Target Information
Target General Information | Top | |||||
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Target ID |
T92072
(Former ID: TTDS00186)
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Target Name |
Adenosine A1 receptor (ADORA1)
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Synonyms |
Adenosine receptor A1; A(1) adenosine receptor
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Gene Name |
ADORA1
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Target Type |
Successful target
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[1] | ||||
Disease | [+] 1 Target-related Diseases | + | ||||
1 | Orthostatic hypotension [ICD-11: BA21] | |||||
Function |
The activity of this receptor is mediated by G proteins which inhibit adenylyl cyclase. Receptor for adenosine.
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BioChemical Class |
GPCR rhodopsin
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UniProt ID | ||||||
Sequence |
MPPSISAFQAAYIGIEVLIALVSVPGNVLVIWAVKVNQALRDATFCFIVSLAVADVAVGA
LVIPLAILINIGPQTYFHTCLMVACPVLILTQSSILALLAIAVDRYLRVKIPLRYKMVVT PRRAAVAIAGCWILSFVVGLTPMFGWNNLSAVERAWAANGSMGEPVIKCEFEKVISMEYM VYFNFFVWVLPPLLLMVLIYLEVFYLIRKQLNKKVSASSGDPQKYYGKELKIAKSLALIL FLFALSWLPLHILNCITLFCPSCHKPSILTYIAIFLTHGNSAMNPIVYAFRIQKFRVTFL KIWNDHFRCQPAPPIDEDLPEERPDD Click to Show/Hide
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3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
ADReCS ID | BADD_A01328 ; BADD_A01334 | |||||
HIT2.0 ID | T35LKG |
Drugs and Modes of Action | Top | |||||
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Approved Drug(s) | [+] 1 Approved Drugs | + | ||||
1 | Caffeine | Drug Info | Approved | Orthostatic hypotension | [2], [3] | |
Clinical Trial Drug(s) | [+] 13 Clinical Trial Drugs | + | ||||
1 | Rolofylline | Drug Info | Phase 3 | Heart failure | [4], [5] | |
2 | AMP-579 | Drug Info | Phase 2 | Hyperlipidaemia | [6] | |
3 | Apaxifylline | Drug Info | Phase 2 | Cognitive impairment | [7] | |
4 | BAY 1067197 | Drug Info | Phase 2 | Heart failure | [8] | |
5 | Capadenoson | Drug Info | Phase 2 | Atrial fibrillation | [9] | |
6 | DTI-0009 | Drug Info | Phase 2 | Atrial fibrillation | [10] | |
7 | SELODENOSON | Drug Info | Phase 2 | Cardiac arrhythmias | [10] | |
8 | SLV320 | Drug Info | Phase 2 | Heart failure | [11], [12] | |
9 | Tonapofylline | Drug Info | Phase 2 | Acute and chronic heart failure | [13] | |
10 | INO-8875 | Drug Info | Phase 1/2 | Glaucoma/ocular hypertension | [14] | |
11 | AST-004 | Drug Info | Phase 1 | Stroke | [15] | |
12 | GS 9667 | Drug Info | Phase 1 | Hypertriglyceridemia | [16], [17] | |
13 | KF-17837 | Drug Info | Phase 1 | Parkinson disease | [18] | |
Discontinued Drug(s) | [+] 11 Discontinued Drugs | + | ||||
1 | CVT-124 | Drug Info | Discontinued in Phase 3 | Autoimmune diabetes | [19] | |
2 | N-0861 | Drug Info | Discontinued in Phase 3 | Cardiac disease | [20] | |
3 | Tecadenoson | Drug Info | Discontinued in Phase 3 | Cardiac arrhythmias | [21], [22] | |
4 | BRL-61063 | Drug Info | Discontinued in Phase 2 | Allergy | [23] | |
5 | FK-352 | Drug Info | Discontinued in Phase 2 | Hypertension | [24] | |
6 | FK-453 | Drug Info | Discontinued in Phase 2 | Renal failure | [25], [26] | |
