Target Information
Target General Information | Top | |||||
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Target ID |
T00140
(Former ID: TTDS00112)
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Target Name |
Arachidonate 5-lipoxygenase (5-LOX)
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Synonyms |
LOG5; 5-lipoxygenase; 5-LO
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Gene Name |
ALOX5
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Target Type |
Successful target
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[1] | ||||
Disease | [+] 3 Target-related Diseases | + | ||||
1 | Asthma [ICD-11: CA23] | |||||
2 | Filariasis [ICD-11: 1F66] | |||||
3 | Thrombocytopenia [ICD-11: 3B64] | |||||
Function |
Catalyzes the first step in leukotriene biosynthesis, and thereby plays a role in inflammatory processes.
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BioChemical Class |
Oxygenase
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UniProt ID | ||||||
EC Number |
EC 1.13.11.34
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Sequence |
MPSYTVTVATGSQWFAGTDDYIYLSLVGSAGCSEKHLLDKPFYNDFERGAVDSYDVTVDE
ELGEIQLVRIEKRKYWLNDDWYLKYITLKTPHGDYIEFPCYRWITGDVEVVLRDGRAKLA RDDQIHILKQHRRKELETRQKQYRWMEWNPGFPLSIDAKCHKDLPRDIQFDSEKGVDFVL NYSKAMENLFINRFMHMFQSSWNDFADFEKIFVKISNTISERVMNHWQEDLMFGYQFLNG CNPVLIRRCTELPEKLPVTTEMVECSLERQLSLEQEVQQGNIFIVDFELLDGIDANKTDP CTLQFLAAPICLLYKNLANKIVPIAIQLNQIPGDENPIFLPSDAKYDWLLAKIWVRSSDF HVHQTITHLLRTHLVSEVFGIAMYRQLPAVHPIFKLLVAHVRFTIAINTKAREQLICECG LFDKANATGGGGHVQMVQRAMKDLTYASLCFPEAIKARGMESKEDIPYYFYRDDGLLVWE AIRTFTAEVVDIYYEGDQVVEEDPELQDFVNDVYVYGMRGRKSSGFPKSVKSREQLSEYL TVVIFTASAQHAAVNFGQYDWCSWIPNAPPTMRAPPPTAKGVVTIEQIVDTLPDRGRSCW HLGAVWALSQFQENELFLGMYPEEHFIEKPVKEAMARFRKNLEAIVSVIAERNKKKQLPY YYLSPDRIPNSVAI Click to Show/Hide
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3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
ADReCS ID | BADD_A03634 | |||||
HIT2.0 ID | T56TXY |
Drugs and Modes of Action | Top | |||||
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Approved Drug(s) | [+] 3 Approved Drugs | + | ||||
1 | Diethylcarbamazine | Drug Info | Approved | Lymphatic filariasis | [2], [3] | |
2 | Zileuton | Drug Info | Approved | Asthma | [4], [5] | |
3 | 3,4-Dihydroxycinnamic Acid | Drug Info | Phase 4 | Thrombocytopenia | [6] | |
Clinical Trial Drug(s) | [+] 22 Clinical Trial Drugs | + | ||||
1 | ABT-761 | Drug Info | Phase 3 | Asthma | [7] | |
2 | Avastin+/-Tarceva | Drug Info | Phase 3 | Non-small-cell lung cancer | [8] | |
3 | Flobufen | Drug Info | Phase 3 | Rheumatoid arthritis | [9] | |
4 | FPL-62064 | Drug Info | Phase 3 | Inflammation | [10] | |
5 | Tenidap | Drug Info | Phase 3 | Rheumatoid arthritis | [11], [12] | |
6 | Darbufelone | Drug Info | Phase 2/3 | Asthma | [13] | |
7 | BAICALEIN | Drug Info | Phase 2 | Influenza virus infection | [14] | |
8 | BIM23A760 | Drug Info | Phase 2 | Acromegaly | [15], [16] | |
9 | CMI-392 | Drug Info | Phase 2 | Psoriasis vulgaris | [17] | |
10 | E-6700 | Drug Info | Phase 2 | Asthma | [18] | |
11 | MK-866 | Drug Info | Phase 2 | Discovery agent | [19] | |
12 | PF-4191834 | Drug Info | Phase 2 | Asthma | [20] | |
13 | PTC299 | Drug Info | Phase 2 | Rheumatoid arthritis | [21], [22] | |
14 | Q301 | Drug Info | Phase 2 | Atopic dermatitis | [23] | |
15 | Rilopirox | Drug Info | Phase 2 | Fungal infection | [24] | |
16 | TA-270 | Drug Info | Phase 2 | Asthma | [25] | |
17 | Tepoxalin | Drug Info | Phase 2 | Asthma | [26] | |
18 | Tipelukast | Drug Info | Phase 2 | Asthma | [27] | |
19 | UCB-35440 | Drug Info | Phase 2 | Rhinitis | [28] | |
20 | WY-50295-tromethamine | Drug Info | Phase 2 | Asthma | [29] | |
21 | BF-389 | Drug Info | Phase 1 | Rheumatoid arthritis | [30] | |
22 | SKF-105809 | Drug Info | Phase 1 | Pain | [31] | |
Discontinued Drug(s) | [+] 43 Discontinued Drugs | + | ||||
1 | Ibuproxam | Drug Info | Withdrawn from market | Respiratory disease | [32] | |
2 | CJ-13610 | Drug Info | Discontinued in Phase 2 | Asthma | [33], [34] | |
3 | DuP-654 | Drug Info | Discontinued in Phase 2 | Pruritus | [35] | |
4 | E-3040 | Drug Info | Discontinued in Phase 2 | Thrombosis | [36] | |
5 | E-6080 | Drug Info | Discontinued in Phase 2 | Asthma | [37] | |
6 | ETH615 | Drug Info | Discontinued in Phase 2 | Dermatitis | [38] | |
7 | FPL-64170 | Drug Info | Discontinued in Phase 2 | Psoriasis vulgaris | [39] | |
8 | Linetastine | Drug Info | Discontinued in Phase 2 | Rhinitis | [40] | |
9 | MK-591 | Drug Info | Discontinued in Phase 2 | Asthma | [41] | |
10 | MK-886 | Drug Info | Discontinued in Phase 2 | Asthma | [42], [43] | |
11 | MLN-977 | Drug Info | Discontinued in Phase 2 | Chronic obstructive pulmonary disease | [44] | |
12 | OPC-21268 | Drug Info | Discontinued in Phase 2 | Cardiac disease | [45], [46] | |
13 | R-68151 | Drug Info | Discontinued in Phase 2 | Psoriasis vulgaris | [47] | |
14 | SC-45662 | Drug Info | Discontinued in Phase 2 | Asthma | [48] | |
15 | TEBUFELONE | Drug Info | Discontinued in Phase 2 | Pain | [49] | |
16 | AZD-4407 | Drug Info | Discontinued in Phase 1 | Chronic obstructive pulmonary disease | [50] | |
17 | CD-581 | Drug Info | Discontinued in Phase 1 | Atopic dermatitis | [51] | |
18 | Licofelone | Drug Info | Discontinued in Phase 1 | Osteoarthritis | [52] | |
19 | A-78773 | Drug Info | Terminated | Asthma | [53] | |
20 | A-79175 | Drug Info | Terminated | Asthma | [54] | |
21 | A-80263 | Drug Info | Terminated | Inflammation | [55] | |
22 | AA-861 | Drug Info | Terminated | Allergy | [56] | |
23 | BI-L-357 | Drug Info | Terminated | Asthma | [57] | |
