Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T44068 | Target Info | |||
| Target Name | Adrenergic receptor beta-1 (ADRB1) | ||||
| Synonyms |
Beta-1 adrenoreceptor; Beta-1 adrenoceptor; Beta-1 adrenergic receptor; B1AR; ADRB1R
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| Target Type | Successful Target | ||||
| Gene Name | ADRB1 | ||||
| Biochemical Class | GPCR rhodopsin | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| Co-Target Name | Dopamine D2 receptor (D2R) | Successful Target | ||||
| UniProt ID | DRD2_HUMAN | |||||
| Gene Name | DRD2 | |||||
| Synonyms |
Dopamine receptor 2; D(2) dopamine receptor
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| Representative Drug(s) | Norepinephrine | Drug Info | IC50 = 0.00008 nM | Click to Show More | [1] | |
| 2 | Epinephrine | Drug Info | Ki = 910 nM | [20] | ||
| Co-Target Name | Adrenergic receptor beta-2 (ADRB2) | Successful Target | ||||
| UniProt ID | ADRB2_HUMAN | |||||
| Gene Name | ADRB2 | |||||
| Synonyms |
Beta-2 adrenoreceptor; Beta-2 adrenoceptor; Beta-2 adrenergic receptor; B2AR; ADRB2R
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| Representative Drug(s) | Isoproterenol | Drug Info | EC50 = 0.1585 nM | Click to Show More | [2] | |
| 2 | Timolol | Drug Info | Ki = 0.2089 nM | [3] | ||
| 3 | Propranolol | Drug Info | Ki = 0.32 nM | [4] | ||
| 4 | Pindolol | Drug Info | Ki = 0.4 nM | [5] | ||
| 5 | Metoprolol | Drug Info | Ki = 220 nM | [4] | ||
| 6 | Bisoprolol | Drug Info | Ki = 250 nM | [4] | ||
| 7 | Epinephrine | Drug Info | Ki = 360 nM | [20] | ||
| 8 | L-796568 | Drug Info | IC50 = 670 nM | [7] | ||
| Co-Target Name | Adrenergic receptor beta-3 (ADRB3) | Successful Target | ||||
| UniProt ID | ADRB3_HUMAN | |||||
| Gene Name | ADRB3 | |||||
| Synonyms |
Beta3AR; Beta3-AR; Beta-3 adrenoreceptor; Beta-3 adrenoceptor; Beta-3 adrenergic receptor; B3AR; ADRB3R
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| Representative Drug(s) | Isoproterenol | Drug Info | EC50 = 0.97 nM | Click to Show More | [6] | |
| 2 | L-796568 | Drug Info | EC50 = 2 nM | [7] | ||
| 3 | Norepinephrine | Drug Info | EC50 = 5.5 nM | [11] | ||
| 4 | Epinephrine | Drug Info | EC50 = 31 nM | [11] | ||
| Co-Target Name | Debrisoquine 4-hydroxylase (CYP2D6) | Successful Target | ||||
| UniProt ID | CP2D6_HUMAN | |||||
| Gene Name | CYP2D6 | |||||
| Synonyms |
P450-DB1; Cytochrome P450-DB1; Cytochrome P450 2D6; CYPIID6; CYP2DL1
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| Representative Drug(s) | Ajmalicine | Drug Info | Ki = 3.3 nM | Click to Show More | [8] | |
| 2 | BUCINDOLOL | Drug Info | IC50 = 50 nM | [14] | ||
| Co-Target Name | Adrenergic receptor alpha-2C (ADRA2C) | Successful Target | ||||
| UniProt ID | ADA2C_HUMAN | |||||
| Gene Name | ADRA2C | |||||
| Synonyms |
Subtype C4; Alpha-2CAR; Alpha-2C adrenoreceptor; Alpha-2C adrenoceptor; Alpha-2C adrenergic receptor; Alpha-2 adrenergic receptor subtype C4; ADRA2RL2; ADRA2L2
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| Representative Drug(s) | Ajmalicine | Drug Info | Ki = 5 nM | Click to Show More | [9] | |
