Target Validation Information
Target ID T97035
Target Name Tyrosine oxidase
Target Type
Successful
Drug Potency against Target 3-hydroxyphenethyl 3,4,5-trihydroxybenzoate Drug Info IC50 = 15210 nM [528984]
4',4-Dihydroxychalcone Drug Info Ki = 2900 nM [530713]
Broussonin C Drug Info Ki = 290 nM [529832]
1-hydroxy-3-(4-(trifluoromethyl)phenyl)urea Drug Info IC50 = 4300 nM [529488]
ASKENDOSIDE B Drug Info IC50 = 13950 nM [527850]
2,4,3',5'-tetrahydroxybibenzyl Drug Info Ki = 5600 nM [528382]
OXYRESVERATROL Drug Info IC50 = 12700 nM [528382]
1-Cyclopentylidenethiosemicarbazide Drug Info IC50 = 170 nM [529513]
Kazinol C Drug Info Ki = 11200 nM [529832]
1-hydroxy-3-phenylurea Drug Info IC50 = 290 nM [529488]
4'-(p-Toluenesulfonamide)-4-hydroxychalcone Drug Info Ki = 12600 nM [530713]
4'-(4-Nitrobenzensulfonamide)-4-hydroxychalcone Drug Info Ki = 11400 nM [530713]
1-Ethylidenethiosemicarbazide Drug Info IC50 = 230 nM [529513]
1-(4-bromophenyl)-3-hydroxyurea Drug Info IC50 = 2700 nM [529488]
1-(4-Methylpent-3-en-2-ylidene)thiosemicarbazide Drug Info IC50 = 11500 nM [529513]
1-(Butan-2-ylidene)thiosemicarbazide Drug Info IC50 = 280 nM [529513]
PHENYLTHIOUREA Drug Info IC50 = 1800 nM [529488]
1-(But-2-enylidene)thiosemicarbazide Drug Info IC50 = 1000 nM [529513]
5-(pyridin-4-yl)-1,3,4-oxadiazole-2(3H)-thione Drug Info Ki = 14200 nM [530900]
5-benzhydryl-1,3,4-thiadiazole-2(3H)-thione Drug Info Ki = 5200 nM [530900]
4-(6-hydroxynaphthalen-2-yl)benzene-1,3-diol Drug Info IC50 = 34 nM [528496]
7-(3,5-dihydroxyphenyl)naphthalene-1,3-diol Drug Info IC50 = 490 nM [528496]
1-(2,5-Dimethyl-1H-pyrrol-1-yl)thiourea Drug Info IC50 = 850 nM [529513]
2,2'-bi(1,3,4-thiadiazole)-5,5'(4H,4'H)-dithione Drug Info Ki = 2900 nM [530900]
1-Cyclohexylidenethiosemicarbazide Drug Info IC50 = 950 nM [529513]
1-(1-(pyrazin-2-yl)ethylidene)thiosemicarbazide Drug Info IC50 = 880 nM [529360]
1-Propylidenethiosemicarbazide Drug Info IC50 = 200 nM [529513]
4'-Amino-4-hydroxychalcone Drug Info Ki = 3900 nM [530713]
1-(Propan-2-ylidene)thiosemicarbazide Drug Info IC50 = 86 nM [529513]
1-(1-(4-fluorophenyl)ethylidene)thiosemicarbazide Drug Info IC50 = 170 nM [529360]
5-phenyl-1,3,4-thiadiazole-2(3H)-thione Drug Info Ki = 1310 nM [530900]
5-(3-hydroxyphenyl)-1,3,4-oxadiazole-2(3H)-thione Drug Info Ki = 18500 nM [530900]
3hydroxy-1-methyl-1-phenylurea Drug Info IC50 = 16000 nM [529488]
2-(ethylthiomethyl)-5-hydroxy-4H-pyran-4-one Drug Info IC50 = 2600 nM [531202]
2-(cyclohexylthiomethyl)-5-hydroxy-4H-pyran-4-one Drug Info IC50 = 87 nM [531202]
6-(3-Hydroxy-phenyl)-naphthalen-2-ol Drug Info IC50 = 6400 nM [528496]
2-(heptylthiomethyl)-5-hydroxy-4H-pyran-4-one Drug Info IC50 = 2650 nM [531202]
2-(hexylthiomethyl)-5-hydroxy-4H-pyran-4-one Drug Info IC50 = 190 nM [531202]
5-benzhydryl-1,3,4-oxadiazole-2(3H)-thione Drug Info Ki = 6760 nM [530900]
1-(1-p-tolylethylidene)thiosemicarbazide Drug Info IC50 = 270 nM [529360]
1-(1-(thiophen-2-yl)ethylidene)thiosemicarbazide Drug Info IC50 = 140 nM [529360]
