Target Information
Target General Information | Top | |||||
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Target ID |
T14342
(Former ID: TTDS00317)
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Target Name |
Human immunodeficiency virus Reverse transcriptase (HIV RT)
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Synonyms |
HIV p66 RT; HIV Exoribonuclease H
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Gene Name |
HIV RT
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Target Type |
Successful target
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[1] | ||||
Disease | [+] 3 Target-related Diseases | + | ||||
1 | Hepatitis virus infection [ICD-11: 1E50-1E51] | |||||
2 | Human immunodeficiency virus disease [ICD-11: 1C60-1C62] | |||||
3 | Virus infection [ICD-11: 1A24-1D9Z] | |||||
Function |
Gag-Pol polyprotein: Mediates, with Gag polyprotein, the essential events in virion assembly, including binding the plasma membrane, making the protein-protein interactions necessary to create spherical particles, recruiting the viral Env proteins, and packaging the genomic RNA via direct interactions with the RNA packaging sequence (Psi). Gag-Pol polyprotein may regulate its own translation, by the binding genomic RNA in the 5'-UTR. At low concentration, the polyprotein would promote translation, whereas at high concentration, the polyprotein would encapsidate genomic RNA and then shut off translation.
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UniProt ID | ||||||
EC Number |
EC 2.7.7.49
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Sequence |
PISPIETVPVKLKPGMDGPKVKQWPLTEEKIKALVEICTEMEKEGKISKIGPENPYNTPV
FAIKKKDSTKWRKLVDFRELNKRTQDFWEVQLGIPHPAGLKKKKSVTVLDVGDAYFSVPL DEDFRKYTAFTIPSINNETPGIRYQYNVLPQGWKGSPAIFQSSMTKILEPFKKQNPDIVI YQYMDDLYVGSDLEIGQHRTKIEELRQHLLRWGLTTPDKKHQKEPPFLWMGYELHPDKWT VQPIVLPEKDSWTVNDIQKLVGKLNWASQIYPGIKVRQLCKLLRGTKALTEVIPLTEEAE LELAENREILKEPVHGVYYDPSKDLIAEIQKQGQGQWTYQIYQEPFKNLKTGKYARMRGA HTNDVKQLTEAVQKITTESIVIWGKTPKFKLPIQKETWETWWTEYWQATWIPEWEFVNTP PLVKLWYQLEKEPIVGAETFYVDGAANRETKLGKAGYVTNKGRQKVVPLTNTTNQKTELQ AIYLALQDSGLEVNIVTDSQYALGIIQAQPDKSESELVNQIIEQLIKKEKVYLAWVPAHK GIGGNEQVDKLVSAGIRKIL Click to Show/Hide
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Drugs and Modes of Action | Top | |||||
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Approved Drug(s) | [+] 16 Approved Drugs | + | ||||
1 | Abacavir | Drug Info | Approved | Human immunodeficiency virus infection | [3] | |
2 | Bictegravir, emtricitabine and tenofovir alafenamide | Drug Info | Approved | Human immunodeficiency virus infection | [4] | |
3 | Delavirdine | Drug Info | Approved | Human immunodeficiency virus infection | [5] | |
4 | Didanosine | Drug Info | Approved | Human immunodeficiency virus infection | [1], [6] | |
5 | Efavirenz | Drug Info | Approved | Human immunodeficiency virus infection | [5] | |
6 | Emtricitabine | Drug Info | Approved | Human immunodeficiency virus infection | [1], [7], [8] | |
7 | Etravirine | Drug Info | Approved | Human immunodeficiency virus-1 infection | [9], [10] | |
