Drug Information
| Drug General Information | Top | |||
|---|---|---|---|---|
| Drug ID |
D0L5UO
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| Former ID |
DCL000102
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| Drug Name |
Darapladib
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| Synonyms |
SB 480848; Darapladib (USAN)
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| Drug Type |
Small molecular drug
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| Indication | Arteriosclerosis [ICD-11: BD40; ICD-9: 440] | Discontinued in Phase 3 | [1], [2] | |
| Company |
GlaxoSmithKline
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| Structure |
 |
Download2D MOL |
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| Formula |
C36H38F4N4O2S
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| Canonical SMILES |
CCN(CC)CCN(CC1=CC=C(C=C1)C2=CC=C(C=C2)C(F)(F)F)C(=O)CN3C4=C(CCC4)C(=O)N=C3SCC5=CC=C(C=C5)F
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| InChI |
1S/C36H38F4N4O2S/c1-3-42(4-2)20-21-43(22-25-8-12-27(13-9-25)28-14-16-29(17-15-28)36(38,39)40)33(45)23-44-32-7-5-6-31(32)34(46)41-35(44)47-24-26-10-18-30(37)19-11-26/h8-19H,3-7,20-24H2,1-2H3
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| InChIKey |
WDPFJWLDPVQCAJ-UHFFFAOYSA-N
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| CAS Number |
CAS 356057-34-6
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| PubChem Compound ID | ||||
| PubChem Substance ID |
14912817, 17397748, 24212669, 51238364, 57373852, 103163821, 104017492, 123055336, 131311864, 134338793, 135195691, 137124696, 140342334, 144115884, 162201858, 163620709, 163686026, 170502612, 175426322, 178103307, 179150370, 185974990, 188932643, 190861993, 198984335, 223385373, 223704897, 228826696, 242060329, 243523950, 249737039, 251971364, 252155042, 252215249, 252451735, 252810760
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| Target and Pathway | Top | |||
|---|---|---|---|---|
| Target(s) | Phospholipase A2 (PLA2G1B) | Target Info | Modulator | [3], [4] |
| BioCyc | Phospholipases | |||
| KEGG Pathway | Glycerophospholipid metabolism | |||
| Ether lipid metabolism | ||||
| Arachidonic acid metabolism | ||||
| Linoleic acid metabolism | ||||
| alpha-Linolenic acid metabolism | ||||
| Metabolic pathways | ||||
| Ras signaling pathway | ||||
| Vascular smooth muscle contraction | ||||
| Pancreatic secretion | ||||
| Fat digestion and absorption | ||||
| Pathway Interaction Database | Fc-epsilon receptor I signaling in mast cells | |||
| Reactome | Acyl chain remodelling of PC | |||
| Acyl chain remodelling of PE | ||||
| Acyl chain remodelling of PI | ||||
| WikiPathways | Glycerophospholipid biosynthesis | |||
| References | Top | |||
|---|---|---|---|---|
| REF 1 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6696). | |||
| REF 2 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016591) | |||
| REF 3 | Darapladib, a reversible lipoprotein-associated phospholipase A2 inhibitor, for the oral treatment of atherosclerosis and coronary artery disease. IDrugs. 2009 Oct;12(10):648-55. | |||
| REF 4 | Darapladib, a lipoprotein-associated phospholipase A2 inhibitor, in diabetic macular edema: a 3-month placebo-controlled study.Ophthalmology.2015 May;122(5):990-6. | |||
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