TBXA2R

Summary

TBXA2R (thromboxane A2 receptor, HGNC:11608) is a protein-coding gene on chromosome 19p13.3, encoding Thromboxane A2 receptor (P21731). Receptor for thromboxane A2 (TXA2), a potent stimulator of platelet aggregation.

This gene encodes a member of the G protein-coupled receptor family. The protein interacts with thromboxane A2 to induce platelet aggregation and regulate hemostasis. A mutation in this gene results in a bleeding disorder. Multiple transcript variants encoding different isoforms have been found for this gene.

Source: NCBI Gene 6915 — RefSeq curated summary.

At a glance

• Gene–disease (curated): qualitative platelet defect (Moderate, ClinGen) — +3 more curated relationships
• Clinical variants (ClinVar): 260 total — 4 likely-pathogenic
• Phenotypes (HPO): 8
• Druggable target: yes — 210 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_001060

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:11608
Approved symbol	TBXA2R
Name	thromboxane A2 receptor
Location	19p13.3
Locus type	gene with protein product
Status	Approved
Ensembl gene	ENSG00000006638
Ensembl biotype	protein_coding
OMIM	188070
Entrez	6915

Gene structure

Transcript identifiers

Ensembl transcripts: 7 — 6 protein_coding, 1 protein_coding_CDS_not_defined

ENST00000375190, ENST00000411851, ENST00000587717, ENST00000589966, ENST00000882306, ENST00000882307, ENST00000882308

RefSeq mRNA: 2 — MANE Select: NM_001060 NM_001060, NM_201636

CCDS: CCDS42467, CCDS54198

Canonical transcript exons

ENST00000375190 — 3 exons

Exon	Start	End
ENSE00001307725	3606530	3606875
ENSE00001338026	3599849	3600717
ENSE00001754466	3594507	3595933

Expression profiles

Bgee: expression breadth ubiquitous, 241 present calls, max score 92.19.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 6.4491 / max 158.8165, expressed in 1226 samples.

FANTOM5 promoters (3 alternative TSS)

Promoter ID	TPM avg	Samples expressed
178322	5.5101	1179
178321	0.9030	342
178320	0.0360	11

Top tissues by expression

276 total, by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
tendon of biceps brachii	UBERON:0008188	92.19	silver quality
type B pancreatic cell	CL:0000169	91.43	gold quality
olfactory bulb	UBERON:0002264	91.28	silver quality
blood vessel layer	UBERON:0004797	90.83	gold quality
descending thoracic aorta	UBERON:0002345	90.53	gold quality
buccal mucosa cell	CL:0002336	90.40	gold quality
popliteal artery	UBERON:0002250	89.49	gold quality
right coronary artery	UBERON:0001625	89.48	gold quality
tibial artery	UBERON:0007610	89.47	gold quality
aorta	UBERON:0000947	89.11	gold quality
thoracic aorta	UBERON:0001515	88.71	gold quality
ascending aorta	UBERON:0001496	88.53	gold quality
skeletal muscle tissue of rectus abdominis	UBERON:0004511	87.73	silver quality
vena cava	UBERON:0004087	87.57	gold quality
left coronary artery	UBERON:0001626	86.21	gold quality
coronary artery	UBERON:0001621	86.17	gold quality
triceps brachii	UBERON:0001509	85.66	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	84.00	gold quality
saphenous vein	UBERON:0007318	83.39	gold quality
pancreatic ductal cell	CL:0002079	82.50	gold quality
renal glomerulus	UBERON:0000074	82.46	gold quality
metanephric glomerulus	UBERON:0004736	82.39	gold quality
body of tongue	UBERON:0011876	81.98	silver quality
gluteal muscle	UBERON:0002000	81.80	gold quality
cervix squamous epithelium	UBERON:0006922	81.18	gold quality
nipple	UBERON:0002030	81.06	gold quality
heart right ventricle	UBERON:0002080	80.84	silver quality
epithelial cell of pancreas	CL:0000083	80.66	silver quality
pharyngeal mucosa	UBERON:0000355	80.57	silver quality
sperm	CL:0000019	80.37	silver quality

Single-cell (SCXA)

Detected in 3 experiment(s), a significant marker in 0.

