Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T99954 | Target Info | |||
| Target Name | Prostacyclin receptor (PTGIR) | ||||
| Synonyms |
Prostanoid IP receptor; Prostaglandin I2 receptor; PRIPR; PGI2 receptor; PGI receptor; IP prostanoid receptor
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| Target Type | Successful Target | ||||
| Gene Name | PTGIR | ||||
| Biochemical Class | GPCR rhodopsin | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 19 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Ramatroban
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Phase 2/3 | Compound Info | ||
| Synonyms |
116649-85-5; Baynas; BAY u3405; Bay u-3405; Bay u 3406; Bay-u-3405; Bay u 3405; BAY-u 3405; UNII-P1ALI72U6C; C21H21FN2O4S; 3-[(3R)-3-[(4-fluorophenyl)sulfonylamino]-1,2,3,4-tetrahydrocarbazol-9-yl]propanoic acid; P1ALI72U6C; 3-(4-Fluorophenylsulfonamido)-1,2,3,4-tetrahydro-9-carbazole propanoic acid; CHEMBL361812; (+)-(3R)-3-(p-Fluorobenzenesulfonamido)-1,2,3,4-tetrahydrocarbazole-9-propionic acid; NCGC00167519-01; EN-137774; DSSTox_RID_81819; Baynas (TN); Ramatroban (JAN/INN); [3H]ramatroban
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
OC-000459
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Phase 2 | Compound Info | ||
| Synonyms |
OC-1768; OC-2125; OC-2184; OC-459; OC-499; ODC-9101; CRTH2 antagonists (asthma/allergy), Oxagen
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| Activity |
IC50 = 57900 nM
|
[1] | |||
| Compound Name |
MK-7246
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Phase 1 | Compound Info | ||
| Synonyms |
IDDBCP261213; IDDBCP271467
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
PGF2alpha
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Clinical trial | Compound Info | ||
| Synonyms |
Amoglandin; Cerviprost; Cyclosin; Enzaprost; Panacelan; prostaglandin F2alpha
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
AH6809
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Investigative | Compound Info | ||
| Synonyms |
AH 6809; AH-6809
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| Activity |
Ki ~ 100000 nM
|
[3] | |||
| Compound Name |
3-(2-(naphthalen-2-ylmethyl)phenyl)acrylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL423815; 3-(2-(naphthalen-2-ylmethyl)phenyl)acrylic acid; SCHEMBL7922112; SCHEMBL7922115; BDBM50097792; 2-(2-Naphthylmethyl)benzeneacrylic acid; (E)-3-(2-Naphthalen-2-ylmethyl-phenyl)-acrylic acid
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| Activity |
Ki ~ 100000 nM
|
[4] | |||
| Compound Name |
1-Methyl-3-[2-[4-[(6-oxo-11,12-dihydrobenzo[c][1]benzazocin-5-yl)methyl]phenyl]phenyl]sulfonyl-1-(2-phenylethyl)urea
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL92539; BDBM50081439
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| Activity |
Ki = 52000 nM
|
[5] | |||
| Compound Name |
{2'-[(Benzyloxycarbonyl-ethyl-amino)-methyl]-6-methoxy-4'-trifluoromethyl-biphenyl-3-yl}-acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1916700; SCHEMBL142883; BDBM50357286
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| Activity |
IC50 = 56200 nM
|
[6] | |||
| Compound Name |
(E)-3-[2-(4-Methylsulfanyl-benzyl)-phenyl]-acrylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL165010; SCHEMBL7929810; SCHEMBL7929816; (E)-3-[2-[(4-methylsulfanylphenyl)methyl]phenyl]prop-2-enoic Acid; BDBM50097794; 2-[4-(Methylthio)benzyl]benzeneacrylic acid
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| Activity |
Ki ~ 76000 nM
|
[4] | |||
| Compound Name |
2-[(6R)-6-[(4-Fluorophenyl)sulfonyl-methylamino]-5,6,7,8-tetrahydropyrido[2,3-b]indol-9-yl]acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL552211; BDBM50296985; (R)-2-(6-(4-fluoro-N-methylphenylsulfonamido)-7,8-dihydro-5H-pyrido[2,3-b]indol-9(6H)-yl)acetic acid
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
(R)-2-(8-(4-Fluoro-N-methylphenylsulfonamido)-6,7,8,9-tetrahydro-5H-pyrido[3,2-b]indol-5-yl)acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL550465; SCHEMBL2516080; BDBM50296983
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
(R)-2-(3-(4-Fluoro-N-methylphenylsulfonamido)-1,2,3,4-tetrahydropyrido[1,2-a]indol-10-yl)acetic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL564920; SCHEMBL3242718; BDBM50296981
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2-[(6R)-6-[(4-Fluorophenyl)sulfonyl-methylamino]-5,6,7,8-tetrahydropyrido[3,4-b]indol-9-yl]acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL550868; BDBM50296984; (R)-2-(6-(4-fluoro-N-methylphenylsulfonamido)-7,8-dihydro-5H-pyrido[3,4-b]indol-9(6H)-yl)acetic acid
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2-[(3R)-3-[(4-Fluorophenyl)sulfonyl-methylamino]-1,2,3,4,4b,8a-hexahydrocarbazol-9-yl]acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL563664; BDBM50296979; 2-((3R)-3-(4-fluoro-N-methylphenylsulfonamido)-3,4-dihydro-1H-carbazol-9(2H,4bH,8aH)-yl)acetic acid
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2-[(9R)-9-[(4-Fluorophenyl)sulfonyl-methylamino]-7,8,9,10-tetrahydropyrido[1,2-b]isoindol-6-yl]acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL564845; BDBM50296982
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
[2'-[(Cyclopropanecarbonyl-ethyl-amino)-methyl]-4'-(6-ethoxy-pyridin-3-yl)-6-methoxy-biphenyl-3-yl]-acetic acid sodium salt
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1668898
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| Activity |
IC50 ~ 100000 nM
|
[7] | |||
| Compound Name |
2-[(8R)-8-[(4-Fluorophenyl)sulfonyl-methylamino]-6,7,8,9-tetrahydropyrazino[2,3-b]indol-5-yl]acetic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL556849; BDBM50296986
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|
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| Activity |
IC50 ~ 100000 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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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
Click to Show/Hide
|
Compound Info | |||
| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | 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 2 | Synthesis and biological evaluation of prostaglandin-F alkylphosphinic acid derivatives as bone anabolic agents for the treatment of osteoporosis. J Med Chem. 2001 Nov 22;44(24):4157-69. | ||||
| REF 3 | Prostanoid receptor EP2 as a therapeutic target. J Med Chem. 2014 Jun 12;57(11):4454-65. | ||||
| REF 4 | Structure-activity relationship on the human EP3 prostanoid receptor by use of solid-support chemistry. Bioorg Med Chem Lett. 2001 Mar 12;11(5):747-9. | ||||
| REF 5 | New class of biphenylene dibenzazocinones as potent ligands for the human EP1 prostanoid receptor. Bioorg Med Chem Lett. 1999 Sep 20;9(18):2699-704. | ||||
| 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 | Sodium [2'-[(cyclopropanecarbonyl-ethyl-amino)-methyl]-4'-(6-ethoxy-pyridin-3-yl)-6-methoxy-biphenyl-3-yl]-acetate (AM432): a potent, selective prostaglandin D2 receptor antagonist. Bioorg Med Chem Lett. 2011 Feb 1;21(3):1036-40. | ||||
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