Target Validation Information
TTD ID T97035
Target Name Tyrosinase (TYR)
Type of Target
Successful
Drug Potency against Target 1'-(4-Methyl-benzyl)-[1,4']bipiperidinyl Drug Info IC50 = 1720 nM [8]
1-(1,4-diacetylphenyl)dithiosemicarbazide Drug Info IC50 = 150 nM [10]
1-(1-(4-bromophenyl)ethylidene)thiosemicarbazide Drug Info IC50 = 520 nM [10]
1-(1-(4-fluorophenyl)ethylidene)thiosemicarbazide Drug Info IC50 = 170 nM [10]
1-(1-(pyrazin-2-yl)ethylidene)thiosemicarbazide Drug Info IC50 = 880 nM [10]
1-(1-(pyridin-3-yl)ethylidene)thiosemicarbazide Drug Info IC50 = 820 nM [10]
1-(1-(thiophen-2-yl)ethylidene)thiosemicarbazide Drug Info IC50 = 140 nM [10]
1-(1-p-tolylethylidene)thiosemicarbazide Drug Info IC50 = 270 nM [10]
1-(1-phenylethylidene)thiosemicarbazide Drug Info IC50 = 340 nM [10]
1-(2,5-Dimethyl-1H-pyrrol-1-yl)thiourea Drug Info IC50 = 850 nM [12]
1-(3-Methylbutylidene)thiosemicarbazide Drug Info IC50 = 620 nM [12]
1-(3-Oxocyclohexylidene)thiosemicarbazide Drug Info IC50 = 15100 nM [12]
1-(3-phenoxypropyl)-4-(piperidin-1-yl)piperidine Drug Info IC50 = 19520 nM [8]
1-(3-Phenylallylidene)thiosemicarbazide Drug Info IC50 = 2700 nM [12]
1-(4-(benzyloxy)phenyl)-3-hydroxyurea Drug Info IC50 = 6300 nM [11]
1-(4-bromophenyl)-3-hydroxyurea Drug Info IC50 = 2700 nM [11]
1-(4-Methylpent-3-en-2-ylidene)thiosemicarbazide Drug Info IC50 = 11500 nM [12]
1-(But-2-enylidene)thiosemicarbazide Drug Info IC50 = 1000 nM [12]
1-(Butan-2-ylidene)thiosemicarbazide Drug Info IC50 = 280 nM [12]
1-(Propan-2-ylidene)thiosemicarbazide Drug Info IC50 = 86 nM [12]
1-Cyclohexylidenethiosemicarbazide Drug Info IC50 = 950 nM [12]
1-Cyclopentylidenethiosemicarbazide Drug Info IC50 = 170 nM [12]
1-Ethylidenethiosemicarbazide Drug Info IC50 = 230 nM [12]
1-hydroxy-3-(4-(trifluoromethyl)phenyl)urea Drug Info IC50 = 4300 nM [11]
1-hydroxy-3-(4-nitrophenyl)urea Drug Info IC50 = 2600 nM [11]
1-hydroxy-3-phenylurea Drug Info IC50 = 290 nM [11]
1-Propylidenethiosemicarbazide Drug Info IC50 = 200 nM [12]
2,2',4,4'-tetrahydroxy-6'-methoxychalcone Drug Info IC50 = 3100 nM [7]
2,2',4,4'-tetrahydroxychalcone Drug Info IC50 = 5000 nM [7]
2,2'-bi(1,3,4-thiadiazole)-5,5'(4H,4'H)-dithione Drug Info Ki = 2900 nM [20]
2,4,3',5'-tetrahydroxybibenzyl Drug Info Ki = 5600 nM [3]
2-(butylthiomethyl)-5-hydroxy-4H-pyran-4-one Drug Info IC50 = 1480 nM [22]
2-(cyclohexylthiomethyl)-5-hydroxy-4H-pyran-4-one Drug Info IC50 = 87 nM [22]
2-(ethylthiomethyl)-5-hydroxy-4H-pyran-4-one Drug Info IC50 = 2600 nM [22]
2-(heptylthiomethyl)-5-hydroxy-4H-pyran-4-one Drug Info IC50 = 2650 nM [22]
2-(hexylthiomethyl)-5-hydroxy-4H-pyran-4-one Drug Info IC50 = 190 nM [22]
2-hydroxy-3-isopropyl-2,4,6-cycloheptatrien-1-one Drug Info Ki = 3300 nM [23]
2-hydroxy-5-isopropyl-2,4,6-cycloheptatrien-1-one Drug Info Ki = 20 nM [23]
2-hydroxyphenethyl 3,4,5-trihydroxybenzoate Drug Info IC50 = 14500 nM [9]
3,4-dihydroxybenzaldehyde-O-ethyloxime Drug Info IC50 = 300 nM [17]
3-hydroxyphenethyl 3,4,5-trihydroxybenzoate Drug Info IC50 = 15210 nM [9]
3hydroxy-1-methyl-1-phenylurea Drug Info IC50 = 16000 nM [11]
4',4-Dihydroxychalcone Drug Info Ki = 2900 nM [19]