Experiment	Marker?	Max mean expression
E-ENAD-27	no	3.81
E-MTAB-6379	no	3.54
E-ANND-3	no	2.67

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): AR, EGR1, ESR1, ESR2, ETS1, EZH2, GATA1, NFE2, PPARG, SP1, SP3, SPI1, TFAP2A, THRB, TP63, WT1

miRNA regulators (miRDB)

46 targeting TBXA2R, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-6851-5P	100.00	65.63	1294
HSA-MIR-3689D	100.00	66.14	1181
HSA-MIR-6870-5P	99.99	68.55	2115
HSA-MIR-4723-5P	99.97	68.70	2034
HSA-MIR-5698	99.97	68.49	2029
HSA-MIR-7111-5P	99.97	68.48	2062
HSA-MIR-651-3P	99.94	73.48	5177
HSA-MIR-6783-3P	99.89	67.92	2059
HSA-MIR-4496	99.88	68.89	2236
HSA-MIR-6780A-5P	99.88	66.69	2776
HSA-MIR-182-5P	99.87	74.03	2589
HSA-MIR-4728-5P	99.85	69.39	4718
HSA-MIR-4739	99.84	65.25	1832
HSA-MIR-1321	99.84	65.30	1811
HSA-MIR-4756-5P	99.84	64.98	1809
HSA-MIR-6785-5P	99.82	68.68	4428
HSA-MIR-1273H-5P	99.77	66.32	2471
HSA-MIR-149-3P	99.72	68.22	3963
HSA-MIR-3714	99.71	70.74	2671
HSA-MIR-6779-5P	99.70	65.76	2363
HSA-MIR-6883-5P	99.69	68.05	3785
HSA-MIR-10393-5P	99.65	68.01	1368
HSA-MIR-1827	99.63	68.57	3265
HSA-MIR-4756-3P	99.62	66.30	1319
HSA-MIR-7106-5P	99.53	67.47	3574
HSA-MIR-1275	99.47	67.90	2749
HSA-MIR-6083	99.47	68.73	2393
HSA-MIR-508-5P	99.41	64.25	1248
HSA-MIR-6852-5P	99.17	66.69	2073
HSA-MIR-6809-5P	99.13	68.45	1223

Literature-anchored findings (GeneRIF, showing 40)

