Target Information
Target General Information | Top | |||||
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Target ID |
T97035
(Former ID: TTDS00373)
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Target Name |
Tyrosinase (TYR)
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Synonyms |
Tumor rejection antigen AB; SK29-AB; Monophenol monooxygenase; LB24-AB
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Gene Name |
TYR
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Target Type |
Successful target
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[1] | ||||
Disease | [+] 2 Target-related Diseases | + | ||||
1 | Acquired hypermelanosis [ICD-11: ED60] | |||||
2 | Acquired hypomelanotic disorder [ICD-11: ED63] | |||||
Function |
Catalyzes the initial and rate limiting step in the cascade of reactions leading to melanin production from tyrosine. In addition to hydroxylating tyrosine to DOPA (3,4-dihydroxyphenylalanine), also catalyzes the oxidation of DOPA to DOPA-quinone, and possibly the oxidation of DHI (5,6-dihydroxyindole) to indole-5,6 quinone. This is a copper-containing oxidase that functions in the formation of pigments such as melanins and other polyphenolic compounds.
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BioChemical Class |
Paired donor oxygen oxidoreductase
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UniProt ID | ||||||
EC Number |
EC 1.14.18.1
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Sequence |
MLLAVLYCLLWSFQTSAGHFPRACVSSKNLMEKECCPPWSGDRSPCGQLSGRGSCQNILL
SNAPLGPQFPFTGVDDRESWPSVFYNRTCQCSGNFMGFNCGNCKFGFWGPNCTERRLLVR RNIFDLSAPEKDKFFAYLTLAKHTISSDYVIPIGTYGQMKNGSTPMFNDINIYDLFVWMH YYVSMDALLGGSEIWRDIDFAHEAPAFLPWHRLFLLRWEQEIQKLTGDENFTIPYWDWRD AEKCDICTDEYMGGQHPTNPNLLSPASFFSSWQIVCSRLEEYNSHQSLCNGTPEGPLRRN PGNHDKSRTPRLPSSADVEFCLSLTQYESGSMDKAANFSFRNTLEGFASPLTGIADASQS SMHNALHIYMNGTMSQVQGSANDPIFLLHHAFVDSIFEQWLRRHRPLQEVYPEANAPIGH NRESYMVPFIPLYRNGDFFISSKDLGYDYSYLQDSDPDSFQDYIKSYLEQASRIWSWLLG AAMVGAVLTALLAGLVSLLCRHKRKQLPEEKQPLLMEKEDYHSLYQSHL Click to Show/Hide
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3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
HIT2.0 ID | T13KGH |
Drugs and Modes of Action | Top | |||||
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Approved Drug(s) | [+] 2 Approved Drugs | + | ||||
1 | Hydroquinone | Drug Info | Approved | Melasma | [2] | |
2 | Monobenzone | Drug Info | Approved | Vitiligo | [3], [4] | |
Clinical Trial Drug(s) | [+] 4 Clinical Trial Drugs | + | ||||
1 | Multi-epitope peptide melanoma vaccine | Drug Info | Phase 3 | Melanoma | [5] | |
2 | MKC-1106-MT | Drug Info | Phase 2 | Melanoma | [6] | |
3 | Multi-epitope tyrosinase/gp100 vaccine | Drug Info | Phase 2 | Melanoma | [7] | |
4 | Polynoma-1 | Drug Info | Phase 2 | Melanoma | [8] | |
Patented Agent(s) | [+] 117 Patented Agents | + | ||||
1 | 3-(phenoxymethyl) benzylamine derivative 4 | Drug Info | Patented | Albinism | [9] | |
2 | 3-(phenoxymethyl) benzylamine derivative 5 | Drug Info | Patented | Albinism | [9] | |
3 | 3-(phenoxymethyl) benzylamine derivative 6 | Drug Info | Patented | Albinism | [9] | |
4 | Aromatic hydrazine carboxyimidoamide derivative 1 | Drug Info | Patented | Albinism | [9] | |
5 | Aromatic hydrazine carboxyimidoamide derivative 3 | Drug Info | Patented | Albinism | [9] | |
6 | Aromatic hydrazine carboxyimidoamide derivative 4 | Drug Info | Patented | Albinism | [9] | |
7 | Aromatic hydrazine carboxyimidoamide derivative 5 | Drug Info | Patented | Albinism | [9] | |
8 | Aromatic hydrazine carboxyimidoamide derivative 6 | Drug Info | Patented | Albinism | [9] | |
9 | Benzimidazole derivative 3 | Drug Info | Patented | Albinism | [9] | |
10 | Benzimidazole derivative 4 | Drug Info | Patented | Albinism | [9] | |
11 | Benzoic acid linked peptide analog 1 | Drug Info | Patented | Albinism | [9] | |
12 | Benzoic acid linked peptide analog 2 | Drug Info | Patented | Albinism | [9] | |
13 | Benzoic acid linked peptide analog 3 | Drug Info | Patented | Albinism | [9] | |
14 | Benzoic acid linked peptide analog 4 | Drug Info | Patented | Albinism | [9] | |
15 | Benzoic acid linked peptide analog 6 | Drug Info | Patented | Albinism | [9] | |