4'-(4-Aminobenzensulfonamide)-4-hydroxychalcone Drug Info Ki = 16700 nM [19]
4'-(4-Fluorobenzensulfonamide)-4-hydroxychalcone Drug Info Ki = 14900 nM [19]
4'-(4-Nitrobenzensulfonamide)-4-hydroxychalcone Drug Info Ki = 11400 nM [19]
4'-(Benzensulfonamide)-4-hydroxychalcone Drug Info Ki = 13300 nM [19]
4'-(p-Toluenesulfonamide)-4-hydroxychalcone Drug Info Ki = 12600 nM [19]
4'-Amino-4-hydroxychalcone Drug Info Ki = 3900 nM [19]
4,4'-(ethane-1,2-diyl)dibenzene-1,3-diol Drug Info IC50 = 370 nM [13]
4-(6-hydroxynaphthalen-2-yl)benzene-1,3-diol Drug Info IC50 = 34 nM [4]
4-adamantyl resorcinol Drug Info IC50 = 900 nM [16]
4-hexyl resorcinol Drug Info IC50 = 980 nM [15]
4-hydroxyphenethyl 3,4,5-trihydroxybenzoate Drug Info IC50 = 4930 nM [9]
5,5'-methylenebis(1,3,4-oxadiazole-2(3H)-thione) Drug Info Ki = 4420 nM [20]
5,5'-methylenebis(1,3,4-thiadiazole-2(3H)-thione) Drug Info Ki = 490 nM [20]
5-(3-hydroxyphenyl)-1,3,4-oxadiazole-2(3H)-thione Drug Info Ki = 18500 nM [20]
5-(4-hydroxyphenyl)-1,3,4-oxadiazole-2(3H)-thione Drug Info Ki = 1770 nM [20]
5-(6-hydroxy-2-naphthyl)-1,2,3-benzenetriol Drug Info IC50 = 2950 nM [21]
5-(6-hydroxynaphthalen-2-yl)benzene-1,3-diol Drug Info IC50 = 16520 nM [4]
5-(pyridin-4-yl)-1,3,4-oxadiazole-2(3H)-thione Drug Info Ki = 14200 nM [20]
5-(pyridin-4-yl)-1,3,4-thiadiazole-2(3H)-thione Drug Info Ki = 2470 nM [20]
5-benzhydryl-1,3,4-oxadiazole-2(3H)-thione Drug Info Ki = 6760 nM [20]
5-benzhydryl-1,3,4-thiadiazole-2(3H)-thione Drug Info Ki = 5200 nM [20]
5-benzyl-1,3,4-oxadiazole-2(3H)-thione Drug Info Ki = 3670 nM [20]
5-cyclohexyl-1,3,4-oxadiazole-2(3H)-thione Drug Info Ki = 4940 nM [20]
5-hydroxy-2-(pentylthiomethyl)-4H-pyran-4-one Drug Info IC50 = 97 nM [22]
5-hydroxy-2-(propylthiomethyl)-4H-pyran-4-one Drug Info IC50 = 1930 nM [22]
5-phenyl-1,3,4-oxadiazole-2(3H)-thione Drug Info Ki = 6470 nM [20]
5-phenyl-1,3,4-thiadiazole-2(3H)-thione Drug Info Ki = 1310 nM [20]
6-(3-Hydroxy-phenyl)-naphthalen-2-ol Drug Info IC50 = 6400 nM [4]
7,3',4'-trihydroxyisoflavone Drug Info IC50 = 5230 nM [18]
7,8,4'-trihydroxyisoflavone Drug Info IC50 = 11210 nM [18]
7-(3,5-dihydroxyphenyl)naphthalene-1,3-diol Drug Info IC50 = 490 nM [4]
ASKENDOSIDE B Drug Info IC50 = 13950 nM [1]
Broussonin C Drug Info Ki = 290 nM [14]
ETHISTERONE Drug Info IC50 = 2610 nM [5]
HINOKITIOL Drug Info Ki = 60 nM [23]
Kazinol C Drug Info Ki = 11200 nM [14]
Kazinol F Drug Info Ki = 770 nM [14]
KAZINOL S Drug Info Ki = 15600 nM [14]
KOJIC ACID Drug Info IC50 = 12000 nM [24]
N-(2,4-dihydroxybenzyl)-3,4,5-trihydroxybenzamide Drug Info IC50 = 17000 nM [2]
N-(2,4-dihydroxybenzyl)-3,4-dihydroxybenzamide Drug Info IC50 = 11000 nM [2]
N-(2,4-dihydroxybenzyl)-3,5-dihydroxybenzamide Drug Info Ki = 1300 nM [2]
N-butylresorcinol Drug Info IC50 = 150 nM [16]
OXYRESVERATROL Drug Info IC50 = 12700 nM [3]
PHENYLTHIOUREA Drug Info IC50 = 1800 nM [11]
SODIUM ZINC DIHYDROLIPOYLHISTIDINATE Drug Info IC50 = 1300 nM [6]
SRI-224 Drug Info IC50 = 110 nM [17]
TROPOLONE Drug Info IC50 = 400 nM [17]
References
REF 1 New tyrosinase inhibitors selected by atomic linear indices-based classification models. Bioorg Med Chem Lett. 2006 Jan 15;16(2):324-30.