| 2 | Norepinephrine | Drug Info | Ki = 63 nM | [16] | ||
| Co-Target Name | Adrenergic receptor Alpha-2 (ADRA2) | Successful Target | ||||
| UniProt ID | ADA2A_HUMAN; ADA2B_HUMAN; ADA2C_HUMAN | |||||
| Gene Name | NO-GeName | |||||
| Synonyms |
Alpha-2 adrenergic receptor; Alpha(2)-adrenoceptor
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| Representative Drug(s) | Epinephrine | Drug Info | Ki = 5 nM | Click to Show More | [10] | |
| 2 | Epinephrine | Drug Info | Ki = 5 nM | [10] | ||
| 3 | Norepinephrine | Drug Info | Ki = 30 nM | [10] | ||
| 4 | Norepinephrine | Drug Info | Ki = 30 nM | [10] | ||
| Co-Target Name | Adrenergic receptor alpha-2A (ADRA2A) | Successful Target | ||||
| UniProt ID | ADA2A_HUMAN | |||||
| Gene Name | ADRA2A | |||||
| Synonyms |
Alpha-2AAR; Alpha-2A adrenoreceptor; Alpha-2A adrenoceptor; Alpha-2A adrenergic receptor; Alpha-2 adrenergic receptor subtype C10; ADRAR; ADRA2R
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| Representative Drug(s) | Ajmalicine | Drug Info | Ki = 8.2 nM | Click to Show More | [9] | |
| 2 | Epinephrine | Drug Info | EC50 = 30.2 nM | [13] | ||
| 3 | Norepinephrine | Drug Info | Ki = 66 nM | [16] | ||
| Co-Target Name | Adrenergic receptor alpha-1A (ADRA1A) | Successful Target | ||||
| UniProt ID | ADA1A_HUMAN | |||||
| Gene Name | ADRA1A | |||||
| Synonyms |
Alpha-adrenergic receptor 1c; Alpha-1C adrenergic receptor; Alpha-1A adrenoreceptor; Alpha-1A adrenoceptor; Alpha-1A adrenergic receptor; Alpha adrenergic receptor 1c; Alpha 1A-adrenoreceptor; Alpha 1A-adrenoceptor; ADRA1C
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| Representative Drug(s) | Norepinephrine | Drug Info | EC50 = 9.1 nM | Click to Show More | [12] | |
| 2 | Epinephrine | Drug Info | EC50 = 400 nM | [10] | ||
| Co-Target Name | Adrenergic receptor alpha-2B (ADRA2B) | Successful Target | ||||
| UniProt ID | ADA2B_HUMAN | |||||
| Gene Name | ADRA2B | |||||
| Synonyms |
Subtype C2; Alpha-2BAR; Alpha-2B adrenoreceptor; Alpha-2B adrenoceptor; Alpha-2B adrenergic receptor; Alpha-2 adrenergic receptor subtype C2; ADRA2RL1; ADRA2L1
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| Representative Drug(s) | Ajmalicine | Drug Info | Ki = 14.5 nM | Click to Show More | [9] | |
| 2 | Norepinephrine | Drug Info | EC50 = 61.66 nM | [15] | ||
| Co-Target Name | 5-HT 1A receptor (HTR1A) | Successful Target | ||||
| UniProt ID | 5HT1A_HUMAN | |||||
| Gene Name | HTR1A | |||||
| Synonyms |
Serotonin receptor 1A; G-21; ADRBRL1; ADRB2RL1; 5-hydroxytryptamine receptor 1A; 5-HT1A receptor; 5-HT1A; 5-HT-1A
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| Representative Drug(s) | Pindolol | Drug Info | Ki = 22.4 nM | [5] | ||
| Co-Target Name | Adrenergic receptor alpha-1B (ADRA1B) | Successful Target | ||||
| UniProt ID | ADA1B_HUMAN | |||||
| Gene Name | ADRA1B | |||||
| Synonyms |
Alpha-1B adrenoreceptor; Alpha-1B adrenoceptor; Alpha-1B adrenergic receptor; Alpha 1B-adrenoreceptor; Alpha 1B-adrenoceptor
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| Representative Drug(s) | Epinephrine | Drug Info | EC50 = 75 nM | [17] | ||
