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

General Information of Drug (ID: DMU24HR)

• Drug Name: LY-292728 Drug Info
• Synonyms: LY-292728; LY 292728; 153034-77-6; CHEMBL292782; 9H-Xanthene-4-propanoicacid,7-carboxy-3-[3-[(5-ethyl-4'-fluoro-2-hydroxy[1,1'-biphenyl]-4-yl)oxy]propoxy]-9-oxo-; ACMC-20ddq7; AC1Q4NQC; AC1L4UN3; SCHEMBL13696764; CTK4C7669; DTXSID00165204; BDBM50029464; 9h-xanthene-4-propanoic acid, 7-carboxy-3-[3-[(5-ethyl-4'-fluoro-2-hydroxy[1,1'-biphenyl]-4-yl)oxy]propoxy]-9-oxo-; L011726; 5-(2-carboxyethyl)-6-[3-[2-ethyl-4-(4-fluorophenyl)-5-hydroxyphenoxy]propoxy]-9-oxoxanthene-2-carboxylic acid
• Cross-matching ID:
  PubChem CID: 192617
  CAS Number: CAS 153034-77-6
  TTD Drug ID: DMU24HR

Molecule-Related Drug Atlas

Drug(s) Targeting Leukotriene B4 receptor 2 (LTB4R2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
LTB4	DME26RS	Human immunodeficiency virus infection	1C62	Phase 2	[2]
Biomed 101	DMQ9KZW	Kidney cancer	2C90.0	Phase 1	[2]
ONO-4057	DMNEA78	Inflammatory bowel disease	DD72	Discontinued in Phase 2	[3]
CP-105696	DM1C4IN	Inflammatory bowel disease	DD72	Discontinued in Phase 1	[4]
LY-255283	DMFIR0S	Asthma	CA23	Terminated	[5]
LY-282210	DMBSFDE	Discovery agent	N.A.	Investigative	[1]
(3S,4R)-3-Benzyl-7-isopropyl-chroman-4-ol	DMET6IS	Discovery agent	N.A.	Investigative	[4]
12S-HETE	DMBEZ09	Discovery agent	N.A.	Investigative	[6]
ZK-158252	DMNMD0J	Discovery agent	N.A.	Investigative	[6]
[3H]LTB4	DMDOJVX	Discovery agent	N.A.	Investigative	[7]

Drug(s) Targeting Leukotriene B4 receptor 1 (LTB4R)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
LTB4	DME26RS	Human immunodeficiency virus infection	1C62	Phase 2	[8]
Amelubant	DMUMCB9	Pulmonary disease	1B10-1F85	Phase 2	[9]
Biomed 101	DMQ9KZW	Kidney cancer	2C90.0	Phase 1	[10]
LY293111	DM03FHA	Pancreatic cancer	2C10	Discontinued in Phase 2	[11]
SB-201993	DMIF4VJ	Psoriasis vulgaris	EA90	Discontinued in Phase 2	[12]
CI-949	DMN4QSW	Asthma	CA23	Discontinued in Phase 2	[13]
CP-195543	DM1OSUR	Rheumatoid arthritis	FA20	Discontinued in Phase 2	[14]
LTB 019	DM6G0PN	Asthma	CA23	Discontinued in Phase 2	[15]
LY-223982	DMWB7DO	Asthma	CA23	Discontinued in Phase 2	[16]
CP-105696	DM1C4IN	Inflammatory bowel disease	DD72	Discontinued in Phase 1	[4]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Leukotriene B4 receptor 1 (LTB4R)	TTN53ZF	LT4R1_HUMAN	Inhibitor	[1]
Leukotriene B4 receptor 2 (LTB4R2)	TTVJX54	LT4R2_HUMAN	Inhibitor	[1]

References

• [1] Biphenylyl-substituted xanthones: highly potent leukotriene B4 receptor antagonists. J Med Chem. 1993 Nov 26;36(24):3982-4.
• [2] Diaryl ether/carboxylic acid derivatives of LY255283: Receptor antagonists of leukotriene B4, Bioorg. Med. Chem. Lett. 3(10):1985-1990 (1993).
• [3] ONO-4057, a novel, orally active leukotriene B4 antagonist: effects on LTB4-induced neutrophil functions. Prostaglandins. 1992 Oct;44(4):261-75.
• [4] 3-Substituted-4-hydroxy-7-chromanylacetic acid derivatives as antagonists of the leukotriene B4 (LTB4) receptor, Bioorg. Med. Chem. Lett. 7(17):2307-2312 (1997).
• [5] o-phenylphenols: potent and orally active leukotriene B4 receptor antagonists. J Med Chem. 1993 Nov 26;36(24):3978-81.
• [6] Hydroxyeicosanoids bind to and activate the low affinity leukotriene B4 receptor, BLT2. J Biol Chem. 2001 Apr 13;276(15):12454-9.
• [7] 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. (Target id: 268).
• [8] LTB4 promotes insulin resistance in obese mice by acting on macrophages, hepatocytes and myocytes. Nat Med. 2015 Mar;21(3):239-47.
• [9] Leukotriene receptor antagonists in children with cystic fibrosis lung disease : anti-inflammatory and clinical effects. Paediatr Drugs. 2005;7(6):353-63.
• [10] Biomed 101, a leukotriene B4 inhibitor, may decrease IL-2 toxicity. 2003 ASCO Annual Meeting. 2003.
• [11] The Role of PPARgamma Receptors and Leukotriene B(4) Receptors in Mediating the Effects of LY293111 in Pancreatic Cancer. PPAR Res. 2008;2008:827096.
• [12] (E)-3-[6-[[(2,6-dichlorophenyl)thio]methyl]-3-(2-phenylethoxy)-2- pyridinyl]-2-propenoic acid: a high-affinity leukotriene B4 receptor antagonist w... J Med Chem. 1996 Sep 13;39(19):3837-41.
• [13] Inhibition of histamine, leukotriene C4/D4, and thromboxane B2 release from human leukocytes and human chopped lung mast cells by the allergic mediator release inhibitor, CI-949. J Allergy Clin Immunol. 1990 Dec;86(6 Pt 1):902-8.
• [14] The synthesis of CP-195543, an LTB4 antagonist for the treatment of inflammatory diseases. Curr Opin Drug Discov Devel. 1999 Nov;2(6):550-6.
• [15] Effect of the oral leukotriene B4 receptor antagonist LTB019 on inflammatory sputum markers in patients with chronic obstructive pulmonary disease. Pulm Pharmacol Ther. 2008;21(2):409-17.
• [16] Specific inhibition of leukotriene B4-induced neutrophil activation by LY223982. J Pharmacol Exp Ther. 1992 Dec;263(3):1009-14.