5-phenyl-1,3,4-oxadiazole-2(3H)-thione Drug Info Ki = 6470 nM [530900]
1-(3-Phenylallylidene)thiosemicarbazide Drug Info IC50 = 2700 nM [529513]
1-(1,4-diacetylphenyl)dithiosemicarbazide Drug Info IC50 = 150 nM [529360]
4'-(4-Aminobenzensulfonamide)-4-hydroxychalcone Drug Info Ki = 16700 nM [530713]
5-(pyridin-4-yl)-1,3,4-thiadiazole-2(3H)-thione Drug Info Ki = 2470 nM [530900]
5,5'-methylenebis(1,3,4-oxadiazole-2(3H)-thione) Drug Info Ki = 4420 nM [530900]
5-cyclohexyl-1,3,4-oxadiazole-2(3H)-thione Drug Info Ki = 4940 nM [530900]
5-hydroxy-2-(pentylthiomethyl)-4H-pyran-4-one Drug Info IC50 = 97 nM [531202]
HINOKITIOL Drug Info Ki = 60 nM [531217]
ETHISTERONE Drug Info IC50 = 2610 nM [528526]
1-(3-phenoxypropyl)-4-(piperidin-1-yl)piperidine Drug Info IC50 = 19520 nM [528953]
N-butylresorcinol Drug Info IC50 = 150 nM [529942]
4-adamantyl resorcinol Drug Info IC50 = 900 nM [529942]
N-(2,4-dihydroxybenzyl)-3,4,5-trihydroxybenzamide Drug Info IC50 = 17000 nM [528063]
KAZINOL S Drug Info Ki = 15600 nM [529832]
1-(1-phenylethylidene)thiosemicarbazide Drug Info IC50 = 340 nM [529360]
1-(1-(pyridin-3-yl)ethylidene)thiosemicarbazide Drug Info IC50 = 820 nM [529360]
SRI-224 Drug Info IC50 = 110 nM [530419]
3,4-dihydroxybenzaldehyde-O-ethyloxime Drug Info IC50 = 300 nM [530419]
TROPOLONE Drug Info IC50 = 400 nM [530419]
1-(1-(4-bromophenyl)ethylidene)thiosemicarbazide Drug Info IC50 = 520 nM [529360]
5-(6-hydroxy-2-naphthyl)-1,2,3-benzenetriol Drug Info IC50 = 2950 nM [531026]
1-(3-Methylbutylidene)thiosemicarbazide Drug Info IC50 = 620 nM [529513]
SODIUM ZINC DIHYDROLIPOYLHISTIDINATE Drug Info IC50 = 1300 nM [528613]
1-(4-(benzyloxy)phenyl)-3-hydroxyurea Drug Info IC50 = 6300 nM [529488]
1-hydroxy-3-(4-nitrophenyl)urea Drug Info IC50 = 2600 nM [529488]
4'-(Benzensulfonamide)-4-hydroxychalcone Drug Info Ki = 13300 nM [530713]
4'-(4-Fluorobenzensulfonamide)-4-hydroxychalcone Drug Info Ki = 14900 nM [530713]
5,5'-methylenebis(1,3,4-thiadiazole-2(3H)-thione) Drug Info Ki = 490 nM [530900]
5-(6-hydroxynaphthalen-2-yl)benzene-1,3-diol Drug Info IC50 = 16520 nM [528496]
4-hexyl resorcinol Drug Info IC50 = 980 nM [529847]
KOJIC ACID Drug Info IC50 = 12000 nM [531245]
2-hydroxy-3-isopropyl-2,4,6-cycloheptatrien-1-one Drug Info Ki = 3300 nM [531217]
N-(2,4-dihydroxybenzyl)-3,4-dihydroxybenzamide Drug Info IC50 = 11000 nM [528063]
N-(2,4-dihydroxybenzyl)-3,5-dihydroxybenzamide Drug Info Ki = 1300 nM [528063]
5-(4-hydroxyphenyl)-1,3,4-oxadiazole-2(3H)-thione Drug Info Ki = 1770 nM [530900]
1'-(4-Methyl-benzyl)-[1,4']bipiperidinyl Drug Info IC50 = 1720 nM [528953]
1-(3-Oxocyclohexylidene)thiosemicarbazide Drug Info IC50 = 15100 nM [529513]
2-hydroxy-5-isopropyl-2,4,6-cycloheptatrien-1-one Drug Info Ki = 20 nM [531217]
5-benzyl-1,3,4-oxadiazole-2(3H)-thione Drug Info Ki = 3670 nM [530900]
2-(butylthiomethyl)-5-hydroxy-4H-pyran-4-one Drug Info IC50 = 1480 nM [531202]
2,2',4,4'-tetrahydroxychalcone Drug Info IC50 = 5000 nM [528649]
2,2',4,4'-tetrahydroxy-6'-methoxychalcone Drug Info IC50 = 3100 nM [528649]