16 | Benzothiazole analog 1 | Drug Info | Patented | Albinism | [9] | |
17 | Benzothiazole analog 3 | Drug Info | Patented | Albinism | [9] | |
18 | Benzothiazole analog 4 | Drug Info | Patented | Albinism | [9] | |
19 | Benzothiazoline derivative 1 | Drug Info | Patented | Albinism | [9] | |
20 | Beta-phenyl-alpha,beta-unsaturated carbonyl derivative 1 | Drug Info | Patented | Albinism | [9] | |
21 | Beta-phenyl-alpha,beta-unsaturated carbonyl derivative 10 | Drug Info | Patented | Albinism | [9] | |
22 | Beta-phenyl-alpha,beta-unsaturated carbonyl derivative 11 | Drug Info | Patented | Albinism | [9] | |
23 | Beta-phenyl-alpha,beta-unsaturated carbonyl derivative 12 | Drug Info | Patented | Albinism | [9] | |
24 | Beta-phenyl-alpha,beta-unsaturated carbonyl derivative 13 | Drug Info | Patented | Albinism | [9] | |
25 | Beta-phenyl-alpha,beta-unsaturated carbonyl derivative 14 | Drug Info | Patented | Albinism | [9] | |
26 | Beta-phenyl-alpha,beta-unsaturated carbonyl derivative 2 | Drug Info | Patented | Albinism | [9] | |
27 | Beta-phenyl-alpha,beta-unsaturated carbonyl derivative 3 | Drug Info | Patented | Albinism | [9] | |
28 | Beta-phenyl-alpha,beta-unsaturated carbonyl derivative 4 | Drug Info | Patented | Albinism | [9] | |
29 | Beta-phenyl-alpha,beta-unsaturated carbonyl derivative 5 | Drug Info | Patented | Albinism | [9] | |
30 | Beta-phenyl-alpha,beta-unsaturated carbonyl derivative 6 | Drug Info | Patented | Albinism | [9] | |
31 | Beta-phenyl-alpha,beta-unsaturated carbonyl derivative 7 | Drug Info | Patented | Albinism | [9] | |
32 | Beta-phenyl-alpha,beta-unsaturated carbonyl derivative 8 | Drug Info | Patented | Albinism | [9] | |
33 | Beta-phenyl-alpha,beta-unsaturated carbonyl derivative 9 | Drug Info | Patented | Albinism | [9] | |
34 | Cyclohexyl carbamate derivative 1 | Drug Info | Patented | Albinism | [9] | |
35 | Cyclohexyl carbamate derivative 2 | Drug Info | Patented | Albinism | [9] | |
36 | Cyclohexyl carbamate derivative 3 | Drug Info | Patented | Albinism | [9] | |
37 | Cyclohexyl carbamate derivative 4 | Drug Info | Patented | Albinism | [9] | |
38 | Cyclohexyl carbamate derivative 6 | Drug Info | Patented | Albinism | [9] | |
39 | Cyclohexyl carbamate derivative 7 | Drug Info | Patented | Albinism | [9] | |
40 | Cyclohexyl carbamate derivative 8 | Drug Info | Patented | Albinism | [9] | |
41 | Diamine derivative 1 | Drug Info | Patented | Albinism | [9] | |
42 | Diamine derivative 2 | Drug Info | Patented | Albinism | [9] | |
43 | Diamine derivative 3 | Drug Info | Patented | Albinism | [9] | |
44 | Dihydroxyfumaric acid derivative 1 | Drug Info | Patented | Albinism | [9] | |
45 | Monoamine derivative 1 | Drug Info | Patented | Albinism | [9] | |
46 | Monoamine derivative 2 | Drug Info | Patented | Albinism | [9] | |
47 | Monoamine derivative 3 | Drug Info | Patented | Albinism | [9] | |
48 | Monoamine derivative 5 | Drug Info | Patented | Albinism | [9] | |
49 | Nicotinyl hydroxamic acid derivative 1 | Drug Info | Patented | Albinism | [9] | |
50 | P-coumaric acid derivative 1 | Drug Info | Patented | Albinism | [9] | |
51 | P-coumaric acid derivative 2 | Drug Info | Patented | Albinism | [9] | |
52 | P-coumaric acid derivative 3 | Drug Info | Patented | Albinism | [9] | |
53 | P-coumaric acid derivative 4 | Drug Info | Patented | Albinism | [9] | |
54 | P-coumaric acid derivative 5 | Drug Info | Patented | Albinism | [9] | |
55 | P-coumaric acid derivative 6 | Drug Info | Patented | Albinism | [9] | |
56 | PMID26815044-Compound-114 | Drug Info | Patented | Albinism | [9] | |
57 | PMID26815044-Compound-115 | Drug Info | Patented | Albinism | [9] | |
58 | PMID26815044-Compound-117 | Drug Info | Patented | Albinism | [9] | |
59 | PMID26815044-Compound-118 | Drug Info | Patented | Albinism | [9] | |
60 | PMID26815044-Compound-121 | Drug Info | Patented | Albinism | [9] | |
61 | PMID26815044-Compound-122 | Drug Info | Patented | Albinism | [9] | |
62 | PMID26815044-Compound-123 | Drug Info | Patented | Albinism | [9] | |
63 | PMID26815044-Compound-124 | Drug Info | Patented | Albinism | [9] | |
64 | PMID26815044-Compound-126 | Drug Info | Patented | Albinism | [9] | |
