General Information of the Protein
Protein ID
PT01800
Protein Name
Cysteinyl leukotriene receptor 1
Secondarily
Protein Name
Cysteinyl leukotriene D4 receptor
G-protein coupled receptor HG55
HMTMF81
Gene Name
CYSLTR1
Secondarily
Gene Name
CYSLT1
Sequence
MDETGNLTVSSATCHDTIDDFRNQVYSTLYSMISVVGFFGNGFVLYVLIKTYHKKSAFQVYMINLAVADLLCVCTLPLRVVYYVHKGIWLFGDFLCRLSTYALYVNLYCSIFFMTAMSFFRCIAIVFPVQNINLVTQKKARFVCVGIWIFVILTSSPFLMAKPQKDEKNNTKCFEPPQDNQTKNHVLVLHYVSLFVGFIIPFVIIIVCYTMIILTLLKKSMKKNLSSHKKAIGMIMVVTAAFLVSFMPYHIQRTIHLHFLHNETKPCDSVLRMQKSVVITLSLAASNCCFDPLLYFFSGGNFRKRLSTFRKHSLSSVTYVPRKKASLPEKGEEICKV
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Organism
Homo sapiens, Human
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
>
Small molecule receptor (family A GPCR)
>
Lipid-like ligand receptor (family A GPCR)
>
Leukotriene receptor
Function
Receptor for cysteinyl leukotrienes mediating bronchoconstriction of individuals with and without asthma. Stimulation by LTD4 results in the contraction and proliferation of smooth muscle, edema, eosinophil migration and damage to the mucus layer in the lung. This response is mediated via a G-protein that activates a phosphatidylinositol-calcium second messenger system. The rank order of affinities for the leukotrienes is LTD4 >> LTE4 = LTC4 >> LTB4.
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Uniprot ID
Primary ID:
Q9Y271

Secondarily ID:
B2R954
D3DTE4
Q5JS94
Q8IV19
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Ensembl ID
ENSG00000173198
HGNC ID
HGNC:17451
Subcellular Location
Cell membrane
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000026 , CHO-K1
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0408242
 Compound Info 
4-[1-(carboxymethyl)-7-[2-[4-[4-(3-chloro-2-methylphenyl)butoxy]phenyl]ethynyl]-2-methylindol-3-yl]butanoic acid
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C34H34ClNO5
  1
1
IC50 = 0.22 nM
 Bioactivity Info 
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CP0382287
 Compound Info 
3-[1-(carboxymethyl)-7-[2-[4-[4-(3-chloro-2-methylphenyl)butoxy]phenyl]ethynyl]-2-methylindol-3-yl]propanoic acid
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C33H32ClNO5
  1
1
IC50 = 0.32 nM
 Bioactivity Info 
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CP0448955
 Compound Info 
2-[1-(carboxymethyl)-7-[2-[4-[4-(3-chloro-2-methylphenyl)butoxy]phenyl]ethynyl]-2-methylindol-3-yl]acetic acid
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C32H30ClNO5
  1
1
IC50 = 0.47 nM
 Bioactivity Info 
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CP0418315
 Compound Info 
4-[1-(carboxymethyl)-7-[(E)-2-[4-[4-(3-chloro-2-methylphenyl)butoxy]phenyl]ethenyl]-2-methylindol-3-yl]butanoic acid
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C34H36ClNO5
  1
1
IC50 = 0.56 nM
 Bioactivity Info 
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CP0484535
 Compound Info 
4-[1-(carboxymethyl)-7-[(E)-2-[4-[4-(3-chloro-2-methylphenyl)butoxy]phenyl]ethenyl]indol-3-yl]butanoic acid
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C33H34ClNO5
  1
1
IC50 = 0.62 nM
 Bioactivity Info 
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CP0170068
 Compound Info 
(R-(R*,S*-(E,E,Z,Z)))-N-(S-(1-(4-Carboxy-1-hydroxybutyl)-2,4,6,9-pentadecatetraenyl)-L-cysteinyl)glycine
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C25H40N2O6S
  2
1
IC50 = 0.7 nM
 Bioactivity Info 
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2
Ki = 0.29 nM
 Bioactivity Info 
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CP0382290
 Compound Info 
4-[3-(2-carboxyethyl)-7-[2-[4-[4-(3-chloro-2-methylphenyl)butoxy]phenyl]ethynyl]-2-methylindol-1-yl]butanoic acid