| Co-Target Name | Human immunodeficiency virus Reverse transcriptase (HIV RT) | Successful Target | ||||
| UniProt ID | POL_HV1B1 | |||||
| Gene Name | HIV RT | |||||
| Synonyms |
HIV p66 RT; HIV Exoribonuclease H
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| Representative Drug(s) | Ajmalicine | Drug Info | IC50 ~ 200 ug.mL-1 | [18] | ||
| Co-Target Name | Voltage-gated potassium channel Kv11.1 (KCNH2) | Successful Target | ||||
| UniProt ID | KCNH2_HUMAN | |||||
| Gene Name | KCNH2 | |||||
| Synonyms |
hERG1; hERG-1; Voltage-gated potassium channel subunit Kv11.1; Potassium voltage-gated channel subfamily H member 2; HERG K+ channel; HERG; H-ERG; Ether-a-go-go-related protein 1; Ether-a-go-go-related gene potassium channel 1; Ether-a-go-go related protein 1; Ether-a-go-go related gene potassium channel 1; Eag related protein 1; Eag homolog; ERG-1; ERG
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| Representative Drug(s) | L-796568 | Drug Info | IC50 = 220 nM | Click to Show More | [7] | |
| 2 | Drug Info | IC50 = 316.23 nM | [19] | |||
| Co-Target Name | Carbonic anhydrase II (CA-II) | Successful Target | ||||
| UniProt ID | CAH2_HUMAN | |||||
| Gene Name | CA2 | |||||
| Synonyms |
Carbonic anhydrase C; Carbonic anhydrase 2; Carbonate dehydratase II; CAC
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| Representative Drug(s) | Dobutamine | Drug Info | Ki = 480 nM | [21] | ||
| Co-Target Name | HUAMN alpha-1 adrenergic receptor (ADRA1) | Literature-reported Target | ||||
| UniProt ID | ADA1A_HUMAN; ADA1B_HUMAN; ADA1D_HUMAN | |||||
| Gene Name | ADRA1A; ADRA1B; ADRA1D | |||||
| Synonyms |
Alpha-1 adrenoreceptor
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| Representative Drug(s) | Isoproterenol | Drug Info | EC50 = 1.5 nM | Click to Show More | [22] | |
| 2 | Atenolol | Drug Info | IC50 = 230 nM | [23] | ||
| Co-Target Name | Taste receptor type 2 member 1 (TAS2R1) | Co-Target | ||||
| UniProt ID | TA2R1_HUMAN | |||||
| Gene Name | TAS2R1 | |||||
| Synonyms |
T2R1; Taste receptor family B member 7; TRB7
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| Representative Drug(s) | Isoproterenol | Drug Info | EC50 = 4.9 nM | [24] | ||
| Co-Target Name | Taste receptor type 2 member 3 (TAS2R3) | Co-Target | ||||
| UniProt ID | TA2R3_HUMAN | |||||
| Gene Name | TAS2R3 | |||||
| Synonyms |
T2R3
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| Representative Drug(s) | Isoproterenol | Drug Info | EC50 = 4.9 nM | [24] | ||
| Co-Target Name | Taste receptor type 2 member 5 (TAS2R5) | Co-Target | ||||
| UniProt ID | TA2R5_HUMAN | |||||
| Gene Name | TAS2R5 | |||||
| Synonyms |
T2R5
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| Representative Drug(s) | Isoproterenol | Drug Info | EC50 = 4.9 nM | [24] | ||
| Co-Target Name | Taste receptor type 2 member 7 (TAS2R7) | Co-Target | ||||
| UniProt ID | TA2R7_HUMAN | |||||
| Gene Name | TAS2R7 | |||||
| Synonyms |
T2R7; Taste receptor family B member 4; TRB4
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| Representative Drug(s) | Isoproterenol | Drug Info | EC50 = 4.9 nM | [24] | ||