65 | PMID26815044-Compound-127 | Drug Info | Patented | Albinism | [9] | |
66 | PMID26815044-Compound-31 | Drug Info | Patented | Albinism | [9] | |
67 | PMID26815044-Compound-32 | Drug Info | Patented | Albinism | [9] | |
68 | PMID26815044-Compound-48 | Drug Info | Patented | Albinism | [9] | |
69 | PMID26815044-Compound-49 | Drug Info | Patented | Albinism | [9] | |
70 | PMID26815044-Compound-50 | Drug Info | Patented | Albinism | [9] | |
71 | PMID26815044-Compound-51 | Drug Info | Patented | Albinism | [9] | |
72 | PMID26815044-Compound-52 | Drug Info | Patented | Albinism | [9] | |
73 | PMID26815044-Compound-64 | Drug Info | Patented | Albinism | [9] | |
74 | PMID26815044-Compound-93 | Drug Info | Patented | Albinism | [9] | |
75 | PMID26815044-Compound-H | Drug Info | Patented | Albinism | [9] | |
76 | PMID26815044-Compound-I | Drug Info | Patented | Albinism | [9] | |
77 | Polyhydroxy benzamide derivative 1 | Drug Info | Patented | Albinism | [9] | |
78 | Polyhydroxy benzamide derivative 2 | Drug Info | Patented | Albinism | [9] | |
79 | Polyhydroxy benzamide derivative 3 | Drug Info | Patented | Albinism | [9] | |
80 | Polyhydroxy benzamide derivative 4 | Drug Info | Patented | Albinism | [9] | |
81 | Polyhydroxy benzamide derivative 5 | Drug Info | Patented | Albinism | [9] | |
82 | Resorcinol compound 1 | Drug Info | Patented | Albinism | [9] | |
83 | Resorcinol compound 10 | Drug Info | Patented | Albinism | [9] | |
84 | Resorcinol compound 11 | Drug Info | Patented | Albinism | [9] | |
85 | Resorcinol compound 12 | Drug Info | Patented | Albinism | [9] | |
86 | Resorcinol compound 13 | Drug Info | Patented | Albinism | [9] | |
87 | Resorcinol compound 14 | Drug Info | Patented | Albinism | [9] | |
88 | Resorcinol compound 15 | Drug Info | Patented | Albinism | [9] | |
89 | Resorcinol compound 16 | Drug Info | Patented | Albinism | [9] | |
90 | Resorcinol compound 17 | Drug Info | Patented | Albinism | [9] | |
91 | Resorcinol compound 18 | Drug Info | Patented | Albinism | [9] | |
92 | Resorcinol compound 2 | Drug Info | Patented | Albinism | [9] | |
93 | Resorcinol compound 20 | Drug Info | Patented | Albinism | [9] | |
94 | Resorcinol compound 21 | Drug Info | Patented | Albinism | [9] | |
95 | Resorcinol compound 22 | Drug Info | Patented | Albinism | [9] | |
96 | Resorcinol compound 23 | Drug Info | Patented | Albinism | [9] | |
97 | Resorcinol compound 24 | Drug Info | Patented | Albinism | [9] | |
98 | Resorcinol compound 25 | Drug Info | Patented | Albinism | [9] | |
99 | Resorcinol compound 26 | Drug Info | Patented | Albinism | [9] | |
100 | Resorcinol compound 27 | Drug Info | Patented | Albinism | [9] | |
101 | Resorcinol compound 28 | Drug Info | Patented | Albinism | [9] | |
102 | Resorcinol compound 30 | Drug Info | Patented | Albinism | [9] | |
103 | Resorcinol compound 31 | Drug Info | Patented | Albinism | [9] | |
104 | Resorcinol compound 32 | Drug Info | Patented | Albinism | [9] | |
105 | Resorcinol compound 33 | Drug Info | Patented | Albinism | [9] | |
106 | Resorcinol compound 34 | Drug Info | Patented | Albinism | [9] | |
107 | Resorcinol compound 4 | Drug Info | Patented | Albinism | [9] | |
108 | Resorcinol compound 5 | Drug Info | Patented | Albinism | [9] | |
109 | Resorcinol compound 6 | Drug Info | Patented | Albinism | [9] | |
110 | Resorcinol compound 7 | Drug Info | Patented | Albinism | [9] | |
111 | Resorcinol compound 8 | Drug Info | Patented | Albinism | [9] | |
112 | Resorcinol compound 9 | Drug Info | Patented | Albinism | [9] | |
113 | Thiazolidine derivative 1 | Drug Info | Patented | Albinism | [9] | |
114 | Thiazolidine derivative 2 | Drug Info | Patented | Albinism | [9] | |
115 | Thiazolidine derivative 3 | Drug Info | Patented | Albinism | [9] | |
116 | Thiazoline derivative 1 | Drug Info | Patented | Albinism | [9] | |
117 | Thiazoline derivative 2 | Drug Info | Patented | Albinism | [9] | |
Mode of Action | [+] 2 Modes of Action | + | ||||
Inhibitor | [+] 212 Inhibitor drugs | + | ||||
1 | Hydroquinone | Drug Info | [1] | |||
2 | Monobenzone | Drug Info | [1] | |||