7,3',4'-trihydroxyisoflavone Drug Info IC50 = 5230 nM [530587]
7,8,4'-trihydroxyisoflavone Drug Info IC50 = 11210 nM [530587]
4-hydroxyphenethyl 3,4,5-trihydroxybenzoate Drug Info IC50 = 4930 nM [528984]
2-hydroxyphenethyl 3,4,5-trihydroxybenzoate Drug Info IC50 = 14500 nM [528984]
4,4'-(ethane-1,2-diyl)dibenzene-1,3-diol Drug Info IC50 = 370 nM [529682]
5-hydroxy-2-(propylthiomethyl)-4H-pyran-4-one Drug Info IC50 = 1930 nM [531202]
Kazinol F Drug Info Ki = 770 nM [529832]
References
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Ref 529360Bioorg Med Chem. 2008 Feb 1;16(3):1096-102.1-(1-Arylethylidene)thiosemicarbazide derivatives: a new class of tyrosinase inhibitors.
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Ref 529360Bioorg Med Chem. 2008 Feb 1;16(3):1096-102.1-(1-Arylethylidene)thiosemicarbazide derivatives: a new class of tyrosinase inhibitors.
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Ref 529360Bioorg Med Chem. 2008 Feb 1;16(3):1096-102.1-(1-Arylethylidene)thiosemicarbazide derivatives: a new class of tyrosinase inhibitors.
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Ref 530900Bioorg Med Chem. 2010 Jun 1;18(11):4042-8. Epub 2010 Apr 13.New potent inhibitors of tyrosinase: novel clues to binding of 1,3,4-thiadiazole-2(3H)-thiones, 1,3,4-oxadiazole-2(3H)-thiones, 4-amino-1,2,4-triazole-5(4H)-thiones, and substituted hydrazides to the dicopper active site.
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Ref 531217Bioorg Med Chem. 2010 Nov 15;18(22):8112-8. Epub 2010 Oct 12.Structural insights into the hot spot amino acid residues of mushroom tyrosinase for the bindings of thujaplicins.
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Ref 528063Bioorg Med Chem Lett. 2006 May 15;16(10):2682-4. Epub 2006 Mar 2.N-Benzylbenzamides: a new class of potent tyrosinase inhibitors.
Ref 529832Bioorg Med Chem. 2009 Jan 1;17(1):35-41. Epub 2008 Nov 18.Tyrosinase inhibitory effects of 1,3-diphenylpropanes from Broussonetia kazinoki.
Ref 529360Bioorg Med Chem. 2008 Feb 1;16(3):1096-102.1-(1-Arylethylidene)thiosemicarbazide derivatives: a new class of tyrosinase inhibitors.
Ref 529360Bioorg Med Chem. 2008 Feb 1;16(3):1096-102.1-(1-Arylethylidene)thiosemicarbazide derivatives: a new class of tyrosinase inhibitors.
Ref 530419Bioorg Med Chem Lett. 2009 Nov 1;19(21):6157-60. Epub 2009 Sep 10.Discovery of 4-functionalized phenyl-O-beta-D-glycosides as a new class of mushroom tyrosinase inhibitors.
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Ref 530419Bioorg Med Chem Lett. 2009 Nov 1;19(21):6157-60. Epub 2009 Sep 10.Discovery of 4-functionalized phenyl-O-beta-D-glycosides as a new class of mushroom tyrosinase inhibitors.
Ref 529360Bioorg Med Chem. 2008 Feb 1;16(3):1096-102.1-(1-Arylethylidene)thiosemicarbazide derivatives: a new class of tyrosinase inhibitors.
Ref 531026Bioorg Med Chem Lett. 2010 Aug 15;20(16):4882-4. Epub 2010 Jun 19.A newly synthesized, potent tyrosinase inhibitor: 5-(6-hydroxy-2-naphthyl)-1,2,3-benzenetriol.