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C35H36ClNO5
  1
1
IC50 = 0.79 nM
 Bioactivity Info 
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CP0382284
 Compound Info 
4-[1-(carboxymethyl)-2-methyl-7-[(E)-2-[4-[4-(2,3,4,5-tetrafluorophenyl)butoxy]phenyl]ethenyl]indol-3-yl]butanoic acid
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C33H31F4NO5
  1
1
IC50 = 0.8 nM
 Bioactivity Info 
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CP0487602
 Compound Info 
4-[1-(carboxymethyl)-7-[(E)-2-[4-[4-(2,3,6-trifluorophenyl)butoxy]phenyl]ethenyl]indol-3-yl]butanoic acid
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C32H30F3NO5
  1
1
IC50 = 1 nM
 Bioactivity Info 
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CP0380609
 Compound Info 
4-[1-(3-carboxypropyl)-7-[2-[4-[4-(3-fluoro-2-methylphenyl)butoxy]phenyl]ethynyl]-2-methylindol-3-yl]butanoic acid
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C36H38FNO5
  1
1
IC50 = 1.1 nM
 Bioactivity Info 
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CP0408236
 Compound Info 
4-[1-(carboxymethyl)-7-[(E)-2-[4-[4-(3-fluoro-2-methylphenyl)butoxy]phenyl]ethenyl]-2-methylindol-3-yl]butanoic acid
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C34H36FNO5
  1
1
IC50 = 1.1 nM
 Bioactivity Info 
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CP0381577
 Compound Info 
4-[1-(3-carboxypropyl)-7-[2-[4-[4-(3-chloro-2-methylphenyl)butoxy]phenyl]ethynyl]-2-methylindol-3-yl]butanoic acid
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C36H38ClNO5
  1
1
IC50 = 1.5 nM
 Bioactivity Info 
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CP0408240
 Compound Info 
4-[1-(carboxymethyl)-7-[(E)-2-[4-(4-phenoxybutoxy)phenyl]ethenyl]indol-3-yl]butanoic acid
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C32H33NO6
  1
1
IC50 = 1.5 nM
 Bioactivity Info 
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CP0411554
 Compound Info 
4-[1-(carboxymethyl)-2-methyl-7-[(E)-2-[4-[4-(2,3,4,6-tetrafluorophenyl)butoxy]phenyl]ethenyl]indol-3-yl]butanoic acid
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C33H31F4NO5
  1
1
IC50 = 1.6 nM
 Bioactivity Info 
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CP0427949
 Compound Info 
4-[1-(3-carboxypropyl)-4-fluoro-7-[2-[4-[4-(3-fluoro-2-methylphenyl)butoxy]phenyl]ethynyl]-2-methylindol-3-yl]butanoic acid
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C36H37F2NO5
  1
1
IC50 = 1.7 nM
 Bioactivity Info 
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CP0566585
 Compound Info 
4-[1-(carboxymethyl)-2-methyl-7-[(E)-2-[4-[4-(2,3,5,6-tetrafluorophenyl)butoxy]phenyl]ethenyl]indol-3-yl]butanoic acid
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C33H31F4NO5
  1
1
IC50 = 2.2 nM
 Bioactivity Info 
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CP0382282
 Compound Info 
4-[1-(carboxymethyl)-2-methyl-7-[(E)-2-[4-[4-(2,3,6-trifluorophenyl)butoxy]phenyl]ethenyl]indol-3-yl]butanoic acid
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C33H32F3NO5
  1
1
IC50 = 2.4 nM
 Bioactivity Info 
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CP0494801
 Compound Info 
4-[1-(3-carboxypropyl)-2-methyl-7-[2-[4-[4-(2,3,4,6-tetrafluorophenyl)butoxy]phenyl]ethynyl]indol-3-yl]butanoic acid
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C35H33F4NO5
  1
1
IC50 = 2.8 nM
 Bioactivity Info 
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CP0484534
 Compound Info 
4-[1-(carboxymethyl)-7-[(E)-2-[4-[4-(3-fluoro-2-methylphenyl)butoxy]phenyl]ethenyl]indol-3-yl]butanoic acid
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C33H34FNO5
  1
1