8 | GS-7340 | Drug Info | Approved | Hepatitis B virus infection | [11] | |
9 | Lamivudine | Drug Info | Approved | Chronic HBV infection | [1] | |
10 | MK-1439 | Drug Info | Approved | Human immunodeficiency virus infection | [4] | |
11 | Nevirapine | Drug Info | Approved | Human immunodeficiency virus infection | [5] | |
12 | Rilpivirine | Drug Info | Approved | Human immunodeficiency virus infection | [12] | |
13 | Sorivudine | Drug Info | Approved | Virus infection | [13] | |
14 | Tenofovir | Drug Info | Approved | Human immunodeficiency virus infection | [14] | |
15 | Tenofovir disoproxil fumarate | Drug Info | Approved | Discovery agent | [13] | |
16 | Zidovudine | Drug Info | Approved | Human immunodeficiency virus infection | [15], [1] | |
Clinical Trial Drug(s) | [+] 28 Clinical Trial Drugs | + | ||||
1 | Epigallocatechin gallate | Drug Info | Phase 3 | Hepatic fibrosis | [17], [18], [19], [20] | |
2 | Glyminox | Drug Info | Phase 3 | Sexually transmitted infection | [21] | |
3 | VM-1500 | Drug Info | Phase 2/3 | Human immunodeficiency virus infection | [22] | |
4 | Alovudine | Drug Info | Phase 2 | Breast cancer | [23] | |
5 | Amdoxovir | Drug Info | Phase 2 | Hepatitis B virus infection | [24] | |
6 | BILR-355 | Drug Info | Phase 2 | Human immunodeficiency virus infection | [25] | |
7 | EMIVIRINE | Drug Info | Phase 2 | Human immunodeficiency virus infection | [26] | |
8 | F4co vaccine | Drug Info | Phase 2 | Human immunodeficiency virus infection | [27], [28] | |
9 | IDX899 | Drug Info | Phase 2 | Human immunodeficiency virus infection | [29] | |
10 | L-697,661 | Drug Info | Phase 2 | Human immunodeficiency virus infection | [30] | |
11 | Lersivirine | Drug Info | Phase 2 | Human immunodeficiency virus infection | [31] | |
12 | Lexipafant | Drug Info | Phase 2 | Nerve injury | [32] | |
13 | OBP-601 | Drug Info | Phase 2 | Human immunodeficiency virus-1 infection | [33] | |
14 | RALURIDINE | Drug Info | Phase 2 | Human immunodeficiency virus infection | [34], [35] | |
15 | Dapivirine | Drug Info | Phase 1/2 | Human immunodeficiency virus infection | [9] | |
16 | TRICIRIBINE | Drug Info | Phase 1/2 | Solid tumour/cancer | [37], [38] | |
17 | Ad35-GRIN/ENV | Drug Info | Phase 1 | Human immunodeficiency virus infection | [42] | |
18 | AIC-292 | Drug Info | Phase 1 | Human immunodeficiency virus infection | [43] | |
19 | ATEVIRDINE | Drug Info | Phase 1 | Human immunodeficiency virus infection | [44] | |
20 | CALANOLIDE A | Drug Info | Phase 1 | Mycobacterium infection | [45] | |
21 | Capravirine | Drug Info | Phase 1 | Human immunodeficiency virus infection | [46] | |
22 | CMX-157 | Drug Info | Phase 1 | Human immunodeficiency virus infection | [47] | |
23 | GW-695634 | Drug Info | Phase 1 | Human immunodeficiency virus infection | [48] | |
24 | KM-023 | Drug Info | Phase 1 | Human immunodeficiency virus infection | [49] | |
25 | MK-6186 | Drug Info | Phase 1 | Human immunodeficiency virus infection | [50] | |
