Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T36059 | Target Info | |||
| Target Name | Adenosine A3 receptor (ADORA3) | ||||
| Synonyms |
Adenosine receptor A3A; Adenosine receptor A3; Adenosine 3 receptor; A3AR; A3 Adenosine receptor
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| Target Type | Clinical trial Target | ||||
| Gene Name | ADORA3 | ||||
| Biochemical Class | GPCR rhodopsin | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| Co-Target Name | Adenosine A2a receptor (ADORA2A) | Successful Target | ||||
| UniProt ID | AA2AR_HUMAN | |||||
| Gene Name | ADORA2A | |||||
| Synonyms |
Adenosine receptor A2a; ADORA2; A2a Adenosine receptor; A(2A) adenosine receptor
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| Representative Drug(s) | SCH-442416 | Drug Info | Ki = 0.048 nM | Click to Show More | [1] | |
| 2 | IB-MECA | Drug Info | Ki = 32 nM | [10] | ||
| 3 | CF102 | Drug Info | Ki = 401 nM | [13] | ||
| Co-Target Name | Dopamine transporter (DAT) | Successful Target | ||||
| UniProt ID | SC6A3_HUMAN | |||||
| Gene Name | SLC6A3 | |||||
| Synonyms |
Solute carrier family 6 member 3; Sodium-dependent dopamine transporter; DAT1; DAT; DA transporter
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| Representative Drug(s) | Vanoxerine | Drug Info | Ki = 0.36 nM | [2] | ||
| Co-Target Name | Opioid receptor sigma 1 (OPRS1) | Successful Target | ||||
| UniProt ID | SGMR1_HUMAN | |||||
| Gene Name | SIGMAR1 | |||||
| Synonyms |
hSigmaR1; Sigma1R; Sigma1-receptor; Sigma non-opioid intracellular receptor 1; Sigma 1-type opioid receptor; SRBP; SR31747-binding protein; SR31747 binding protein 1; SR-BP; SIG-1R; Opioid receptor, sigma 1, isoform 1; OPRS1 protein; Aging-associated gene 8 protein; AAG8
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| Representative Drug(s) | Vanoxerine | Drug Info | IC50 = 1 nM | [3] | ||
| Co-Target Name | Adenosine A1 receptor (ADORA1) | Successful Target | ||||
| UniProt ID | AA1R_HUMAN | |||||
| Gene Name | ADORA1 | |||||
| Synonyms |
Adenosine receptor A1; A(1) adenosine receptor
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| Representative Drug(s) | SCH-442416 | Drug Info | Ki = 1.111 nM | Click to Show More | [1] | |
| 2 | IB-MECA | Drug Info | Ki = 3.73 nM | [5] | ||
| 3 | CF102 | Drug Info | Ki = 5.26 nM | [6] | ||
| 4 | Tonapofylline | Drug Info | Ki = 7 nM | [7] | ||
| 5 | Tonapofylline | Drug Info | Ki = 7.4 nM | [8] | ||
| Co-Target Name | Peroxisome proliferator-activated receptor gamma (PPAR-gamma) | Successful Target | ||||
| UniProt ID | PPARG_HUMAN | |||||
| Gene Name | PPARG | |||||
| Synonyms |
PPAR-gamma; Nuclear receptor subfamily 1 group C member 3; NR1C3
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| Representative Drug(s) | CF102 | Drug Info | Ki = 2.18 nM | [4] | ||
| Co-Target Name | Adenosine A2b receptor (ADORA2B) | Successful Target | ||||
| UniProt ID | AA2BR_HUMAN | |||||
| Gene Name | ADORA2B | |||||
| Synonyms |
Adenosine receptor A2b; A2b Adenosine receptor
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| Representative Drug(s) | IB-MECA | Drug Info | EC50 = 31.62 nM | Click to Show More | [9] | |
| 2 | Tonapofylline | Drug Info | Ki = 90 nM | [8] | ||
| 3 | Tonapofylline | Drug Info | Ki = 90 nM | [12] | ||
| Co-Target Name | Serotonin transporter (SERT) | Successful Target | ||||
| UniProt ID | SC6A4_HUMAN | |||||
| Gene Name | SLC6A4 | |||||
| Synonyms |
Solute carrier family 6 member 4; HTT; 5HTT; 5HT transporter
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| Representative Drug(s) | Vanoxerine | Drug Info | IC50 = 73 nM | [11] | ||