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Ref 528613Bioorg Med Chem. 2007 Mar 1;15(5):1967-75. Epub 2006 Dec 31.Modulating effects of a novel skin-lightening agent, alpha-lipoic acid derivative, on melanin production by the formation of DOPA conjugate products.
Ref 529488Bioorg Med Chem Lett. 2008 Jun 15;18(12):3607-10. Epub 2008 May 4.Analogues of N-hydroxy-N'-phenylthiourea and N-hydroxy-N'-phenylurea as inhibitors of tyrosinase and melanin formation.
Ref 529488Bioorg Med Chem Lett. 2008 Jun 15;18(12):3607-10. Epub 2008 May 4.Analogues of N-hydroxy-N'-phenylthiourea and N-hydroxy-N'-phenylurea as inhibitors of tyrosinase and melanin formation.
Ref 530713Eur J Med Chem. 2010 May;45(5):2010-7. Epub 2010 Jan 28.Evaluation of anti-pigmentary effect of synthetic sulfonylamino chalcone.
Ref 530713Eur J Med Chem. 2010 May;45(5):2010-7. Epub 2010 Jan 28.Evaluation of anti-pigmentary effect of synthetic sulfonylamino chalcone.
Ref 530900Bioorg Med Chem. 2010 Jun 1;18(11):4042-8. Epub 2010 Apr 13.New potent inhibitors of tyrosinase: novel clues to binding of 1,3,4-thiadiazole-2(3H)-thiones, 1,3,4-oxadiazole-2(3H)-thiones, 4-amino-1,2,4-triazole-5(4H)-thiones, and substituted hydrazides to the dicopper active site.
Ref 528496Bioorg Med Chem Lett. 2007 Jan 15;17(2):461-4. Epub 2006 Oct 12.Syntheses of hydroxy substituted 2-phenyl-naphthalenes as inhibitors of tyrosinase.
Ref 529847Bioorg Med Chem Lett. 2009 Jan 1;19(1):36-9. Epub 2008 Nov 13.PEG-immobilization of cardol and soluble polymer-supported synthesis of some cardol-coumarin derivatives: preliminary evaluation of their inhibitory activity on mushroom tyrosinase.
Ref 531245Bioorg Med Chem Lett. 2010 Dec 15;20(24):7393-6. Epub 2010 Oct 14.A novel ring-expanded product with enhanced tyrosinase inhibitory activity from classical Fe-catalyzed oxidation of rosmarinic acid,a potent antioxidative Lamiaceae polyphenol.
Ref 531217Bioorg Med Chem. 2010 Nov 15;18(22):8112-8. Epub 2010 Oct 12.Structural insights into the hot spot amino acid residues of mushroom tyrosinase for the bindings of thujaplicins.
Ref 528063Bioorg Med Chem Lett. 2006 May 15;16(10):2682-4. Epub 2006 Mar 2.N-Benzylbenzamides: a new class of potent tyrosinase inhibitors.
Ref 528063Bioorg Med Chem Lett. 2006 May 15;16(10):2682-4. Epub 2006 Mar 2.N-Benzylbenzamides: a new class of potent tyrosinase inhibitors.
Ref 530900Bioorg Med Chem. 2010 Jun 1;18(11):4042-8. Epub 2010 Apr 13.New potent inhibitors of tyrosinase: novel clues to binding of 1,3,4-thiadiazole-2(3H)-thiones, 1,3,4-oxadiazole-2(3H)-thiones, 4-amino-1,2,4-triazole-5(4H)-thiones, and substituted hydrazides to the dicopper active site.
Ref 528953Eur J Med Chem. 2007 Nov-Dec;42(11-12):1370-81. Epub 2007 Feb 23.Dragon method for finding novel tyrosinase inhibitors: Biosilico identification and experimental in vitro assays.
Ref 529513Eur J Med Chem. 2009 Apr;44(4):1773-8. Epub 2008 Apr 27.A class of potent tyrosinase inhibitors: alkylidenethiosemicarbazide compounds.
Ref 531217Bioorg Med Chem. 2010 Nov 15;18(22):8112-8. Epub 2010 Oct 12.Structural insights into the hot spot amino acid residues of mushroom tyrosinase for the bindings of thujaplicins.
Ref 530900Bioorg Med Chem. 2010 Jun 1;18(11):4042-8. Epub 2010 Apr 13.New potent inhibitors of tyrosinase: novel clues to binding of 1,3,4-thiadiazole-2(3H)-thiones, 1,3,4-oxadiazole-2(3H)-thiones, 4-amino-1,2,4-triazole-5(4H)-thiones, and substituted hydrazides to the dicopper active site.
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