26 | PT-112 | Drug Info | Phase 1 | Solid tumour/cancer | [51] | |
27 | TROVIRDINE HYDROCHLORIDE | Drug Info | Phase 1 | Human immunodeficiency virus infection | [52] | |
28 | UC-781 | Drug Info | Phase 1 | Human immunodeficiency virus infection | [53], [54] | |
Discontinued Drug(s) | [+] 31 Discontinued Drugs | + | ||||
1 | AZT-P-DDI | Drug Info | Discontinued in Phase 2 | Human immunodeficiency virus infection | [57] | |
2 | DMP-961 | Drug Info | Discontinued in Phase 2 | Human immunodeficiency virus infection | [58] | |
3 | Elvucitabine | Drug Info | Discontinued in Phase 2 | Human immunodeficiency virus infection | [59] | |
4 | FOZIVUDINE TIDOXIL | Drug Info | Discontinued in Phase 2 | Human immunodeficiency virus infection | [60] | |
5 | L-696229 | Drug Info | Discontinued in Phase 2 | Human immunodeficiency virus infection | [61] | |
6 | Lodenosine | Drug Info | Discontinued in Phase 2 | Human immunodeficiency virus infection | [62] | |
7 | Loviride | Drug Info | Discontinued in Phase 2 | Human immunodeficiency virus infection | [63] | |
8 | R-18893 | Drug Info | Discontinued in Phase 2 | Human immunodeficiency virus infection | [64] | |
9 | DPC-082 | Drug Info | Discontinued in Phase 1 | Human immunodeficiency virus infection | [66] | |
10 | L-697639 | Drug Info | Discontinued in Phase 1 | Human immunodeficiency virus infection | [67] | |
11 | PNU-142721 | Drug Info | Discontinued in Phase 1 | Human immunodeficiency virus infection | [68] | |
12 | R-82150 | Drug Info | Discontinued in Phase 1 | Human immunodeficiency virus infection | [69] | |
13 | A-79296 | Drug Info | Terminated | Herpes simplex virus infection | [71] | |
14 | ANX-201 | Drug Info | Terminated | Cytomegalovirus infection | [72] | |
15 | BAY-Z-4305 | Drug Info | Terminated | Human immunodeficiency virus-1 infection | [73] | |
16 | BEA-005 | Drug Info | Terminated | Cytomegalovirus infection | [74] | |
17 | C-AFG | Drug Info | Terminated | Virus infection | [75] | |
18 | DMP-963 | Drug Info | Terminated | Human immunodeficiency virus infection | [76] | |
19 | DPC-A78277 | Drug Info | Terminated | Human immunodeficiency virus infection | [77] | |
20 | GS-9148 | Drug Info | Terminated | Human immunodeficiency virus infection | [78] | |
21 | MEN-10690 | Drug Info | Terminated | Human immunodeficiency virus-1 infection | [79] | |
22 | MEN-10880 | Drug Info | Terminated | Human immunodeficiency virus-1 infection | [80] | |
23 | MEN-10979 | Drug Info | Terminated | Human immunodeficiency virus-1 infection | [81] | |
24 | MIV-170 | Drug Info | Terminated | Human immunodeficiency virus infection | [82] | |
25 | MSC-204 | Drug Info | Terminated | Human immunodeficiency virus infection | [83] | |
26 | Navuridine | Drug Info | Terminated | Human immunodeficiency virus infection | [84] | |
27 | RDEA-427 | Drug Info | Terminated | Human immunodeficiency virus infection | [85] | |
28 | RDEA-640 | Drug Info | Terminated | Human immunodeficiency virus infection | [85] | |
29 | SPD-756 | Drug Info | Terminated | Human immunodeficiency virus infection | [86] | |
