General Information of the Protein
Protein ID
PT01819
Protein Name
Thromboxane A2 receptor
Secondarily
Protein Name
Prostanoid TP receptor
Gene Name
TBXA2R
Sequence
MWPNGSSLGPCFRPTNITLEERRLIASPWFAASFCVVGLASNLLALSVLAGARQGGSHTRSSFLTFLCGLVLTDFLGLLVTGTIVVSQHAALFEWHAVDPGCRLCRFMGVVMIFFGLSPLLLGAAMASERYLGITRPFSRPAVASQRRAWATVGLVWAAALALGLLPLLGVGRYTVQYPGSWCFLTLGAESGDVAFGLLFSMLGGLSVGLSFLLNTVSVATLCHVYHGQEAAQQRPRDSEVEMMAQLLGIMVVASVCWLPLLVFIAQTVLRNPPAMSPAGQLSRTTEKELLIYLRVATWNQILDPWVYILFRRAVLRRLQPRLSTRPRSLSLQPQLTQRSGLQ
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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 thromboxane A2 (TXA2), a potent stimulator of platelet aggregation. The activity of this receptor is mediated by a G-protein that activates a phosphatidylinositol-calcium second messenger system. In the kidney, the binding of TXA2 to glomerular TP receptors causes intense vasoconstriction. Activates phospholipase C.
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Uniprot ID
Primary ID:
P21731

Secondarily ID:
O75228
Q6DK52
Q9UCY1
Q9UCY2
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HGNC ID
HGNC:11608
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
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0383448
 Compound Info 
5-[2-[5-chloro-2-[(4-fluorophenyl)methoxy]phenyl]-5-methylpyrrol-1-yl]-2-methylbenzoic acid
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C26H21ClFNO3
  2
1
IC50 = 39.81 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
2
Ki = 15.85 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0438269
 Compound Info 
7-[3,5-Dihydroxy-2-(3-hydroxy-4-phenoxy-butyl)-cyclopentyl]-heptanoic acid
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C22H34O6
  1
1
IC50 = 6909 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0388465
 Compound Info 
2-[1-[4-[[(2R)-1-ethyl-2,3-dihydroindol-2-yl]methoxy]-2-methylbenzoyl]-2-methylindol-3-yl]acetic acid
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C30H30N2O4
  1
1
IC50 = 7600 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0095751
 Compound Info 
(5Z,13E,15S)-9alpha,11alpha,15-trihydroxyprosta-5,13-dien-1-oic acid
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C20H34O5
  1
1
IC50 > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0295469
 Compound Info 
(Z)-7-{(1R,2R,3R,5S)-2-[(E)-(R)-4-(3-Chloro-phenoxy)-3-hydroxy-but-1-enyl]-3,5-dihydroxy-cyclopentyl}-hept-5-enoic acid
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C22H29ClO6
  1
1
IC50 > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0372737
 Compound Info 
7-[3,5-Dihydroxy-2-(3-hydroxy-4-m-tolylsulfanyl-butyl)-cyclopentyl]-heptanoic acid
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C23H36O5S
  1
1
IC50 > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0374214
 Compound Info 
7-{2-[4-(3-Chloro-phenylsulfanyl)-3-hydroxy-butyl]-3,5-dihydroxy-cyclopentyl}-heptanoic acid
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C22H33ClO5S
  1
1
IC50 > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0377752
 Compound Info 
7-[3,5-Dihydroxy-2-(3-hydroxy-4-phenylamino-butyl)-cyclopentyl]-heptanoic acid
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C22H35NO5
  1
1
IC50 > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0395236
 Compound Info 
7-{2-[4-(3-Fluoro-phenylsulfanyl)-3-hydroxy-butyl]-3,5-dihydroxy-cyclopentyl}-heptanoic acid
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C22H33FO5S
  1
1
IC50 > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0402541
