Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T74456 | Target Info | |||
| Target Name | Angiotensin II receptor type-1 (AGTR1) | ||||
| Synonyms |
Type-1 angiotensin II receptor; Angiotensin II type-1 receptor; Angiotensin II receptor 1; Angiotensin 1 receptor; AT2R1B; AT2R1; AT1BR; AT1AR; AT1; AGTR1B; AGTR1A
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| Target Type | Successful Target | ||||
| Gene Name | AGTR1 | ||||
| Biochemical Class | GPCR rhodopsin | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| Co-Target Name | Endothelin A receptor (EDNRA) | Successful Target | ||||
| UniProt ID | EDNRA_HUMAN | |||||
| Gene Name | EDNRA | |||||
| Synonyms |
HET-AR; Endothelin-1 receptor; Endothelin receptor type A; Endothelin receptor A; ETRA; ETA-R; ETA receptor; ETA; ET-A
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| Representative Drug(s) | Irbesartan | Drug Info | Ki ~ 0.0001 nM | Click to Show More | [1] | |
| 2 | Sparsentan | Drug Info | Ki = 9.3 nM | [5] | ||
| Co-Target Name | Angiotensin II receptor type-2 (AGTR2) | Successful Target | ||||
| UniProt ID | AGTR2_HUMAN | |||||
| Gene Name | AGTR2 | |||||
| Synonyms |
Type-2 angiotensin II receptor; Angiotensin II type-2 receptor; Angiotensin II receptor 2; AT2
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| Representative Drug(s) | ANGIOTENSIN II | Drug Info | IC50 = 0.08 nM | Click to Show More | [2] | |
| 2 | SARALASIN | Drug Info | Ki = 0.15 nM | [3] | ||
| 3 | Telmisartan | Drug Info | IC50 = 0.33 nM | [4] | ||
| 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) | Telmisartan | Drug Info | EC50 = 700 nM | [6] | ||
| Co-Target Name | Liver organic anion transporter 1 (SLCO1B1) | Literature-reported Target | ||||
| UniProt ID | SO1B1_HUMAN | |||||
| Gene Name | SLCO1B1 | |||||
| Synonyms |
Solute carrier organic anion transporter family member 1B1; Solute carrier family 21 member 6; Sodium-independent organic anion-transporting polypeptide 2; SLC21A6; OATPC; OATP2; OATP-C; OATP-2; Liver-specific organic anion transporter 1; LST1; LST-1
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| Representative Drug(s) | Olmesartan medoxomil | Drug Info | Ki = 540 nM | [7] | ||
| Co-Target Name | Liver organic anion transporter 2 (SLCO1B3) | Literature-reported Target | ||||
| UniProt ID | SO1B3_HUMAN | |||||
| Gene Name | SLCO1B3 | |||||
| Synonyms |
Solute carrier organic anion transporter family member 1B3; Solute carrier family 21 member 8; SLC21A8; Organic anion-transporting polypeptide 8; Organic anion transporter 8; OATP8; OATP1B3; OATP-8; Liver-specific organic anion transporter 2; LST2; LST-2
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| Representative Drug(s) | Olmesartan medoxomil | Drug Info | Ki = 750 nM | Click to Show More | [7] | |
| 2 | Telmisartan | Drug Info | Ki = 960 nM | [7] | ||
| Co-Target Name | Cytochrome P450 2J2 (CYP2J2) | Co-Target | ||||
| UniProt ID | CP2J2_HUMAN | |||||
| Gene Name | CYP2J2 | |||||
| Synonyms |
Albendazole monooxygenase (hydroxylating); Albendazole monooxygenase (sulfoxide-forming); Arachidonic acid epoxygenase; Hydroperoxy icosatetraenoate isomerase; CYPIIJ2
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| Representative Drug(s) | Telmisartan | Drug Info | Ki = 100 nM | [8] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Discovery of N-isoxazolyl biphenylsulfonamides as potent dual angiotensin II and endothelin A receptor antagonists. J Med Chem. 2002 Aug 29;45(18):3829-35. | ||||
| REF 2 | Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH. Bioorg Med Chem. 2017 Jan 15;25(2):471-82. | ||||
| REF 3 | cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain... J Med Chem. 2008 Nov 27;51(22):7094-8. | ||||
| REF 4 | Design, synthesis and biological evaluation of 6-substituted aminocarbonyl benzimidazole derivatives as nonpeptidic angiotensin II AT1 receptor antagonists. Eur J Med Chem. 2012 Mar;49:183-90. | ||||
| REF 5 | Designed multiple ligands. An emerging drug discovery paradigm. J Med Chem. 2005 Oct 20;48(21):6523-43. | ||||
| REF 6 | Evaluation of selected 3D virtual screening tools for the prospective identification of peroxisome proliferator-activated receptor (PPAR) gamma partial agonists. Eur J Med Chem. 2016 Nov 29;124:49-62. | ||||
| REF 7 | Structure-based identification of OATP1B1/3 inhibitors. Mol Pharmacol. 2013 Jun;83(6):1257-67. | ||||
| REF 8 | Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors. Drug Metab Dispos. 2013 Jan;41(1):60-71. | ||||
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