REF 2 N-Benzylbenzamides: a new class of potent tyrosinase inhibitors. Bioorg Med Chem Lett. 2006 May 15;16(10):2682-4.
REF 3 Chemical transformations of oxyresveratrol (trans-2,4,3',5'-tetrahydroxystilbene) into a potent tyrosinase inhibitor and a strong cytotoxic agent. Bioorg Med Chem Lett. 2006 Nov 1;16(21):5650-3.
REF 4 Syntheses of hydroxy substituted 2-phenyl-naphthalenes as inhibitors of tyrosinase. Bioorg Med Chem Lett. 2007 Jan 15;17(2):461-4.
REF 5 TOMOCOMD-CARDD descriptors-based virtual screening of tyrosinase inhibitors: evaluation of different classification model combinations using bond-b... Bioorg Med Chem. 2007 Feb 1;15(3):1483-503.
REF 6 Modulating effects of a novel skin-lightening agent, alpha-lipoic acid derivative, on melanin production by the formation of DOPA conjugate products. Bioorg Med Chem. 2007 Mar 1;15(5):1967-75.
REF 7 Synthesis and evaluation of 2',4',6'-trihydroxychalcones as a new class of tyrosinase inhibitors. Bioorg Med Chem. 2007 Mar 15;15(6):2396-402.
REF 8 Dragon method for finding novel tyrosinase inhibitors: Biosilico identification and experimental in vitro assays. Eur J Med Chem. 2007 Nov-Dec;42(11-12):1370-81.
REF 9 Synthetic tyrosyl gallate derivatives as potent melanin formation inhibitors. Bioorg Med Chem Lett. 2007 Oct 1;17(19):5462-4.
REF 10 1-(1-Arylethylidene)thiosemicarbazide derivatives: a new class of tyrosinase inhibitors. Bioorg Med Chem. 2008 Feb 1;16(3):1096-102.
REF 11 Analogues of N-hydroxy-N'-phenylthiourea and N-hydroxy-N'-phenylurea as inhibitors of tyrosinase and melanin formation. Bioorg Med Chem Lett. 2008 Jun 15;18(12):3607-10.
REF 12 A class of potent tyrosinase inhibitors: alkylidenethiosemicarbazide compounds. Eur J Med Chem. 2009 Apr;44(4):1773-8.
REF 13 Molecular design of potent tyrosinase inhibitors having the bibenzyl skeleton. Bioorg Med Chem Lett. 2008 Oct 1;18(19):5252-4.
REF 14 Tyrosinase inhibitory effects of 1,3-diphenylpropanes from Broussonetia kazinoki. Bioorg Med Chem. 2009 Jan 1;17(1):35-41.
REF 15 PEG-immobilization of cardol and soluble polymer-supported synthesis of some cardol-coumarin derivatives: preliminary evaluation of their inhibitor... Bioorg Med Chem Lett. 2009 Jan 1;19(1):36-9.
REF 16 Studies on depigmenting activities of dihydroxyl benzamide derivatives containing adamantane moiety. Bioorg Med Chem Lett. 2009 Mar 1;19(5):1532-3.
REF 17 Discovery of 4-functionalized phenyl-O-beta-D-glycosides as a new class of mushroom tyrosinase inhibitors. Bioorg Med Chem Lett. 2009 Nov 1;19(21):6157-60.
REF 18 Natural ortho-dihydroxyisoflavone derivatives from aged Korean fermented soybean paste as potent tyrosinase and melanin formation inhibitors. Bioorg Med Chem Lett. 2010 Feb 1;20(3):1162-4.
REF 19 Evaluation of anti-pigmentary effect of synthetic sulfonylamino chalcone. Eur J Med Chem. 2010 May;45(5):2010-7.
REF 20 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-triaz... Bioorg Med Chem. 2010 Jun 1;18(11):4042-8.
REF 21 A newly synthesized, potent tyrosinase inhibitor: 5-(6-hydroxy-2-naphthyl)-1,2,3-benzenetriol. Bioorg Med Chem Lett. 2010 Aug 15;20(16):4882-4.
REF 22 Kojyl thioether derivatives having both tyrosinase inhibitory and anti-inflammatory properties. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6569-71.
REF 23 Structural insights into the hot spot amino acid residues of mushroom tyrosinase for the bindings of thujaplicins. Bioorg Med Chem. 2010 Nov 15;18(22):8112-8.
REF 24 A novel ring-expanded product with enhanced tyrosinase inhibitory activity from classical Fe-catalyzed oxidation of rosmarinic acid, a potent antio... Bioorg Med Chem Lett. 2010 Dec 15;20(24):7393-6.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.