 Compound Info 
7-{(1R,2R,3R,5S)-2-[(R)-4-(3-Chloro-phenoxy)-3-hydroxy-butyl]-3,5-dihydroxy-cyclopentyl}-heptanoic acid
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C22H33ClO6
  1
1
IC50 > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0402565
 Compound Info 
7-[(1R,2R,3R,5S)-3,5-Dihydroxy-2-((R)-3-hydroxy-5-phenyl-pentyl)-cyclopentyl]-heptanoic acid
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C23H36O5
  1
1
IC50 > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0432809
 Compound Info 
7-[(1R,2R,3R,5S)-3,5-Dihydroxy-2-((S)-3-hydroxy-octyl)-cyclopentyl]-heptanoic acid
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C20H38O5
  1
1
IC50 > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0432810
 Compound Info 
7-{3,5-Dihydroxy-2-[3-hydroxy-4-(thiazol-2-ylsulfanyl)-butyl]-cyclopentyl}-heptanoic acid
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C19H31NO5S2
  1
1
IC50 > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0433187
 Compound Info 
7-[3,5-Dihydroxy-2-(3-hydroxy-4-phenylsulfanyl-butyl)-cyclopentyl]-heptanoic acid
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C22H34O5S
  1
1
IC50 > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0445340
 Compound Info 
7-{3,5-Dihydroxy-2-[3-hydroxy-4-(thiophen-2-ylsulfanyl)-butyl]-cyclopentyl}-heptanoic acid
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C20H32O5S2
  1
1
IC50 > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0448266
 Compound Info 
7-{3,5-Dihydroxy-2-[3-hydroxy-4-(3-trifluoromethyl-phenylsulfanyl)-butyl]-cyclopentyl}-heptanoic acid
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C23H33F3O5S
  1
1
IC50 > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0425413
 Compound Info 
2-[2-methyl-1-[2-methyl-4-[[(2S)-4-methyl-2,3-dihydro-1,4-benzoxazin-2-yl]methoxy]benzoyl]indol-3-yl]acetic acid
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C29H28N2O5
  1
1
IC50 > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0431698
 Compound Info 
2-[1-[2-chloro-4-[[(2S)-4-methyl-2,3-dihydro-1,4-benzoxazin-2-yl]methoxy]benzoyl]-5-fluoro-2-methylindol-3-yl]acetic acid
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C28H24ClFN2O5
  1
1
IC50 > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0400679
 Compound Info 
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
  1
1
Ki = 260 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0376006
 Compound Info 
2-[2,5-dimethyl-1-[4-[[(2S)-4-methyl-2,3-dihydro-1,4-benzoxazin-2-yl]methoxy]benzoyl]indol-3-yl]acetic acid
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C29H28N2O5
  1
1
Ki > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0378355
 Compound Info 
2-[5-fluoro-2-methyl-1-[4-[[(2S)-4-methyl-2,3-dihydro-1,4-benzoxazin-2-yl]methoxy]benzoyl]indol-3-yl]acetic acid
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C28H25FN2O5
  1
1
Ki > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0388261
 Compound Info 
2-[2-methyl-1-[4-[[(2S)-4-methyl-2,3-dihydro-1,4-benzoxazin-2-yl]methoxy]benzoyl]indol-3-yl]acetic acid
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C28H26N2O5
  1
1
Ki > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0377711
 Compound Info 
2-[4-methyl-3-[[2-methyl-4-[[(2S)-4-methyl-2,3-dihydro-1,4-benzoxazin-2-yl]methoxy]benzoyl]amino]phenyl]acetic acid
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C27H28N2O5
  1
1
Ki > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0380709
 Compound Info 