24 | BU-4601A | Drug Info | Terminated | Asthma | [58] | |
25 | BW A4C | Drug Info | Terminated | Arthritis | [59] | |
26 | BW B70C | Drug Info | Terminated | Asthma | [60] | |
27 | BW755C | Drug Info | Terminated | Inflammation | [61] | |
28 | CGS-26529 | Drug Info | Terminated | Inflammation | [62] | |
29 | CI-986 | Drug Info | Terminated | Rheumatoid arthritis | [63] | |
30 | CMI-206 | Drug Info | Terminated | Inflammation | [64] | |
31 | Epocarbazolin-A | Drug Info | Terminated | Asthma | [65] | |
32 | ER-34122 | Drug Info | Terminated | Inflammation | [66], [67] | |
33 | KC-11404 | Drug Info | Terminated | Asthma | [68] | |
34 | KC-11425 | Drug Info | Terminated | Asthma | [69] | |
35 | LY-221068 | Drug Info | Terminated | Arthritis | [70] | |
36 | PD-146176 | Drug Info | Terminated | Arteriosclerosis | [71] | |
37 | R zileuton | Drug Info | Terminated | Asthma | [72] | |
38 | RWJ-63556 | Drug Info | Terminated | Arthritis | [73] | |
39 | Sch-40120 | Drug Info | Terminated | Pruritus | [74] | |
40 | SKF-104351 | Drug Info | Terminated | Rheumatoid arthritis | [75] | |
41 | WY-28342 | Drug Info | Terminated | Rheumatoid arthritis | [76] | |
42 | ZD-7717 | Drug Info | Terminated | Asthma | [77] | |
43 | ZM-230487 | Drug Info | Terminated | Asthma | [78] | |
Mode of Action | [+] 3 Modes of Action | + | ||||
Inhibitor | [+] 160 Inhibitor drugs | + | ||||
1 | Diethylcarbamazine | Drug Info | [1] | |||
2 | Zileuton | Drug Info | [79], [80], [81], [82], [83], [84] | |||
3 | 3,4-Dihydroxycinnamic Acid | Drug Info | [85], [86], [87] | |||
4 | Silymarin | Drug Info | [88] | |||
5 | ABT-761 | Drug Info | [89], [90], [91] | |||
6 | Avastin+/-Tarceva | Drug Info | [92] | |||
7 | BAICALEIN | Drug Info | [93] | |||
8 | BIM23A760 | Drug Info | [84], [94] | |||
9 | PF-4191834 | Drug Info | [95] | |||
10 | PTC299 | Drug Info | [96] | |||
11 | Q301 | Drug Info | [97] | |||
12 | Rilopirox | Drug Info | [98] | |||
13 | TA-270 | Drug Info | [99] | |||
14 | Tepoxalin | Drug Info | [100] | |||
15 | WY-50295-tromethamine | Drug Info | [29] | |||
16 | SKF-105809 | Drug Info | [31] | |||
17 | Ibuproxam | Drug Info | [103] | |||
18 | CJ-13610 | Drug Info | [34] | |||
19 | CV-6504 | Drug Info | [104], [105] | |||
20 | DuP-654 | Drug Info | [106] | |||
21 | E-3040 | Drug Info | [107] | |||
22 | E-6080 | Drug Info | [108] | |||
23 | ETH615 | Drug Info | [84] | |||
24 | FPL-64170 | Drug Info | [109] | |||
25 | Linetastine | Drug Info | [84], [110] | |||
26 | MK-591 | Drug Info | [111], [112] | |||
27 | MLN-977 | Drug Info | [114] | |||
28 | OPC-21268 | Drug Info | [115] | |||
29 | R-68151 | Drug Info | [84], [116] | |||
30 | SC-45662 | Drug Info | [117] | |||
31 | TEBUFELONE | Drug Info | [118] | |||
32 | AZD-4407 | Drug Info | [119] | |||
33 | CD-581 | Drug Info | [2] | |||
34 | Licofelone | Drug Info | [120], [121], [122], [123] | |||
35 | A-78773 | Drug Info | [124] | |||
36 | A-79175 | Drug Info | [125], [126] | |||
37 | A-80263 | Drug Info | [127] | |||
38 | AA-861 | Drug Info | [128], [129], [130], [131] | |||
39 | BI-L-357 | Drug Info | [132] | |||
40 | BU-4601A | Drug Info | [133] | |||
41 | BW A4C | Drug Info | [134], [135], [136] | |||
42 | BW B70C | Drug Info | [136] | |||
43 | BW755C | Drug Info | [137] | |||
44 | CGS 8515 | Drug Info | [138] | |||
45 | CGS-26529 | Drug Info | [139] | |||
46 | Epocarbazolin-A | Drug Info | [65] | |||
47 | LY-221068 | Drug Info | [142] | |||
48 | NAFAZATROM | Drug Info | [143] | |||
49 | R zileuton | Drug Info | [145] | |||
50 | R-85355 | Drug Info | [116] | |||
51 | REV-5901 | Drug Info | [93] | |||
52 | ZM-230487 | Drug Info | [150] | |||
53 | 1,2-Dihydro-indazol-3-one | Drug Info | [93] | |||
54 | 1,2-Dihydroxy-10H-anthracen-9-one | Drug Info | [92] | |||
55 | 1,3,8-Trihydroxy-6-methyl-10H-anthracen-9-one | Drug Info | [92] | |||
56 | 1,5-Dihydroxy-10H-anthracen-9-one | Drug Info | [92] | |||
57 | 1,8,9-Trimethoxy-9,10-dihydro-anthracene | Drug Info | [92] | |||
58 | 1,8-Dichloro-10H-anthracen-9-one | Drug Info | [92] | |||
59 | 1,8-Dihydroxy-2-propionyl-10H-anthracen-9-one | Drug Info | [92] | |||
60 | 1-Benzyl-1,2-dihydro-indazol-3-one | Drug Info | [93] | |||
61 | 1-furan-2-yl-3-pyridin-2-yl-propenone (FPP-3) | Drug Info | [151] | |||
62 | 1-Hydroxy-10H-anthracen-9-one | Drug Info | [92] | |||
63 | 1-Hydroxy-8-methoxy-10H-anthracen-9-one | Drug Info | [92] | |||
64 | 1-Methyl-1,2-dihydro-indazol-3-one | Drug Info | [93] | |||
65 | 10-Acetyl-1,8-dihydroxy-10H-anthracen-9-one | Drug Info | [92] | |||
66 | 10-Benzoyl-1,8-dihydroxy-10H-anthracen-9-one | Drug Info | [92] | |||
67 | 15-hydroxyeicosatetraenoic acid | Drug Info | [84], [152] | |||
68 | 2'-Nitro-biphenyl-4-carboxylic acid hydroxyamide | Drug Info | [153] | |||
69 | 2-(1H-Indol-3-ylmethyl)-1,2-dihydro-indazol-3-one | Drug Info | [93] | |||
70 | 2-(3-Phenyl-propyl)-1,2-dihydro-indazol-3-one | Drug Info | [93] | |||
71 | 2-(4-Butoxy-phenoxy)-N-hydroxy-acetamide | Drug Info | [153] | |||
72 | 2-(4-Butoxy-phenoxy)-N-hydroxy-N-methyl-acetamide | Drug Info | [153] | |||
73 | 2-(4-Butoxy-phenoxy)-N-hydroxy-propionamide | Drug Info | [153] | |||
74 | 2-(4-Butoxy-phenyl)-N-hydroxy-N-methyl-acetamide | Drug Info | [153] | |||
75 | 2-(4-hydroxylphenyl)-3-(3,5-dihydroxylphenyl) propenoic acid (NNU-hdpa) | Drug Info | [154] | |||
76 | 2-(4-Methoxy-phenyl)-5-phenyl-thiazol-4-ol | Drug Info | [155] | |||
77 | 2-(4-Phenyl-butyl)-1,2-dihydro-indazol-3-one | Drug Info | [93] | |||
78 | 2-Benzyl-1,2-dihydro-indazol-3-one | Drug Info | [93] | |||
79 | 2-Biphenyl-4-yl-N-hydroxy-N-methyl-acetamide | Drug Info | [153] | |||
