Co-Target(s) Information
Target General Information | Top | ||||
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Target ID | T53601 | Target Info | |||
Target Name | Bacterial 50S ribosomal RNA (Bact 50S rRNA) | ||||
Target Type | Successful Target | ||||
Gene Name | NO-GeName | ||||
UniProt ID |
Co-Targets of This Target | Top | |||||
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Co-Target Name | Cytochrome P450 3A (CYP3A) | Successful Target | ||||
UniProt ID | CP3A4_HUMAN; CP3A5_HUMAN; CP3A7_HUMAN; CP343_HUMAN | |||||
Gene Name | NO-GeName | |||||
Representative Drug(s) | Telithromycin | Drug Info | Ki = 2.4 nM | [1] | ||
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) | Erythromycin | Drug Info | IC50 = 39 nM | [2] | ||
Co-Target Name | Motilin receptor (MLNR) | Clinical trial Target | ||||
UniProt ID | MTLR_HUMAN | |||||
Gene Name | MLNR | |||||
Synonyms |
MLNR; Gprotein coupled receptor 38
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Representative Drug(s) | Erythromycin | Drug Info | IC50 = 43.65 nM | [3] | ||
Co-Target Name | Albendazole monooxygenase (CYP3A4) | Clinical trial Target | ||||
UniProt ID | CP3A4_HUMAN | |||||
Gene Name | CYP3A4 | |||||
Synonyms |
Taurochenodeoxycholate 6-alpha-hydroxylase; Quinine 3-monooxygenase; P450-PCN1; Nifedipine oxidase; NF-25; HLp; Cytochrome P450-PCN1; Cytochrome P450 NF-25; Cytochrome P450 HLp; Cytochrome P450 3A4; Cytochrome P450 3A3; CYPIIIA4; CYPIIIA3; CYP3A3; Albendazole sulfoxidase; Albendazole monooxygenase (sulfoxide-forming); 1,8-cineole 2-exo-monooxygenase
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Representative Drug(s) | Erythromycin | Drug Info | IC50 = 190 nM | [4] |
References | Top | ||||
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REF 1 | Discovery of azetidinyl ketolides for the treatment of susceptible and multidrug resistant community-acquired respiratory tract infections. J Med Chem. 2009 Dec 10;52(23):7446-57. | ||||
REF 2 | Structure-activity relationships of 9-substituted-9-dihydroerythromycin-based motilin agonists: optimizing for potency and safety. J Med Chem. 2009 Nov 12;52(21):6851-9. | ||||
REF 3 | Macrolide-type motilin receptor agonists: Acid-stable 12-O-methyl-8,9-anhydroerythromycin A 6,9-hemiacetals. Bioorg Med Chem Lett. 1995 Apr 20;5(8):835-8. | ||||
REF 4 | Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate. J Med Chem. 2009 Feb 26;52(4):1180-9. |
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