Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T61722 | Target Info | |||
| Target Name | Prostaglandin D2 receptor 2 (PTGDR2) | ||||
| Synonyms |
PTGDR2; Chemoattractant receptor-homologous molecule expressed on Th2 cells; CD294
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| Target Type | Clinical trial Target | ||||
| Gene Name | PTGDR2 | ||||
| Biochemical Class | GPCR rhodopsin | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 41 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
3-[6-(4-Fluoro-benzenesulfonylamino)-1,2,3,4-tetrahydro-carbazol-9-yl]-2-methyl-propionic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL264243; BDBM50162914
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| Activity |
Ki ~ 50000 nM
|
[1] | |||
| Compound Name |
3-[6-(Propane-1-sulfonylamino)-1,2,3,4-tetrahydro-carbazol-9-yl]-propionic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL360243; BDBM50162890
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| Activity |
Ki ~ 50000 nM
|
[1] | |||
| Compound Name |
4-Anilino-1-benzoyl-2-methyl-1,2,3,4-tetrahydroquinoline
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Investigative | Compound Info | ||
| Synonyms |
(2-Methyl-4-(phenylamino)-3,4-dihydroquinolin-1(2H)-yl)(phenyl)methanone; Methanone,[3,4-dihydro-2-methyl-4-(phenylamino)-1(2H)-quinolinyl]phenyl-; 2-methyl-4-(phenylamino)(1,2,3,4-tetrahydroquinolyl) phenyl ketone; CBMicro_014647; Cambridge id 5228479; Oprea1_677532; Oprea1_793479; CHEMBL1079830; CTK5F5698; DTXSID20341109; SMSF0004931; SBB041945; AKOS000270645; AKOS016039881; MCULE-6438707783; ST002624; BIM-0014444.P001; EU-0041844; AB00075954-01; 1-Benzoyl-2-methyl-N-phenyl-1,2,3,4-tetrahydro-4-quinolinamine #; 1-benzoyl-2-methyl-N-phenyl-1,2,3,4-tetrahydroquinolin-4-amine; Quinoline, 1,2,3,4-tetrahydro-1-benzoyl-2-methyl-4-phenylamino-; (4-Anilino-2-methyl-3,4-dihydroquinolin-1(2H)-yl)(phenyl)methanone
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
3-[6-(4-Fluoro-benzenesulfonylamino)-1,2,3,4-tetrahydro-carbazol-9-yl]-butyric acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL183595; BDBM50162920
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| Activity |
Ki ~ 50000 nM
|
[1] | |||
| Compound Name |
3-[6-(Toluene-2-sulfonylamino)-1,2,3,4-tetrahydro-carbazol-9-yl]-propionic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL182387; BDBM50162904
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| Activity |
Ki ~ 50000 nM
|
[1] | |||
| Compound Name |
3-[6-(3-Phenyl-ureido)-1,2,3,4-tetrahydro-carbazol-9-yl]-propionic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL180834; BDBM50162912
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| Activity |
Ki ~ 50000 nM
|
[1] | |||
| Compound Name |
N-(2-Methyl-1,2,3,4-tetrahydroquinolin-4-yl)-N-phenylacetamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1076041; CBMicro_015277; Cambridge id 5249233; Oprea1_315087; Oprea1_671581; SCHEMBL5402565; BDBM50312298; STK040971; AKOS000611573; AKOS022077335; MCULE-7171442129; ST002621; BIM-0015268.P001; DB-110017; EU-0073373; N-(2-methyl(4-1,2,3,4-tetrahydroquinolyl))-N-phenylacetamide; (+/-)-N-(2-methyl-1,2,3,4-tetrahydroquinolin-4-yl)-N-phenylacetamide
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
{2-[6-(4-Fluoro-benzenesulfonylamino)-1,2,3,4-tetrahydro-carbazol-9-yl]-ethyl}-phosphonic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL181611; BDBM50162907
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| Activity |
Ki ~ 50000 nM
|
[1] | |||
| Compound Name |
4-(2-(2,4-Dichlorophenylsulfonamido)-4-(ethylcarbamoyl)phenoxy)-3-methoxybenzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL570205; BDBM50302825
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
3-(6-Amino-1,2,3,4-tetrahydro-carbazol-9-yl)-propionic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL359684; BDBM50162910
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| Activity |
Ki ~ 50000 nM
|
[1] | |||
| Compound Name |
3-(6-Benzoylamino-1,2,3,4-tetrahydro-carbazol-9-yl)-propionic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL360074; BDBM50162915
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|
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| Activity |
