Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T84160 Target Info
Target Name 5-HT 3 receptor (5HT3R)
Synonyms
5-hydroxytryptamine receptor type 3; 5-hydroxytryptamine receptor 3; 5-HT3R; 5-HT3 receptor; 5-HT-3
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Target Type Successful Target
Gene Name NO-GeName
Biochemical Class GPCR rhodopsin
UniProt ID
NOUNIPROTAC
Co-Targets of This Target  Top
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) LITOXETINE Drug Info IC50 = 5.9 nM [1]
Co-Target Name 5-HT 3 receptor (5HT3R) Successful Target
UniProt ID 5HT3A_HUMAN; 5HT3B_HUMAN; 5HT3C_HUMAN; 5HT3D_HUMAN; 5HT3E_HUMAN
Gene Name NO-GeName
Synonyms
5-hydroxytryptamine receptor type 3; 5-hydroxytryptamine receptor 3; 5-HT3R; 5-HT3 receptor; 5-HT-3
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Representative Drug(s) Ondansetron Drug Info Ki = 7.6 nM [2]
Co-Target Name Solute carrier family 47 member 1 (SLC47A1) Successful Target
UniProt ID S47A1_HUMAN
Gene Name SLC47A1
Synonyms
hMATE-1; Multidrug and toxin extrusion protein 1; MATE1; MATE-1
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Representative Drug(s) Ondansetron Drug Info IC50 < 10 nM [3]
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) Ondansetron Drug Info IC50 = 400 nM [4]
Co-Target Name Multidrug and toxin extrusion protein 2 (MATE2) Literature-reported Target
UniProt ID S47A2_HUMAN
Gene Name SLC47A2
Synonyms
hMATE-2; Solute carrier family 47 member 2; MATE2; MATE-2; Kidney-specific H(+)/organic cation antiporter
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Representative Drug(s) Ondansetron Drug Info IC50 = 160 nM [3]
Co-Target Name Solute carrier family 22 member 2 (SLC22A2) Co-Target
UniProt ID S22A2_HUMAN
Gene Name SLC22A2
Synonyms
Organic cation transporter 2; hOCT2
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Representative Drug(s) Ondansetron Drug Info IC50 = 890 nM [5]
References  Top
REF 1 Bioorg Med Chem Lett. 2009 Oct 15;19(20):5893-7. Epub 2009 Aug 21.Design and optimisation of selective serotonin re-uptake inhibitors with high synthetic accessibility: part 2.
REF 2 5-HT3 receptor antagonists. 3. Quinoline derivatives which may be effective in the therapy of irritable bowel syndrome. J Med Chem. 1993 Oct 29;36(22):3286-92.
REF 3 Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling. J Med Chem. 2013 Feb 14;56(3):781-795.
REF 4 Discovery of 2-substituted benzoxazole carboxamides as 5-HT3 receptor antagonists. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6538-41.
REF 5 Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2. J Med Chem. 2011 Jul 14;54(13):4548-58.

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