| Co-Target Name | Taste receptor type 2 member 10 (TAS2R10) | Co-Target | ||||
| UniProt ID | T2R10_HUMAN | |||||
| Gene Name | TAS2R10 | |||||
| Synonyms |
T2R10; Taste receptor family B member 2; TRB2
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| Representative Drug(s) | Isoproterenol | Drug Info | EC50 = 4.9 nM | [24] | ||
| Co-Target Name | Taste receptor type 2 member 13 (TAS2R13) | Co-Target | ||||
| UniProt ID | T2R13_HUMAN | |||||
| Gene Name | TAS2R13 | |||||
| Synonyms |
T2R13; Taste receptor family B member 3; TRB3
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| Representative Drug(s) | Isoproterenol | Drug Info | EC50 = 4.9 nM | [24] | ||
| Co-Target Name | Taste receptor type 2 member 19 (TAS2R19) | Co-Target | ||||
| UniProt ID | T2R19_HUMAN | |||||
| Gene Name | TAS2R19 | |||||
| Synonyms |
Taste receptor type 2 member 23; Taste receptor type 2 member 48; T2R48
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| Representative Drug(s) | Isoproterenol | Drug Info | EC50 = 4.9 nM | [24] | ||
| Co-Target Name | Taste receptor type 2 member 20 (TAS2R20) | Co-Target | ||||
| UniProt ID | T2R20_HUMAN | |||||
| Gene Name | TAS2R20 | |||||
| Synonyms |
Taste receptor type 2 member 49; T2R49; Taste receptor type 2 member 56; T2R56
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| Representative Drug(s) | Isoproterenol | Drug Info | EC50 = 4.9 nM | [24] | ||
| Co-Target Name | Taste receptor type 2 member 30 (TAS2R30) | Co-Target | ||||
| UniProt ID | T2R30_HUMAN | |||||
| Gene Name | TAS2R30 | |||||
| Synonyms |
T2R30; Taste receptor type 2 member 47; T2R47
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| Representative Drug(s) | Isoproterenol | Drug Info | EC50 = 4.9 nM | [24] | ||
| Co-Target Name | Taste receptor type 2 member 38 (TAS2R38) | Co-Target | ||||
| UniProt ID | T2R38_HUMAN | |||||
| Gene Name | TAS2R38 | |||||
| Synonyms |
T2R38; PTC bitter taste receptor; Taste receptor type 2 member 61; T2R61
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| Representative Drug(s) | Isoproterenol | Drug Info | EC50 = 4.9 nM | [24] | ||
| Co-Target Name | Taste receptor type 2 member 39 (TAS2R39) | Co-Target | ||||
| UniProt ID | T2R39_HUMAN | |||||
| Gene Name | TAS2R39 | |||||
| Synonyms |
T2R39; Taste receptor type 2 member 57; T2R57
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| Representative Drug(s) | Isoproterenol | Drug Info | EC50 = 4.9 nM | [24] | ||
| Co-Target Name | Taste receptor type 2 member 40 (TAS2R40) | Co-Target | ||||
| UniProt ID | T2R40_HUMAN | |||||
| Gene Name | TAS2R40 | |||||
| Synonyms |
T2R40; G-protein coupled receptor 60; Taste receptor type 2 member 58; T2R58
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| Representative Drug(s) | Isoproterenol | Drug Info | EC50 = 4.9 nM | [24] | ||
| Co-Target Name | Taste receptor type 2 member 42 (TAS2R42) | Co-Target | ||||
| UniProt ID | T2R42_HUMAN | |||||
| Gene Name | TAS2R42 | |||||
| Synonyms |
T2R42; Taste receptor type 2 member 55; T2R55
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| Representative Drug(s) | Isoproterenol | Drug Info | EC50 = 4.9 nM | [24] | ||
