m6A7-Broccoli RNA as substrate incubated for 3 mins under shaking condition and measured after 2 hrs by fluorescence based analysis | B | 5.52 | pIC50 | 3000 | nM | IC50 | J Med Chem (2021) 64: 16974-17003 [PMID:34792334] |
| epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] | ||||||||
| ChEMBL | Inhibition of Epidermal growth factor receptor-dependent phosphorylation | B | 6.92 | pIC50 | 120 | nM | IC50 | J Med Chem (1999) 42: 1018-1026 [PMID:10090785] |
| GtoPdb | - | - | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (1999) 42: 1018-26 [PMID:10090785] |
| ChEMBL | Inhibition of Epidermal growth factor receptor | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (1999) 42: 1018-1026 [PMID:10090785] |
| ChEMBL | Inhibitory concentration against Epidermal growth factor receptor tyrosine kinase activity | B | 8.3 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 5389-5394 [PMID:15454232] |
| ChEMBL | Inhibition of EGFR (unknown origin) | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2022) 65: 935-954 [PMID:33970631] |
| ChEMBL | Inhibition of EGFR (unknown origin) | B | 8.8 | pIC50 | 1.6 | nM | IC50 | Eur J Med Chem (2021) 225: 113766-113766 [PMID:34425313] |
| ChEMBL | Inhibition of EGFR | B | 9.5 | pIC50 | 0.32 | nM | IC50 | J Med Chem (2008) 51: 1179-1188 [PMID:18271520] |
| ChEMBL | Concentration required to inhibit the phosphorylation of a 14-residue fragment of phospholipase C gamma 1 by Epidermal growth factor receptor from A431 cell vesicles | B | 9.51 | pIC50 | 0.31 | nM | IC50 | J Med Chem (1996) 39: 267-276 [PMID:8568816] |
| epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3608] [GtoPdb: 1797] [UniProtKB: Q01279] | ||||||||
| ChEMBL | Inhibition of EGF-dependent mouse keratinocyte MK cell proliferation | F | 7 | pIC50 | <100 | nM | IC50 | J Med Chem (1999) 42: 1018-1026 [PMID:10090785] |
| Fructose-1,6-bisphosphatase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3975] [UniProtKB: P09467] | ||||||||
| ChEMBL | Concentration required to inhibit the human liver recombinant fructose-1,6-bisphosphatase. | B | 5.89 | pIC50 | 1300 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 17-21 [PMID:11140724] |
| Fructose-1,6-bisphosphatase in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2263] [UniProtKB: P00636] | ||||||||
| ChEMBL | Compound was evaluated for its concentration required to inhibit the porcine kidney F16BPase | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 17-21 [PMID:11140724] |
| Fructose-1,6-bisphosphatase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4391] [UniProtKB: P19112] | ||||||||
| ChEMBL | Compound was evaluated for its concentration required to inhibit the rat liver F16BPase | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 17-21 [PMID:11140724] |
| MAPK interacting serine/threonine kinase 1/MAP kinase-interacting serine/threonine-protein kinase MNK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4718] [GtoPdb: 2104] [UniProtKB: Q9BUB5] | ||||||||
| ChEMBL | Inhibition of MNK1 | B | 6.28 | pIC50 | 530 | nM | IC50 | J Med Chem (2010) 53: 6618-6628 [PMID:20722422] |
| mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539] | ||||||||
| ChEMBL | Inhibitory concentration against alpha mitogen activated protein kinase p38 activity | B | 6.25 | pIC50 | 560 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 5389-5394 [PMID:15454232] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay | F | 5.1 | pIC50 | 7943.28 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay | F | 5.1 | pIC50 | 7943.28 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay | F | 5.3 | pIC50 | 5011.87 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay | F | 5.6 | pIC50 | 2511.89 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| platelet derived growth factor receptor beta/platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095189] [GtoPdb: 1804, 1803] [UniProtKB: P09619, P16234] | ||||||||