3 | 3-(phenoxymethyl) benzylamine derivative 4 | Drug Info | [9] | |||
4 | 3-(phenoxymethyl) benzylamine derivative 5 | Drug Info | [9] | |||
5 | 3-(phenoxymethyl) benzylamine derivative 6 | Drug Info | [9] | |||
6 | Aromatic hydrazine carboxyimidoamide derivative 1 | Drug Info | [9] | |||
7 | Aromatic hydrazine carboxyimidoamide derivative 3 | Drug Info | [9] | |||
8 | Aromatic hydrazine carboxyimidoamide derivative 4 | Drug Info | [9] | |||
9 | Aromatic hydrazine carboxyimidoamide derivative 5 | Drug Info | [9] | |||
10 | Aromatic hydrazine carboxyimidoamide derivative 6 | Drug Info | [9] | |||
11 | Benzimidazole derivative 3 | Drug Info | [9] | |||
12 | Benzimidazole derivative 4 | Drug Info | [9] | |||
13 | Benzoic acid linked peptide analog 1 | Drug Info | [9] | |||
14 | Benzoic acid linked peptide analog 2 | Drug Info | [9] | |||
15 | Benzoic acid linked peptide analog 3 | Drug Info | [9] | |||
16 | Benzoic acid linked peptide analog 4 | Drug Info | [9] | |||
17 | Benzoic acid linked peptide analog 6 | Drug Info | [9] | |||
18 | Benzothiazole analog 1 | Drug Info | [9] | |||
19 | Benzothiazole analog 3 | Drug Info | [9] | |||
20 | Benzothiazole analog 4 | Drug Info | [9] | |||
21 | Benzothiazoline derivative 1 | Drug Info | [9] | |||
22 | Beta-phenyl-alpha,beta-unsaturated carbonyl derivative 1 | Drug Info | [9] | |||
23 | Beta-phenyl-alpha,beta-unsaturated carbonyl derivative 10 | Drug Info | [9] | |||
24 | Beta-phenyl-alpha,beta-unsaturated carbonyl derivative 11 | Drug Info | [9] | |||
25 | Beta-phenyl-alpha,beta-unsaturated carbonyl derivative 12 | Drug Info | [9] | |||
26 | Beta-phenyl-alpha,beta-unsaturated carbonyl derivative 13 | Drug Info | [9] | |||
27 | Beta-phenyl-alpha,beta-unsaturated carbonyl derivative 14 | Drug Info | [9] | |||
28 | Beta-phenyl-alpha,beta-unsaturated carbonyl derivative 2 | Drug Info | [9] | |||
29 | Beta-phenyl-alpha,beta-unsaturated carbonyl derivative 3 | Drug Info | [9] | |||
30 | Beta-phenyl-alpha,beta-unsaturated carbonyl derivative 4 | Drug Info | [9] | |||
31 | Beta-phenyl-alpha,beta-unsaturated carbonyl derivative 5 | Drug Info | [9] | |||
32 | Beta-phenyl-alpha,beta-unsaturated carbonyl derivative 6 | Drug Info | [9] | |||
33 | Beta-phenyl-alpha,beta-unsaturated carbonyl derivative 7 | Drug Info | [9] | |||
34 | Beta-phenyl-alpha,beta-unsaturated carbonyl derivative 8 | Drug Info | [9] | |||
35 | Beta-phenyl-alpha,beta-unsaturated carbonyl derivative 9 | Drug Info | [9] | |||
36 | Cyclohexyl carbamate derivative 1 | Drug Info | [9] | |||
37 | Cyclohexyl carbamate derivative 2 | Drug Info | [9] | |||
38 | Cyclohexyl carbamate derivative 3 | Drug Info | [9] | |||
39 | Cyclohexyl carbamate derivative 4 | Drug Info | [9] | |||
40 | Cyclohexyl carbamate derivative 6 | Drug Info | [9] | |||
41 | Cyclohexyl carbamate derivative 7 | Drug Info | [9] | |||
42 | Cyclohexyl carbamate derivative 8 | Drug Info | [9] | |||
43 | Diamine derivative 1 | Drug Info | [9] | |||
44 | Diamine derivative 2 | Drug Info | [9] | |||
45 | Diamine derivative 3 | Drug Info | [9] | |||
46 | Dihydroxyfumaric acid derivative 1 | Drug Info | [9] | |||
47 | Monoamine derivative 1 | Drug Info | [9] | |||
48 | Monoamine derivative 2 | Drug Info | [9] | |||
49 | Monoamine derivative 3 | Drug Info | [9] | |||
50 | Monoamine derivative 5 | Drug Info | [9] | |||
51 | Nicotinyl hydroxamic acid derivative 1 | Drug Info | [9] | |||
52 | P-coumaric acid derivative 1 | Drug Info | [9] | |||
53 | P-coumaric acid derivative 2 | Drug Info | [9] | |||
54 | P-coumaric acid derivative 3 | Drug Info | [9] | |||
55 | P-coumaric acid derivative 4 | Drug Info | [9] | |||
56 | P-coumaric acid derivative 5 | Drug Info | [9] | |||
57 | P-coumaric acid derivative 6 | Drug Info | [9] | |||
58 | PMID26815044-Compound-114 | Drug Info | [9] | |||
59 | PMID26815044-Compound-115 | Drug Info | [9] | |||
60 | PMID26815044-Compound-117 | Drug Info | [9] | |||
61 | PMID26815044-Compound-118 | Drug Info | [9] | |||
62 | PMID26815044-Compound-121 | Drug Info | [9] | |||
63 | PMID26815044-Compound-122 | Drug Info | [9] | |||
64 | PMID26815044-Compound-123 | Drug Info | [9] | |||
65 | PMID26815044-Compound-124 | Drug Info | [9] | |||