7 | FK-838 | Drug Info | Discontinued in Phase 2 | Hypertension | [27] | |
8 | GW-493838 | Drug Info | Discontinued in Phase 2 | Neuropathic pain | [28] | |
9 | GR-79236 | Drug Info | Discontinued in Phase 1 | Diabetic complication | [29], [30] | |
10 | SDZ-WAG-994 | Drug Info | Discontinued in Phase 1 | Hypertension | [31] | |
11 | METHYLTHIOADENOSINE | Drug Info | Terminated | Multiple sclerosis | [33] | |
Preclinical Drug(s) | [+] 1 Preclinical Drugs | + | ||||
1 | BAY 60-6583 | Drug Info | Preclinical | Myocardial ischemia | [32] | |
Mode of Action | [+] 4 Modes of Action | + | ||||
Antagonist | [+] 42 Antagonist drugs | + | ||||
1 | Caffeine | Drug Info | [1], [34] | |||
2 | Rolofylline | Drug Info | [5] | |||
3 | Apaxifylline | Drug Info | [36] | |||
4 | SLV320 | Drug Info | [12] | |||
5 | CVT-124 | Drug Info | [50], [51] | |||
6 | N-0861 | Drug Info | [52] | |||
7 | FK-352 | Drug Info | [54] | |||
8 | (E)-8-(3-chlorostyryl)-caffeine | Drug Info | [66] | |||
9 | 4-Ethoxy-7-((E)-styryl)-furo[3,2-g]chromen-5-one | Drug Info | [97] | |||
10 | 8-cyclopentyltheophylline | Drug Info | [102] | |||
11 | AS100 | Drug Info | [108] | |||
12 | AS70 | Drug Info | [108] | |||
13 | AS99 | Drug Info | [108] | |||
14 | ATL802 | Drug Info | [109] | |||
15 | CPFPX | Drug Info | [112] | |||
16 | flavone | Drug Info | [97] | |||
17 | FR194921 | Drug Info | [116] | |||
18 | isobutylmethylxanthine | Drug Info | [122], [123] | |||
19 | KF26777 | Drug Info | [125] | |||
20 | MRE 2029F20 | Drug Info | [130] | |||
21 | MRE 3008F20 | Drug Info | [111] | |||
22 | MRS1041 | Drug Info | [97] | |||
23 | MRS1042 | Drug Info | [97] | |||
24 | MRS1062 | Drug Info | [97] | |||
25 | MRS1065 | Drug Info | [97] | |||
26 | MRS1084 | Drug Info | [97] | |||
27 | MRS1086 | Drug Info | [97] | |||
28 | MRS1093 | Drug Info | [97] | |||
29 | MRS1132 | Drug Info | [97] | |||
30 | MRS1191 | Drug Info | [127] | |||
31 | MRS1523 | Drug Info | [127] | |||
32 | MRS923 | Drug Info | [97] | |||
33 | MRS928 | Drug Info | [97] | |||
34 | PSB-10 | Drug Info | [140] | |||
35 | PSB-11 | Drug Info | [140] | |||
36 | PSB36 | Drug Info | [141] | |||
37 | PSB603 | Drug Info | [139] | |||
38 | sakuranetin | Drug Info | [97] | |||
39 | VUF5574 | Drug Info | [147] | |||
40 | WRC-0571 | Drug Info | [148] | |||
41 | xanthine amine congener | Drug Info | [122] | |||
42 | [3H]DPCPX | Drug Info | [149] | |||
Modulator | [+] 7 Modulator drugs | + | ||||
1 | AMP-579 | Drug Info | [35] | |||
2 | BAY 1067197 | Drug Info | [37] | |||
3 | FK-453 | Drug Info | [55] | |||
4 | FK-838 | Drug Info | [56] | |||
5 | GW-493838 | Drug Info | [38] | |||
6 | L-97-1 intravenous | Drug Info | [127] | |||
7 | Paeoniflorin | Drug Info | [127] | |||
Agonist | [+] 23 Agonist drugs | + | ||||
1 | Capadenoson | Drug Info | [38] | |||
2 | DTI-0009 | Drug Info | [39], [40] | |||
3 | SELODENOSON | Drug Info | [39], [40], [41] | |||
4 | INO-8875 | Drug Info | [44] | |||
5 | AST-004 | Drug Info | [45] | |||
6 | GS 9667 | Drug Info | [46] | |||
7 | PMID27387065-Compound-6 | Drug Info | [49] | |||
8 | Tecadenoson | Drug Info | [50], [51] | |||
9 | GR-79236 | Drug Info | [57] | |||
10 | SDZ-WAG-994 | Drug Info | [58] | |||