Ki ~ 50000 nM
|
[1] | |||
| Compound Name |
2-[(7R)-7-[(4-Fluorophenyl)sulfonyl-methylamino]-6,7,8,9-tetrahydropyrido[2,3-b]indolizin-10-yl]acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL557117; BDBM50296987
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| Activity |
IC50 = 51000 nM
|
[4] | |||
| Compound Name |
{2-[({[(4-Methylphenyl)amino]acetyl}hydrazono)methyl]phenoxy}acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL216175; ZINC4982104; BDBM50200274; STK009210; AKOS000960902
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| Activity |
IC50 = 60200 nM
|
[5] | |||
| Compound Name |
2-[2-[2-[[(4S,5R)-4-Methyl-2-oxo-5-phenyl-1,3-oxazolidin-3-yl]methyl]-4-(trifluoromethyl)phenyl]phenyl]acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1916690; BDBM50357294
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| Activity |
IC50 = 62000 nM
|
[6] | |||
| Compound Name |
(+/-)-N-(2-Methyl-1-(phenylsulfonyl)-1,2,3,4-tetrahydroquinolin-4-yl)-N-phenylacetamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1081772; SCHEMBL13776136; BDBM50312300
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| Activity |
IC50 = 62000 nM
|
[2] | |||
| Compound Name |
3-[3-[2-[[(4S,5R)-4-Methyl-2-oxo-5-phenyl-1,3-oxazolidin-3-yl]methyl]-4-(trifluoromethyl)phenyl]phenyl]propanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1916689; BDBM50357293
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| Activity |
IC50 = 75000 nM
|
[6] | |||
| Compound Name |
(2-{(E)-[2-(1H-Benzimidazol-1-ylacetyl)hydrazinylidene]methyl}phenoxy)acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL216122; BDBM50200253; STK024521; ZINC31841316; AKOS005379909; (2-{(E)-[(1H-benzimidazol-1-ylacetyl)hydrazono]methyl}phenoxy)acetic acid; (2-{[(1H-benzimidazol-1-ylacetyl)hydrazono]methyl}phenoxy)acetic acid
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| Activity |
IC50 = 81700 nM
|
[5] | |||
| Compound Name |
3-[2-[[(4S,5R)-4-Methyl-2-oxo-5-phenyl-1,3-oxazolidin-3-yl]methyl]-4-(trifluoromethyl)phenyl]benzoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1916688; BDBM50357292
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| Activity |
IC50 = 91000 nM
|
[6] | |||
| Compound Name |
[2-(3'-Cyano-biphenyl-2-ylmethyl)-4-(4-fluoro-phenyl)-thiazol-5-yl]-acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL603187; SCHEMBL5056633; BDBM50309406; 2-(2-((3''-cyanobiphenyl-2-yl)methyl)-4-(4-fluorophenyl)thiazol-5-yl)acetic acid; 2-[2-[[2-(3-cyanophenyl)phenyl]methyl]-4-(4-fluorophenyl)-1,3-thiazol-5-yl]acetic acid
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| Activity |
IC50 ~ 100000 nM
|
[7] | |||
| Compound Name |
2-(4-(4-Chlorophenyl)-2-((6-chloropyridin-2-yl)(phenyl)methyl)thiazol-5-yl)acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL597542; BDBM50309281
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|
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| Activity |
IC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
2-(2-(Bis(4-fluorophenyl)methyl)-4-(2-(pyrrolidin-1-yl)pyridin-4-yl)thiazol-5-yl)acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL602137; BDBM50309328
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| Activity |
IC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
2-(4-(4-Chlorophenyl)-2-(1-phenylpropyl)thiazol-5-yl)acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL606858; SCHEMBL5060247; BDBM50309256; 2-[4-(4-chlorophenyl)-2-(1-phenylpropyl)-1,3-thiazol-5-yl]acetic acid
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| Activity |
IC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
2-(2-(2-Fluorophenylamino)-4-(4-phenoxyphenyl)thiazol-5-yl)acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL598964; Oprea1_620512; ZINC657580; BDBM50309419
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| Activity |
IC50 ~ 100000 nM
|
[7] | |||
| Compound Name |
2-(2-(2-Bromobenzyl)-4-(4-fluorophenyl)thiazol-5-yl)acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL590310; SCHEMBL5052402; BDBM50309409; [2-(2-Bromo-benzyl)-4-(4-fluoro-phenyl)-thiazol-5-yl]-acetic acid; 2-[2-[(2-bromophenyl)methyl]-4-(4-fluorophenyl)-1,3-thiazol-5-yl]acetic acid