30 | UC-38 | Drug Info | Terminated | Human immunodeficiency virus infection | [87] | |
31 | UC-84 | Drug Info | Terminated | Human immunodeficiency virus infection | [88] | |
Mode of Action | [+] 2 Modes of Action | + | ||||
Inhibitor | [+] 144 Inhibitor drugs | + | ||||
1 | Abacavir | Drug Info | [89] | |||
2 | Bictegravir, emtricitabine and tenofovir alafenamide | Drug Info | [4] | |||
3 | Didanosine | Drug Info | [91] | |||
4 | GS-7340 | Drug Info | [11] | |||
5 | MK-1439 | Drug Info | [4], [92] | |||
6 | Rilpivirine | Drug Info | [9] | |||
7 | Tenofovir | Drug Info | [95] | |||
8 | Zidovudine | Drug Info | [95] | |||
9 | Epigallocatechin gallate | Drug Info | [97] | |||
10 | Glyminox | Drug Info | [98] | |||
11 | VM-1500 | Drug Info | [99] | |||
12 | BILR-355 | Drug Info | [13], [102] | |||
13 | Lersivirine | Drug Info | [107] | |||
14 | Lexipafant | Drug Info | [9] | |||
15 | OBP-601 | Drug Info | [108] | |||
16 | RALURIDINE | Drug Info | [13], [109] | |||
17 | Dapivirine | Drug Info | [9] | |||
18 | TRICIRIBINE | Drug Info | [110] | |||
19 | AIC-292 | Drug Info | [112] | |||
20 | CALANOLIDE A | Drug Info | [114] | |||
21 | Capravirine | Drug Info | [115] | |||
22 | CMX-157 | Drug Info | [116] | |||
23 | GW-695634 | Drug Info | [117] | |||
24 | KM-023 | Drug Info | [118] | |||
25 | MK-6186 | Drug Info | [119] | |||
26 | PT-112 | Drug Info | [120] | |||
27 | PT-302 | Drug Info | [121] | |||
28 | UC-781 | Drug Info | [123] | |||
29 | AZT-P-DDI | Drug Info | [13], [124] | |||
30 | DMP-961 | Drug Info | [13], [125] | |||
31 | FOZIVUDINE TIDOXIL | Drug Info | [13], [127] | |||
32 | L-696229 | Drug Info | [13], [128] | |||
33 | Lodenosine | Drug Info | [129] | |||
34 | Loviride | Drug Info | [130] | |||
35 | DPC-082 | Drug Info | [13], [132] | |||
36 | L-697639 | Drug Info | [133] | |||
37 | LY-73497 | Drug Info | [121] | |||
38 | PNU-142721 | Drug Info | [134] | |||
39 | BAY-Z-4305 | Drug Info | [138] | |||
40 | DMP-963 | Drug Info | [13], [125] | |||
41 | DPC-A78277 | Drug Info | [141] | |||
42 | GS-9148 | Drug Info | [142] | |||
43 | MIV-170 | Drug Info | [145] | |||
44 | Navuridine | Drug Info | [147] | |||
45 | RDEA-427 | Drug Info | [148] | |||
46 | RDEA-640 | Drug Info | [149] | |||
47 | SPD-756 | Drug Info | [150] | |||
48 | 1-(1-Phenyl-propyl)-3-thiazol-2-yl-thiourea | Drug Info | [153] | |||
49 | 1-(2-Furan-2-yl-ethyl)-3-thiazol-2-yl-thiourea | Drug Info | [121] | |||
50 | 1-(2-Phenoxy-ethyl)-3-thiazol-2-yl-thiourea | Drug Info | [153] | |||
51 | 1-(2-Phenyl-propyl)-3-thiazol-2-yl-thiourea | Drug Info | [121] | |||
52 | 1-(3-Phenyl-propyl)-3-thiazol-2-yl-thiourea | Drug Info | [121] | |||
53 | 1-(4-Butyl-thiazol-2-yl)-3-phenethyl-thiourea | Drug Info | [121] | |||
54 | 1-(4-Cyano-thiazol-2-yl)-3-phenethyl-thiourea | Drug Info | [121] | |||
55 | 1-Adamantan-1-ylmethyl-3-thiazol-2-yl-thiourea | Drug Info | [153] | |||
56 | 1-Benzenesulfonyl-2-nitro-benzene | Drug Info | [154] | |||
57 | 1-Benzothiazol-2-yl-3-phenethyl-thiourea | Drug Info | [121] | |||