80 | 2-Furan-2-ylmethyl-1,2-dihydro-indazol-3-one | Drug Info | [93] | |||
81 | 2-Methyl-1,2-dihydro-indazol-3-one | Drug Info | [93] | |||
82 | 2-Naphthalen-1-ylmethyl-1,2-dihydro-indazol-3-one | Drug Info | [93] | |||
83 | 2-Naphthalen-2-ylmethyl-1,2-dihydro-indazol-3-one | Drug Info | [93] | |||
84 | 2-Phenethyl-1,2-dihydro-indazol-3-one | Drug Info | [93] | |||
85 | 2-Phenyl-1,2-dihydro-indazol-3-one | Drug Info | [93] | |||
86 | 2-Pyridin-2-ylmethyl-1,2-dihydro-indazol-3-one | Drug Info | [93] | |||
87 | 2-Pyridin-3-ylmethyl-1,2-dihydro-indazol-3-one | Drug Info | [135], [93] | |||
88 | 2-Pyridin-4-ylmethyl-1,2-dihydro-indazol-3-one | Drug Info | [93] | |||
89 | 2-Thiazol-5-ylmethyl-1,2-dihydro-indazol-3-one | Drug Info | [93] | |||
90 | 2-Thiophen-2-ylmethyl-1,2-dihydro-indazol-3-one | Drug Info | [93] | |||
91 | 3,4-Dihydroxy-10H-anthracen-9-one | Drug Info | [92] | |||
92 | 3-(4-Butoxy-phenyl)-N-hydroxy-N-methyl-acrylamide | Drug Info | [153] | |||
93 | 3-Benzoyl-N-hydroxy-benzamide | Drug Info | [153] | |||
94 | 3-Biphenyl-3-yl-N-hydroxy-N-methyl-acrylamide | Drug Info | [153] | |||
95 | 3-Biphenyl-4-yl-N-hydroxy-N-methyl-acrylamide | Drug Info | [153] | |||
96 | 4,5-Dihydroxy-10H-anthracen-9-one | Drug Info | [92] | |||
97 | 4,5-Dimethoxy-10H-anthracen-9-one | Drug Info | [92] | |||
98 | 4-(1H-indol-3-yl)-1-morpholinobutan-1-one | Drug Info | [156] | |||
99 | 4-Bromo-N-hydroxy-benzamide | Drug Info | [153] | |||
100 | 4-Butoxy-N-hydroxy-N-methyl-benzamide | Drug Info | [153] | |||
101 | 4-Hydroxy-5-methoxy-10H-anthracen-9-one | Drug Info | [92] | |||
102 | 4-Pentadeca-1,3,6-trienylsulfanyl-butyric acid | Drug Info | [143] | |||
103 | 5,8-Dihydroxy-1,4-naphthoquinone | Drug Info | [92] | |||
104 | 5-Chloro-N-(4-ethylphenyl)benzo[d]oxazol-2-amine | Drug Info | [157] | |||
105 | 5-Chloro-N-phenylbenzo[d]oxazol-2-amine | Drug Info | [157] | |||
106 | 5-Methoxy-N-phenylbenzo[d]oxazol-2-amine | Drug Info | [157] | |||
107 | 5-Methyl-2-p-tolyl-thiazol-4-ol | Drug Info | [155] | |||
108 | 5-Methyl-N-phenylbenzo[d]oxazol-2-amine | Drug Info | [157] | |||
109 | 5S-HETE | Drug Info | [84], [152] | |||
110 | 7-tert-butyl-2, 3-dihydro-3, 3-dimethyl substituted dihydrofuran 30 (DHDMBF30) | Drug Info | [158] | |||
111 | ACACETIN | Drug Info | [159] | |||
112 | Acanthus ilicifolius Linn | Drug Info | [137] | |||
113 | Acetic acid 2-phenyl-5-propyl-thiazol-4-yl ester | Drug Info | [155] | |||
114 | Acetic acid 5-butyl-2-phenyl-thiazol-4-yl ester | Drug Info | [155] | |||
115 | Anthracene-2-carboxylic acid hydroxyamide | Drug Info | [153] | |||
116 | ANTHRONE | Drug Info | [92] | |||
117 | Biphenyl-3-carboxylic acid hydroxyamide | Drug Info | [153] | |||
118 | Biphenyl-4-carboxylic acid hydroxyamide | Drug Info | [153] | |||
119 | BUDDLEDIN A | Drug Info | [159] | |||
120 | BW A360C | Drug Info | [136] | |||
121 | BW B218C | Drug Info | [136] | |||
122 | Chebulagic acid | Drug Info | [163] | |||
123 | CYLINDOL A | Drug Info | [164] | |||
124 | Heme | Drug Info | [166] | |||
125 | Hexanoic acid 2,5-diphenyl-thiazol-4-yl ester | Drug Info | [155] | |||
126 | Hyperforin | Drug Info | [167] | |||
127 | L-652,343 | Drug Info | [169] | |||
128 | N-(2-Ethylphenyl)-5-methylbenzo[d]oxazol-2-amine | Drug Info | [157] | |||
129 | N-(3-Bromophenyl)-5-methoxybenzo[d]oxazol-2-amine | Drug Info | [157] | |||
130 | N-(4-Ethylphenyl)-5-methylbenzo[d]oxazol-2-amine | Drug Info | [157] | |||
131 | N-(4-Ethylphenyl)benzo[d]oxazol-2-amine | Drug Info | [157] | |||
132 | N-Hydroxy-2-methyl-3-naphthalen-2-yl-acrylamide | Drug Info | [153] | |||
133 | N-Hydroxy-2-naphthalen-2-yl-acetamide | Drug Info | [153] | |||
134 | N-Hydroxy-3-naphthalen-2-yl-acrylamide | Drug Info | [153] | |||
135 | N-Hydroxy-3-naphthalen-2-yl-N-p-tolyl-acrylamide | Drug Info | [153] | |||
136 | N-Hydroxy-3-naphthalen-2-yl-N-phenyl-acrylamide | Drug Info | [153] | |||
137 | N-Hydroxy-3-naphthalen-2-yl-propionamide | Drug Info | [153] | |||
138 | N-Hydroxy-3-phenyl-acrylamide | Drug Info | [153] | |||
139 | N-hydroxy-4-(naphthalen-1-yl)benzamide | Drug Info | [153] | |||
140 | N-Hydroxy-4-iodo-benzamide | Drug Info | [153] | |||
141 | N-Hydroxy-4-isobutyl-benzamide | Drug Info | [153] | |||
142 | N-Hydroxy-4-naphthalen-2-yl-benzamide | Drug Info | [153] | |||
143 | N-Hydroxy-N-methyl-2,3,3-triphenyl-acrylamide | Drug Info | [153] | |||
144 | N-Hydroxy-N-methyl-2-naphthalen-2-yl-propionamide | Drug Info | [153] | |||
145 | N-Hydroxy-N-methyl-3-naphthalen-1-yl-acrylamide | Drug Info | [153] | |||
146 | N-Hydroxy-N-methyl-3-naphthalen-2-yl-acrylamide | Drug Info | [103] | |||
147 | N-Hydroxy-N-methyl-3-naphthalen-2-yl-propionamide | Drug Info | [153] | |||
148 | N-Hydroxy-N-methyl-3-phenanthren-2-yl-acrylamide | Drug Info | [153] | |||
149 | N-Hydroxy-N-methyl-3-phenanthren-3-yl-acrylamide | Drug Info | [153] | |||
150 | N-Hydroxy-N-methyl-3-phenanthren-9-yl-acrylamide | Drug Info | [153] | |||
151 | N-Hydroxy-N-methyl-benzamide | Drug Info | [153] | |||
152 | N-hydroxy-N-[1-(4-isobutylphenyl)ethyl]urea | Drug Info | [170] | |||
153 | N-Phenylbenzo[d]oxazol-2-amine | Drug Info | [157] | |||
154 | Naphthalene-2-carboxylic acid hydroxyamide | Drug Info | [153] | |||
155 | Phenanthrene-2-carboxylic acid hydroxyamide | Drug Info | [153] | |||
156 | Phenanthrene-3-carboxylic acid hydroxyamide | Drug Info | [153] | |||
157 | PHENIDONE | Drug Info | [164] | |||
158 | PYROGALLOL | Drug Info | [92] | |||
159 | SK&F 107649 | Drug Info | [173] | |||
160 | TZI-41127 | Drug Info | [174] | |||
Modulator | [+] 28 Modulator drugs | + | ||||
