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

General Information of Drug (ID: DMYZ72J)

• Drug Name: CGP-57698 Drug Info
• Synonyms: 168082-74-4

Indication

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[1]

• Cross-matching ID:
  PubChem CID: 9888588
  CAS Number: CAS 168082-74-4
  TTD Drug ID: DMYZ72J

Molecule-Related Drug Atlas

Drug(s) Targeting Leukotriene CysLT1 receptor (CYSLTR1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Montelukast	DMD157S	Allergic asthma	CA23.0	Approved	[2]
Zafirlukast	DMHNQOG	Asthma	CA23	Approved	[3]
Pranlukast	DMYHDCA	Allergic rhinitis	CA08.0	Approved	[4]
Cinalukast	DMFIC0M	Asthma	CA23	Approved	[5]
KP-496	DMCO8UZ	Asthma	CA23	Phase 2	[6]
BAY-X-7195	DM2XE80	Asthma	CA23	Phase 2	[7]
Masilukast	DMDTI0L	Asthma	CA23	Phase 2	[8]
LM-1507.NA	DMW6VA0	Asthma	CA23	Phase 2	[9]
Iralukast	DMQ3RWN	Asthma	CA23	Phase 2	[10]
YM-57158	DMS31YW	Allergic rhinitis	CA08.0	Phase 1	[11]

Drug(s) Targeting Leukotriene CysLT2 receptor (CYSLTR2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BAY-X-7195	DM2XE80	Asthma	CA23	Phase 2	[7]
AS-35	DMC2WI7	Asthma	CA23	Discontinued in Phase 2	[12]
DS-4574	DM8GZWC	Asthma	CA23	Discontinued in Phase 2	[13]
Sulukast	DMBSLZV	Asthma	CA23	Discontinued in Phase 2	[14]
ICI-198615	DM0195G	Asthma	CA23	Terminated	[15]
MDL-43291	DMBIDQX	Asthma	CA23	Terminated	[16]
LY-290154	DMPZ7AO	Asthma	CA23	Terminated	[17]
FPL-55712	DMF1CDK	Asthma	CA23	Terminated	[18]
LTE4	DMCPB0Q	Discovery agent	N.A.	Investigative	[19]
LTC4	DM702WR	Discovery agent	N.A.	Investigative	[20]

Drug(s) Affected By Cysteinyl leukotriene receptor 1 (CYSLTR1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Zafirlukast	DMHNQOG	Asthma	CA23	Approved	[1]
Pranlukast	DMYHDCA	Allergic rhinitis	CA08.0	Approved	[1]
Hydrogen peroxide	DM1NG5W	Infectious disease	1A00-CA43.1	Approved	[21]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[22]
Aspirin	DM672AH	Acute coronary syndrome	BA41	Approved	[23]
(+)-JQ1	DM1CZSJ	Testicular cancer	2C80	Phase 1	[24]
PMID28870136-Compound-48	DMPIM9L	N. A.	N. A.	Patented	[21]
LTC4	DM702WR	Discovery agent	N.A.	Investigative	[1]
LTE4	DMCPB0Q	Discovery agent	N.A.	Investigative	[25]
BAYu9773	DMXQ14V	Discovery agent	N.A.	Investigative	[1]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Leukotriene CysLT1 receptor (CYSLTR1)	TTGKOY9	CLTR1_HUMAN	Modulator	[1]
Leukotriene CysLT2 receptor (CYSLTR2)	TT0PZR5	CLTR2_HUMAN	Modulator	[1]

Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
Cysteinyl leukotriene receptor 1 (CYSLTR1)	OT904HBN	CLTR1_HUMAN	Protein Interaction/Cellular Processes	[1]

References

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• [4] Beneficial effects of leukotriene receptor antagonists in the prevention of cedar pollinosis in a community setting. J Investig Allergol Clin Immunol. 2009;19(3):195-203.
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• [6] Effects of KP-496, a novel dual antagonist for leukotriene D4 and thromboxane A2 receptors, on contractions induced by various agonists in the guinea pig trachea. Allergol Int. 2006 Dec;55(4):403-10.
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• [10] Pharmacological characterization of the cysteinyl-leukotriene antagonists CGP 45715A (iralukast) and CGP 57698 in human airways in vitro. Br J Pharmacol. 1998 Feb;123(3):590-8.
• [11] In vitro pharmacologic profile of YM158, a new dual antagonist for LTD4 and TXA2 receptors. J Pharmacol Exp Ther. 1998 Nov;287(2):633-9.
• [12] Inhibition of radiolabeled leukotriene-binding by AS-35 in guinea pig lung membrane fraction. Jpn J Pharmacol. 1992 Apr;58(4):357-64.
• [13] Inhibitory effect of DS-4574, a mast cell stabilizer with peptidoleukotriene receptor antagonism, on gastric acid secretion in rats. Eur J Pharmacol. 1994 Apr 1;255(1-3):229-34.
• [14] The pharmacological evaluation of LY 170680, a novel leukotriene D4 and E4 antagonist in the guinea-pig. Br J Pharmacol. 1989 Sep;98(1):259-67.
• [15] Heterogeneity of binding sites for ICI 198,615 in human lung parenchyma. Biochem Pharmacol. 1992 Oct 6;44(7):1411-5.
• [16] Conformationally restricted leukotriene receptor antagonists: [(octahydro-2-oxo-7-tetradecylidene-2H-1-benzopyran-8-yl)thio]ace tic acids. Pharmacology. 1990;40(5):271-6.
• [17] DOI: 10.1021/op060036x
• [18] Effect of the leukotriene receptor antagonists FPL 55712, LY 163443, and MK-571 on the elimination of cysteinyl leukotrienes in the rat. Br J Pharmacol. 1991 Apr;102(4):865-70.
• [19] Differential signaling of cysteinyl leukotrienes and a novel cysteinyl leukotriene receptor 2 (CysLT agonist, N-methyl-leukotriene C in calcium reporter and beta arrestin assays. Mol Pharmacol. 2011 Feb;79(2):270-8.
• [20] Molecular cloning and characterization of a second human cysteinyl leukotriene receptor: discovery of a subtype selective agonist. Mol Pharmacol. 2000 Dec;58(6):1601-8.
• [21] Oxidative stress modulates theophylline effects on steroid responsiveness. Biochem Biophys Res Commun. 2008 Dec 19;377(3):797-802.
• [22] Transcriptional and Metabolic Dissection of ATRA-Induced Granulocytic Differentiation in NB4 Acute Promyelocytic Leukemia Cells. Cells. 2020 Nov 5;9(11):2423. doi: 10.3390/cells9112423.
• [23] Differential contribution of the CysLTR1 gene in patients with aspirin hypersensitivity. J Clin Immunol. 2007 Nov;27(6):613-9. doi: 10.1007/s10875-007-9115-x. Epub 2007 Jul 20.
• [24] Bromodomain-containing protein 4 (BRD4) regulates RNA polymerase II serine 2 phosphorylation in human CD4+ T cells. J Biol Chem. 2012 Dec 14;287(51):43137-55.
• [25] Characterization of the leukotriene D4 receptor in dimethylsulphoxide-differentiated U937 cells: comparison with the leukotriene D4 receptor in human lung and guinea-pig lung. Eur J Pharmacol. 1993 Feb 15;244(3):239-50. doi: 10.1016/0922-4106(93)90149-4.