Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T74238 | Target Info | |||
| Target Name | Leukotriene CysLT2 receptor (CYSLTR2) | ||||
| Synonyms |
hGPCR21; PSEC0146; HPN321; Gprotein coupled receptor HG57; Gprotein coupled receptor GPCR21; G-protein coupled receptor HG57; G-protein coupled receptor GPCR21; Cysteinyl leukotriene receptor 2; CysLTR2; CYSLT2R; CYSLT2
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| Target Type | Clinical trial Target | ||||
| Gene Name | CYSLTR2 | ||||
| Biochemical Class | GPCR rhodopsin | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 22 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Zafirlukast
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Approved | Compound Info | ||
| Synonyms |
Accolate; Accoleit; Aeronix; Olmoran; Respix; Zafirst; AstraZeneca brand of zafirlukast; Menarini brand of zafirlukast; Novartis brand of zafirlukast; Zeneca brand of zafirkulast; Accolate (TN); Accoleit (TN); Vanticon (TN); Zafirlukast [USAN:BAN:INN]; Accolate, Accoleit, Vanticon, Zafirlukast; Zafirlukast (JAN/USAN/INN); Cyclopentyl N-[3-[[2-methoxy-4-[(2-methylphenyl)sulfonylcarbamoyl]phenyl]methyl]-1-methylindol-5-yl]carbamate; Cyclopentyl 3-(2-methoxy-4-((o-tolylsulfonyl)carbamoyl)benzyl)-1-methylindole-5-carbamate; Cyclopentyl 3-[2-methoxy-4-(2-methylphenylsulfonylcarbamoyl)benzyl]-1-methyl-1H-indol-5-ylcarbamate; Cyclopentyl [3-(2-methoxy-4-{[(2-methylphenyl)sulfonyl]carbamoyl}benzyl)-1-methyl-1H-indol-5-yl]carbamate; Cyclopentyl (1-methyl-3-{[2-(methyloxy)-4-({[(2-methylphenyl)sulfonyl]amino}carbonyl)phenyl]methyl}-1H-indol-5-yl)carbamate; Carbamic acid, (3-((2-methoxy-4-((((2-methylphenyl)sulfonyl)amino)carbonyl)phenyl)methyl)-1-methyl-1H-indol-5-yl)-, cyclopentyl ester; 4-(5-cyclopentyloxy-carbonylamino-1-methyl-indol-3-ylmethyl)-3-methoxy-N-o-tolylsulfonylbenzamide; 4-(5-cyclopentyloxycarbonylamino-1-methyl-1H-indol-3-ylmethyl)-3-methoxy-N-o-tolylsulfonylbenzamide; 4-(5-cyclopentyloxycarbonylamino-2-methylindol-3-yl-methyl)-3-methoxy-N-O-tolylsulfonylbenzamide
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| Activity |
IC50 = 58000 nM
|
[1] | |||
| Compound Name |
3-[3-[3-[(E)-2-(7-Chloroquinolin-2-yl)ethenyl]anilino]-3-oxopropyl]-1H-indole-2-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3808985; BDBM50172345
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| Activity |
IC50 = 50000 nM
|
[1] | |||
| Compound Name |
3-[(E)-3-[3-[(E)-2-(7-Chloroquinolin-2-yl)ethenyl]anilino]-3-oxoprop-1-enyl]-1H-indole-2-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3809230; BDBM50172348
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| Activity |
IC50 = 58000 nM
|
[1] | |||
| Compound Name |
3-[(E)-3-[3-[(E)-2-(7-Chloroquinolin-2-yl)ethenyl]anilino]-3-oxoprop-1-enyl]-4,6-difluoro-1H-indole-2-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3808968; BDBM50172338
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| Activity |
IC50 = 76000 nM
|
[1] | |||
| Compound Name |
6-Chloro-3-[(E)-3-[3-[(E)-2-(7-chloroquinolin-2-yl)ethenyl]anilino]-3-oxoprop-1-enyl]-1H-indole-2-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3809333; BDBM50172342
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| Activity |
IC50 = 87000 nM
|
[1] | |||
| Compound Name |
4,6-Dichloro-3-[(E)-3-[[3-[(E)-2-(7-chloroquinolin-2-yl)ethenyl]phenyl]methoxy]-3-oxoprop-1-enyl]-1H-indole-2-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3808623; BDBM50172333
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| Activity |
IC50 ~ 100000 nM
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[1] | |||
| Compound Name |
4,6-Dichloro-3-[(E)-3-(4-cyanobutoxy)-3-oxoprop-1-enyl]-1H-indole-2-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3810333; BDBM50172352
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
4,6-Dichloro-3-[(E)-3-oxo-3-phenoxyprop-1-enyl]-1H-indole-2-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3809809; BDBM50172332