58 | 1-Benzyl-3-thiazol-2-yl-thiourea | Drug Info | [121] | |||
59 | 1-Furan-2-ylmethyl-3-thiazol-2-yl-thiourea | Drug Info | [153] | |||
60 | 1-nitro-2-(2-nitrophenylsulfonyl)benzene | Drug Info | [154] | |||
61 | 1-Thiazol-2-yl-3-(2-p-tolyl-ethyl)-thiourea | Drug Info | [153] | |||
62 | 10-Allyl-10H-dibenzo[b,f][1,4]oxazepin-11-one | Drug Info | [155] | |||
63 | 10-Ethyl-10H-dibenzo[b,f][1,4]oxazepin-11-one | Drug Info | [155] | |||
64 | 10-Isopropyl-10H-dibenzo[b,f][1,4]oxazepin-11-one | Drug Info | [155] | |||
65 | 10-Propyl-10H-dibenzo[b,f][1,4]oxazepin-11-one | Drug Info | [155] | |||
66 | 10-Propyl-10H-dibenzo[b,f][1,4]thiazepin-11-one | Drug Info | [155] | |||
67 | 2',3'-ddATP | Drug Info | [156] | |||
68 | 2'-3'-dideoxy-7-deaza-guaninetriphosphate | Drug Info | [156] | |||
69 | 2'-deoxythymidine triphosphate | Drug Info | [156] | |||
70 | 2-Amino-6-(2-chloro-phenylsulfanyl)-benzonitrile | Drug Info | [154] | |||
71 | 2-Amino-6-(2-cyano-benzenesulfinyl)-benzonitrile | Drug Info | [154] | |||
72 | 2-Amino-6-(2-cyano-benzenesulfonyl)-benzonitrile | Drug Info | [154] | |||
73 | 2-Amino-6-(2-cyano-phenylsulfanyl)-benzonitrile | Drug Info | [154] | |||
74 | 2-Amino-6-(3-bromo-benzenesulfinyl)-benzonitrile | Drug Info | [154] | |||
75 | 2-Amino-6-(3-bromo-phenylsulfanyl)-benzonitrile | Drug Info | [154] | |||
76 | 2-Amino-6-(3-chloro-benzenesulfonyl)-benzonitrile | Drug Info | [154] | |||
77 | 2-Amino-6-(3-chloro-phenylsulfanyl)-benzonitrile | Drug Info | [154] | |||
78 | 2-Amino-6-(3-cyano-benzenesulfonyl)-benzonitrile | Drug Info | [154] | |||
79 | 2-Amino-6-(3-cyano-phenylsulfanyl)-benzonitrile | Drug Info | [154] | |||
80 | 2-Amino-6-(3-fluoro-phenylsulfanyl)-benzonitrile | Drug Info | [154] | |||
81 | 2-Amino-6-(3-methoxy-phenylsulfanyl)-benzonitrile | Drug Info | [154] | |||
82 | 2-Amino-6-(4-chloro-phenylsulfanyl)-benzonitrile | Drug Info | [154] | |||
83 | 2-Amino-6-(naphthalene-1-sulfonyl)-benzonitrile | Drug Info | [154] | |||
84 | 2-Amino-6-(naphthalene-2-sulfonyl)-benzonitrile | Drug Info | [154] | |||
85 | 2-Amino-6-(toluene-2-sulfonyl)-benzonitrile | Drug Info | [154] | |||
86 | 2-Amino-6-(toluene-3-sulfinyl)-benzonitrile | Drug Info | [154] | |||
87 | 2-Amino-6-(toluene-3-sulfonyl)-benzonitrile | Drug Info | [154] | |||
88 | 2-Amino-6-(toluene-4-sulfonyl)-benzonitrile | Drug Info | [154] | |||
89 | 2-Amino-6-m-tolylsulfanyl-benzonitrile | Drug Info | [154] | |||
90 | 2-Amino-6-phenylsulfanyl-benzonitrile | Drug Info | [154] | |||
91 | 2-Benzylsulfanyl-6-chloro-pyrimidin-4-ylamine | Drug Info | [157] | |||
92 | 3'thiacytidine | Drug Info | [158] | |||
93 | 6-Benzyl-2-cyclohexylsulfanyl-3H-pyrimidin-4-one | Drug Info | [159] | |||
94 | 6-Benzyl-2-isobutylsulfanyl-3H-pyrimidin-4-one | Drug Info | [159] | |||
95 | Benzimidazole 5-carboxamide | Drug Info | [9] | |||
96 | CORILAGIN | Drug Info | [160] | |||
97 | Deoxyfluorothymidine | Drug Info | [158] | |||
98 | Dihydropyrone | Drug Info | [9] | |||
99 | Ethyl 1-[(1H-benzimidazol-5(6)-yl)sulfonyl]-1H-pyrrole-2-carboxylate | Drug Info | [162] | |||
