General Information of the Protein
Protein ID
PT01054
Protein Name
Prostaglandin D2 receptor
Secondarily
Protein Name
Prostanoid DP receptor
Gene Name
PTGDR
Sequence
MKSPFYRCQNTTSVEKGNSAVMGGVLFSTGLLGNLLALGLLARSGLGWCSRRPLRPLPSVFYMLVCGLTVTDLLGKCLLSPVVLAAYAQNRSLRVLAPALDNSLCQAFAFFMSFFGLSSTLQLLAMALECWLSLGHPFFYRRHITLRLGALVAPVVSAFSLAFCALPFMGFGKFVQYCPGTWCFIQMVHEEGSLSVLGYSVLYSSLMALLVLATVLCNLGAMRNLYAMHRRLQRHPRSCTRDCAEPRADGREASPQPLEELDHLLLLALMTVLFTMCSLPVIYRAYYGAFKDVKEKNRTSEEAEDLRALRFLSVISIVDPWIFIIFRSPVFRIFFHKIFIRPLRYRSRCSNSTNMESSL
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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)
>
Prostanoid receptor
Function
Receptor for prostaglandin D2 (PGD2). The activity of this receptor is mainly mediated by G(s) proteins that stimulate adenylate cyclase, resulting in an elevation of intracellular cAMP. A mobilization of calcium is also observed, but without formation of inositol 1,4,5-trisphosphate (By similarity). Involved in PLA2G3-dependent maturation of mast cells. PLA2G3 is secreted by immature mast cells and acts on nearby fibroblasts upstream to PTDGS to synthesize PGD2, which in turn promotes mast cell maturation and degranulation via PTGDR (By similarity).
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Uniprot ID
Primary ID:
Q13258

Secondarily ID:
G3V5L3
Q13250
Q13251
Q1ZZ52
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Ensembl ID
ENSG00000168229
HGNC ID
HGNC:9591
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: CL000011 , CHO
Compound ID Compound Name Compound Formula
CP0437055
2-[1-[4-[[(2S)-7-fluoro-4-methyl-2,3-dihydro-1,4-benzoxazin-2-yl]methoxy]benzoyl]-2-methylindol-4-yl]acetic acid
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C28H25FN2O5
 2
1
IC50 = 0.81 nM
   TI
   LI
   LO
   TS
2
Ki = 5.3 nM
   TI
   LI
   LO
   TS
CP0400679
2-[2-methyl-1-[4-[[(2S)-4-methyl-2,3-dihydro-1,4-benzoxazin-2-yl]methoxy]benzoyl]indol-4-yl]acetic acid
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C28H26N2O5
 2
1
IC50 = 1.2 nM
   TI
   LI
   LO
   TS
2
Ki = 3.5 nM
   TI
   LI
   LO
   TS
CP0485482
2-[2-methyl-1-[4-[[(2R)-4-methyl-2,3-dihydro-1,4-benzoxazin-2-yl]methoxy]benzoyl]indol-4-yl]acetic acid
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C28H26N2O5
 2
1
IC50 = 10 nM
   TI
   LI
   LO
   TS
2
Ki = 170 nM
   TI
   LI
   LO
   TS
CP0439527
2-[1-[4-[[(3R)-2,3-dihydro-1,4-benzodioxin-3-yl]methoxy]benzoyl]-2-methylindol-4-yl]acetic acid
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C27H23NO6
 2
1
IC50 = 30 nM
   TI
   LI
   LO
   TS
2
Ki = 10 nM
   TI
   LI
   LO
   TS
CP0451828
2-[1-[4-(2,3-dihydro-1-benzofuran-2-ylmethoxy)benzoyl]-2-methylindol-4-yl]acetic acid
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C27H23NO5
 2
1
IC50 = 30 nM
   TI
   LI
   LO
   TS
2
Ki = 20 nM
   TI
   LI
   LO
   TS
CP0486394
2-[1-[4-(3,4-dihydro-2H-chromen-2-ylmethoxy)benzoyl]-2-methylindol-4-yl]acetic acid
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C28H25NO5
 2
1
IC50 = 30 nM
   TI
   LI
   LO
   TS
2
Ki = 50 nM
   TI
   LI
   LO
   TS
CP0486387
2-[1-[4-(1,3-benzodioxol-2-ylmethoxy)benzoyl]-2-methylindol-4-yl]acetic acid
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C26H21NO6
 2
1
IC50 = 50 nM
   TI
   LI
   LO
   TS
2
Ki = 30 nM
   TI
   LI
   LO
   TS
CP0086399
2-[6-chloro-2-[4-(4-ethylphenyl)benzoyl]-3,4-dihydro-1H-pyrido[4,3-b]indol-5-yl]acetic acid
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C28H25ClN2O3
 1
1
IC50 = 120 nM
   TI
   LI
   LO
   TS
CP0374553
2-[2-methyl-1-[4-(2-phenoxyethoxy)benzoyl]indol-4-yl]acetic acid
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C26H23NO5
 2
1
IC50 = 250 nM
   TI
   LI
   LO
   TS
2
Ki = 290 nM
   TI
   LI
   LO
   TS
CP0442380
2-[1-[4-[[(3S)-2,3-dihydro-1,4-benzodioxin-3-yl]methoxy]benzoyl]-2-methylindol-4-yl]acetic acid
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C27H23NO6
 2
1
IC50 = 270 nM
   TI
   LI
   LO
   TS
2
Ki = 130 nM
   TI
   LI
   LO
   TS
CP0156868
2-[6-chloro-8-fluoro-2-(naphthalene-1-carbonyl)-3,4-dihydro-1H-pyrido[4,3-b]indol-5-yl]acetic acid
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C24H18ClFN2O3
 1
1
IC50 = 310 nM