11 | BAY 60-6583 | Drug Info | [59] | |||
12 | (R,S)-PHPNECA | Drug Info | [67] | |||
13 | (S)-PIA | Drug Info | [68] | |||
14 | 2-chloroadenosine | Drug Info | [90] | |||
15 | 5-Cl-5-deoxy-(+/-)-ENBA | Drug Info | [75] | |||
16 | CP608,039 | Drug Info | [111] | |||
17 | LUF5831 | Drug Info | [129] | |||
18 | MRS5151 | Drug Info | [131] | |||
19 | N(6)-cyclohexyladenosine | Drug Info | [132] | |||
20 | PENECA | Drug Info | [67] | |||
21 | TCPA | Drug Info | [144] | |||
22 | [3H]CCPA | Drug Info | [142], [73] | |||
23 | [3H]HEMADO | Drug Info | [150] | |||
Inhibitor | [+] 239 Inhibitor drugs | + | ||||
1 | Tonapofylline | Drug Info | [42], [43] | |||
2 | KF-17837 | Drug Info | [47] | |||
3 | SCH-442416 | Drug Info | [48] | |||
4 | BRL-61063 | Drug Info | [53] | |||
5 | ARISTEROMYCIN | Drug Info | [60] | |||
6 | METHYLTHIOADENOSINE | Drug Info | [61] | |||
7 | METRIFUDIL | Drug Info | [62] | |||
8 | ZM-241385 | Drug Info | [63] | |||
9 | (1-Phenyl-propyl)-(9-phenyl-9H-purin-6-yl)-amine | Drug Info | [64] | |||
10 | (1H-Imidazo[4,5-c]quinolin-4-yl)-phenyl-amine HCl | Drug Info | [65] | |||
11 | (2-Chloro-9-methyl-9H-purin-6-yl)-phenyl-amine | Drug Info | [64] | |||
12 | (9-Methyl-9H-purin-6-yl)-phenyl-amine | Drug Info | [64] | |||
13 | 1,3-Diallyl-3,7-dihydro-purine-2,6-dione | Drug Info | [69] | |||
14 | 1,3-Diethyl-3,7-dihydro-purine-2,6-dione | Drug Info | [69] | |||
15 | 1,3-Diisobutyl-3,7-dihydro-purine-2,6-dione | Drug Info | [69] | |||
16 | 1,3-Dipropyl-3,7-dihydro-purine-2,6-dione | Drug Info | [69] | |||
17 | 1-Butyl-8-phenyl-3,7-dihydro-purine-2,6-dione | Drug Info | [70] | |||
18 | 1-Methyl-8-phenyl-3,7-dihydro-purine-2,6-dione | Drug Info | [71] | |||
19 | 1-METHYLXANTHINE | Drug Info | [69] | |||
20 | 1-Propyl-3,7-dihydro-purine-2,6-dione | Drug Info | [72] | |||
21 | 1H-Imidazo[4,5-c]quinolin-4-ylamine HCl | Drug Info | [65] | |||
22 | 2'-Me-tecadenoson | Drug Info | [73] | |||
23 | 2,4-Dichloro-N-(4-phenyl-thiazol-2-yl)-benzamide | Drug Info | [74] | |||
24 | 2,5'-dichloro-5'-deoxy-N6-cyclopentyladenosine | Drug Info | [75] | |||
25 | 2,6,8-triphenyl-9H-purine | Drug Info | [76] | |||
26 | 2,6-bis(4-tolyl)-9H-purine | Drug Info | [76] | |||
27 | 2,6-dimethyl-8-ethyl-1-deazapurine | Drug Info | [77] | |||
28 | 2,6-diphenyl-1-deazapurine | Drug Info | [77] | |||
29 | 2,6-diphenyl-8-(1-ethylpropyl)-1-deazapurine | Drug Info | [77] | |||
30 | 2,6-diphenyl-8-ethyl-1-deazapurine | Drug Info | [77] | |||
31 | 2,6-diphenyl-8-methyl-1-deazapurine | Drug Info | [77] | |||
32 | 2,6-diphenyl-8-tButyl-1-deazapurine | Drug Info | [77] | |||
33 | 2,6-diphenyl-9H-purine | Drug Info | [76] | |||
34 | 2,6-Diphenyl-pyrimidin-4-ylamine | Drug Info | [78] | |||
35 | 2,6-dphenyl-8-propyl-1-deazapurine | Drug Info | [77] | |||
36 | 2-(1H-benzo[d]imidazol-2-yl)quinoxaline | Drug Info | [79] | |||
37 | 2-(2''-indolylethyloxy)adenosine | Drug Info | [80] | |||
38 | 2-(2-furyl)-6-(1H-pyrazol-1-yl)pyrimidin-4-amine | Drug Info | [81] | |||
39 | 2-(3''(5''-chloro-indolyl)ethyloxy)adenosine | Drug Info | [80] | |||
40 | 2-(3''(7''-bromo-indolyl)ethyloxy)adenosine | Drug Info | [80] | |||
41 | 2-(3''-(4''-bromo-indolyl)ethyloxy)adenosine | Drug Info | [80] | |||