| Co-Target Name | Taste receptor type 2 member 43 (TAS2R43) | Co-Target | ||||
| UniProt ID | T2R43_HUMAN | |||||
| Gene Name | TAS2R43 | |||||
| Synonyms |
T2R43; Taste receptor type 2 member 52; T2R52
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| Representative Drug(s) | Isoproterenol | Drug Info | EC50 = 4.9 nM | [24] | ||
| Co-Target Name | Taste receptor type 2 member 45 (TAS2R45) | Co-Target | ||||
| UniProt ID | T2R45_HUMAN | |||||
| Gene Name | TAS2R45 | |||||
| Synonyms |
T2R45; G-protein coupled receptor 59
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| Representative Drug(s) | Isoproterenol | Drug Info | EC50 = 4.9 nM | [24] | ||
| Co-Target Name | Taste receptor type 2 member 46 (TAS2R46) | Co-Target | ||||
| UniProt ID | T2R46_HUMAN | |||||
| Gene Name | TAS2R46 | |||||
| Synonyms |
T2R46; Taste receptor type 2 member 54; T2R54
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| Representative Drug(s) | Isoproterenol | Drug Info | EC50 = 4.9 nM | [24] | ||
| Co-Target Name | Taste receptor type 2 member 50 (TAS2R50) | Co-Target | ||||
| UniProt ID | T2R50_HUMAN | |||||
| Gene Name | TAS2R50 | |||||
| Synonyms |
T2R50; Taste receptor type 2 member 51; T2R51
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| Representative Drug(s) | Isoproterenol | Drug Info | EC50 = 4.9 nM | [24] | ||
| Co-Target Name | Carbonic anhydrase VA (CA5A) | Co-Target | ||||
| UniProt ID | CAH5A_HUMAN | |||||
| Gene Name | CA5A | |||||
| Synonyms |
Carbonic anhydrase 5A, mitochondrial; Carbonate dehydratase VA; CA-VA
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| Representative Drug(s) | Dobutamine | Drug Info | Ki = 730 nM | [21] | ||
| Co-Target Name | Carbonic anhydrase VB (CA5B) | Co-Target | ||||
| UniProt ID | CAH5B_HUMAN | |||||
| Gene Name | CA5B | |||||
| Synonyms |
Carbonic anhydrase 5B, mitochondrial; Carbonate dehydratase VB; Carbonic anhydrase VB; CA-VB
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| Representative Drug(s) | Dobutamine | Drug Info | Ki = 890 nM | [21] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Novel photoaffinity label for the dopamine D2 receptor: synthesis of 4-azido-5-iodo-2-methoxy-N-[1-(phenylmethyl)-4-piperidinyl] benzamide (iodoazidoclebopride, IAC) and the corresponding 125I-labeled analogue (125IAC). J Med Chem. 1985 Apr;28(4):405-7. | ||||
| REF 2 | Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists. J Med Chem. 2006 May 4;49(9):2758-71. | ||||
| REF 3 | Discovery of -Adrenergic Receptors Blocker-Carbonic Anhydrase Inhibitor Hybrids for Multitargeted Antiglaucoma Therapy. J Med Chem. 2018 Jun 28;61(12):5380-5394. | ||||
| REF 4 | Development of covalent antagonists for beta1- and beta2-adrenergic receptors. Bioorg Med Chem. 2019 Jul 1;27(13):2959-2971. | ||||
| REF 5 | Indoloxypropanolamine analogues as 5-HT(1A) receptor antagonists. Bioorg Med Chem Lett. 2007 Oct 15;17(20):5600-4. | ||||
| REF 6 | Discovery of a novel series of biphenyl benzoic acid derivatives as potent and selective human beta3-adrenergic receptor agonists with good oral bioavailability. Part I. J Med Chem. 2008 Mar 27;51(6):1925-44. | ||||