| ChEMBL | Inhibition of Platelet-derived growth factor receptor-dependent phosphorylation | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (1999) 42: 1018-1026 [PMID:10090785] |
| protein kinase C alpha/Protein kinase C alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL299] [GtoPdb: 1482] [UniProtKB: P17252] | ||||||||
| ChEMBL | Inhibition of Protein kinase C alpha | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1999) 42: 1018-1026 [PMID:10090785] |
| protein kinase, membrane associated tyrosine/threonine 1/Tyrosine- and threonine-specific cdc2-inhibitory kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3984] [GtoPdb: 2167] [UniProtKB: Q99640] | ||||||||
| ChEMBL | Displacement of (6-FAM)KI(pY)VV from PKMYT1 kinase domain (unknown origin) by fluorescence polarization binding assay | B | 4.58 | pKi | 26302.68 | nM | Ki | Eur J Med Chem (2019) 161: 479-492 [PMID:30388464] |
| ChEMBL | Inhibition of N-[3',6'-dihydroxy-3-oxo-3H-spiro(2-benzofuran-1,9'-xanthen)-5-yl]-N'-[2-(4-{4-[N-(2-chloro-6-methylphenyl)-5-carboxamido]-thiazol-2-yl})-amino-2-methyl-pyrimid-6-yl)piperazinyl]-ethyl]thiourea binding to human PKMYT1 kinase doamin expressed in Escherichia coli BL21 after 120 mins by fluorescence polarization asay | B | 4.58 | pKi | 26200 | nM | Ki | Bioorg Med Chem (2018) 26: 4014-4024 [PMID:29941193] |
| ChEMBL | Displacement of (6-FAM)KI(pY)VV from PKMYT1 kinase domain (unknown origin) by fluorescence polarization binding assay | B | 4.58 | pKi | 26200 | nM | Ki | Eur J Med Chem (2019) 161: 479-492 [PMID:30388464] |
| ChEMBL | Inhibition of human full length PKMYT1 expressed in HEK293 cells using EFS (247 to 259 residues) as substrate after 1 hr by fluorescence polarization immunoasay | B | 5.73 | pKi | 1870 | nM | Ki | Bioorg Med Chem (2018) 26: 4014-4024 [PMID:29941193] |
| ChEMBL | Displacement of (6-FAM)KI(pY)VV from full length PKMYT1 (unknown origin) by fluorescence polarization immuno assay | B | 5.73 | pKi | 1870 | nM | Ki | Eur J Med Chem (2019) 161: 479-492 [PMID:30388464] |
| ChEMBL | Inhibition of N-[3',6'-dihydroxy-3-oxo-3H-spiro(2-benzofuran-1,9'-xanthen)-5-yl]-N'-[2-(4-{4-[N-(2-chloro-6-methylphenyl)-5-carboxamido]-thiazol-2-yl})-amino-2-methyl-pyrimid-6-yl)piperazinyl]-ethyl]thiourea binding to human PKMYT1 kinase doamin expressed in Escherichia coli BL21 after 120 mins by fluorescence polarization asay | B | 4.26 | pIC50 | 55000 | nM | IC50 | Bioorg Med Chem (2018) 26: 4014-4024 [PMID:29941193] |
| ChEMBL | Displacement of (6-FAM)KI(pY)VV from PKMYT1 kinase domain (unknown origin) by fluorescence polarization binding assay | B | 4.26 | pIC50 | 55000 | nM | IC50 | Eur J Med Chem (2019) 161: 479-492 [PMID:30388464] |
| ChEMBL | Inhibition of human full length PKMYT1 expressed in HEK293 cells using EFS (247 to 259 residues) as substrate after 1 hr by fluorescence polarization immunoasay | B | 4.71 | pIC50 | 19600 | nM | IC50 | Bioorg Med Chem (2018) 26: 4014-4024 [PMID:29941193] |
| ChEMBL | Displacement of (6-FAM)KI(pY)VV from full length PKMYT1 (unknown origin) by fluorescence polarization immuno assay | B | 4.71 | pIC50 | 19600 | nM | IC50 | Eur J Med Chem (2019) 161: 479-492 [PMID:30388464] |
| 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 p60 c-Src tyrosine kinase | B | 5.57 | pIC50 | 2700 | nM | IC50 | J Med Chem (1999) 42: 1018-1026 [PMID:10090785] |
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]