42 | 2-(3''-(5''-bromo-indolyl)ethyloxy)adenosine | Drug Info | [80] | |||
43 | 2-(3''-(5''-fluoro-indolyl)ethyloxy)adenosine | Drug Info | [80] | |||
44 | 2-(3''-(5''-hydroxyindolyl)ethyloxy)adenosine | Drug Info | [80] | |||
45 | 2-(3''-(5''-iodo-indolyl)ethyloxy)adenosine | Drug Info | [80] | |||
46 | 2-(3''-(5''-methoxy-indolyl)ethyloxy)adenosine | Drug Info | [80] | |||
47 | 2-(3''-(6''-bromo-indolyl)ethyloxy)adenosine | Drug Info | [80] | |||
48 | 2-(3''-(6''-chloro-indolyl)ethyloxy)adenosine | Drug Info | [80] | |||
49 | 2-(3''-indolylethyloxy)adenosine | Drug Info | [80] | |||
50 | 2-(3''-pyrrolylethyloxy)adenosine | Drug Info | [80] | |||
51 | 2-(4-chloro-1H-benzo[d]imidazol-2-yl)quinoxaline | Drug Info | [82] | |||
52 | 2-(4-chlorophenyl)-6-phenyl-9H-purine | Drug Info | [76] | |||
53 | 2-(4-ethylthiobenzimidazol-2-yl)quinoxaline | Drug Info | [82] | |||
54 | 2-(4-hydroxypent-1-yl)-N6-methoxyadenosine | Drug Info | [83] | |||
55 | 2-(4-methoxyphenyl)-6-phenyl-9H-purine | Drug Info | [76] | |||
56 | 2-(4-methyl-1H-benzo[d]imidazol-2-yl)quinoxaline | Drug Info | [79] | |||
57 | 2-(5-cyano-1-pent-1-ynyl)-N6-methoxyadenosine | Drug Info | [83] | |||
58 | 2-(6-amino-8-bromo-9H-purin-9-yl)ethanol | Drug Info | [84] | |||
59 | 2-(6-Cyclopentylamino-purin-9-yl)-ethanol | Drug Info | [64] | |||
60 | 2-(hex-1-ynyl)-N6-methoxyadenosine | Drug Info | [83] | |||
61 | 2-Amino-4,6-di-furan-2-yl-nicotinonitrile | Drug Info | [85] | |||
62 | 2-Amino-4,6-di-thiophen-2-yl-nicotinonitrile | Drug Info | [85] | |||
63 | 2-Amino-4,6-diphenyl-nicotinonitrile | Drug Info | [85] | |||
64 | 2-Amino-4,6-diphenyl-pyrimidin-5-carbonitrile | Drug Info | [78] | |||
65 | 2-Amino-4,6-diphenyl-pyrimidine | Drug Info | [78] | |||
66 | 2-Amino-4-furan-2-yl-6-phenyl-nicotinonitrile | Drug Info | [85] | |||
67 | 2-Amino-4-phenyl-6-thiophen-2-yl-nicotinonitrile | Drug Info | [85] | |||
68 | 2-Amino-6-furan-2-yl-4-phenyl-nicotinonitrile | Drug Info | [85] | |||
69 | 2-amino-6-phenyl-4-p-tolylnicotinonitrile | Drug Info | [86] | |||
70 | 2-Amino-6-phenyl-4-thiophen-2-yl-nicotinonitrile | Drug Info | [85] | |||
71 | 2-amino-N-benzyl-6-phenyl-9H-purine-9-carboxamide | Drug Info | [87] | |||
72 | 2-azido-N6-methyl-9-(beta-D-ribofuranosyl)adenine | Drug Info | [88] | |||
73 | 2-chloro-2'-C-methyl-tecadenoson | Drug Info | [73] | |||
74 | 2-chloro-4-(thiazol-2-yl)thieno[3,2-d]pyrimidine | Drug Info | [89] | |||
75 | 2-chloro-4-(thiophen-2-yl)thieno[3,2-d]pyrimidine | Drug Info | [89] | |||
76 | 2-Cyclopentyl-1H-imidazo[4,5-c]quinolin-4-ylamine | Drug Info | [65] | |||
77 | 2-ethyl-4-(furan-2-yl)thieno[3,2-d]pyrimidine | Drug Info | [89] | |||
78 | 2-ethyl-4-(furan-3-yl)thieno[3,2-d]pyrimidine | Drug Info | [89] | |||
79 | 2-ethyl-4-(pyridin-2-yl)thieno[3,2-d]pyrimidine | Drug Info | [89] | |||
80 | 2-ethyl-4-(thiazol-2-yl)thieno[3,2-d]pyrimidine | Drug Info | [89] | |||
81 | 2-ethyl-4-(thiophen-2-yl)thieno[3,2-d]pyrimidine | Drug Info | [89] | |||
82 | 2-ethynyl-N6-methoxyadenosine | Drug Info | [83] | |||
83 | 2-m-tolyl-2H-pyrazolo[3,4-c]quinolin-4(5H)-one | Drug Info | [91] | |||
84 | 2-m-tolyl-2H-pyrazolo[3,4-c]quinolin-4-amine | Drug Info | [91] | |||
85 | 2-p-tolyl-2H-pyrazolo[3,4-c]quinolin-4(5H)-one | Drug Info | [91] | |||
