Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMNEVKA)

Drug Name

E2012 Drug Info

Synonyms

870843-42-8; E 2012; (E)-1-[(1S)-1-(4-FLUOROPHENYL)ETHYL]-3-[3-METHOXY-4-(4-METHYL-1H-IMIDAZOL-1-YL)BENZYLIDENE]PIPERIDIN-2-ONE; E-2012; UNII-3LSD4Y5F0F; 3LSD4Y5F0F; CHEMBL1224151; J-501810; (3E)-1-[(1S)-1-(4-fluorophenyl)ethyl]-3-[[3-methoxy-4-(4-methylimidazol-1-yl)phenyl]methylidene]piperidin-2-one; (e)-1-((1s)-1-(4-fluorophenyl)ethyl)-3-(3-methoxy-4-(4-methyl-1h-imidazol-1-yl)benzylidene)piperidin-2-one; PUOAETJYKQITMO-LANLRWRYSA-N

Indication

Disease Entry	ICD 11	Status	REF
Alzheimer disease	8A20	Phase 1	[1]

Cross-matching ID

PubChem CID: 11560787
CAS Number: CAS 870843-42-8
TTD Drug ID: DMNEVKA

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Approved Drug(s)

Clinical Trial Drug(s)

Download the Complete Related Drug List

Drug(s) Targeting Gamma-secretase (GS)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Nirogacestat	DMUP5Z0	Desmoid tumour	2F7C	Approved	[3]
(S)-FLURBIPROFEN	DMF2O4T	Myalgia	FB56.2	Preregistration	[4]
AMG 386	DMQJXL4	Breast cancer	2C60-2C65	Phase 3	[5]
Semagacestat	DML83IW	Parkinson disease	8A00.0	Phase 3	[6]
R-flurbiprofen	DMFIVSR	N. A.	N. A.	Phase 2	[4]
MK-0752	DMLTAES	Alzheimer disease	8A20	Phase 2	[7]
BMS-708163	DM51LTG	Alzheimer disease	8A20	Phase 2	[8]
CHF-5074	DMTE071	Alzheimer disease	8A20	Phase 2	[9]
RO-4929097	DMXA6B3	Breast cancer	2C60-2C65	Phase 2	[10]
AL102	DMCTWIB	Desmoid tumour	2F7C	Phase 2	[11]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

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Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Gamma-secretase (GS)	TT9W8GU	APH1A_HUMAN; APH1B_HUMAN; PEN2_HUMAN; NICA_HUMAN; PSN1_HUMAN	Modulator	[2]

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References

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: 7358).
2	Chemical Biology, Molecular Mechanism and Clinical Perspective of -Secretase Modulators in Alzheimer's Disease.Curr Neuropharmacol.2011 Dec;9(4):598-622.
3	Pharmacodynamics and pharmacokinetics of the gamma-secretase inhibitor PF-3084014.J Pharmacol Exp Ther.2010 Jul;334(1):269-77.
4	The geminal dimethyl analogue of Flurbiprofen as a novel Abeta42 inhibitor and potential Alzheimer's disease modifying agent. Bioorg Med Chem Lett. 2006 Apr 15;16(8):2219-23.
5	Clinical pipeline report, company report or official report of Roche (2009).
6	A phase 3 trial of semagacestat for treatment of Alzheimer's disease. N Engl J Med. 2013 Jul 25;369(4):341-50.
7	Determination of the gamma-secretase inhibitor MK-0752 in human plasma by online extraction and electrospray tandem mass spectrometry (HTLC-ESI-MS/MS). J Chromatogr B Analyt Technol Biomed Life Sci. 2010 Sep 1;878(25):2348-52.
8	Safety and tolerability of the gamma-secretase inhibitor avagacestat in a phase 2 study of mild to moderate Alzheimer disease. Arch Neurol. 2012 Nov;69(11):1430-40.
9	CHF5074, a novel gamma-secretase modulator, attenuates brain beta-amyloid pathology and learning deficit in a mouse model of Alzheimer's disease.Br J Pharmacol.2009 Mar;156(6):982-93.
10	Phase I study of RO4929097, a gamma secretase inhibitor of Notch signaling, in patients with refractory metastatic or locally advanced solid tumors. J Clin Oncol. 2012 Jul 1;30(19):2348-53.
11	Clinical pipeline report, company report or official report of Ayala Pharmaceuticals.