66 | PMID26815044-Compound-126 | Drug Info | [9] | |||
67 | PMID26815044-Compound-127 | Drug Info | [9] | |||
68 | PMID26815044-Compound-31 | Drug Info | [9] | |||
69 | PMID26815044-Compound-32 | Drug Info | [9] | |||
70 | PMID26815044-Compound-48 | Drug Info | [9] | |||
71 | PMID26815044-Compound-49 | Drug Info | [9] | |||
72 | PMID26815044-Compound-50 | Drug Info | [9] | |||
73 | PMID26815044-Compound-51 | Drug Info | [9] | |||
74 | PMID26815044-Compound-52 | Drug Info | [9] | |||
75 | PMID26815044-Compound-64 | Drug Info | [9] | |||
76 | PMID26815044-Compound-93 | Drug Info | [9] | |||
77 | PMID26815044-Compound-H | Drug Info | [9] | |||
78 | PMID26815044-Compound-I | Drug Info | [9] | |||
79 | Polyhydroxy benzamide derivative 1 | Drug Info | [9] | |||
80 | Polyhydroxy benzamide derivative 2 | Drug Info | [9] | |||
81 | Polyhydroxy benzamide derivative 3 | Drug Info | [9] | |||
82 | Polyhydroxy benzamide derivative 4 | Drug Info | [9] | |||
83 | Polyhydroxy benzamide derivative 5 | Drug Info | [9] | |||
84 | Resorcinol compound 1 | Drug Info | [9] | |||
85 | Resorcinol compound 10 | Drug Info | [9] | |||
86 | Resorcinol compound 11 | Drug Info | [9] | |||
87 | Resorcinol compound 12 | Drug Info | [9] | |||
88 | Resorcinol compound 13 | Drug Info | [9] | |||
89 | Resorcinol compound 14 | Drug Info | [9] | |||
90 | Resorcinol compound 15 | Drug Info | [9] | |||
91 | Resorcinol compound 16 | Drug Info | [9] | |||
92 | Resorcinol compound 17 | Drug Info | [9] | |||
93 | Resorcinol compound 18 | Drug Info | [9] | |||
94 | Resorcinol compound 2 | Drug Info | [9] | |||
95 | Resorcinol compound 20 | Drug Info | [9] | |||
96 | Resorcinol compound 21 | Drug Info | [9] | |||
97 | Resorcinol compound 22 | Drug Info | [9] | |||
98 | Resorcinol compound 23 | Drug Info | [9] | |||
99 | Resorcinol compound 24 | Drug Info | [9] | |||
100 | Resorcinol compound 25 | Drug Info | [9] | |||
101 | Resorcinol compound 26 | Drug Info | [9] | |||
102 | Resorcinol compound 27 | Drug Info | [9] | |||
103 | Resorcinol compound 28 | Drug Info | [9] | |||
104 | Resorcinol compound 30 | Drug Info | [9] | |||
105 | Resorcinol compound 31 | Drug Info | [9] | |||
106 | Resorcinol compound 32 | Drug Info | [9] | |||
107 | Resorcinol compound 33 | Drug Info | [9] | |||
108 | Resorcinol compound 34 | Drug Info | [9] | |||
109 | Resorcinol compound 4 | Drug Info | [9] | |||
110 | Resorcinol compound 5 | Drug Info | [9] | |||
111 | Resorcinol compound 6 | Drug Info | [9] | |||
112 | Resorcinol compound 7 | Drug Info | [9] | |||
113 | Resorcinol compound 8 | Drug Info | [9] | |||
114 | Resorcinol compound 9 | Drug Info | [9] | |||
115 | Thiazolidine derivative 1 | Drug Info | [9] | |||
116 | Thiazolidine derivative 2 | Drug Info | [9] | |||
117 | Thiazolidine derivative 3 | Drug Info | [9] | |||
118 | Thiazoline derivative 1 | Drug Info | [9] | |||
119 | Thiazoline derivative 2 | Drug Info | [9] | |||
120 | (+/-)-Daedalin A | Drug Info | [12] | |||
121 | 1'-(4-Methyl-benzyl)-[1,4']bipiperidinyl | Drug Info | [13] | |||
122 | 1-(1,4-diacetylphenyl)dithiosemicarbazide | Drug Info | [14] | |||
123 | 1-(1-(4-bromophenyl)ethylidene)thiosemicarbazide | Drug Info | [14] | |||
124 | 1-(1-(4-fluorophenyl)ethylidene)thiosemicarbazide | Drug Info | [14] | |||
125 | 1-(1-(pyrazin-2-yl)ethylidene)thiosemicarbazide | Drug Info | [14] | |||
126 | 1-(1-(pyridin-3-yl)ethylidene)thiosemicarbazide | Drug Info | [14] | |||
127 | 1-(1-(thiophen-2-yl)ethylidene)thiosemicarbazide | Drug Info | [14] | |||
128 | 1-(1-p-tolylethylidene)thiosemicarbazide | Drug Info | [14] | |||
129 | 1-(1-phenylethylidene)thiosemicarbazide | Drug Info | [14] | |||
130 | 1-(2,5-Dimethyl-1H-pyrrol-1-yl)thiourea | Drug Info | [15] | |||
131 | 1-(3-Methylbutylidene)thiosemicarbazide | Drug Info | [15] | |||
132 | 1-(3-phenoxypropyl)-4-(piperidin-1-yl)piperidine | Drug Info | [13] | |||
133 | 1-(3-Phenylallylidene)thiosemicarbazide | Drug Info | [15] | |||
134 | 1-(4-(benzyloxy)phenyl)-3-hydroxyurea | Drug Info | [16] | |||
135 | 1-(4-bromophenyl)-3-hydroxyurea | Drug Info | [16] | |||
136 | 1-(4-Methylpent-3-en-2-ylidene)thiosemicarbazide | Drug Info | [15] | |||