1 | Flobufen | Drug Info | [9] | |||
2 | FPL-62064 | Drug Info | [10] | |||
3 | Tenidap | Drug Info | [12] | |||
4 | Darbufelone | Drug Info | [13] | |||
5 | CMI-392 | Drug Info | [17] | |||
6 | E-6700 | Drug Info | [18] | |||
7 | MK-866 | Drug Info | [19] | |||
8 | Tipelukast | Drug Info | [101] | |||
9 | UCB-35440 | Drug Info | [102] | |||
10 | BF-389 | Drug Info | [30] | |||
11 | MK-886 | Drug Info | [113] | |||
12 | CI-986 | Drug Info | [63] | |||
13 | CMI-206 | Drug Info | [140] | |||
14 | ER-34122 | Drug Info | [66], [67] | |||
15 | KC-11404 | Drug Info | [68] | |||
16 | PD-146176 | Drug Info | [144] | |||
17 | RWJ-63556 | Drug Info | [73] | |||
18 | Sch-40120 | Drug Info | [146] | |||
19 | SKF-104351 | Drug Info | [147] | |||
20 | WY-28342 | Drug Info | [148] | |||
21 | ZD-7717 | Drug Info | [149] | |||
22 | BW-858C | Drug Info | [160] | |||
23 | BW-A137C | Drug Info | [161] | |||
24 | CGS-23885 | Drug Info | [162] | |||
25 | FR-122788 | Drug Info | [165] | |||
26 | ICI-211965 | Drug Info | [168] | |||
27 | SB-202235 | Drug Info | [171] | |||
28 | SC-41661A | Drug Info | [172] | |||
Antagonist | [+] 1 Antagonist drugs | + | ||||
1 | KC-11425 | Drug Info | [141] |
Cell-based Target Expression Variations | Top | |||||
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Cell-based Target Expression Variations |
Drug Binding Sites of Target | Top | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Ligand Name: Arachidonic acid | Ligand Info | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Structure Description | S663D Stable-5-LOX in complex with Arachidonic Acid | PDB:3V99 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Method | X-ray diffraction | Resolution | 2.25 Å | Mutation | Yes | [175] | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
PDB Sequence |
SYTVTVATGS
14 QEHAGTDDYI24 YLSLVGSAGC34 SEKHLLDKGS44 FERGAVDSYD54 VTVDEELGEI 64 QLVRIEKRKY74 GSNDDWYLKY84 ITLKTPHGDY94 IEFPCYRWIT104 GDVEVVLRDG 114 RAKLARDDQI124 HILKQHRRKE134 LETRQKQYRW144 MEWNPGFPLS154 IDAKCHKDLP 164 RDIQFDSFVL179 NYSKAMENLF189 QSSWNDFADF207 EKIFVKISNT217 ISERVMNHWQ 227 EDLMFGYQFL237 NGANPVLIRR247 CTELPEKLPV257 TTEMVECSLE267 RQLSLEQEVQ 277 QGNIFIVDFE287 LLDGIDCTLQ303 FLAAPICLLY313 KNLANKIVPI323 AIQLNQIPGD 333 ENPIFLPSDA343 KYDWLLAKIW353 VRSSDFHVHQ363 TITHLLRTHL373 VSEVFGIAMY 383 RQLPAVHPIF393 KLLVAHVRFT403 IAINTKAREQ413 GGHVQMVQRA439 MKDLTYASLC 449 FPEAIKARGM459 ESKEDIPYYF469 YRDDGLLVWE479 AIRTFTAEVV489 DIYYEGDQVV 499 EEDPELQDFV509 NDVYVYGMRG519 RKSSGFPKSV529 KSREQLSEYL539 TVVIFTASAQ 549 HAAVNFGQYD559 WASWIPNAPP569 TMRAPPPTAK579 GVVTIEQIVD589 TLPDRGRSCW 599 HLGAVWALSQ609 FELFLGMYPE622 EHFIEKPVKE632 AMARFRKNLE642 AIVSVIAERN 652 ENLQLPYYYL662 DPDRIPNSVA672
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☰Loading data... Dynamically generated for selected residues. Nodes can be dragged or clicked. Label: Selection: Name:
PDB ID: Option 1, search with your selection (all residues are selected by default) in the loaded structures: Option 2, search with PDB ID and chain name: PDB ID: Chain Name: Option 3, search with a PDB file: Foldseek web server. 1. your selection (all residues are selected by default) in the loaded structures to 2 (Optional). Once you see the structure neighbors, you can view the alignment in iCn3D by inputing a list of PDB chain IDs or AlphaFold UniProt IDs below. The PDB chain IDs are the same as the record names such as "1HHO_A". The UniProt ID is the text between "AF-" and "-F1". For example, the UniProt ID for the record name "AF-P69905-F1-model_v4" is "P69905". Chain ID List: BCIF/MMTF ID: PDB ID: Very high (pLDDT > 90) Confident (90 > pLDDT > 70) Low (70 > pLDDT > 50) Very low (pLDDT < 50) AlphaFold Uniprot ID: PAE Map: NCBI Protein Accession: PDB File: Multiple PDB Files: The custom JSON file on residue colors has the following format for proteins("ALA" and "ARG") and nucleotides("G" and "A"): {"ALA":"#C8C8C8", "ARG":"#145AFF", ..., "G":"#008000", "A":"#6080FF", ...} Residue Color File: The custom file for the structure has two columns separated by space or tab: residue number, and score in the range of 0-100. If you click "Apply Custom Color" button, the scores 0, 50 and 100 correspond to the three colors specified below. If you click "Apply Custom Tube", the selected residues will be displayed in a style similar to "B-factor Tube". Custom File: 1. Score to Color: 0: 50: 100: or 2. You can define your own reference numbers in a custom file using Excel, and then export it as a CSV file. An example file is shown below with cells separated by commas. refnum,11,12,,21,22,,10C,11C,20CThe first row defines the reference residue numbers, which could be any strings. The 1st cell could be anything. The rest cells are reference residue numbers (e.g., 11, 21, 10C, etc.) or empty cells. Each chain has a separate row. The first cell of the second row is the chain ID "1TUP_A". The rest cells are the corresponding real residue numbers for reference residue numbers in the first row. For example, the reference numbers for residues 100, 101, and 132 in the chain 1TUP_A are 11, 12, and 22, respectively. The fourth row shows another set of reference numners for the chain "1TUP_C". It could be a chain from a different structure. To select all residues corresponding to the reference numbers, you can simplay replace ":" with "%" in the Specification. For example, "%12" selects the residue 101 in 1TUP_A and the residue 111 in 1TUP_B. ".A%12" has the chain "A" filter and selects the residue 101 in 1TUP_A. Custom File: ID1: ID2: VAST+ based on VAST: VAST+ based on TM-align: All chains will be aligned to the first chain in the comma-separated chain IDs. Each chain ID has the form of PDBID_chain (e.g., 1HHO_A, case sensitive) or UniprotID (e.g., P69905 for AlphaFold structures). Chain IDs: (Note: To align chains in custom PDB files, you could load them in "File > Open File > PDB Files (appendable)" and click "Analysis > Defined Sets". Finally select multiple chains in Defined Sets and click "File > Realign Selection".) All chains will be aligned to the first chain in the comma-separated chain IDs. Each chain ID has the form of PDBID_chain (e.g., 1HHO_A, case sensitive) or UniprotID (e.g., P69905 for AlphaFold structures). Chain IDs: The sequence alignment (followed by structure alignment) is based on residue numbers in the First/Master chain: (Note: To align chains in custom PDB files, you could load them in "File > Open File > PDB Files (appendable)" and click "Analysis > Defined Sets". Finally select multiple chains in Defined Sets and click "File > Realign Selection".) All chains will be aligned to the first chain in the comma-separated chain IDs. Each chain ID has the form of PDBID_chain (e.g., 1HHO_A, case sensitive) or UniprotID (e.g., P69905 for AlphaFold structures). Chain IDs: Each alignment is defined as " | "-separated residue lists in one line. "10-50" means a range of residues from 10 to 50. Option 1: Option 2: All chains will be aligned to the first chain in the comma-separated chain IDs. Each chain ID has the form of PDBID_chain (e.g., 1HHO_A, case sensitive) or UniprotID (e.g., P69905 for AlphaFold structures). Chain IDs: Each alignment is defined as " | "-separated residue lists in one line. "10-50" means a range of residues from 10 to 50. Please specify the mutations with a comma separated mutation list. Each mutation can be specified as "[uppercase PDB ID or AlphaFold UniProt ID]_[Chain Name]_[Residue Number]_[One Letter Mutant Residue]". E.g., the mutation of N501Y in the E chain of PDB 6M0J can be specified as "6M0J_E_501_Y". For AlphaFold structures, the "Chain ID" is "A". If you load a custom structure without PDB or UniProt ID, you can open "Seq. & Annotations" window and find the chain ID such as "stru_A". The part before the underscore is the structure ID, which can be used to specify the mutation such as "stru_A_...". Remember to choose "Show Mutation in: Current Page". Mutations: ID Type: PDB IDAlphaFold UniProt ID Show Mutation in: Current PageNew Page Mol2 File: SDF File: XYZ File: URL in the same host: Multiple mmCIF Files: mmCIF ID: Note: The "biological unit" is the biochemically active form of a biomolecule, or Note: The "biological unit" is the biochemically active form of a biomolecule, BLAST search with the protein sequence ID or FASTA sequence as input. If the protein accession is not a PDB chain, the corresponding AlphaFold UniProt structure is used. Enter a protein sequence ID (or FASTA sequence) and the aligned protein accession, which can be found using the Protein Sequence ID(NCBI protein accession of a sequence): or FASTA sequence: Aligned Protein Accession (or a chain of a PDB): ESM Metagenomic Atlas. The sequence should be less than 400 characters. For any sequence longer than 400, please see the discussion here. The sequence to structure prediction is done via FASTA sequence: Protein/Gene name: PubChem CID/Name/InchI: Chemical SMILES: Share Link URL: Collection File: Structures: 2fofc contour at default threshold or at: σ fofc contour at default threshold or at: σ 2fofc contour at default threshold or at: σ URL in the same host: fofc contour at default threshold or at: σ URL in the same host: Custom Color: Grid Size: Salt Concentration: M Potential contour at: kT/e(25.6mV at 298K) Note: Only the selected residues are used for DelPhi potential calculation by solving linear Poisson-Boltzmann equation. Grid Size: Salt Concentration: M Surface with max potential at: kT/e(25.6mV at 298K) Surface: Opacity: Wireframe: Note: Only the selected residues are used for DelPhi potential calculation by solving linear Poisson-Boltzmann equation. Potential contour at: kT/e(25.6mV at 298K) Note: Always load a PDB file before loading a PQR or DelPhi potential file. Potential contour at: kT/e(25.6mV at 298K) Grid Size: Salt Concentration: M PQR URL in the same host: Phi URL in the same host: Cube URL in the same host: Note: Always load a PDB file before loading a PQR or DelPhi potential file. Symmetry: Distance: Contact Type:
4. Sort Interactions on: to show two lines of residue nodes to show map with atom details to show interactions with strength parameters in 0-200:
(Note: you can also adjust thresholds at #1 to add/remove interactions.) 5. and select new sets 1. Select sets below or use your current selection: 2. 1. Select sets below or use your current selection. 2. 1. Select sets below or use your current selection: 2. Overall maximum RMSD: Å 3. 1. Select sets below: 2. 1. Select sets below: 2. 1. Select sets below: 2. 1. Select sets below: 2. Hold Ctrl key to select multiple nodes/lines. Green: H-Bonds; Cyan: Salt Bridge/Ionic; Grey: Contacts Magenta: Halogen Bonds; Red: π-Cation; Blue: π-Stacking Scale: Hold Ctrl key to select multiple nodes. Scale: Note: Nodes/Residues can be dragged. Both nodes and dashed lines/interactions can be clicked to select residues. Color legend for interactions (dashed lines): Green: H-Bonds; Cyan: Salt Bridge/Ionic; Grey: Contacts Magenta: Halogen Bonds; Red: π-Cation; Blue: π-Stacking Scale: Hold Ctrl key to select multiple nodes. Scale: Hold Ctrl key to select multiple nodes. Scale:
