Drug Information
| Drug General Information | Top | |||
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| Drug ID |
D09WYL
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| Former ID |
DIB010428
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| Drug Name |
GSK-557296
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| Synonyms |
Epelsiban; Epelsiban besylate; Premature ejaculation therapeutic (oral), GlaxoSmithKline
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| Drug Type |
Small molecular drug
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| Indication | Premature ejaculation [ICD-11: HA03.0Z; ICD-10: F52.4; ICD-9: 302.75] | Phase 2 | [1] | |
| Company |
GlaxoSmithKline plc
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| Structure |
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Download2D MOL |
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| Formula |
C30H38N4O4
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| Canonical SMILES |
CCC(C)C1C(=O)NC(C(=O)N1C(C2=C(N=C(C=C2)C)C)C(=O)N3CCOCC3)C4CC5=CC=CC=C5C4
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| InChI |
1S/C30H38N4O4/c1-5-18(2)26-28(35)32-25(23-16-21-8-6-7-9-22(21)17-23)29(36)34(26)27(24-11-10-19(3)31-20(24)4)30(37)33-12-14-38-15-13-33/h6-11,18,23,25-27H,5,12-17H2,1-4H3,(H,32,35)/t18-,25+,26+,27+/m0/s1
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| InChIKey |
UWHCWRQFNKUYCG-QUZACWSFSA-N
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| CAS Number |
CAS 872599-83-2
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| PubChem Compound ID | ||||
| Target and Pathway | Top | |||
|---|---|---|---|---|
| Target(s) | Oxytocin receptor (OTR) | Target Info | Antagonist | [2] |
| KEGG Pathway | Calcium signaling pathway | |||
| cAMP signaling pathway | ||||
| Neuroactive ligand-receptor interaction | ||||
| Oxytocin signaling pathway | ||||
| NetPath Pathway | TGF_beta_Receptor Signaling Pathway | |||
| Panther Pathway | Oxytocin receptor mediated signaling pathway | |||
| Reactome | Vasopressin-like receptors | |||
| G alpha (q) signalling events | ||||
| WikiPathways | GPCRs, Class A Rhodopsin-like | |||
| Myometrial Relaxation and Contraction Pathways | ||||
| Oxytocin signaling | ||||
| Gastrin-CREB signalling pathway via PKC and MAPK | ||||
| Peptide GPCRs | ||||
| GPCR ligand binding | ||||
| GPCR downstream signaling | ||||
| References | Top | |||
|---|---|---|---|---|
| REF 1 | ClinicalTrials.gov (NCT01021553) A Study To Evaluate the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Two Oral Doses of GSK557296 in a Study in Men With Premature Ejaculation. U.S. National Institutes of Health. | |||
| REF 2 | Inhibition of ejaculation by the non-peptide oxytocin receptor antagonist GSK557296: a multi-level site of action. Br J Pharmacol. 2013 Aug;169(7):1477-85. | |||
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