| Co-Target Name | Norepinephrine transporter (NET) | Successful Target | ||||
| UniProt ID | SC6A2_HUMAN | |||||
| Gene Name | SLC6A2 | |||||
| Synonyms |
Solute carrier family 6 member 2; Sodium-dependent noradrenaline transporter; SLC6A2; NET1; NET; NAT1
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| Representative Drug(s) | Vanoxerine | Drug Info | IC50 = 79 nM | [11] | ||
| Co-Target Name | Peroxisome proliferator-activated receptor delta (PPARD) | Clinical trial Target | ||||
| UniProt ID | PPARD_HUMAN | |||||
| Gene Name | PPARD | |||||
| Synonyms |
Peroxisomeproliferator-activated receptor beta; Peroxisomeproliferator activated receptor beta/delta; Peroxisome proliferator-activated receptor beta; PPARdelta; PPARB; PPAR-delta; PPAR-beta; Nuclear receptor subfamily 1 group C member 2; Nuclear hormone receptor 1; NUCI; NUC1; NR1C2
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| Representative Drug(s) | CF102 | Drug Info | Ki = 0.43 nM | [4] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Scaffold decoration at positions 5 and 8 of 1,2,4-triazolo[1,5-c]pyrimidines to explore the antagonist profiling on adenosine receptors: a preliminary structure-activity relationship study. J Med Chem. 2014 Jul 24;57(14):6210-25. | ||||
| REF 2 | Synthesis, biodistribution, and primate imaging of fluorine-18 labeled 2beta-carbo-1'-fluoro-2-propoxy-3beta-(4-chlorophenyl)tr opanes. Ligands for the imaging of dopamine transporters by positron emission tomography. J Med Chem. 2000 Feb 24;43(4):639-48. | ||||
| REF 3 | Conformational analysis, pharmacophore identification, and comparative molecular field analysis of ligands for the neuromodulatory sigma 3 receptor. J Med Chem. 1994 Nov 25;37(24):4109-17. | ||||
| REF 4 | Polypharmacology of N6-(3-Iodobenzyl)adenosine-5'-N-methyluronamide (IB-MECA) and Related A 3 Adenosine Receptor Ligands: Peroxisome Proliferator Activated Receptor (PPAR) gamma Partial Agonist and PPAR delta Antagonist Activity Suggests Their Antidiabetic Potential. J Med Chem. 2017 Sep 14;60(17):7459-75. | ||||
| REF 5 | 5'-N-substituted carboxamidoadenosines as agonists for adenosine receptors. J Med Chem. 1999 Apr 22;42(8):1384-92. | ||||
| REF 6 | N6-ethyl-2-alkynyl NECAs, selective human A3 adenosine receptor agonists. Bioorg Med Chem Lett. 2006 May 1;16(9):2416-8. | ||||
| REF 7 | Tricyclic imidazoline derivatives as potent and selective adenosine A1 receptor antagonists. J Med Chem. 2006 Nov 30;49(24):7132-9. | ||||
| REF 8 | Potent and orally bioavailable 8-bicyclo[2.2.2]octylxanthines as adenosine A1 receptor antagonists. J Med Chem. 2006 Nov 30;49(24):7119-31. | ||||
| REF 9 | Design, synthesis and evaluation of N6-substituted 2-aminoadenosine-5'-N-methylcarboxamides as A3 adenosine receptor agonists. Medchemcomm. 2014;5:192-6. | ||||
| REF 10 | Mutagenesis reveals structure-activity parallels between human A2A adenosine receptors and biogenic amine G protein-coupled receptors. J Med Chem. 1997 Aug 1;40(16):2588-95. | ||||
| REF 11 | Piperidine analogues of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (GBR 12909): high affinity ligands for the dopamine transporter. J Med Chem. 2002 Sep 12;45(19):4371-4. | ||||
| REF 12 | 2-Amino-5-benzoyl-4-phenylthiazoles: Development of potent and selective adenosine A1 receptor antagonists. Bioorg Med Chem. 2010 Mar 15;18(6):2195-2203. | ||||
| REF 13 | Modulation of A2B adenosine receptor by 1-Benzyl-3-ketoindole derivatives. Eur J Med Chem. 2013 Nov;69:331-7. | ||||
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