137 | 1-(But-2-enylidene)thiosemicarbazide | Drug Info | [15] | |||
138 | 1-(Butan-2-ylidene)thiosemicarbazide | Drug Info | [15] | |||
139 | 1-Cyclohexylidenethiosemicarbazide | Drug Info | [15] | |||
140 | 1-Cyclopentylidenethiosemicarbazide | Drug Info | [15] | |||
141 | 1-Ethylidenethiosemicarbazide | Drug Info | [15] | |||
142 | 1-hydroxy-3-(4-(trifluoromethyl)phenyl)urea | Drug Info | [16] | |||
143 | 1-hydroxy-3-(4-nitrophenyl)urea | Drug Info | [16] | |||
144 | 1-hydroxy-3-phenylurea | Drug Info | [16] | |||
145 | 1-Propylidenethiosemicarbazide | Drug Info | [15] | |||
146 | 2,2',4,4',6'-pentahydroxychalcone | Drug Info | [17] | |||
147 | 2,2',4,4'-tetrahydroxy-6'-methoxychalcone | Drug Info | [17] | |||
148 | 2,2',4,4'-tetrahydroxychalcone | Drug Info | [17] | |||
149 | 2,2'-bi(1,3,4-thiadiazole)-5,5'(4H,4'H)-dithione | Drug Info | [18] | |||
150 | 2,4,3',5'-tetrahydroxybibenzyl | Drug Info | [19] | |||
151 | 2-(butylthiomethyl)-5-hydroxy-4H-pyran-4-one | Drug Info | [20] | |||
152 | 2-(cyclohexylthiomethyl)-5-hydroxy-4H-pyran-4-one | Drug Info | [20] | |||
153 | 2-(ethylthiomethyl)-5-hydroxy-4H-pyran-4-one | Drug Info | [20] | |||
154 | 2-(heptylthiomethyl)-5-hydroxy-4H-pyran-4-one | Drug Info | [20] | |||
155 | 2-(hexylthiomethyl)-5-hydroxy-4H-pyran-4-one | Drug Info | [20] | |||
156 | 2-hydroxy-3-isopropyl-2,4,6-cycloheptatrien-1-one | Drug Info | [21] | |||
157 | 2-hydroxyphenethyl 3,4,5-trihydroxybenzoate | Drug Info | [22] | |||
158 | 3,4-dihydroxybenzaldehyde-O-ethyloxime | Drug Info | [23] | |||
159 | 3-(2,4-dihydroxyphenyl)propionic acid | Drug Info | [24] | |||
160 | 3-hydroxyphenethyl 3,4,5-trihydroxybenzoate | Drug Info | [22] | |||
161 | 3hydroxy-1-methyl-1-phenylurea | Drug Info | [16] | |||
162 | 4',4-Dihydroxychalcone | Drug Info | [25] | |||
163 | 4'-(4-Aminobenzensulfonamide)-4-hydroxychalcone | Drug Info | [25] | |||
164 | 4'-(4-Fluorobenzensulfonamide)-4-hydroxychalcone | Drug Info | [25] | |||
165 | 4'-(4-Nitrobenzensulfonamide)-4-hydroxychalcone | Drug Info | [25] | |||
166 | 4'-(Benzensulfonamide)-4-hydroxychalcone | Drug Info | [25] | |||
167 | 4'-(p-Toluenesulfonamide)-4-hydroxychalcone | Drug Info | [25] | |||
168 | 4'-Amino-4-hydroxychalcone | Drug Info | [25] | |||
169 | 4,4'-(ethane-1,2-diyl)dibenzene-1,3-diol | Drug Info | [26] | |||
170 | 4-(6-hydroxynaphthalen-2-yl)benzene-1,3-diol | Drug Info | [27] | |||
171 | 4-adamantyl resorcinol | Drug Info | [28] | |||
172 | 4-hexyl resorcinol | Drug Info | [29] | |||
173 | 5,5'-methylenebis(1,3,4-oxadiazole-2(3H)-thione) | Drug Info | [18] | |||
174 | 5,5'-methylenebis(1,3,4-thiadiazole-2(3H)-thione) | Drug Info | [18] | |||
175 | 5-(3-hydroxyphenyl)-1,3,4-oxadiazole-2(3H)-thione | Drug Info | [18] | |||
176 | 5-(4-hydroxyphenyl)-1,3,4-oxadiazole-2(3H)-thione | Drug Info | [18] | |||
177 | 5-(6-hydroxynaphthalen-2-yl)benzene-1,3-diol | Drug Info | [27] | |||
178 | 5-(pyridin-4-yl)-1,3,4-oxadiazole-2(3H)-thione | Drug Info | [18] | |||
179 | 5-(pyridin-4-yl)-1,3,4-thiadiazole-2(3H)-thione | Drug Info | [18] | |||
180 | 5-benzhydryl-1,3,4-oxadiazole-2(3H)-thione | Drug Info | [18] | |||
181 | 5-benzhydryl-1,3,4-thiadiazole-2(3H)-thione | Drug Info | [18] | |||
182 | 5-cyclohexyl-1,3,4-oxadiazole-2(3H)-thione | Drug Info | [18] | |||
183 | 5-hydroxy-2-(pentylthiomethyl)-4H-pyran-4-one | Drug Info | [20] | |||
184 | 5-phenyl-1,3,4-oxadiazole-2(3H)-thione | Drug Info | [18] | |||
185 | 5-phenyl-1,3,4-thiadiazole-2(3H)-thione | Drug Info | [18] | |||
186 | 5-{8(Z),-pentadecenyl}resorcinol | Drug Info | [30] | |||
187 | 5-{8(Z),11(Z),14-pentadecatrienyl}resorcinol | Drug Info | [30] | |||
188 | 5-{8(Z),11(Z)-pentadecadienyl}resorcinol | Drug Info | [30] | |||
189 | 6-(3-Hydroxy-phenyl)-naphthalen-2-ol | Drug Info | [27] | |||
190 | 7,3',4'-trihydroxyisoflavone | Drug Info | [31] | |||
191 | 7,8,4'-trihydroxyisoflavone | Drug Info | [31] | |||
192 | 7-(3,5-dihydroxyphenyl)naphthalene-1,3-diol | Drug Info | [27] | |||
193 | ASKENDOSIDE B | Drug Info | [32] | |||
194 | Broussonin C | Drug Info | [33] | |||
195 | Crocusatin-K | Drug Info | [34] | |||
196 | DAEDALIN A | Drug Info | [12] | |||
197 | ETHISTERONE | Drug Info | [35] | |||