Contour at: σ Contour at: σ Contour at: % of maximum EM values 1. Select the first set: 2. Sphere with a radius: Å 3. Select the second set to apply the sphere: 4. the sphere around the first set of atoms interacting/contacting residue pairs in a file 1. Extracellular membrane Z-axis position: Å 2. intracellular membrane Z-axis position: Å 3. the adjusted membranes 1. Z-axis position of the first X-Y plane: Å 2. Z-axis position of the second X-Y plane: Å 3. the region between the planes to Defined Sets 2. Size: 3. Color: 4. Pick TWO atoms while holding "Alt" key 5. 2. Size: 3. Color: 4. 1. Pick TWO atoms while holding "Alt" key 2. Line Color: 3. 1. Pick TWO atoms while holding "Alt" key 2. Color: 3. 1. Select two sets
3. 1. Select two sets
2. Line style: 3. Line radius: 4. Color: 5. Opacity: 6. 1. Select a set: 2. Shape: 3. Radius: 4. Color: 5. Opacity: 6. 1. Select sets for pairwise distances
Note: Each set is represented by a vector, which is the X-axis of the principle axes. The angles between the vectors are then calculated. 1. Select sets for pairwise angles
1. Pick TWO atoms while holding "Alt" key 2. Coil Radius: (for coils, default 0.3) Stick Radius: (for sticks, default 0.4) Cross-Linkage Radius: (for cross-linkages, default 0.4) Trace Radius: (for C alpha trace, O3' trace, default 0.4) Ribbon Thickness: (for helix and sheet ribbons, nucleotide ribbons, default 0.2) Protein Ribbon Width: (for helix and sheet ribbons, default 1.3) Nucleotide Ribbon Width: (for nucleotide ribbons, default 0.8) Ball Scale: (for styles 'Ball and Stick' and 'Dot', default 0.3) 1. Shininess: (for the shininess of the 3D objects, default 40) 2. Three directional lights: Key Light: (for the light strength of the key light, default 0.8) Fill Light: (for the light strength of the fill light, default 0.4) Back Light: (for the light strength of the back light, default 0.2) 3. Thickness: Line Radius: (for stabilizers, hydrogen bonds, distance lines, default 0.1) Coil Radius: (for coils, default 0.3) Stick Radius: (for sticks, default 0.4) Cross-Linkage Radius: (for cross-linkages, default 0.4) Trace Radius: (for C alpha trace, O3' trace, default 0.4) Ribbon Thickness: (for helix and sheet ribbons, nucleotide ribbons, default 0.2) Protein Ribbon Width: (for helix and sheet ribbons, default 1.3) Nucleotide Ribbon Width: (for nucleotide ribbons, default 0.8) Ball Scale: (for styles 'Ball and Stick' and 'Dot', default 0.3) 4. Show Glycan Cartoon: (0: hide, 1: show, default 0) 5. Show Membrane: (0: hide, 1: show, default 1) 6. Enlarge Command Window: (0: Regular, 1: Large, default 0) 1. URLs Used in Browsers Please copy one of the URLs below. They show the same result. (To add a title to share link, click "Windows > Your Note" and click "File > Share Link" again.) Original URL with commands: Lifelong Short URL:(To replace this URL, send a pull request to update share.html at iCn3D GitHub) Lifelong Short URL + Window Title:(To update the window title, click "Analysis > Your Note/Window Title".) 2. Commands Used in Jupyter Noteboook Please copy the following commands into a cell in Jupyter Notebook to show the same result. More details are at https://github.com/ncbi/icn3d/tree/master/jupyternotebook. Annotations:
Zoom: mouse wheel; Move: left button; Select Multiple Nodes: Ctrl Key and drag an Area Force on Nodes: Label Size: Internal Edges: Color each residue based on the percentage of solvent accessilbe surface area. The color ranges from blue, to white, to red for a percentage of 0, 35(variable), and 100, respectively. Middle Percentage(White): % Select residue based on the percentage of solvent accessilbe surface area. The values are in the range of 0-100. Min Percentage: % Max Percentage: % Select residue based on B-factor/pLDDT. The values are in the range of 0-100. Min B-factor/pLDDT: % Max B-factor/pLDDT: % X: Y: Z: Vector 2, X: Y: Z: The angle is: degree. 1: 5: 9: 13: 2: 6: 10: 14: 3: 7: 11: 15: Choose an Ig template for selected residues: Choose an Ig template to align with selected residues: |
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Click to View More Binding Site Information of This Target with Different Ligands |
Different Human System Profiles of Target | Top |
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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 Tissue Distribution
of target is determined from a proteomics study that quantified more than 12,000 genes across 32 normal human tissues. Tissue Specificity (TS) score was used to define the enrichment of target across tissues.
The distribution of targets among different tissues or organs need to be taken into consideration when assessing the target druggability, as it is generally accepted that the wider the target distribution, the greater the concern over potential adverse effects
(Nat Rev Drug Discov, 20: 64-81, 2021).
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 Tissue Distribution
Human Pathway Affiliation
Biological Network Descriptors
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There is no similarity protein (E value < 0.005) for this target
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Note:
If a protein has TS (tissue specficity) scores at least in one tissue >= 2.5, this protein is called tissue-enriched (including tissue-enriched-but-not-specific and tissue-specific). In the plots, the vertical lines are at thresholds 2.5 and 4.
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KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
