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

General Information of Drug (ID: DMJ0A5U)

Drug Name

EFIPLADIB Drug Info

Synonyms

Efipladib; 381683-94-9; UNII-S97YUG2A91; S97YUG2A91; CHEMBL272342; PLA-902; Efipladib [USAN:INN]; Efipladib (USAN); 4-(3-(1-benzhydryl-5-chloro-2-(2-((3,4-dichlorophenyl)methylsulfonamido)ethyl)-1H-indol-3-yl)propyl)benzoic acid; SCHEMBL1500831; HIZOPJQOPKRKFM-UHFFFAOYSA-N; ZINC85536943; BDBM50226792; D06674; 4-{3-[1-benzhydryl-5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1H-indol-3-yl]propyl}benzoic acid

Indication

Disease Entry	ICD 11	Status	REF
Asthma	CA23	Terminated	[1]

Cross-matching ID

PubChem CID: 9853499
CAS Number: CAS 381683-94-9
TTD Drug ID: DMJ0A5U

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Clinical Trial Drug(s)

Investigative Drug(s)

Download the Complete Related Drug List

Drug(s) Targeting Cytosolic phospholipase A2 (GIVA cPLA2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
ZPL521	DMPZE2G	Atopic dermatitis	EA80	Phase 1/2	[3]
1,1,1-Trifluoro-7-phenylheptan-2-one	DMLHVWP	Discovery agent	N.A.	Investigative	[4]
ARACHIDONYL TRIFLUOROMETHYLKETONE	DMHL48F	Discovery agent	N.A.	Investigative	[5]
1,1,1-Trifluoro-8-phenyl-octan-2-one	DMYENI7	Discovery agent	N.A.	Investigative	[4]
AR-C70484XX	DMU3A57	Discovery agent	N.A.	Investigative	[6]
1-Imidazol-1-yl-3-(4-octylphenoxy)propan-2-one	DM3JHVL	Discovery agent	N.A.	Investigative	[6]
AX-006	DMDWCY7	Discovery agent	N.A.	Investigative	[7]
N-(4-Ethoxybutyl)-2-oxohexadecanamide	DM012TN	Discovery agent	N.A.	Investigative	[8]
[3,4''']biflavone	DMHU4NS	Discovery agent	N.A.	Investigative	[9]
1,1,1-Trifluoro-6-(naphthalen-2-yl)hexan-2-one	DMZ2VE3	Discovery agent	N.A.	Investigative	[10]
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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
Cytosolic phospholipase A2 (GIVA cPLA2)	TTT1JVS	PA24A_HUMAN	Inhibitor	[2]

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References

1	Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib. J Med Chem. 2008 Jun 26;51(12):3388-413.
2	Reactions of functionalized sulfonamides: application to lowering the lipophilicity of cytosolic phospholipase A2alpha inhibitors. J Med Chem. 2009 Feb 26;52(4):1156-71.
3	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
4	Synthesis of polyfluoro ketones for selective inhibition of human phospholipase A2 enzymes. J Med Chem. 2008 Dec 25;51(24):8027-37.
5	85-kDa cPLA(2) plays a critical role in PPAR-mediated gene transcription in human hepatoma cells. Am J Physiol Gastrointest Liver Physiol. 2002 Apr;282(4):G586-97.
6	1-Indol-1-yl-propan-2-ones and related heterocyclic compounds as dual inhibitors of cytosolic phospholipase A(2)alpha and fatty acid amide hydrolase. Bioorg Med Chem. 2010 Jan 15;18(2):945-52.
7	2-Oxoamide inhibitors of phospholipase A2 activity and cellular arachidonate release based on dipeptides and pseudodipeptides. Bioorg Med Chem. 2009 Jul 1;17(13):4833-43.
8	Structure-activity relationships of natural and non-natural amino acid-based amide and 2-oxoamide inhibitors of human phospholipase A(2) enzymes. Bioorg Med Chem. 2008 Dec 15;16(24):10257-69.
9	Inhibitory effect of synthetic C-C biflavones on various phospholipase A(2)s activity. Bioorg Med Chem. 2007 Nov 15;15(22):7138-43.
10	Potent and selective fluoroketone inhibitors of group VIA calcium-independent phospholipase A2. J Med Chem. 2010 May 13;53(9):3602-10.