IC50 = 2.9 nM
 Bioactivity Info 
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CP0428430
 Compound Info 
4-[1-(carboxymethyl)-7-[(E)-2-[4-[4-(3-chlorophenyl)butoxy]phenyl]ethenyl]indol-3-yl]butanoic acid
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C32H32ClNO5
  1
1
IC50 = 3.1 nM
 Bioactivity Info 
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CP0382286
 Compound Info 
4-[1-(carboxymethyl)-7-[(E)-2-[4-(4-phenylbutoxy)phenyl]ethenyl]indol-3-yl]butanoic acid
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C32H33NO5
  1
1
IC50 = 3.4 nM
 Bioactivity Info 
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CP0456062
 Compound Info 
4-[1-(3-carboxypropyl)-7-[2-[4-[4-(3-chloro-2-methylphenyl)butoxy]phenyl]ethynyl]-4-fluoro-2-methylindol-3-yl]butanoic acid
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C36H37ClFNO5
  1
1
IC50 = 3.4 nM
 Bioactivity Info 
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CP0428421
 Compound Info 
4-[1-(carboxymethyl)-2-methyl-7-[(E)-2-[4-(4-phenylbutoxy)phenyl]ethenyl]indol-3-yl]butanoic acid
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C33H35NO5
  1
1
IC50 = 4.1 nM
 Bioactivity Info 
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CP0484537
 Compound Info 
4-[3-(carboxymethyl)-7-[2-[4-[4-(3-chloro-2-methylphenyl)butoxy]phenyl]ethynyl]-2-methylindol-1-yl]butanoic acid
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C34H34ClNO5
  1
1
IC50 = 5.5 nM
 Bioactivity Info 
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CP0432238
 Compound Info 
4-[1-(3-carboxypropyl)-4-fluoro-2-methyl-7-[2-[4-[4-(2,3,4,6-tetrafluorophenyl)butoxy]phenyl]ethynyl]indol-3-yl]butanoic acid
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C35H32F5NO5
  1
1
IC50 = 7.4 nM
 Bioactivity Info 
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CP0379267
 Compound Info 
4-(3-carboxypropyl)-8-[[4-(4-phenylbutoxy)benzoyl]amino]-2,3-dihydro-1,4-benzoxazine-2-carboxylic acid
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C30H32N2O7
  1
1
IC50 = 8.5 nM
 Bioactivity Info 
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CP0531079
 Compound Info 
3-[1-(2-carboxyethyl)-7-[2-[4-[4-(3-chloro-2-methylphenyl)butoxy]phenyl]ethynyl]-2-methylindol-3-yl]propanoic acid
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C34H34ClNO5
  1
1
IC50 = 10 nM
 Bioactivity Info 
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CP0408238
 Compound Info 
4-[1-(3-carboxypropyl)-7-[2-[4-[4-(3-chloro-2-methylphenyl)butoxy]phenyl]ethynyl]-6-fluoro-2-methylindol-3-yl]butanoic acid
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C36H37ClFNO5
  1
1
IC50 = 11 nM
 Bioactivity Info 
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CP0382289
 Compound Info 
3-[3-(carboxymethyl)-7-[2-[4-[4-(3-chloro-2-methylphenyl)butoxy]phenyl]ethynyl]-2-methylindol-1-yl]propanoic acid
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C33H32ClNO5
  1
1
IC50 = 12 nM
 Bioactivity Info 
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CP0408239
 Compound Info 
4-[3-(carboxymethyl)-4-[(E)-2-[4-(4-phenoxybutoxy)phenyl]ethenyl]indol-1-yl]butanoic acid
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C32H33NO6
  1
1
IC50 = 12 nM
 Bioactivity Info 
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CP0456063
 Compound Info 
4-[1-(3-carboxypropyl)-7-[2-[4-[4-(3-chloro-2-methylphenyl)butoxy]phenyl]ethynyl]-5-fluoro-2-methylindol-3-yl]butanoic acid
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C36H37ClFNO5
  1
1
IC50 = 16 nM
 Bioactivity Info 
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CP0448956
 Compound Info 
