fisetin [Ligand Id: 5182] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL31574 (5-desoxyquercetin, C.i. 75620, C.i. natural brown 1, Fisetin, Fisidenolon 1521, NSC-407010, NSC-656275) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 3-oxoacyl-acyl-carrier protein reductase in Plasmodium falciparum (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4513] [UniProtKB: Q965D6] | ||||||||
| ChEMBL | Inhibition of FabG | B | 5.39 | pIC50 | 4100 | nM | IC50 | J Med Chem (2006) 49: 3345-3353 [PMID:16722653] |
| acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303] | ||||||||
| ChEMBL | Inhibition of AChE (unknown origin) | B | 7.92 | pIC50 | 12 | nM | IC50 | Med Chem Res (2013) 22: 3061-3075 |
| Alpha-glucosidase MAL62 in Saccharomyces cerevisiae (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4357] [UniProtKB: P07265] | ||||||||
| ChEMBL | Inhibition of baker's yeast alpha-glucosidase using p-nitrophenyl-alpha-D-glucopyranoside as substrate by spectrophotometry | B | 1.11 | pIC50 | 1.11 | - | logIC50 | Med Chem Res (2012) 21: 3984-3993 |
| 12S-LOX/Arachidonate 12-lipoxygenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3687] [GtoPdb: 1387] [UniProtKB: P18054] | ||||||||
| ChEMBL | Inhibition of 12-hLO | B | 6.02 | pIC50 | 950 | nM | IC50 | Bioorg Med Chem (2007) 15: 7408-7425 [PMID:17869117] |
| 15-LOX-1/Arachidonate 15-lipoxygenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2903] [GtoPdb: 1388] [UniProtKB: P16050] | ||||||||
| ChEMBL | Inhibition of 15-hLO1 | B | 5.85 | pIC50 | 1400 | nM | IC50 | Bioorg Med Chem (2007) 15: 7408-7425 [PMID:17869117] |
| 15-LOX-2/Arachidonate 15-lipoxygenase, type II in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2457] [GtoPdb: 1389] [UniProtKB: O15296] | ||||||||
| ChEMBL | Inhibition of 15-hLO2 | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem (2007) 15: 7408-7425 [PMID:17869117] |
| Arginase I/Arginase-1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3232699] [GtoPdb: 1244] [UniProtKB: P07824] | ||||||||
| ChEMBL | Inhibition of recombinant rat liver arginase expressed without histidine tail assessed as urea formation using L-arginine as substrate after 15 mins by Berthelot assay | B | 5.85 | pIC50 | 1400 | nM | IC50 | Medchemcomm (2016) 7: 214-223 |
| butyrylcholinesterase/Butyrylcholinesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1914] [GtoPdb: 2471] [UniProtKB: P06276] | ||||||||
| ChEMBL | Inhibition of human plasma BChE by Ellman's method | B | 4.05 | pKi | 90000 | nM | Ki | Eur J Med Chem (2010) 45: 186-192 [PMID:19879672] |
| casein kinase 2, alpha prime polypeptide subunit/casein kinase 2, beta polypeptide subunit/casein kinase 2, alpha 1 polypeptide subunit/Casein kinase II in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2095191] [GtoPdb: 1550, 1551, 1549] [UniProtKB: P19784, P67870, P68400] | ||||||||
| ChEMBL | Inhibition of CK2 (unknown origin) | B | 6.77 | pKi | 170 | nM | Ki | Eur J Med Chem (2016) 115: 148-160 [PMID:27017545] |
| ChEMBL | Inhibition of recombinant human CK2 expressed in Escherichia coli using RRRADDSDDDDD as substrate after 10 mins | B | 6 | pIC50 | <1000 | nM | IC50 | J Med Chem (2015) 58: 7400-7408 [PMID:26322379] |
| ChEMBL | Inhibition of CK2 (unknown origin) | B | 6.46 | pIC50 | 350 | nM | IC50 | Bioorg Med Chem (2013) 21: 6681-6689 [PMID:24011954] |
| casein kinase 2, alpha 1 polypeptide subunit/Casein kinase II alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3629] [GtoPdb: 1549] [UniProtKB: P68400] | ||||||||
| ChEMBL | Inhibition of CK2alpha (unknown origin) | B | 6.46 | pKi | 350 | nM | Ki | Eur J Med Chem (2019) 181: 111581-111581 [PMID:31400711] |
| Cruzipain in Trypanosoma cruzi (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3563] [UniProtKB: P25779] | ||||||||
| ChEMBL | Inhibition of Trypanosoma cruzi cruzain by quantitative high throughput screening | B | 4.22 | pIC50 | >60000 | nM | IC50 | J Med Chem (2010) 53: 37-51 [PMID:19908840] |
| ChEMBL | Inhibition of Trypanosoma cruzi cruzain by Flexstation microplate spectrofluorimetry | B | 4.52 | pIC50 | 30000 | nM | IC50 | J Med Chem (2010) 53: 37-51 [PMID:19908840] |
| cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094127] [GtoPdb: 1961] [UniProtKB: O95067, P06493, P14635, Q8WWL7] | ||||||||