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| Activity |
IC50 ~ 100000 nM
|
[7] | |||
| Compound Name |
2-(2-(2-Chlorophenylamino)-4-(4-phenoxyphenyl)thiazol-5-yl)acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL598965; Oprea1_483146; BDBM50309418; ZINC13425541; AKOS000594323; MCULE-7737671576
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| Activity |
IC50 ~ 100000 nM
|
[7] | |||
| Compound Name |
{2-[(E)-{2-[(3-Methyl-1H-pyrazol-5-yl)carbonyl]hydrazinylidene}methyl]phenoxy}acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL217287; BDBM50200261; STK249286; AKOS005422835; BIM-0049446.P001; ST50420168; [2-(({[(3-methyl-1H-pyrazol-5-yl)carbonyl]hydrazono}methyl)phenoxy]acetic acid; 2-(2-{(1E)-2-[(3-methylpyrazol-5-yl)carbonylamino]-2-azavinyl}phenoxy)acetic a cid
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| Activity |
IC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
2-Amino-4-(4-chlorophenyl)thiazole-5-acetic acid
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Investigative | Compound Info | ||
| Synonyms |
[2-Amino-4-(4-chloro-phenyl)-thiazol-5-yl]-acetic acid; 2-[2-amino-4-(4-chlorophenyl)-1,3-thiazol-5-yl]acetic acid; CHEMBL600846; [2-amino-4-(4-chlorophenyl)-1,3-thiazol-5-yl]acetic acid; (2-Amino-4-(4-chlorophenyl)-1,3-thiazol-5-yl)acetic acid; 2-(2-amino-4-(4-chlorophenyl)thiazol-5-yl)acetic acid; BRN 0535972; 2-amino-4-(4-chlorophenyl)-thiazole-5-acetic acid; 2-Amino-4-p-chlorophenylthiazole-5-acetic acid; Kwas 2-amino-4-p-chlorofenylo-tiazolo-5-octowy [Polish]; Kwas 2-amino-4-p-chlorofenylo-tiazolo-5-octowy; 5-Thiazoleacetic acid, 2-amino-4-(4-chlorophenyl)-; Thiazole-5-acetic acid, 2-amino-4-(p-chlorophenyl)-; SCHEMBL10359068; CTK7J2650; DTXSID30198045; ZINC3643763; 4292AE; BBL012314; BDBM50309300; MFCD01681656; SBB027417; STK739587; AKOS000302437; MCULE-3524357544; VS-03279; BB 0218709; ST50305929; VU0610883-1; F3325-0072; 3-AMINO-3-(3-BROMO-4-HYDROXY-5-METHOXY-PHENYL)-PROPIONICACID
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| Activity |
IC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
2-(2-(Bis(4-fluorophenyl)methyl)-4-(2-(dimethylamino)pyridin-4-yl)thiazol-5-yl)acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL591044; BDBM50309326
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| Activity |
IC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
2-(5-Methyl-6-(4-(methylsulfonyl)phenylsulfonyl)-6H-thieno[2,3-b]pyrrol-4-yl)acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1684721; SCHEMBL400709; BDBM50338152; 2-[5-methyl-6-(4-methylsulfonylphenyl)sulfonylthieno[2,3-b]pyrrol-4-yl]acetic acid
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| Activity |
IC50 ~ 100000 nM
|
[9] | |||
| Compound Name |
2-(4-(2-(Azetidin-1-yl)pyridin-4-yl)-2-(bis(4-fluorophenyl)methyl)thiazol-5-yl)acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL591281; BDBM50309327
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| Activity |
IC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
2-(4-(6-Amino-5-methylpyridin-3-yl)-2-(bis(4-fluorophenyl)methyl)thiazol-5-yl)acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL592782; BDBM50309331
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| Activity |
IC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
2-(4-(2-(4-Acetylpiperazin-1-yl)pyridin-4-yl)-2-(bis(4-fluorophenyl)methyl)thiazol-5-yl)acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL607084; BDBM50309329
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| Activity |
IC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
2-(4-(4-Chlorophenyl)-2-(4-phenylpiperidin-4-yl)thiazol-5-yl)acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL591751; SCHEMBL5052331; BDBM50309257; 2-[4-(4-chlorophenyl)-2-(4-phenylpiperidin-4-yl)-1,3-thiazol-5-yl]acetic acid
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| Activity |
IC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
2-(2-Benzhydryl-4-(5-chloro-2-methoxyphenyl)thiazol-5-yl)acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL590399; SCHEMBL5060666; BDBM50309289; 2-[2-benzhydryl-4-(5-chloro-2-methoxyphenyl)-1,3-thiazol-5-yl]acetic acid
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| Activity |