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Arachidonic acid metabolism | hsa00590 | Affiliated Target |
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Class: Metabolism => Lipid metabolism | Pathway Hierarchy | ||
Fc epsilon RI signaling pathway | hsa04664 | Affiliated Target |
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Class: Organismal Systems => Immune system | Pathway Hierarchy | ||
Serotonergic synapse | hsa04726 | Affiliated Target |
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Class: Organismal Systems => Nervous system | Pathway Hierarchy | ||
Ovarian steroidogenesis | hsa04913 | Affiliated Target |
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Class: Organismal Systems => Endocrine system | Pathway Hierarchy |
Degree | 7 | Degree centrality | 7.52E-04 | Betweenness centrality | 8.13E-04 |
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Closeness centrality | 1.93E-01 | Radiality | 1.33E+01 | Clustering coefficient | 4.76E-02 |
Neighborhood connectivity | 4.71E+00 | Topological coefficient | 2.11E-01 | Eccentricity | 13 |
Download | Click to Download the Full PPI Network of This Target | ||||
Chemical Structure based Activity Landscape of Target | Top |
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Drug Property Profile of Target | Top | |
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(1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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(5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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"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 | |||||
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Co-Targets |
Target Poor or Non Binders | Top | |||||
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Target Poor or Non Binders |
Target Regulators | Top | |||||
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Target-regulating microRNAs | ||||||
Target-interacting Proteins |
Target Profiles in Patients | Top | |||||
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Target Expression Profile (TEP) |
Target Affiliated Biological Pathways | Top | |||||
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BioCyc | [+] 6 BioCyc Pathways | + | ||||
1 | Aspirin-triggered lipoxin biosynthesis | |||||
2 | Resolvin D biosynthesis | |||||
3 | Leukotriene biosynthesis | |||||
4 | Lipoxin biosynthesis | |||||
5 | Aspirin triggered resolvin D biosynthesis | |||||
6 | Aspirin triggered resolvin E biosynthesis | |||||
KEGG Pathway | [+] 5 KEGG Pathways | + | ||||
1 | Arachidonic acid metabolism | |||||
2 | Metabolic pathways | |||||
3 | Serotonergic synapse | |||||
4 | Ovarian steroidogenesis | |||||
5 | Toxoplasmosis | |||||
NetPath Pathway | [+] 1 NetPath Pathways | + | ||||
1 | IL4 Signaling Pathway | |||||
Pathwhiz Pathway | [+] 1 Pathwhiz Pathways | + | ||||
1 | Arachidonic Acid Metabolism | |||||
WikiPathways | [+] 4 WikiPathways | + | ||||
1 | Vitamin D Receptor Pathway | |||||
2 | Arachidonic acid metabolism | |||||
3 | Eicosanoid Synthesis | |||||
4 | Selenium Micronutrient Network |
Target-Related Models and Studies | Top | |||||
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Target Validation | ||||||
Target QSAR Model |
References | Top | |||||
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REF 1 | Inhibition of leukotriene formation by diethylcarbamazine modifies the acid-base balance in the rabbits with blast injuries of the lungs. Vojnosanit Pregl. 1999 May-Jun;56(3):243-7. | |||||
REF 2 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
REF 3 | Opportunities and challenges in antiparasitic drug discovery. Nat Rev Drug Discov. 2005 Sep;4(9):727-40. | |||||
REF 4 | 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: 5297). | |||||
REF 5 | Current and emerging drugs for idiopathic pulmonary fibrosis. Expert Opin Emerg Drugs. 2007 Nov;12(4):627-46. | |||||
REF 6 | ClinicalTrials.gov (NCT02556814) Caffeic Acid Combining High-dose Dexamethasone in Management of ITP. U.S. National Institutes of Health. | |||||
REF 7 | ABT-761 (Abbott). Curr Opin Investig Drugs. 2001 Jan;2(1):68-71. | |||||
REF 8 | Clinical pipeline report, company report or official report of Roche. | |||||
REF 9 | Pharmacological profile of the novel potent antirheumatic 4-(2',4'-difluorobiphenyl-4-yl)-2-methyl-4-oxobutanoic acid. Arzneimittelforschung. 1997 May;47(5):648-52. | |||||
REF 10 | FPL 62064, a topically active 5-lipoxygenase/cyclooxygenase inhibitor. Agents Actions. 1990 Jun;30(3-4):432-42. | |||||
REF 11 | 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: 2395). | |||||
REF 12 | The in vitro free radical scavenging activity of tenidap, a new dual cyclo-oxygenase and 5-1ipoxygenase inhibitor. Mediators Inflamm. 1992;1(2):141-3. | |||||
REF 13 | Novel dual cyclooxygenase and lipoxygenase inhibitors targeting hyaluronan-CD44v6 pathway and inducing cytotoxicity in colon cancer cells. Bioorg Med Chem. 2013 May 1;21(9):2551-9. | |||||
REF 14 | ClinicalTrials.gov (NCT03830684) A Randomized, Double-blind, Placebo-controlled, Multicenter and Phase IIa Clinical Trial for the Effectiveness and Safety of Baicalein Tablets in the Treatment of Improve Other Aspects of Healthy Adult With Influenza Fever. U.S. National Institutes of Health. | |||||
REF 15 | BIM-23A760, a chimeric molecule directed towards somatostatin and dopamine receptors, vs universal somatostatin receptors ligands in GH-secreting pituitary adenomas partial responders to octreotide. J Endocrinol Invest. 2005;28(11 Suppl International):21-7. | |||||