86 | 2-p-tolyl-2H-pyrazolo[3,4-c]quinolin-4-amine | Drug Info | [91] | |||
87 | 2-Phenyl-1H-imidazo[4,5-c]quinolin-4-ylamine | Drug Info | [65] | |||
88 | 2-phenyl-2H-pyrazolo[3,4-c]quinolin-4(5H)-one | Drug Info | [91] | |||
89 | 2-phenyl-2H-pyrazolo[3,4-c]quinolin-4-amine | Drug Info | [91] | |||
90 | 2-phenylpropoxyadenosine | Drug Info | [80] | |||
91 | 2-tolyl-6-phenyl-9H-purine | Drug Info | [76] | |||
92 | 2-[(4-acetylphenyl)ethynyl]-N6-methoxyadenosine | Drug Info | [83] | |||
93 | 2-[(4-fluorophenyl)ethynyl]-N6-methoxyadenosine | Drug Info | [83] | |||
94 | 3,4-Dichloro-N-(4-phenyl-thiazol-2-yl)-benzamide | Drug Info | [74] | |||
95 | 3-(3-chloro-1H-pyrazol-5-yl)quinoxalin-2(1H)-one | Drug Info | [79] | |||
96 | 3-Benzyl-7-methyl-[1,8]naphthyridin-4-ol | Drug Info | [92] | |||
97 | 3-Benzyl-7-methyl-[1,8]naphthyridine-4-thiol | Drug Info | [92] | |||
98 | 3-Chloro-N-(4-phenyl-thiazol-2-yl)-benzamide | Drug Info | [74] | |||
99 | 3-noradamantyl-1,3-dipropylxanthine | Drug Info | [93] | |||
100 | 4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one | Drug Info | [94] | |||
101 | 4-(ethylthio)-6-phenyl-1,3,5-triazin-2-amine | Drug Info | [86] | |||
102 | 4-(furan-2-yl)-7H-pyrrolo[2,3-d]pyrimidin-2-amine | Drug Info | [95] | |||
103 | 4-(furan-2-yl)thieno[3,2-d]pyrimidin-2-amine | Drug Info | [87] | |||
104 | 4-(thiazol-2-yl)thieno[3,2-d]pyrimidin-2-amine | Drug Info | [89] | |||
105 | 4-Amino-2,6-diphenyl-pyrimidine-5-carbonitrile | Drug Info | [78] | |||
106 | 4-Bromo-N-(4-phenyl-thiazol-2-yl)-benzamide | Drug Info | [74] | |||
107 | 4-Chloro-7-methyl-2-phenyl-[1,8]naphthyridine | Drug Info | [96] | |||
108 | 4-Chloro-N-(4-phenyl-thiazol-2-yl)-benzamide | Drug Info | [74] | |||
109 | 4-Methoxy-N-(3-phenyl-isoquinolin-1-yl)-benzamide | Drug Info | [74] | |||
110 | 4-Methyl-N-(4-phenyl-thiazol-2-yl)-benzamide | Drug Info | [74] | |||
111 | 4-Nitro-N-(4-phenyl-thiazol-2-yl)-benzamide | Drug Info | [74] | |||
112 | 4-tert-Butyl-N-(4-phenyl-thiazol-2-yl)-benzamide | Drug Info | [74] | |||
113 | 5,7-dibromo-9H-pyrido[3,4-b]indol-6-ol | Drug Info | [98] | |||
114 | 5,7-diphenyl-3H-imidazo[4,5-b]pyridin-2-ol | Drug Info | [77] | |||
115 | 6-(furan-2-yl)-9H-purin-2-amine | Drug Info | [95] | |||
116 | 6-ethylamino-2-(3''-indolyl)ethyloxy)adenosine | Drug Info | [80] | |||
117 | 6-guanidino-2-(3''-indolylethyloxy)adenosine | Drug Info | [80] | |||
118 | 7-(3,6,9,12-tetraoxatricos-22-enyl)theophylline | Drug Info | [99] | |||
119 | 7-Bromo-2-phenyl-[1,8]naphthyridin-4-ol | Drug Info | [100] | |||
120 | 7-Chloro-2-phenyl-[1,8]naphthyridin-4-ol | Drug Info | [100] | |||
121 | 7-Dimethylamino-2-phenyl-[1,8]naphthyridin-4-ol | Drug Info | [100] | |||
122 | 7-Methyl-2-propyl-[1,8]naphthyridin-4-ol | Drug Info | [100] | |||
123 | 8-Bromo-9-(2,3-dihydroxypropyl)-9H-adenine | Drug Info | [101] | |||
124 | 8-Bromo-9-(2-butyl)-9H-adenine | Drug Info | [101] | |||
125 | 8-Bromo-9-(2-hydroxypropyl)-9H-adenine | Drug Info | [101] | |||
126 | 8-Bromo-9-(3-hydroxypropyl)-9H-adenine | Drug Info | [101] | |||
127 | 8-Bromo-9-(but-3-enyl)-9H-adenine | Drug Info | [101] | |||
128 | 8-Bromo-9-(sec-butyl)-9H-adenine | Drug Info | [101] | |||
