AG 490 [Ligand Id: 5916] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL56543 (AG-490) |
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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 EGF-dependent proliferation of human and guinea pig keratinocytes; range 7-15 uM | F | 5.15 | pIC50 | 7000 | nM | IC50 | J Med Chem (2001) 44: 281-297 [PMID:11462969] |
| ChEMBL | Inhibition of HER14 (human EGFR overexpressing) cell proliferation. | F | 5.46 | pIC50 | 3500 | nM | IC50 | J Med Chem (1991) 34: 1896-1907 [PMID:1676428] |
| ChEMBL | Inhibition of EGFR in human A431 cells | B | 5.7 | pIC50 | 2000 | nM | IC50 | J Nat Prod (1992) 55: 1529-1560 [PMID:1479375] |
| ChEMBL | Inhibition of polyGAT phosphorylation | B | 5.7 | pIC50 | 2000 | nM | IC50 | J Med Chem (1991) 34: 1896-1907 [PMID:1676428] |
| ChEMBL | Inhibitory activity against epidermal growth factor receptor (EGFR) | B | 6.3 | pIC50 | 501.19 | nM | IC50 | J Med Chem (2003) 46: 4657-4668 [PMID:14561085] |
| GtoPdb | Inhibition of substrate phosphorylation. | - | 6.4 | pIC50 | 400 | nM | IC50 | J Med Chem (1991) 34: 1896-907 [PMID:1676428] |
| ChEMBL | In vitro inhibition of HER1 autophosphorylation. | B | 7 | pIC50 | 100 | nM | IC50 | J Med Chem (1991) 34: 1896-1907 [PMID:1676428] |
| ChEMBL | Inhibition of Epidermal growth factor receptor autophosphorylation | B | 7 | pIC50 | 100 | nM | IC50 | J Med Chem (1999) 42: 3412-3420 [PMID:10464027] |
| ChEMBL | Inhibition of EGFR autophosphorylation | B | 7 | pIC50 | 100 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
| GluN1/GluN2A/Glutamate NMDA receptor; Grin1/Grin2a in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096680] [GtoPdb: 455, 456] [UniProtKB: P35439, Q00959] | ||||||||
| ChEMBL | Antagonistic activity against N-methyl-D-aspartate glutamate receptor 1/2A. | F | 4.72 | pIC50 | 19000 | nM | IC50 | J Med Chem (1999) 42: 3412-3420 [PMID:10464027] |
| GluN1/GluN2B/Glutamate NMDA receptor; Grin1/Grin2b in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096666] [GtoPdb: 455, 457] [UniProtKB: P35439, Q00960] | ||||||||
| ChEMBL | Antagonistic activity against N-methyl-D-aspartate glutamate receptor 1/2B. | F | 4.35 | pIC50 | 45000 | nM | IC50 | J Med Chem (1999) 42: 3412-3420 [PMID:10464027] |
| GluN1/GluN2C/Glutamate NMDA receptor; Grin1/Grin2c in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096911] [GtoPdb: 455, 458] [UniProtKB: P35439, Q00961] | ||||||||
| ChEMBL | Antagonistic activity against N-methyl-D-aspartate glutamate receptor 1/2C. | F | 4 | pIC50 | 100000 | nM | IC50 | J Med Chem (1999) 42: 3412-3420 [PMID:10464027] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay | F | 4.9 | pIC50 | 12589.25 | 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 3D7 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 | 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 W2 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 Dd2 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| erb-b2 receptor tyrosine kinase 2/Receptor protein-tyrosine kinase erbB-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1824] [GtoPdb: 2019] [UniProtKB: P04626] | ||||||||
| ChEMBL | Inhibition of ERBB2 receptor autophosphorylation | B | 4.87 | pIC50 | 13500 | nM | IC50 | J Med Chem (1999) 42: 3412-3420 [PMID:10464027] |
| ChEMBL | In vitro inhibition of ERBB2 receptor kinase autophosphorylation. | B | 4.87 | pIC50 | 13500 | nM | IC50 | J Med Chem (1991) 34: 1896-1907 [PMID:1676428] |
| ChEMBL | Inhibitory activity tested against protein kinase HER-2 | B | 4.87 | pIC50 | 13489.63 | nM | IC50 | J Med Chem (2003) 46: 4657-4668 [PMID:14561085] |
| Janus kinase 1/Tyrosine-protein kinase JAK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458] | ||||||||
| ChEMBL | Inhibition of JAK1 | B | 5.47 | pIC50 | 3380 | nM | IC50 | Science (2003) 302: 875-878 [PMID:14593182] |
| Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674] | ||||||||
| ChEMBL | Inhibition of JAK2 | B | 5 | pIC50 | >10000 | nM | IC50 | Science (2003) 302: 875-878 [PMID:14593182] |
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]
