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Literature summary for 1.14.18.1 extracted from

  • Ghani, U.; Ullah, N.
    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 (2010), Bioorg. Med. Chem., 18, 4042-4048.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
2,2':4',2''-ter-1,3,4-oxadiazole-5,5',5''(4H,4''H)-trithione
-
Agaricus bisporus
2,2':4',2''-ter-1,3,4-thiadiazole-5,5',5''(4H,4''H)-trithione
-
Agaricus bisporus
4,4'-diamino-3-(4-hydroxyphenyl)-1'H-1,3'-bi-1,2,4-triazole-5,5'(4H,4'H)-dithione
-
Agaricus bisporus
4,4'-diamino-3-(pyridin-4-yl)-1'H-1,3'-bi-1,2,4-triazole-5,5'(4H,4'H)-dithione
-
Agaricus bisporus
4-(benzyloxy)-N'-(hydrazinylcarbonyl)benzohydrazide
-
Agaricus bisporus
5'-(3-hydroxyphenyl)-2,3'-bi-1,3,4-oxadiazole-2',5(4H)-dithione
-
Agaricus bisporus
5'-(4-hydroxyphenyl)-2,3'-bi-1,3,4-oxadiazole-2',5(4H)-dithione
-
Agaricus bisporus
5'-(4-hydroxyphenyl)-2,3'-bi-1,3,4-thiadiazole-2',5(4H)-dithione
-
Agaricus bisporus
5'-(4-[[tert-butyl(dimethyl)silyl]oxy]phenyl)-2,3'-bi-1,3,4-thiadiazole-2',5(4H)-dithione
-
Agaricus bisporus
5'-(diphenylmethyl)-2,3'-bi-1,3,4-oxadiazole-2',5(4H)-dithione
-
Agaricus bisporus
5'-(diphenylmethyl)-2,3'-bi-1,3,4-thiadiazole-2',5(4H)-dithione
-
Agaricus bisporus
5'-(naphthalen-1-yl)-2,3'-bi-1,3,4-oxadiazole-2',5(4H)-dithione
-
Agaricus bisporus
5'-(pyridin-4-yl)-2,3'-bi-1,3,4-oxadiazole-2',5(4H)-dithione
-
Agaricus bisporus
5'-(pyridin-4-yl)-2,3'-bi-1,3,4-thiadiazole-2',5(4H)-dithione
-
Agaricus bisporus
5'-benzyl-2,3'-bi-1,3,4-oxadiazole-2',5(4H)-dithione
-
Agaricus bisporus
5'-cyclohexyl-2,3'-bi-1,3,4-oxadiazole-2',5(4H)-dithione
-
Agaricus bisporus
5'-phenyl-2,3'-bi-1,3,4-oxadiazole-2',5(4H)-dithione
-
Agaricus bisporus
5'-phenyl-2,3'-bi-1,3,4-thiadiazole-2',5(4H)-dithione
-
Agaricus bisporus
5'-[(5-thioxo-4,5-dihydro-1,3,4-oxadiazol-2-yl)methyl]-2,3'-bi-1,3,4-oxadiazole-2',5(4H)-dithione
-
Agaricus bisporus
5'-[(5-thioxo-4,5-dihydro-1,3,4-thiadiazol-2-yl)methyl]-2,3'-bi-1,3,4-thiadiazole-2',5(4H)-dithione
-
Agaricus bisporus
5'-[3-(5-thioxo-4,5-dihydro-1,3,4-oxadiazol-2-yl)propyl]-2,3'-bi-1,3,4-oxadiazole-2',5(4H)-dithione
-
Agaricus bisporus
5'-[3-(benzyloxy)phenyl]-2,3'-bi-1,3,4-oxadiazole-2',5(4H)-dithione
-
Agaricus bisporus
5'-[4-(benzyloxy)phenyl]-2,3'-bi-1,3,4-oxadiazole-2',5(4H)-dithione
-
Agaricus bisporus
kojic acid
-
Agaricus bisporus
N'-(hydrazinylcarbonyl)-4-hydroxybenzohydrazide
-
Agaricus bisporus
N'-(hydrazinylcarbonyl)naphthalene-2-carbohydrazide
-
Agaricus bisporus

Metals/Ions

Metals/Ions Comment Organism Structure
Cu2+ the enzyme contains copper Agaricus bisporus

Organism

Organism UniProt Comment Textmining
Agaricus bisporus
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
L-Dopa + O2
-
Agaricus bisporus L-dopaquinone + H2O
-
?

Synonyms

Synonyms Comment Organism
monophenol, o-diphenol:oxygen oxidoreductase
-
Agaricus bisporus
tyrosinase
-
Agaricus bisporus