129 | 8-Bromo-9-cyclobutyl-9H-adenine | Drug Info | [101] | |||
130 | 8-Bromo-9-cyclohexyl-9H-adenine | Drug Info | [101] | |||
131 | 8-Bromo-9-cyclopentyl-9H-adenine | Drug Info | [101] | |||
132 | 8-Bromo-9-ethyl-9H-adenine | Drug Info | [101] | |||
133 | 8-bromo-9-isobutyl-9H-purin-6-amine | Drug Info | [84] | |||
134 | 8-Bromo-9-isopropyl-9H-adenine | Drug Info | [101] | |||
135 | 8-Bromo-9-methyl-9H-adenine | Drug Info | [101] | |||
136 | 8-Bromo-9-phenylethyl-9H-adenine | Drug Info | [101] | |||
137 | 8-Bromo-9-propyl-9H-adenine | Drug Info | [101] | |||
138 | 8-cyclohexyl-6-(4-tolyl)-2-phenyl-9H-purine | Drug Info | [76] | |||
139 | 8-PHENYL THEOPHYLLINE | Drug Info | [65] | |||
140 | 8-Phenyl-1-propyl-3,7-dihydro-purine-2,6-dione | Drug Info | [103] | |||
141 | 8-Phenyl-3,7-dihydro-purine-2,6-dione | Drug Info | [103] | |||
142 | 8-propyl-2,6-diphenyl-9H-purine | Drug Info | [76] | |||
143 | 9-(3-aminobenzyl)-6-(furan-2-yl)-9H-purin-2-amine | Drug Info | [87] | |||
144 | 9-(3-nitrobenzyl)-6-(furan-2-yl)-9H-purin-2-amine | Drug Info | [87] | |||
145 | 9-(4-nitrobenzyl)-6-(furan-2-yl)-9H-purin-2-amine | Drug Info | [87] | |||
146 | 9-Allyl-8-bromo-9H-adenine | Drug Info | [101] | |||
147 | 9-benzyl-6-(furan-2-yl)-9H-purin-2-amine | Drug Info | [87] | |||
148 | 9-Benzyl-8-bromo-9H-adenine | Drug Info | [101] | |||
149 | 9-Cyclobutyl-9H-adenine | Drug Info | [101] | |||
150 | 9-Cyclopentyl-9H-adenine | Drug Info | [64] | |||
151 | 9-Ethyl-8-phenylethynyl-9H-purin-6-ylamine | Drug Info | [104] | |||
152 | 9-Ethyl-9H-adenine | Drug Info | [101] | |||
153 | 9-Isopropyl-9H-adenine | Drug Info | [101] | |||
154 | 9-Methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine | Drug Info | [105] | |||
155 | 9-Methyl-9H-adenine | Drug Info | [61] | |||
156 | 9-Phenyl-9H-purin-6-ylamine | Drug Info | [64] | |||
157 | 9-Propyl-9H-adenine | Drug Info | [101] | |||
158 | A-987306 | Drug Info | [106] | |||
159 | Anthoptilide C | Drug Info | [107] | |||
160 | Cirsimarin | Drug Info | [110] | |||
161 | Cyclohexyl-(2-phenylsulfanyl-9H-purin-6-yl)-amine | Drug Info | [113] | |||
162 | Cyclohexyl-(9-ethyl-9H-purin-6-yl)-amine | Drug Info | [64] | |||
163 | Cyclohexyl-(9-methyl-9H-purin-6-yl)-amine | Drug Info | [64] | |||
164 | Cyclopentyl-(9-cyclopentyl-9H-purin-6-yl)-amine | Drug Info | [64] | |||
165 | Cyclopentyl-(9-ethyl-9H-purin-6-yl)-amine | Drug Info | [64] | |||
166 | Cyclopentyl-(9-methyl-9H-purin-6-yl)-amine | Drug Info | [64] | |||
167 | Cyclopentyl-(9-phenyl-9H-purin-6-yl)-amine | Drug Info | [64] | |||
168 | DEPX | Drug Info | [114] | |||
169 | Ethyl 5-benzoyl-4-phenylthiazol-2-ylcarbamate | Drug Info | [42] | |||
170 | FR-166124 | Drug Info | [115] | |||
171 | GNF-PF-2224 | Drug Info | [117], [118], [119], [120] | |||
172 | GNF-PF-2700 | Drug Info | [84] | |||
173 | Hexanoic Acid (2,6-diphenylpyrimidin-4-yl)amide | Drug Info | [121] | |||
174 | Isoguanosine | Drug Info | [124] | |||
175 | Kuanoniamine D | Drug Info | [126] | |||
176 | L-249313 | Drug Info | [47] | |||
177 | LUF-5417 | Drug Info | [42] | |||
178 | LUF-5433 | Drug Info | [42] | |||
179 | LUF-5735 | Drug Info | [121] | |||
180 | LUF-5737 | Drug Info | [121] | |||
181 | LUF-5764 | Drug Info | [121] | |||
182 | LUF-5767 | Drug Info | [121] | |||