   TI
   LI
   LO
   TS
CP0042410
2-[8-chloro-2-(naphthalene-1-carbonyl)-3,4-dihydro-1H-pyrido[4,3-b]indol-5-yl]acetic acid
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C24H19ClN2O3
 1
1
IC50 = 690 nM
   TI
   LI
   LO
   TS
CP0042409
2-[2-[4-(4-ethylphenyl)benzoyl]-3,4-dihydro-1H-pyrido[4,3-b]indol-5-yl]acetic acid
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C28H26N2O3
 1
1
IC50 = 780 nM
   TI
   LI
   LO
   TS
CP0055416
2-[2-(naphthalene-1-carbonyl)-3,4-dihydro-1H-pyrido[4,3-b]indol-5-yl]acetic acid
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C24H20N2O3
 1
1
IC50 = 780 nM
   TI
   LI
   LO
   TS
CP0087804
ACT-129968
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C24H19FN2O3
 1
1
IC50 = 1290 nM
   TI
   LI
   LO
   TS
CP0261961
2-[2-(naphthalene-1-carbonyl)-8-(trifluoromethyl)-3,4-dihydro-1H-pyrido[4,3-b]indol-5-yl]acetic acid
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C25H19F3N2O3
 1
1
IC50 = 2200 nM
   TI
   LI
   LO
   TS
CP0130562
2-[8-methyl-2-(naphthalene-1-carbonyl)-3,4-dihydro-1H-pyrido[4,3-b]indol-5-yl]acetic acid
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C25H22N2O3
 1
1
IC50 = 2700 nM
   TI
   LI
   LO
   TS
CP0055418
2-[6-chloro-2-(3-chlorobenzoyl)-8-fluoro-3,4-dihydro-1H-pyrido[4,3-b]indol-5-yl]acetic acid
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C20H15Cl2FN2O3
 1
1
IC50 = 4100 nM
   TI
   LI
   LO
   TS
CP0050067
2-[2-[(5-acetyl-2-methoxyphenyl)methylsulfanyl]benzimidazol-1-yl]acetic acid
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C19H18N2O4S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0115424
2-[2-[[5-(butylcarbamoyl)-2-methoxyphenyl]methylsulfanyl]-5-fluorobenzimidazol-1-yl]acetic acid
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C22H24FN3O4S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0126760
2-[2-[(5-acetyl-2-methoxyphenyl)methylsulfanyl]-5-fluorobenzimidazol-1-yl]acetic acid
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C19H17FN2O4S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0154070
2-[2-[[5-(2,3-dihydroindole-1-carbonyl)-2-methoxyphenyl]methylsulfanyl]-5-fluorobenzimidazol-1-yl]acetic acid
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C26H22FN3O4S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0045673
2-[2-(3-chlorobenzoyl)-8-fluoro-3,4-dihydro-1H-pyrido[4,3-b]indol-5-yl]acetic acid
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C20H16ClFN2O3
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0055420
2-[2-(3-chlorobenzoyl)-3,4-dihydro-1H-pyrido[4,3-b]indol-5-yl]acetic acid
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C20H17ClN2O3
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0055873
2-[8-fluoro-2-[2-(1H-indol-3-yl)acetyl]-3,4-dihydro-1H-pyrido[4,3-b]indol-5-yl]acetic acid
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C23H20FN3O3
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0055874
2-[8-fluoro-2-(thiophene-2-carbonyl)-3,4-dihydro-1H-pyrido[4,3-b]indol-5-yl]acetic acid
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C18H15FN2O3S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0055877
2-[2-benzoyl-8-(trifluoromethyl)-3,4-dihydro-1H-pyrido[4,3-b]indol-5-yl]acetic acid
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C21H17F3N2O3
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0070143
2-(2-benzoyl-3,4-dihydro-1H-pyrido[4,3-b]indol-5-yl)acetic acid
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C20H18N2O3
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0083568
2-[8-fluoro-2-(3-naphthalen-1-ylpropanoyl)-3,4-dihydro-1H-pyrido[4,3-b]indol-5-yl]acetic acid
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C26H23FN2O3
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0086409
2-[8-fluoro-2-(2-naphthalen-1-ylacetyl)-3,4-dihydro-1H-pyrido[4,3-b]indol-5-yl]acetic acid
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C25H21FN2O3
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0445860
2-[1-[4-(3,4-dihydro-2H-chromen-3-ylmethoxy)benzoyl]-2-methylindol-4-yl]acetic acid
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C28H25NO5
 1
1
Ki = 390 nM
   TI
   LI
   LO
   TS
CP0391849