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0223
-
kojic acid in 50 mM Na-phosphate buffer (pH 6.8), at 25°C Agaricus bisporus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00019
-
in 50 mM Na-phosphate buffer (pH 6.8), at 25°C Agaricus bisporus 5'-(4-hydroxyphenyl)-2,3'-bi-1,3,4-thiadiazole-2',5(4H)-dithione
0.00049
-
in 50 mM Na-phosphate buffer (pH 6.8), at 25°C Agaricus bisporus 5'-[(5-thioxo-4,5-dihydro-1,3,4-thiadiazol-2-yl)methyl]-2,3'-bi-1,3,4-thiadiazole-2',5(4H)-dithione
0.00053
-
in 50 mM Na-phosphate buffer (pH 6.8), at 25°C Agaricus bisporus 5'-(4-[[tert-butyl(dimethyl)silyl]oxy]phenyl)-2,3'-bi-1,3,4-thiadiazole-2',5(4H)-dithione
0.00101
-
in 50 mM Na-phosphate buffer (pH 6.8), at 25°C Agaricus bisporus 4,4'-diamino-3-(pyridin-4-yl)-1'H-1,3'-bi-1,2,4-triazole-5,5'(4H,4'H)-dithione
0.00131
-
in 50 mM Na-phosphate buffer (pH 6.8), at 25°C Agaricus bisporus 5'-phenyl-2,3'-bi-1,3,4-thiadiazole-2',5(4H)-dithione
0.00135
-
in 50 mM Na-phosphate buffer (pH 6.8), at 25°C Agaricus bisporus 5'-[4-(benzyloxy)phenyl]-2,3'-bi-1,3,4-oxadiazole-2',5(4H)-dithione
0.00177
-
in 50 mM Na-phosphate buffer (pH 6.8), at 25°C Agaricus bisporus 5'-(4-hydroxyphenyl)-2,3'-bi-1,3,4-oxadiazole-2',5(4H)-dithione
0.0019
-
in 50 mM Na-phosphate buffer (pH 6.8), at 25°C Agaricus bisporus 5'-[3-(5-thioxo-4,5-dihydro-1,3,4-oxadiazol-2-yl)propyl]-2,3'-bi-1,3,4-oxadiazole-2',5(4H)-dithione
0.0024
-
in 50 mM Na-phosphate buffer (pH 6.8), at 25°C Agaricus bisporus 4,4'-diamino-3-(4-hydroxyphenyl)-1'H-1,3'-bi-1,2,4-triazole-5,5'(4H,4'H)-dithione
0.00247
-
in 50 mM Na-phosphate buffer (pH 6.8), at 25°C Agaricus bisporus 5'-(pyridin-4-yl)-2,3'-bi-1,3,4-thiadiazole-2',5(4H)-dithione
0.0029
-
in 50 mM Na-phosphate buffer (pH 6.8), at 25°C Agaricus bisporus 2,2':4',2''-ter-1,3,4-thiadiazole-5,5',5''(4H,4''H)-trithione
0.00364
-
in 50 mM Na-phosphate buffer (pH 6.8), at 25°C Agaricus bisporus 5'-[3-(benzyloxy)phenyl]-2,3'-bi-1,3,4-oxadiazole-2',5(4H)-dithione
0.00367
-
in 50 mM Na-phosphate buffer (pH 6.8), at 25°C Agaricus bisporus 5'-benzyl-2,3'-bi-1,3,4-oxadiazole-2',5(4H)-dithione
0.00442
-
in 50 mM Na-phosphate buffer (pH 6.8), at 25°C Agaricus bisporus 5'-[(5-thioxo-4,5-dihydro-1,3,4-oxadiazol-2-yl)methyl]-2,3'-bi-1,3,4-oxadiazole-2',5(4H)-dithione
0.00494
-
in 50 mM Na-phosphate buffer (pH 6.8), at 25°C Agaricus bisporus 5'-cyclohexyl-2,3'-bi-1,3,4-oxadiazole-2',5(4H)-dithione
0.0052
-
in 50 mM Na-phosphate buffer (pH 6.8), at 25°C Agaricus bisporus 5'-(diphenylmethyl)-2,3'-bi-1,3,4-thiadiazole-2',5(4H)-dithione
0.00647
-
in 50 mM Na-phosphate buffer (pH 6.8), at 25°C Agaricus bisporus 5'-phenyl-2,3'-bi-1,3,4-oxadiazole-2',5(4H)-dithione
0.00676
-
in 50 mM Na-phosphate buffer (pH 6.8), at 25°C Agaricus bisporus 5'-(diphenylmethyl)-2,3'-bi-1,3,4-oxadiazole-2',5(4H)-dithione
0.0142
-
in 50 mM Na-phosphate buffer (pH 6.8), at 25°C Agaricus bisporus 5'-(pyridin-4-yl)-2,3'-bi-1,3,4-oxadiazole-2',5(4H)-dithione
0.0185
-
in 50 mM Na-phosphate buffer (pH 6.8), at 25°C Agaricus bisporus 5'-(3-hydroxyphenyl)-2,3'-bi-1,3,4-oxadiazole-2',5(4H)-dithione
0.0336
-
in 50 mM Na-phosphate buffer (pH 6.8), at 25°C Agaricus bisporus 5'-(naphthalen-1-yl)-2,3'-bi-1,3,4-oxadiazole-2',5(4H)-dithione
0.049
-
in 50 mM Na-phosphate buffer (pH 6.8), at 25°C Agaricus bisporus 4-(benzyloxy)-N'-(hydrazinylcarbonyl)benzohydrazide
0.0694
-
in 50 mM Na-phosphate buffer (pH 6.8), at 25°C Agaricus bisporus 2,2':4',2''-ter-1,3,4-oxadiazole-5,5',5''(4H,4''H)-trithione
0.1772
-
in 50 mM Na-phosphate buffer (pH 6.8), at 25°C Agaricus bisporus N'-(hydrazinylcarbonyl)-4-hydroxybenzohydrazide
0.996
-
in 50 mM Na-phosphate buffer (pH 6.8), at 25°C Agaricus bisporus N'-(hydrazinylcarbonyl)naphthalene-2-carbohydrazide