Drug Information
| Drug General Information | Top | |||
|---|---|---|---|---|
| Drug ID |
D07OFM
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| Former ID |
DNCL003593
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| Drug Name |
GSK525762
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| Synonyms |
GSK-525762
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| Drug Type |
Small molecular drug
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| Indication | Haematological malignancy [ICD-11: 2B33.Y] | Phase 1 | [1] | |
| Solid tumour/cancer [ICD-11: 2A00-2F9Z; ICD-10: C76-C80; ICD-9: 140-229] | Phase 1 | [2], [3], [4], [5] | ||
| Company |
GlaxoSmithKline
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| Structure |
 |
Download2D MOL
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| Formula |
C22H22ClN5O2
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| Canonical SMILES |
CCNC(=O)CC1C2=NN=C(N2C3=C(C=C(C=C3)OC)C(=N1)C4=CC=C(C=C4)Cl)C
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| InChI |
1S/C22H22ClN5O2/c1-4-24-20(29)12-18-22-27-26-13(2)28(22)19-10-9-16(30-3)11-17(19)21(25-18)14-5-7-15(23)8-6-14/h5-11,18H,4,12H2,1-3H3,(H,24,29)/t18-/m0/s1
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| InChIKey |
AAAQFGUYHFJNHI-SFHVURJKSA-N
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| CAS Number |
CAS 1260907-17-2
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| PubChem Compound ID | ||||
| PubChem Substance ID | ||||
| ChEBI ID |
CHEBI:95082
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| Target and Pathway | Top | |||
|---|---|---|---|---|
| Target(s) | Bromodomain and extraterminal domain protein (BET) | Target Info | Inhibitor | [1] |
| Bromodomain-containing protein 4 (BRD4) | Target Info | Modulator | [6], [7] | |
| KEGG Pathway | SNARE interactions in vesicular transport | |||
| Reactome | COPII (Coat Protein 2) Mediated Vesicle Transport | |||
| WikiPathways | Chemical Compounds to monitor Proteins | |||
| miR-targeted genes in squamous cell - TarBase | ||||
| miR-targeted genes in muscle cell - TarBase | ||||
| miR-targeted genes in lymphocytes - TarBase | ||||
| References | Top | |||
|---|---|---|---|---|
| REF 1 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||
| REF 2 | 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: 7033). | |||
| REF 3 | Selective inhibition of BET bromodomains. Nature. 2010 Dec 23;468(7327):1067-73. | |||
| REF 4 | Suppression of inflammation by a synthetic histone mimic. Nature. 2010 Dec 23;468(7327):1119-23. | |||
| REF 5 | Small molecules, big targets: drug discovery faces the protein-protein interaction challenge.Nat Rev Drug Discov. 2016 Aug;15(8):533-50. | |||
| REF 6 | Targeting bromodomains: epigenetic readers of lysine acetylation.Nat Rev Drug Discov.2014 May;13(5):337-56. | |||
| REF 7 | BET inhibitor resistance emerges from leukaemia stem cells.Nature.2015 Sep 24;525(7570):538-42. | |||
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