198 | HINOKITIOL | Drug Info | [21] | |||
199 | Kazinol C | Drug Info | [33] | |||
200 | KAZINOL S | Drug Info | [33] | |||
201 | KOJIC ACID | Drug Info | [36] | |||
202 | N-(2,4-dihydroxybenzyl)-3,4,5-trihydroxybenzamide | Drug Info | [37] | |||
203 | N-(2,4-dihydroxybenzyl)-3,4-dihydroxybenzamide | Drug Info | [37] | |||
204 | N-(2,4-dihydroxybenzyl)-3,5-dihydroxybenzamide | Drug Info | [37] | |||
205 | N-butylresorcinol | Drug Info | [28] | |||
206 | OXYRESVERATROL | Drug Info | [19] | |||
207 | PHENYLTHIOUREA | Drug Info | [16] | |||
208 | ROSMARINIC ACID | Drug Info | [36] | |||
209 | S-2-(o-toluidino)-2-oxoethyl carbamothioate | Drug Info | [38] | |||
210 | SODIUM ZINC DIHYDROLIPOYLHISTIDINATE | Drug Info | [39] | |||
211 | SRI-224 | Drug Info | [23] | |||
212 | TROPOLONE | Drug Info | [23] | |||
Modulator | [+] 1 Modulator drugs | + | ||||
1 | MKC-1106-MT | Drug Info | [11] |
Cell-based Target Expression Variations | Top | |||||
---|---|---|---|---|---|---|
Cell-based Target Expression Variations |
Different Human System Profiles of Target | Top |
---|---|
Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Pathway Affiliation
of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.
Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes
(Pharmacol Rev, 58: 259-279, 2006).
Biological Network Descriptors
of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database.
The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information
(Front Pharmacol, 9, 1245, 2018;
Curr Opin Struct Biol. 44:134-142, 2017).
Human Similarity Proteins
Human Pathway Affiliation
Biological Network Descriptors
|
There is no similarity protein (E value < 0.005) for this target
|
KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
---|---|---|---|
Tyrosine metabolism | hsa00350 | Affiliated Target |
|
Class: Metabolism => Amino acid metabolism | Pathway Hierarchy | ||
Melanogenesis | hsa04916 | Affiliated Target |
|
Class: Organismal Systems => Endocrine system | Pathway Hierarchy |
Degree | 4 | Degree centrality | 4.30E-04 | Betweenness centrality | 3.46E-07 |
---|---|---|---|---|---|
Closeness centrality | 5.26E-04 | Radiality | 1.53E-02 | Clustering coefficient | 1.67E-01 |
Neighborhood connectivity | 2.25E+00 | Topological coefficient | 3.50E-01 | Eccentricity | 2 |
Download | Click to Download the Full PPI Network of This Target | ||||
Chemical Structure based Activity Landscape of Target | Top |
---|---|
Drug Property Profile of Target | Top | |
---|---|---|
(1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
|
||
(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
|
||
(5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
|
||
"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five |
Co-Targets | Top | |||||
---|---|---|---|---|---|---|
Co-Targets |
Target Poor or Non Binders | Top | |||||
---|---|---|---|---|---|---|
Target Poor or Non Binders |
Target Regulators | Top | |||||
---|---|---|---|---|---|---|
Target-regulating microRNAs |
Target Profiles in Patients | Top | |||||
---|---|---|---|---|---|---|
Target Expression Profile (TEP) |
Target Affiliated Biological Pathways | Top | |||||
---|---|---|---|---|---|---|
BioCyc | [+] 3 BioCyc Pathways | + | ||||
1 | (S)-reticuline biosynthesis | |||||
2 | Eumelanin biosynthesis | |||||
3 | L-dopachrome biosynthesis | |||||
KEGG Pathway | [+] 4 KEGG Pathways | + | ||||
1 | Tyrosine metabolism | |||||
2 | Riboflavin metabolism | |||||
3 | Metabolic pathways | |||||
4 | Melanogenesis | |||||
Pathwhiz Pathway | [+] 2 Pathwhiz Pathways | + | ||||
1 | Riboflavin Metabolism | |||||
2 | Tyrosine Metabolism | |||||
WikiPathways | [+] 1 WikiPathways | + | ||||
1 | Dopamine metabolism |
Target-Related Models and Studies | Top | |||||
---|---|---|---|---|---|---|
Target Validation |
References | Top | |||||
---|---|---|---|---|---|---|
REF 1 | Identification of an Alkylhydroquinone from Rhus succedanea as an Inhibitor of Tyrosinase and Melanogenesis. J Agric Food Chem. 2009 Mar 25;57(6):2200-5. | |||||
REF 2 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
REF 3 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6830). | |||||
