AG1478 [Ligand Id: 4862] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL7917 (AG-1478)
  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Mouse [ChEMBL: CHEMBL3608] [GtoPdb: 1797] [UniProtKB: Q01279]
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  • MAPK interacting serine/threonine kinase 1/MAP kinase-interacting serine/threonine-protein kinase MNK1 in Human [ChEMBL: CHEMBL4718] [GtoPdb: 2104] [UniProtKB: Q9BUB5]
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  • mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
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  • platelet derived growth factor receptor beta/platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor in Human [ChEMBL: CHEMBL2095189] [GtoPdb: 18041803] [UniProtKB: P09619P16234]
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  • protein kinase C alpha/Protein kinase C alpha in Human [ChEMBL: CHEMBL299] [GtoPdb: 1482] [UniProtKB: P17252]
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  • protein kinase, membrane associated tyrosine/threonine 1/Tyrosine- and threonine-specific cdc2-inhibitory kinase in Human [ChEMBL: CHEMBL3984] [GtoPdb: 2167] [UniProtKB: Q99640]
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  • SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 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: 18041803] [UniProtKB: P09619P16234]
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 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 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 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 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]
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 26:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]