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
4,6-Dichloro-3-[(E)-3-cyclohexyloxy-3-oxoprop-1-enyl]-1H-indole-2-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3808815; BDBM50172356
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
5-Chloro-3-[(E)-3-[3-[(E)-2-(7-chloroquinolin-2-yl)ethenyl]anilino]-3-oxoprop-1-enyl]-1H-indole-2-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3809556; BDBM50172343
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| Activity |
IC50 ~ 100000 nM
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[1] | |||
| Compound Name |
3-[(E)-3-[[3-[(E)-2-(7-Chloroquinolin-2-yl)ethenyl]phenyl]methoxy]-3-oxoprop-1-enyl]-1H-indole-2-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3809628; BDBM50172351
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| Activity |
IC50 ~ 100000 nM
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[1] | |||
| Compound Name |
4,6-Dichloro-3-[(E)-3-(cyclohexylmethoxy)-3-oxoprop-1-enyl]-1H-indole-2-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3809862; BDBM50172355
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
4,6-Dichloro-3-[(E)-3-[3-[(E)-2-(7-chloroquinolin-2-yl)ethenyl]anilino]-3-oxoprop-1-enyl]-1H-indole-2-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3808880; BDBM50172349
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
4,6-Dichloro-3-[(E)-3-oxo-3-pentoxyprop-1-enyl]-1H-indole-2-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3809152; BDBM50172354
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| Activity |
IC50 ~ 100000 nM
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[1] | |||
| Compound Name |
4,6-Dichloro-3-[(E)-3-oxo-3-(3-phenylpropoxy)prop-1-enyl]-1H-indole-2-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3810209; BDBM50172359
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| Activity |
IC50 ~ 100000 nM
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[1] | |||
| Compound Name |
[3-[(E)-2-(7-Chloroquinolin-2-yl)ethenyl]phenyl]methyl (E)-3-(4,6-dichloro-1H-indol-3-yl)prop-2-enoate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3810142; BDBM50172350
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
3-[(E)-3-[3-[(E)-2-(7-Chloroquinolin-2-yl)ethenyl]anilino]-3-oxoprop-1-enyl]-6-methoxy-1H-indole-2-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3808608; BDBM50172336
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| Activity |
IC50 ~ 100000 nM
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[1] | |||
| Compound Name |
4,6-Dichloro-3-[(E)-3-(4-methylpentoxy)-3-oxoprop-1-enyl]-1H-indole-2-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3809106; BDBM50172353
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| Activity |
IC50 ~ 100000 nM
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[1] | |||
| Compound Name |
4,6-Dichloro-3-[(E)-3-oxo-3-phenylmethoxyprop-1-enyl]-1H-indole-2-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3810094; BDBM50172331
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
4,6-Dichloro-3-[(E)-3-oxo-3-(4-phenylbutoxy)prop-1-enyl]-1H-indole-2-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3808722; BDBM50172357
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
7-Chloro-3-[(E)-3-[3-[(E)-2-(7-chloroquinolin-2-yl)ethenyl]anilino]-3-oxoprop-1-enyl]-1H-indole-2-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3809483; BDBM50172341
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
4,6-Dichloro-3-[(E)-3-oxo-3-(2-phenylethoxy)prop-1-enyl]-1H-indole-2-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3810389; BDBM50172360
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Discovery of 3-Substituted 1H-Indole-2-carboxylic Acid Derivatives as a Novel Class of CysLT1 Selective Antagonists. ACS Med Chem Lett. 2016 Jan 22;7(3):335-9. | ||||
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