IC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
[4-(4-Fluoro-phenyl)-2-(2'-methoxy-biphenyl-2-ylmethyl)-thiazol-5-yl]-acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL591516; SCHEMBL5052362; BDBM50309403; 2-(4-(4-fluorophenyl)-2-((2''-methoxybiphenyl-2-yl)methyl)thiazol-5-yl)acetic acid; 2-[4-(4-fluorophenyl)-2-[[2-(2-methoxyphenyl)phenyl]methyl]-1,3-thiazol-5-yl]acetic acid
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| Activity |
IC50 ~ 100000 nM
|
[7] | |||
| Compound Name |
[4-(4-Fluoro-phenyl)-2-(3'-trifluoromethoxy-biphenyl-2-ylmethyl)-thiazol-5-yl]-acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL591517; SCHEMBL5055111; BDBM50309402; 2-(4-(4-fluorophenyl)-2-((3''-(trifluoromethoxy)biphenyl-2-yl)methyl)thiazol-5-yl)acetic acid; 2-[4-(4-fluorophenyl)-2-[[2-[3-(trifluoromethoxy)phenyl]phenyl]methyl]-1,3-thiazol-5-yl]acetic acid
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| Activity |
IC50 ~ 100000 nM
|
[7] | |||
| Compound Name |
2-(4-(4-Chlorophenyl)-2-(cyclohexyl(phenyl)methyl)thiazol-5-yl)acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL600363; SCHEMBL5062281; BDBM50309274; [4-(4-Chloro-phenyl)-2-(cyclohexyl-phenyl-methyl)-thiazol-5-yl]-acetic acid; 2-[4-(4-chlorophenyl)-2-[cyclohexyl(phenyl)methyl]-1,3-thiazol-5-yl]acetic acid
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| Activity |
IC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
2-(2-Benzhydryl-4-(4-(trifluoromethyl)phenyl)thiazol-5-yl)acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL601279; SCHEMBL5056410; BDBM50309288; 2-[2-benzhydryl-4-[4-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl]acetic acid
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| Activity |
IC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
2-(2-(Bis(4-fluorophenyl)methyl)-4-(4-sulfamoylphenyl)thiazol-5-yl)acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL597333; BDBM50309306
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| Activity |
IC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
2-(4-(4-Chlorophenyl)-2-(2-phenoxybenzyl)thiazol-5-yl)acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL591042; SCHEMBL5056446; BDBM50309400; [4-(4-Chloro-phenyl)-2-(2-phenoxy-benzyl)-thiazol-5-yl]-acetic acid; 2-[4-(4-chlorophenyl)-2-[(2-phenoxyphenyl)methyl]-1,3-thiazol-5-yl]acetic acid
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| Activity |
IC50 ~ 100000 nM
|
[7] | |||
| Compound Name |
2-(2-Benzhydryl-4-(2,5-dimethoxyphenyl)thiazol-5-yl)acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL605357; SCHEMBL5056601; BDBM50309290; 2-[2-benzhydryl-4-(2,5-dimethoxyphenyl)-1,3-thiazol-5-yl]acetic acid
Click to Show/Hide
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| Activity |
IC50 ~ 100000 nM
|
[8] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Isosteric ramatroban analogs: selective and potent CRTH-2 antagonists. Bioorg Med Chem Lett. 2005 Mar 15;15(6):1749-53. | ||||
| REF 2 | Tetrahydroquinoline derivatives as CRTH2 antagonists. Bioorg Med Chem Lett. 2009 Dec 15;19(24):6840-4. | ||||
| REF 3 | Discovery and optimization of CRTH2 and DP dual antagonists. Bioorg Med Chem Lett. 2009 Nov 15;19(22):6419-23. | ||||
| REF 4 | Novel tricyclic antagonists of the prostaglandin D2 receptor DP2 with efficacy in a murine model of allergic rhinitis. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4647-51. | ||||
| REF 5 | Novel selective orally active CRTH2 antagonists for allergic inflammation developed from in silico derived hits. J Med Chem. 2006 Nov 16;49(23):6638-41. | ||||
| REF 6 | Discovery and optimization of a biphenylacetic acid series of prostaglandin D2 receptor DP2 antagonists with efficacy in a murine model of allergic rhinitis. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6608-12. | ||||
| REF 7 | Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 1. Bioorg Med Chem Lett. 2010 Feb 1;20(3):1177-80. | ||||
| REF 8 | Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 2. Bioorg Med Chem Lett. 2010 Feb 1;20(3):1181-5. | ||||
| REF 9 | Thienopyrrole acetic acids as antagonists of the CRTH2 receptor. Bioorg Med Chem Lett. 2011 Mar 15;21(6):1861-4 | ||||
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