183 | LUF-5816 | Drug Info | [77] | |||
184 | LUF-5853 | Drug Info | [78] | |||
185 | LUF-5956 | Drug Info | [76] | |||
186 | LUF-5957 | Drug Info | [76] | |||
187 | LUF-5962 | Drug Info | [76] | |||
188 | LUF-5978 | Drug Info | [77] | |||
189 | LUF-5980 | Drug Info | [77] | |||
190 | LUF-5981 | Drug Info | [77] | |||
191 | LUF-6258 | Drug Info | [128] | |||
192 | N*6*-Cyclohexyl-N*2*-ethyl-9H-purine-2,6-diamine | Drug Info | [113] | |||
193 | N*6*-Cyclohexyl-N*2*-phenyl-9H-purine-2,6-diamine | Drug Info | [113] | |||
194 | N*6*-Cyclooctyl-N*2*-phenyl-9H-purine-2,6-diamine | Drug Info | [113] | |||
195 | N-(2,6-diphenylpyrimidin-4-yl)-2-ethylbutyramide | Drug Info | [121] | |||
196 | N-(2,6-diphenylpyrimidin-4-yl)-3-methylbutyramide | Drug Info | [121] | |||
197 | N-(2,6-diphenylpyrimidin-4-yl)acetamide | Drug Info | [121] | |||
198 | N-(2,6-diphenylpyrimidin-4-yl)benzamide | Drug Info | [121] | |||
199 | N-(2,6-diphenylpyrimidin-4-yl)butyramide | Drug Info | [121] | |||
200 | N-(2,6-diphenylpyrimidin-4-yl)isobutyramide | Drug Info | [121] | |||
201 | N-(2,6-diphenylpyrimidin-4-yl)propionamide | Drug Info | [121] | |||
202 | N-(2-(furan-2-yl)-3,4'-bipyridin-6-yl)acetamide | Drug Info | [133] | |||
203 | N-(4,5-diphenylpyrimidin-2-yl)acetamide | Drug Info | [121] | |||
204 | N-(4,6-diphenylpyrimidin-2-yl)-2-ethylbutyramide | Drug Info | [121] | |||
205 | N-(4,6-diphenylpyrimidin-2-yl)-3-chlorobenzamide | Drug Info | [121] | |||
206 | N-(4,6-diphenylpyrimidin-2-yl)-3-methylbutyramide | Drug Info | [121] | |||
207 | N-(4,6-diphenylpyrimidin-2-yl)benzamide | Drug Info | [121] | |||
208 | N-(4,6-diphenylpyrimidin-2-yl)propionamide | Drug Info | [121] | |||
209 | N-(4-Phenyl-thiazol-2-yl)-benzamide | Drug Info | [74] | |||
210 | N-(5-Benzoyl-4-phenylthiazol-2-yl)benzamide | Drug Info | [42] | |||
211 | N6-((+/-)-endo-norborn-2-yl)adenosine | Drug Info | [75] | |||
212 | N6-CYCLOPENTYLADENOSINE | Drug Info | [73] | |||
213 | N6-methoxy-2-phenylethynyladenosine | Drug Info | [83] | |||
214 | N6-methoxy-2-[(2-pyridinyl)ethynyl]adenosine | Drug Info | [83] | |||
215 | N6-methoxy-2-[(3-pyridinyl)ethynyl]-adenosine | Drug Info | [83] | |||
216 | N6-methoxy-2-[(4-methoxyphenyl)ethynyl]adenosine | Drug Info | [83] | |||
217 | N6-methoxy-2-[(4-methylphenyl)ethynyl]adenosine | Drug Info | [83] | |||
218 | N6-methoxy-2-[(4-pentylphenyl)ethynyl]adenosine | Drug Info | [83] | |||
219 | N6-methoxy-2-[(4-pyridinyl)ethynyl]adenosine | Drug Info | [83] | |||
220 | N6-methoxy-2-[2-(trimethylsilyl)ethynyl]adenosine | Drug Info | [83] | |||
221 | N6-[(4-Amino)-phenyl]-9-benzyl-2-phenyladenine | Drug Info | [134] | |||
222 | N6-[(4-Nitro)-phenyl]-9-benzyl-2-phenyladenine | Drug Info | [134] | |||
223 | P-IODOAMPHETAMINE | Drug Info | [135] | |||
224 | PD-115199 | Drug Info | [136] | |||
225 | PD-81723 | Drug Info | [137] | |||
226 | Pentanoic acid (4,6-diphenylpyrimidin-2-yl)amide | Drug Info | [121] | |||
227 | Phenyl(2-(trifluoromethyl)quinolin-4-yl)methanol | Drug Info | [138] | |||
228 | Phenyl-(9-phenyl-9H-purin-6-yl)-amine | Drug Info | [64] | |||
229 | PSB-0788 | Drug Info | [139] | |||
230 | PSB-1115 | Drug Info | [139] | |||
231 | PSB-601 | Drug Info | [139] | |||
