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 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]