2-[1-(2,5-dichlorophenyl)sulfonyl-5-fluoro-2-methylindol-3-yl]acetic acid
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C17H12Cl2FNO4S
 1
1
Ki = 1872 nM
   TI
   LI
   LO
   TS
CP0378076
(1-Benzenesulfonyl-5-fluoro-2-methyl-1H-indol-3-yl)-acetic acid
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C17H14FNO4S
 1
1
Ki = 4860 nM
   TI
   LI
   LO
   TS
CP0498276
2-[5-fluoro-1-(3-fluorophenyl)sulfonyl-2-methylindol-3-yl]acetic acid
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C17H13F2NO4S
 1
1
Ki = 6890 nM
   TI
   LI
   LO
   TS
CP0391851
2-[5-fluoro-1-(4-methoxyphenyl)sulfonyl-2-methylindol-3-yl]acetic acid
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C18H16FNO5S
 1
1
Ki = 7710 nM
   TI
   LI
   LO
   TS
CP0378230
2-[1-(4-chlorophenyl)sulfonyl-5-fluoro-2-methylindol-3-yl]acetic acid
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C17H13ClFNO4S
 1
1
Ki = 8460 nM
   TI
   LI
   LO
   TS
CP0259564
2-[5-fluoro-2-methyl-1-(4-methylsulfonylphenyl)sulfonylindol-3-yl]acetic acid
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C18H16FNO6S2
 1
1
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0446446
2-[5-fluoro-2-methyl-1-(4-methylphenyl)sulfonylindol-3-yl]acetic acid
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C18H16FNO4S
 1
1
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0456427
2-(1-butylsulfonyl-5-fluoro-2-methylindol-3-yl)acetic acid
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C15H18FNO4S
 1
1
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0485411
2-[1-(1,2-dimethylimidazol-4-yl)sulfonyl-5-fluoro-2-methylindol-3-yl]acetic acid
   Show/Hide
C16H16FN3O4S
 1
1
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0503860
2-[5-fluoro-1-(4-fluorophenyl)sulfonyl-2-methylindol-3-yl]acetic acid
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C17H13F2NO4S
 1
1
Ki > 10000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0343798
2-[(3R)-4-[(4-chlorophenyl)methyl]-7-fluoro-5-methylsulfonyl-2,3-dihydro-1H-cyclopenta[b]indol-3-yl]acetic acid
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C21H19ClFNO4S
 1
1 IC50 = 1.4 nM
CP0095751
(5Z,13E,15S)-9alpha,11alpha,15-trihydroxyprosta-5,13-dien-1-oic acid
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C20H34O5
 1
1 IC50 = 4500 nM
CP0070143
2-(2-benzoyl-3,4-dihydro-1H-pyrido[4,3-b]indol-5-yl)acetic acid
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C20H18N2O3
 1
1 IC50 > 10000 nM
CP0231084
2-(4-(4-chlorobenzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid
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C21H19ClFNO4S
 1
1 Ki = 0.57 nM
CP0041889
2-((R)-4-(4-chlorobenzyl)-5-(1-hydroxyethyl)-7-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid
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C23H24ClNO5S
 1
1 Ki = 1.8 nM
CP0108218
(R)-2-(4-(4-chlorobenzyl)-5-acetyl-7-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid
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C23H22ClNO5S
 1
1 Ki = 2.6 nM
CP0032668
(R)-2-(7-(4-fluoro-N-methylphenylsulfonamido)-6,7,8,9-tetrahydropyrido[1,2-a]indol-10-yl)acetic acid
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C21H21FN2O4S
 1
1 Ki = 373 nM
CP0112284
CHEMBL3933704
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C23H26FNO5
 1
1 Ki = 1850 nM
CP0112283
APD-811
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C23H26ClNO5
 1
1 Ki = 2600 nM
Clinical Information about the Protein
Target 1 ( Prostaglandin D2 receptor (PTGDR) )
Target Type Clinical trial Target
Disease 5 Target-related Diseases  5
1 Asthma [ICD-11: CA23]
2 Allergy [ICD-11: 4A80-4A85]
3 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
4 Coronary heart disease [ICD-11: BA80.Z]
5 Rhinitis [ICD-11: FA20]
Approved Drug(s) 1 Approved Drug  1
1 LAROPIPRANT Phase 4
Coronary heart disease
Clinical Trial Drug(s) 4 Clinical Trial Drugs  4
1 Setipiprant Phase 3
Asthma
2 AMG 853 Phase 2
Asthma
3 S-555739 Phase 2
Allergy
4 PGF2alpha Clinical trial
Solid tumour/cancer
Discontinued Drug(s) 1 Discontinued Drug  1
1 S-5751 Discontinued in Phase 2
Rhinitis
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT02987 Prostaglandin D2 receptor Mus musculus, Mouse