2-[4-chloro-3-[[2-chloro-4-[[(2S)-4-methyl-2,3-dihydro-1,4-benzoxazin-2-yl]methoxy]benzoyl]amino]phenyl]acetic acid
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C25H22Cl2N2O5
  1
1
Ki > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0387733
 Compound Info 
2-[3-methyl-5-[[2-methyl-4-[[(2S)-4-methyl-2,3-dihydro-1,4-benzoxazin-2-yl]methoxy]benzoyl]amino]phenyl]acetic acid
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C27H28N2O5
  1
1
Ki > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0390164
 Compound Info 
2-[3-[[2-chloro-4-[[(2S)-4-methyl-2,3-dihydro-1,4-benzoxazin-2-yl]methoxy]benzoyl]amino]-4-fluorophenyl]acetic acid
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C25H22ClFN2O5
  1
1
Ki > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0494477
 Compound Info 
2-[3-[[2-methyl-4-[[(2S)-4-methyl-2,3-dihydro-1,4-benzoxazin-2-yl]methoxy]benzoyl]amino]phenyl]acetic acid
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C26H26N2O5
  1
1
Ki > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000026 , CHO-K1
 Cell Line Info 
Cell Line ID: CL000053 , COS-7
 Cell Line Info 
Cell Line ID: CL000006 , HEK293
 Cell Line Info 
Cell Line ID: CL000050 , HEK293-A
 Cell Line Info 
Cell Line ID: CL000065 , HEK293-EBNA
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0272414
 Compound Info 
US11149018, Example 34
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C26H27BrClN3O3
  1
1 IC50 ~ 2210 nM
CP0070143
 Compound Info 
2-(2-benzoyl-3,4-dihydro-1H-pyrido[4,3-b]indol-5-yl)acetic acid
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C20H18N2O3
  1
1 IC50 > 25000 nM
CP0048953
 Compound Info 
(R)-3-(3-(4-fluorophenylsulfonamido)-1,2,3,4-tetrahydrocarbazol-9-yl)propanoic acid
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C21H21FN2O4S
  2
1 Ki = 0.58 nM
2 Ki = 4.5 nM
CP0108218
 Compound Info 
(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 = 1200 nM
CP0032668
 Compound Info 
(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
  2
1 Ki = 3804 nM
2 Ki ~ 3804 nM
CP0041889
 Compound Info 
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 = 7100 nM
Clinical Information about the Protein
Target 1 ( Thromboxane A2 receptor (TBXA2R) )
Target Type Successful Target
Disease 11 Target-related Diseases  11
1 Erectile dysfunction [ICD-11: HA01.1]
2 Acute myocardial infarction [ICD-11: BA41]
3 Perennial allergic rhinitis [ICD-11: CA08.03]
4 Aspirin-induced asthma [ICD-11: CA23.20]
5 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
6 Coronary heart disease [ICD-11: BA80.Z]
7 Allergic asthma [ICD-11: CA23.0]
8 Thrombosis [ICD-11: DB61-GB90]
9 Angina pectoris [ICD-11: BA40]
10 Asthma [ICD-11: CA23]
11 Cardiovascular disease [ICD-11: BA00-BE2Z]
Approved Drug(s) 3 Approved Drugs  3
1 Alprostadil
 Drug Info 
Approved
Erectile dysfunction
2 Ridogrel
 Drug Info 
Approved
Acute myocardial infarction
3 LAROPIPRANT
 Drug Info 
Phase 4
Coronary heart disease
Clinical Trial Drug(s) 3 Clinical Trial Drugs  3
1 Ramatroban
 Drug Info 
Phase 2/3
Perennial allergic rhinitis
2 Ifetroban
 Drug Info 
Phase 2
Aspirin-induced asthma
3 PGF2alpha
 Drug Info 
Clinical trial
Solid tumour/cancer
Discontinued Drug(s) 6 Discontinued Drugs  6
1 Seratrodast
 Drug Info 
Discontinued in Phase 3
Allergic asthma
2 Linotroban
 Drug Info 
Discontinued in Phase 2
Thrombosis
3 CGS-22652
 Drug Info 
Discontinued in Phase 1
Angina pectoris
4 Sulotroban
 Drug Info 
Terminated
Asthma
5 UP-116-77
 Drug Info 
Terminated
Thrombosis
6 Vapiprost
 Drug Info 
Terminated
Cardiovascular disease