| ChEMBL | Inhibition of cyclin-dependent kinase 1/cyclinB | B | 6.1 | pIC50 | 790 | nM | IC50 | J Med Chem (2005) 48: 737-743 [PMID:15689157] |
| cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941] | ||||||||
| ChEMBL | Inhibition of CDK2 | B | 5.3 | pIC50 | 5000 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 1284-1287 [PMID:17178224] |
| cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535, Q15078] | ||||||||
| ChEMBL | Inhibition of Cyclin-dependent kinase 5-p25nck5a | B | 6.24 | pIC50 | 570 | nM | IC50 | J Med Chem (2005) 48: 737-743 [PMID:15689157] |
| cyclin dependent kinase 6/Cyclin-dependent kinase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2508] [GtoPdb: 1978] [UniProtKB: Q00534] | ||||||||
| ChEMBL | Inhibition of human cyclin-dependent kinase 6 complex with a virus-encoded cyclin from herpesvirus saimiri (Vcyclin) | B | 6.07 | pIC50 | 850 | nM | IC50 | J Med Chem (2005) 48: 737-743 [PMID:15689157] |
| ChEMBL | Inhibition of Homo sapiens (human) cyclin-dependent kinase 6 | B | 6.07 | pIC50 | 850 | nM | IC50 | Med Chem Res (2010) 19: 817-835 |
| Enoyl-acyl-carrier protein reductase in Plasmodium falciparum (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4150] [UniProtKB: Q965D5] | ||||||||
| ChEMBL | Inhibition of FabI | B | 6 | pIC50 | 1000 | nM | IC50 | J Med Chem (2006) 49: 3345-3353 [PMID:16722653] |
| ChEMBL | Inhibition of Plasmodium falciparum FabI | B | 6 | pIC50 | 1000 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 4779-4781 [PMID:20637612] |
| Fatty acid synthase in Plasmodium falciparum (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4512] [UniProtKB: Q965D7] | ||||||||
| ChEMBL | Inhibition of FabZ | B | 5.7 | pIC50 | 2000 | nM | IC50 | J Med Chem (2006) 49: 3345-3353 [PMID:16722653] |
| Glyoxalase I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2424] [UniProtKB: Q04760] | ||||||||
| ChEMBL | Inhibition constant of compound against binding of Yeast Glyoxalase I | B | 4.88 | pKi | 13182.57 | nM | Ki | J Med Chem (1988) 31: 1396-1406 [PMID:3290487] |
| Human immunodeficiency virus type 1 integrase in Human immunodeficiency virus 1 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3471] [UniProtKB: Q7ZJM1] | ||||||||
| ChEMBL | IC50 was measured as concentration required to inhibit 50% of HIV-integrase cleavage | B | 4.55 | pIC50 | 28400 | nM | IC50 | J Med Chem (1995) 38: 890-897 [PMID:7699704] |
| ChEMBL | IC50 was measured as concentration required to inhibit 50% of HIV-integrase integration | B | 5.07 | pIC50 | 8500 | nM | IC50 | J Med Chem (1995) 38: 890-897 [PMID:7699704] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum NF54 | F | 5.09 | pIC50 | 8200 | nM | IC50 | J Med Chem (2006) 49: 3345-3353 [PMID:16722653] |
| ChEMBL | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum NF54 | F | 5.09 | pIC50 | 8200 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 4779-4781 [PMID:20637612] |
| ChEMBL | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 | F | 5.19 | pIC50 | 6500 | nM | IC50 | J Med Chem (2006) 49: 3345-3353 [PMID:16722653] |
| Salivary alpha-amylase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2478] [UniProtKB: P0DUB6] | ||||||||
| ChEMBL | Inhibition of human salivary alpha-amylase | B | 4.71 | pIC50 | 19600 | nM | IC50 | J Med Chem (2008) 51: 3555-3561 [PMID:18507367] |
| Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309] | ||||||||
| ChEMBL | Inhibition of PIM1 kinase | B | 0.07 | pIC50 | 0.07 | uM | -Log IC50 | Bioorg Med Chem (2007) 15: 6463-6473 [PMID:17637507] |
| spleen associated tyrosine kinase/Tyrosine-protein kinase SYK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2599] [GtoPdb: 2230] [UniProtKB: P43405] | ||||||||
| ChEMBL | Inhibition of SYK | B | 4.82 | pIC50 | 15000 | nM | IC50 | J Med Chem (2012) 55: 3614-3643 [PMID:22257213] |
| ChEMBL | Inhibition of SYK in human mast cells assessed as reduction in mast cell degranulation | B | 4.72 | pEC50 | 19000 | nM | EC50 | J Med Chem (2012) 55: 3614-3643 [PMID:22257213] |
| xanthine dehydrogenase/Xanthine dehydrogenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1929] [GtoPdb: 2646] [UniProtKB: P47989] | ||||||||
| ChEMBL | Inhibition of xanthine oxidase assessed as decrease in uric acid production by spectrophotometry | B | 5.36 | pIC50 | 4330 | nM | IC50 | J Nat Prod (1998) 61: 71-76 [PMID:9461655] |
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]
