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 |
|---|---|---|---|---|---|---|---|---|
| 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 | 8.8 | 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 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]