100 | Ethyl 1-[(1H-benzotriazol-5(6)-yl)sulfonyl]-1H-pyrrole-2-carboxylate | Drug Info | [162] | |||
101 | HI-172 | Drug Info | [163] | |||
102 | HI-240 | Drug Info | [164] | |||
103 | HI-241 | Drug Info | [165] | |||
104 | HI-242 | Drug Info | [165] | |||
105 | HI-244 | Drug Info | [153] | |||
106 | HI-281 | Drug Info | [163] | |||
107 | HI-443 | Drug Info | [164] | |||
108 | HI-445 | Drug Info | [163] | |||
109 | Indole N -acetamide | Drug Info | [9] | |||
110 | ISODISPAR B | Drug Info | [166] | |||
111 | NSC-380292 | Drug Info | [167] | |||
112 | NSC-625487 | Drug Info | [13], [168] | |||
113 | PT-101 | Drug Info | [121] | |||
114 | PT-102 | Drug Info | [165] | |||
115 | PT-103 | Drug Info | [121] | |||
116 | PT-104 | Drug Info | [120] | |||
117 | PT-106 | Drug Info | [121] | |||
118 | PT-108 | Drug Info | [121] | |||
119 | PT-109 | Drug Info | [120] | |||
120 | PT-110 | Drug Info | [120] | |||
121 | PT-113 | Drug Info | [120] | |||
122 | PT-114 | Drug Info | [120] | |||
123 | PT-115 | Drug Info | [120] | |||
124 | PT-306 | Drug Info | [121] | |||
125 | PT-307 | Drug Info | [121] | |||
126 | PT-308 | Drug Info | [121] | |||
127 | PT-309 | Drug Info | [121] | |||
128 | PT-310 | Drug Info | [121] | |||
129 | PT-311 | Drug Info | [121] | |||
130 | PT-312 | Drug Info | [121] | |||
131 | PT-313 | Drug Info | [121] | |||
132 | PT-314 | Drug Info | [121] | |||
133 | PT-315 | Drug Info | [121] | |||
134 | PT-316 | Drug Info | [121] | |||
135 | PT-319 | Drug Info | [121] | |||
136 | PT-320 | Drug Info | [121] | |||
137 | PT-322 | Drug Info | [121] | |||
138 | R-87027 | Drug Info | [169] | |||
139 | RTI-20 | Drug Info | [170] | |||
140 | Tetrahydroimidazo[4,5,1-jk]-[1,4]benzodiazepin-2(1H)-one | Drug Info | [171] | |||
141 | UK-129485 | Drug Info | [173] | |||
142 | [(40-OH) MeLeu]4-CsA derivatives | Drug Info | [174] | |||
143 | [(40-OH)MeLeu]4-Cyclosporin A | Drug Info | [174] | |||
144 | [(D)MeSer]3-[(40-OH) MeLeu]4-Cyclosporin A | Drug Info | [174] | |||
Modulator | [+] 30 Modulator drugs | + | ||||
1 | Delavirdine | Drug Info | [90] | |||
2 | Efavirenz | Drug Info | [90] | |||
3 | Emtricitabine | Drug Info | [7], [8] | |||
4 | Etravirine | Drug Info | [10] | |||
5 | Lamivudine | Drug Info | [90] | |||
6 | Nevirapine | Drug Info | [93] | |||
7 | Sorivudine | Drug Info | [1], [94] | |||
8 | Tenofovir disoproxil fumarate | Drug Info | [7], [96] | |||
9 | Alovudine | Drug Info | [100] | |||
10 | Amdoxovir | Drug Info | [101] | |||
11 | EMIVIRINE | Drug Info | [103] | |||
12 | IDX899 | Drug Info | [105] | |||
13 | L-697,661 | Drug Info | [106] | |||
14 | ATEVIRDINE | Drug Info | [113] | |||
15 | TROVIRDINE HYDROCHLORIDE | Drug Info | [122] | |||
16 | Elvucitabine | Drug Info | [126] | |||
17 | R-18893 | Drug Info | [131] | |||
18 | R-82150 | Drug Info | [135] | |||
19 | A-79296 | Drug Info | [136] | |||
20 | ANX-201 | Drug Info | [137] | |||
21 | BEA-005 | Drug Info | [139] | |||
22 | C-AFG | Drug Info | [140] | |||
23 | MEN-10690 | Drug Info | [143] | |||
24 | MEN-10880 | Drug Info | [143] | |||