| REF 7 | Discovery of Vibegron: A Potent and Selective 3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder. J Med Chem. 2016 Jan 28;59(2):609-23. | ||||
| REF 8 | Development of a pharmacophore for inhibition of human liver cytochrome P-450 2D6: molecular modeling and inhibition studies. J Med Chem. 1993 Apr 30;36(9):1136-45. | ||||
| REF 9 | Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications. J Med Chem. 1995 Sep 15;38(19):3681-716. | ||||
| REF 10 | Syntheses and adrenergic activities of ring-fluorinated epinephrines. J Med Chem. 1988 Oct;31(10):1972-7. | ||||
| REF 11 | Stereospecific synthesis and bio-activity of novel beta(3)-adrenoceptor agonists and inverse agonists. Bioorg Med Chem. 2008 Mar 1;16(5):2473-88. | ||||
| REF 12 | Discovery of Novel Indazole Derivatives as Orally Available beta. J Med Chem. 2017 Apr 27;60(8):3252-65. | ||||
| REF 13 | A combined ligand- and structure-based approach for the identification of rilmenidine-derived compounds which synergize the antitumor effects of doxorubicin. Bioorg Med Chem. 2016 Jul 15;24(14):3174-83. | ||||
| REF 14 | A 3D-QSAR model for CYP2D6 inhibition in the aryloxypropanolamine series. Bioorg Med Chem Lett. 2005 Sep 1;15(17):3816-20. | ||||
| REF 15 | Alpha2-adrenoreceptors profile modulation. 4. From antagonist to agonist behavior. J Med Chem. 2008 Jul 24;51(14):4289-99. | ||||
| REF 16 | Synthesis and pharmacologic evaluation of 2-endo-amino-3-exo-isopropylbicyclo[2.2.1]heptane: a potent imidazoline1 receptor specific agent. J Med Chem. 1996 Mar 15;39(6):1193-5. | ||||
| REF 17 | Synthesis, Purification, and Selective beta 2-AR Agonist and Bronchodilatory Effects of Catecholic Tetrahydroisoquinolines from Portulaca oleracea. J Nat Prod. 2019 Nov 22;82(11):2986-2993. | ||||
| REF 18 | Evaluation of natural products as inhibitors of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase. J Nat Prod. 1991 Jan-Feb;54(1):143-54. | ||||
| REF 19 | Prediction of Thorough QT study results using action potential simulations based on ion channel screens. J Pharmacol Toxicol Methods. Nov-Dec 2014;70(3):246-54. | ||||
| REF 20 | Structure-guided development of dual 2 adrenergic/dopamine D2 receptor agonists. Bioorg Med Chem. 2016 Jun 15;24(12):2641-53. | ||||
| REF 21 | Carbonic anhydrase inhibitors. Antioxidant polyphenols effectively inhibit mammalian isoforms I-XV. Bioorg Med Chem Lett. 2010 Sep 1;20(17):5050-3. | ||||
| REF 22 | Disodium (R,R)-5-[2-[[2-(3-chlorophenyl)-2-hydroxyethyl]-amino] propyl]-1,3-benzodioxole-2,2-dicarboxylate (CL 316,243). A potent beta-adrenergic agonist virtually specific for beta 3 receptors. A promising antidiabetic and antiobesity agent. J Med Chem. 1992 Aug 7;35(16):3081-4. | ||||
| REF 23 | Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor. Bioorg Med Chem. 2013 May 15;21(10):2764-71. | ||||
| REF 24 | EP patent application no. 2769216A1, ASSAYS FOR IDENTIFYING COMPOUNDS THAT MODULATE BITTER TASTE. | ||||
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