REF 16 | Emerging drugs for acromegaly. Expert Opin Emerg Drugs. 2008 Jun;13(2):273-93. | |||||
REF 17 | Anti-inflammatory activities of LDP-392, a dual PAF receptor antagonist and 5-lipoxygenase inhibitor. Pharmacol Res. 2001 Sep;44(3):213-20. | |||||
REF 18 | Structure-activity relationships of (E)-3-(1,4-benzoquinonyl)-2-[(3-pyridyl)-alkyl]-2-propenoic acid derivatives that inhibit both 5-lipoxygenase and thromboxane A2 synthetase. J Med Chem. 1996 Aug 2;39(16):3148-57. | |||||
REF 19 | Inhibition of leukotriene synthesis with MK-886 prevents a rise in blood pressure and reduces noradrenaline-evoked contraction in L-NAME-treated rats | |||||
REF 20 | ClinicalTrials.gov (NCT01147458) A Study Of The Safety And Efficacy Of PF-04191834 In Patients With Osteoarthritis Of The Knee. U.S. National Institutes of Health. | |||||
REF 21 | 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: 6040). | |||||
REF 22 | The effects of antiinflammatory and antiallergic drugs on cytokine release after stimulation of human whole blood by lipopolysaccharide and zymosan A. Inflamm Res. 1995 Jul;44(7):269-74. | |||||
REF 23 | ClinicalTrials.gov (NCT03571620) Safety and Efficacy Study of Q301 in Mild to Moderate Adolescents and Adults Atopic Dermatitis Patients. U.S. National Institutes of Health. | |||||
REF 24 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006112) | |||||
REF 25 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010788) | |||||
REF 26 | Effects of tepoxalin, a dual inhibitor of cyclooxygenase/5-lipoxygenase, on events associated with NSAID-induced gastrointestinal inflammation. Prostaglandins Leukot Essent Fatty Acids. 1997 Jun;56(6):417-23. | |||||
REF 27 | ClinicalTrials.gov (NCT02503657) Safety and Tolerability Study in Subjects With Idiopathic Pulmonary Fibrosis (IPF). | |||||
REF 28 | Clinical pipeline report, company report or official report of UCB. | |||||
REF 29 | WY-50295 tromethamine: a 5-lipoxygenase inhibitor without activity in human whole blood. Prostaglandins Leukot Essent Fatty Acids. 1999 Jan;60(1):31-41. | |||||
REF 30 | Antiarthritic profile of BF-389--a novel anti-inflammatory agent with low ulcerogenic liability. Agents Actions. 1992 Sep;37(1-2):90-8. | |||||
REF 31 | Analgetic activity of SK&F 105809, a dual inhibitor of arachidonic acid metabolism. Agents Actions Suppl. 1991;32:113-7. | |||||
REF 32 | Anti-inflammatory agents: determination of ibuproxam and its metabolite humans. Correlation between bioavailability, tolerance and chemico-physical characteristics. Arzneimittelforschung. 1980;30(9):1607-9. | |||||
REF 33 | 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: 5169). | |||||
REF 34 | Emerging drugs for the treatment of chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2006 May;11(2):275-91. | |||||
REF 35 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003690) | |||||
REF 36 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005994) | |||||
REF 37 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001952) | |||||
REF 38 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006733) | |||||
REF 39 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005063) | |||||
REF 40 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002311) | |||||
REF 41 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001712) | |||||
REF 42 | 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: 2655). | |||||
REF 43 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000073) | |||||
REF 44 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007577) | |||||
REF 45 | 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: 2196). | |||||
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REF 47 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003630) | |||||
REF 48 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001362) | |||||
REF 49 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002346) | |||||
REF 50 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009803) | |||||
REF 51 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008118) | |||||
REF 52 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003927) | |||||
REF 53 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003598) | |||||
REF 54 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004773) | |||||
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REF 56 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000099) | |||||
REF 57 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002162) | |||||
REF 58 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005261) | |||||
REF 59 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000230) | |||||
REF 60 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002163) | |||||
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REF 69 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005461) | |||||
REF 70 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002348) | |||||
REF 71 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010267) | |||||
REF 72 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026867) | |||||
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REF 74 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003693) | |||||
REF 75 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000933) | |||||
REF 76 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005582) | |||||
REF 77 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007338) | |||||
REF 78 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005134) | |||||
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