25 | MEN-10979 | Drug Info | [144] | |||
26 | MSC-204 | Drug Info | [146] | |||
27 | UC-38 | Drug Info | [151] | |||
28 | UC-84 | Drug Info | [152] | |||
29 | E-EBU-dM | Drug Info | [161] | |||
30 | TNK-651 | Drug Info | [172] |
Drug Binding Sites of Target | Top | |||||
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Ligand Name: 2'-deoxythymidine triphosphate | Ligand Info | |||||
Structure Description | STRUCTURE OF A CATALYTIC COMPLEX OF HIV-1 REVERSE TRANSCRIPTASE: IMPLICATIONS FOR NUCLEOSIDE ANALOG DRUG RESISTANCE | PDB:1RTD | ||||
Method | X-ray diffraction | Resolution | 3.20 Å | Mutation | Yes | [175] |
PDB Sequence |
KISPIETVPV
10 KLKPGMDGPK20 VKQWPLTEEK30 IKALVEICTE40 MEKEGKISKI50 GPENPYNTPV 60 FAIKKKDSTK70 WRKLVDFREL80 NKRTQDFWEV90 QLGIPHPAGL100 KKKKSVTVLD 110 VGDAYFSVPL120 DEDFRKYTAF130 TIPSINNETP140 GIRYQYNVLP150 QGWKGSPAIF 160 QSSMTKILEP170 FRKQNPDIVI180 YQYMDDLYVG190 SDLEIGQHRT200 KIEELRQHLL 210 RWGLTTPDKK220 HQKEPPFLWM230 GYELHPDKWT240 VQPIVLPEKD250 SWTVNDICKL 260 VGKLNWASQI270 YPGIKVRQLC280 KLLRGTKALT290 EVIPLTEEAE300 LELAENREIL 310 KEPVHGVYYD320 PSKDLIAEIQ330 KQGQGQWTYQ340 IYQEPFKNLK350 TGKYARMRGA 360 HTNDVKQLTE370 AVQKITTESI380 VIWGKTPKFK390 LPIQKETWET400 WWTEYWQATW 410 IPEWEFVNTP420 PLVKLWYQLE430 KEPIVGAETF440 YVDGAANRET450 KLGKAGYVTN 460 KGRQKVVPLT470 DTTNQKTQLQ480 AIYLALQDSG490 LEVNIVTDSQ500 YALGIIQAQP 510 DESESELVNQ520 IIEQLIKKEK530 VYLAWVPAHK540 GIGGNEQVDK550 LVSA |
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Ligand Name: (2-Acetyl-5-methylanilino)(2,6-dibromophenyl)acetamide | Ligand Info | |||||
Structure Description | STRUCTURE OF HIV-1 REVERSE TRANSCRIPTASE IN A COMPLEX WITH THE NONNUCLEOSIDE INHIBITOR ALPHA-APA R 95845 AT 2.8 ANGSTROMS RESOLUTION | PDB:1HNI | ||||
Method | X-ray diffraction | Resolution | 2.80 Å | Mutation | No | [176] |
PDB Sequence |
PISPIETVPV
10 KLKPGMDGPK20 VKQWPLTEEK30 IKALVEICTE40 MEKEGKISKI50 GPENPYNTPV 60 FAIKKKDSTK70 WRKLVDFREL80 NKRTQDFWEV90 QLGIPHPAGL100 KKKKSVTVLD 110 VGDAYFSVPL120 DEDFRKYTAF130 TIPSINNETP140 GIRYQYNVLP150 QGWKGSPAIF 160 QSSMTKILEP170 FKKQNPDIVI180 YQYMDDLYVG190 SDLEIGQHRT200 KIEELRQHLL 210 RWGLTTPDKK220 HQKEPPFLWM230 GYELHPDKWT240 VQPIVLPEKD250 SWTVNDIQKL 260 VGKLNWASQI270 YPGIKVRQLS280 KLLRGTKALT290 EVIPLTEEAE300 LELAENREIL 310 KEPVHGVYYD320 PSKDLIAEIQ330 KQGQGQWTYQ340 IYQEPFKNLK350 TGKYARMRGA 360 HTNDVKQLTE370 AVQKITTESI380 VIWGKTPKFK390 LPIQKETWET400 WWTEYWQATW 410 IPEWEFVNTP420 PLVKLWYQLE430 KEPIVGAETF440 YVDGAANRET450 KLGKAGYVTN 460 KGRQKVVPLT470 NTTNQKTELQ480 AIYLALQDSG490 LEVNIVTDSQ500 YALGIIQAQP 510 DKSESELVNQ520 IIEQLIKKEK530 VYLAWVPAHK540 GIGGNEQVDK550 LVSAGIRK |
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Click to View More Binding Site Information of This Target with Different Ligands |
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-Related Models and Studies | Top | |||||
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Target Validation | ||||||
Target QSAR Model |
References | Top | |||||
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