4-[1-(2-carboxyethyl)-7-[2-[4-[4-(3-chloro-2-methylphenyl)butoxy]phenyl]ethynyl]-2-methylindol-3-yl]butanoic acid
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C35H36ClNO5
  1
1
IC50 = 17 nM
 Bioactivity Info 
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CP0448958
 Compound Info 
5-[3-(2-carboxyethyl)-7-[2-[4-[4-(3-chloro-2-methylphenyl)butoxy]phenyl]ethynyl]-2-methylindol-1-yl]pentanoic acid
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C36H38ClNO5
  1
1
IC50 = 25 nM
 Bioactivity Info 
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CP0484536
 Compound Info 
4-[1-(carboxymethyl)-7-[(E)-2-[4-[4-(2-methoxyphenyl)butoxy]phenyl]ethenyl]-2-methylindol-3-yl]butanoic acid
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C34H37NO6
  1
1
IC50 = 46 nM
 Bioactivity Info 
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CP0382291
 Compound Info 
5-[3-(3-carboxypropyl)-7-[2-[4-[4-(3-chloro-2-methylphenyl)butoxy]phenyl]ethynyl]-2-methylindol-1-yl]pentanoic acid
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C37H40ClNO5
  1
1
IC50 = 56 nM
 Bioactivity Info 
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CP0533704
 Compound Info 
5-[3-(carboxymethyl)-7-[2-[4-[4-(3-chloro-2-methylphenyl)butoxy]phenyl]ethynyl]-2-methylindol-1-yl]pentanoic acid
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C35H36ClNO5
  1
1
IC50 = 65 nM
 Bioactivity Info 
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CP0379718
 Compound Info 
3-[(3-carboxycyclohexyl)carbamoyl]-4-[3-[4-(4-cyclohexyloxybutoxy)phenyl]propoxy]benzoic acid
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C34H45NO8
  1
1
IC50 > 10000 nM
 Bioactivity Info 
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Cell Line ID: CL000011 , CHO
 Cell Line Info 
Cell Line ID: CL000053 , COS-7
 Cell Line Info 
Cell Line ID: CL000006 , HEK293
 Cell Line Info 
Cell Line ID: CL000125 , MCB3901
 Cell Line Info 
Cell Line ID: CL000100 , U-937
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0037675
 Compound Info 
2-[1-[[(1R)-1-[3-[(E)-2-(7-chloroquinolin-2-yl)ethenyl]phenyl]-3-[2-(2-hydroxypropan-2-yl)phenyl]propyl]sulfanylmethyl]cyclopropyl]acetic acid
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C35H36ClNO3S
  2
1 IC50 = 0.5 nM
2 IC50 = 2.3 nM
CP0045344
 Compound Info 
4-(5-cyclopentyloxycarbonylamino-1-methyl-1H-indol-3-ylmethyl)-3-methoxy-N-o-tolylsulfonylbenzamide
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C31H33N3O6S
  1
1 IC50 = 1.9 nM
CP0145665
 Compound Info 
8-[4-(4-phenylbutyloxy)benzoyl]amino-2-(tetrazol-5-yl)-4-oxo-4H-1-benzopyran
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C27H23N5O4
  1
1 IC50 = 4.3 nM
CP0170068
 Compound Info 
(R-(R*,S*-(E,E,Z,Z)))-N-(S-(1-(4-Carboxy-1-hydroxybutyl)-2,4,6,9-pentadecatetraenyl)-L-cysteinyl)glycine
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C25H40N2O6S
  2
1 IC50 = 7 nM
2 Ki = 0.6 nM
Clinical Information about the Protein
Target 1 ( Leukotriene CysLT1 receptor (CYSLTR1) )
Target Type Successful Target
Disease 1 Target-related Disease  1
1 Asthma [ICD-11: CA23]
Approved Drug(s) 4 Approved Drugs  4
1 Cinalukast
 Drug Info 
Approved
Asthma
2 Montelukast
 Drug Info 
Approved
Asthma
3 Pranlukast
 Drug Info 
Approved
Asthma
4 Zafirlukast
 Drug Info 
Approved
Asthma
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 Masilukast
 Drug Info 
Phase 2
Asthma
Discontinued Drug(s) 6 Discontinued Drugs  6
1 Ablukast
 Drug Info 
Discontinued in Phase 3
Asthma
2 RG-7152
 Drug Info 
Discontinued in Phase 1
Asthma
3 FPL-55712
 Drug Info 
Terminated
Asthma
4 ICI-198615
 Drug Info 
Terminated
Asthma
5 LM-1376
 Drug Info 
Terminated
Asthma
6 Tomelukast
 Drug Info 
Terminated
Asthma