232 | R-N6-(phenylisopropyl)adenosine | Drug Info | [142], [80] | |||
233 | SB-298 | Drug Info | [139] | |||
234 | SCH-63390 | Drug Info | [143] | |||
235 | ST-1535 | Drug Info | [105] | |||
236 | VCP-28 | Drug Info | [145] | |||
237 | VUF-8507 | Drug Info | [146] | |||
238 | [3H]NECA | Drug Info | [151] | |||
239 | [3H]OSIP339391 | Drug Info | [84] |
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 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
|
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.
|
KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
---|---|---|---|
cGMP-PKG signaling pathway | hsa04022 | Affiliated Target |
|
Class: Environmental Information Processing => Signal transduction | Pathway Hierarchy | ||
cAMP signaling pathway | hsa04024 | Affiliated Target |
|
Class: Environmental Information Processing => Signal transduction | Pathway Hierarchy | ||
Sphingolipid signaling pathway | hsa04071 | Affiliated Target |
|
Class: Environmental Information Processing => Signal transduction | Pathway Hierarchy | ||
Neuroactive ligand-receptor interaction | hsa04080 | Affiliated Target |
|
Class: Environmental Information Processing => Signaling molecules and interaction | Pathway Hierarchy | ||
Regulation of lipolysis in adipocytes | hsa04923 | Affiliated Target |
|
Class: Organismal Systems => Endocrine system | Pathway Hierarchy | ||
Renin secretion | hsa04924 | Affiliated Target |
|
Class: Organismal Systems => Endocrine system | Pathway Hierarchy | ||
Click to Show/Hide the Information of Affiliated Human Pathways |
Degree | 1 | Degree centrality | 1.07E-04 | Betweenness centrality | 0.00E+00 |
---|---|---|---|---|---|
Closeness centrality | 1.84E-01 | Radiality | 1.31E+01 | Clustering coefficient | 0.00E+00 |
Neighborhood connectivity | 1.60E+01 | Topological coefficient | 1.00E+00 | Eccentricity | 12 |
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 Profiles in Patients | Top | |||||
---|---|---|---|---|---|---|
Target Expression Profile (TEP) |
Target Affiliated Biological Pathways | Top | |||||
---|---|---|---|---|---|---|
KEGG Pathway | [+] 5 KEGG Pathways | + | ||||
1 | cGMP-PKG signaling pathway | |||||
2 | cAMP signaling pathway | |||||
3 | Sphingolipid signaling pathway | |||||
4 | Neuroactive ligand-receptor interaction | |||||
5 | Morphine addiction | |||||
NetPath Pathway | [+] 2 NetPath Pathways | + | ||||
1 | TCR Signaling Pathway | |||||
2 | RANKL Signaling Pathway | |||||
Panther Pathway | [+] 2 Panther Pathways | + | ||||
1 | Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway | |||||
2 | Heterotrimeric G-protein signaling pathway-Gq alpha and Go alpha mediated pathway | |||||
Reactome | [+] 2 Reactome Pathways | + | ||||
1 | Adenosine P1 receptors | |||||
2 | G alpha (i) signalling events | |||||
WikiPathways | [+] 4 WikiPathways | + | ||||
1 | Nucleotide GPCRs | |||||
2 | GPCRs, Class A Rhodopsin-like | |||||
3 | GPCR ligand binding | |||||
4 | GPCR downstream signaling |
Target-Related Models and Studies | Top | |||||
---|---|---|---|---|---|---|
Target Validation | ||||||
Target QSAR Model |
References | Top | |||||
---|---|---|---|---|---|---|
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