REF 4 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 008173. | |||||
REF 5 | ClinicalTrials.gov (NCT00036816) Vaccine Therapy in Treating Patients With Melanoma of the Eye. U.S. National Institutes of Health. | |||||
REF 6 | ClinicalTrials.gov (NCT01026051) Safety, Immune and Tumor Response to a Multi-component Immune Based Therapy (MKC1106-MT) for Patients With Melanoma. U.S. National Institutes of Health. | |||||
REF 7 | ClinicalTrials.gov (NCT00003362) Vaccine Therapy Plus Immune Adjuvants in Treating Patients With Advanced Melanoma. U.S. National Institutes of Health. | |||||
REF 8 | An immuno-oncology company developing a novel polyvalent antigen therapy for the treatment of melanoma. Polynoma. 2015. | |||||
REF 9 | Tyrosinase inhibitors: a patent review (2011-2015).Expert Opin Ther Pat. 2016;26(3):347-62. | |||||
REF 10 | Safety and immunogenicity of vaccination with MART-1 (26-35, 27L), gp100 (209-217, 210M), and tyrosinase (368-376, 370D) in-adjuvant with PF-3512676 and GM-CSF in metastatic melanoma. Correction in: volume 35 on page 650. | |||||
REF 11 | Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41. | |||||
REF 12 | Asymmetric syntheses of daedalin A and quercinol and their tyrosinase inhibitory activity. Bioorg Med Chem Lett. 2010 Feb 1;20(3):1063-4. | |||||
REF 13 | 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 14 | 1-(1-Arylethylidene)thiosemicarbazide derivatives: a new class of tyrosinase inhibitors. Bioorg Med Chem. 2008 Feb 1;16(3):1096-102. | |||||
REF 15 | A class of potent tyrosinase inhibitors: alkylidenethiosemicarbazide compounds. Eur J Med Chem. 2009 Apr;44(4):1773-8. | |||||
REF 16 | 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 17 | 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 18 | 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 19 | 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 20 | Kojyl thioether derivatives having both tyrosinase inhibitory and anti-inflammatory properties. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6569-71. | |||||
REF 21 | 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 22 | Synthetic tyrosyl gallate derivatives as potent melanin formation inhibitors. Bioorg Med Chem Lett. 2007 Oct 1;17(19):5462-4. | |||||
REF 23 | 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 24 | Enhanced substituted resorcinol hydrophobicity augments tyrosinase inhibition potency. J Med Chem. 2007 May 31;50(11):2676-81. | |||||
REF 25 | Evaluation of anti-pigmentary effect of synthetic sulfonylamino chalcone. Eur J Med Chem. 2010 May;45(5):2010-7. | |||||
REF 26 | Molecular design of potent tyrosinase inhibitors having the bibenzyl skeleton. Bioorg Med Chem Lett. 2008 Oct 1;18(19):5252-4. | |||||
REF 27 | Syntheses of hydroxy substituted 2-phenyl-naphthalenes as inhibitors of tyrosinase. Bioorg Med Chem Lett. 2007 Jan 15;17(2):461-4. | |||||
REF 28 | Studies on depigmenting activities of dihydroxyl benzamide derivatives containing adamantane moiety. Bioorg Med Chem Lett. 2009 Mar 1;19(5):1532-3. | |||||
REF 29 | 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 30 | Tyrosinase inhibitors from Anacardium occidentale fruits. J Nat Prod. 1994 Apr;57(4):545-51. | |||||
REF 31 | 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 32 | New tyrosinase inhibitors selected by atomic linear indices-based classification models. Bioorg Med Chem Lett. 2006 Jan 15;16(2):324-30. | |||||
REF 33 | Tyrosinase inhibitory effects of 1,3-diphenylpropanes from Broussonetia kazinoki. Bioorg Med Chem. 2009 Jan 1;17(1):35-41. | |||||
REF 34 | Antityrosinase principles and constituents of the petals of Crocus sativus. J Nat Prod. 2004 Mar;67(3):437-40. | |||||
REF 35 | 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 36 | 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. | |||||
REF 37 | N-Benzylbenzamides: a new class of potent tyrosinase inhibitors. Bioorg Med Chem Lett. 2006 May 15;16(10):2682-4. | |||||
REF 38 | Discovery of small-molecule inhibitors of tyrosinase. Bioorg Med Chem Lett. 2007 Dec 15;17(24):6871-5. | |||||
REF 39 | 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. |
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