• Prostaglandin endoperoxides and thromboxane A2 activate the same receptor isoforms in human platelets. (PMID:11848439)
• Mapping of a ligand-binding site for the human thromboxane A2 receptor protein. (PMID:11877412)
• These results suggest TXA2 receptor polymorphism strongly interacts with IL-4R alpha polymorphism as a major determinant of high serum immunoglobulin E levels in atopic dermatitis. (PMID:11922633)
• The role of TXA2R 5’ UTR in differential isoform expression was studied. Exons E1 & E1b associated with TXA2R transcript(s), but their expression was mutually exclusive. Major transcription initiation sites were between -115 & -92 in E1 & at -99 in E1b. (PMID:12180983)
• Transcriptional activity of the 5’flanking region (PMID:12213432)
• analysis of third extracellular loop of human thromboxane A2 receptor (PMID:12781781)
• Thromboxane A2 (TXA2)-mediated platelet secretion and aggregation are important in thrombosis and the stable TXA2 analogue, U46619, induces two waves of platelet secretion, each of which precedes a distinct wave of platelet aggregation (PMID:12796499)
• These experiments indicate that the expression of the human thromboxane A2 receptor is differently regulated in platelet precursor cells by the protein kinase A and C pathway. (PMID:14580363)
• results indicate that oxidative stress induces maturation and stabilization of the thromboxane A(2)Receptor beta protein probably by intracellular translocation (PMID:14583632)
• TXA2 receptors mediated concurrent platelet aggregation and shape change responses, that are differentially modulated by different signaling pathways (PMID:14602550)
• A novel role is shown for isoform-specific regulation of angiogenesis by TBXA2R, providing the 1st functional significance for the existence of 2 TP isoforms in humans, & clarifying the mechanism by which TP signaling regulates FGFR1 kinetics & signaling. (PMID:14963009)
• Nm23-H2 had a cytoplasmic and nuclear localization but was induced to translocate to the plasma membrane upon stimulation of thromboxane A2 receptor beta to show extensive co-localization with the receptor. (PMID:14976202)
• Constitutive endocytosis of thromboxane A2 receptor forms a pool of receptors in the perinuclear recycling endosome from which they recycle to the cell surface, a process involved in preserving receptor sensitivity to agonist stimulation. (PMID:15134434)
• Results describe a three-dimensional structural model for the thromboxane A(2) receptor. (PMID:15233797)
• TPbeta, but not TPalpha, expression is required for the inhibition of VEGF-induced migration and angiogenesis. TP stimulation appears to limit angiogenesis, at least in part, by inhibiting the pro-angiogenic cytokine VEGF. (PMID:15242977)
• important physiological activators of platelets and exert their effects by acting on cell surface receptors (PMID:15354262)
• prostacyclin and thromboxane receptor dimerization facilitates thromboxane receptor-mediated cAMP generation (PMID:15471868)
• Thromboxane A2 receptor receptor activation causes DNA synthesis and cell proliferation of human bronchial smooth muscle cell (PMID:15519496)
• the actin cytoskeleton plays an essential role in TPbeta endocytosis (PMID:15845539)
• an interaction between Rab11 and TPbeta directs TPbeta recycling (PMID:16126723)
• data provide direct evidence for the role of PPARgamma in the regulation of human TBXA2R gene expression within the vasculature and point to further critical differences in the modes of transcriptional regulation of TBXA2R alpha and TBXA2R beta in humans (PMID:16156795)
• analysis of the molecular mechanism of how the human TXA2 receptor interacts with G alpha 13 to activate intracellular signaling (PMID:16212421)
• analysis of key amino acids (in particular Asp(193)) involved in TPR ligand coordination (PMID:16837469)
• analysis of functional polymorphisms of the thromboxane A2 receptor (PMID:16953279)
• Food intake increases this receptor’s platelet activation in type 2 diabetes but not in normal controls. (PMID:17192347)
• Studies confirm that TPbeta isoform but not TPalpha is palmitoylated at Cys347, and to a lesser extent at Cys373/377 a modification that induces signalling and internalization. (PMID:17229546)
• Specific single nucleotide polymorphisms and haplotypes may have utility as genetic markers for the risk of cerebral infarction. (PMID:17249521)
• Results suggest that TP beta binds to alpha 7 and PA28 gamma, and the cell-surface expression of TP beta is lower than that of TP alpha. (PMID:17499743)
• PRDX4 interacts with and regulates TBXA2R. (PMID:17644091)
• Expression of prostaglandin E(2) receptors (EP(2), EP(3), EP(4)), prostaglandin D(2) receptor (DP(2)), prostanoid thromboxane A(2) receptor (TP) and to a lesser extent EP(1) were observed in several hair follicle compartments. (PMID:18005048)
• TPr stimulation triggers reactive oxygen species-mediated LKB1-dependent AMPK activation, which in return inhibits cellular protein synthesis in VSMCs. (PMID:18063812)
• These results reveal the possibly important molecular mechanisms in TP signaling and provide structural information to characterize other prostanoid receptor signalings. (PMID:18073117)
• RACK1 directly binds to the C-terminus and the first intracellular loop of the beta isoform of the thromboxane A(2) receptor (PMID:18088317)
• analysis of regulation of platelet responses to P2Y and thromboxane receptor activation (PMID:18088343)
• TBXA2R are expressed in prostate cancer and activation of TBXA2R regulates prostate cancer cell motility and cytoskeleton reorganization through activation of RhoA. (PMID:18172303)
• New roles for TPalpha and TPbeta and, through studies in aortic smooth muscle cells, reveal an additional mode of regulation of vascular smooth muscle contractile responses by TXA(2). (PMID:18502100)
• studies provide a basis for the high-yield expression and purification of the G protein-coupled receptor for the structural and functional characterization using biophysics approaches (PMID:18529068)
• Data suggest that expression of prostanoid receptors (prostaglandin E2 EP3-I, prostacyclin, and thromboxane A2 receptors) in vascular inflammation could influence cell responses dependent on the constitutive activation of ghrelin receptors. (PMID:18573679)
• endocannabinoid 2-arachidonoylglycerol induced platelet activation with a dose-dependent mechanism that required engagement of platelet TxA(2) receptors (PMID:18647220)
• Regulation of the human thromboxane A2 receptor gene by Sp1, Egr1, NF-E2, GATA-1, and Ets-1 in megakaryocytes. (PMID:18698092)

Cross-species orthologs

4 orthologs

Organism	Symbol	Gene ID
danio_rerio	tbxa2r	ENSDARG00000104717
mus_musculus	Tbxa2r	ENSMUSG00000034881
rattus_norvegicus	Tbxa2r	ENSRNOG00000020585
drosophila_melanogaster	CG7497	FBGN0036742

Paralogs (7): PTGER3 (ENSG00000050628), PTGFR (ENSG00000122420), PTGER2 (ENSG00000125384), PTGIR (ENSG00000160013), PTGER1 (ENSG00000160951), PTGDR (ENSG00000168229), PTGER4 (ENSG00000171522)

Protein

Protein identifiers

Thromboxane A2 receptor — P21731 (reviewed: P21731)

Alternative names: Prostanoid TP receptor

All UniProt accessions (2): P21731, K7ER80

UniProt curated annotations — full annotation on UniProt →

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. Activates adenylyl cyclase. Inhibits adenylyl cyclase.

Subunit / interactions. Interacts with RPGRIP1L. Interacts with PSMA3. Interacts with RACK1; the interaction regulates TBXA2R cell surface expression.

Subcellular location. Cell membrane.

Disease relevance. Bleeding disorder, platelet-type, 13 (BDPLT13) [MIM:614009] A disorder characterized by reduced platelet aggregation and a tendency to mild mucocutaneous bleeding. Disease susceptibility is associated with variants affecting the gene represented in this entry.

Similarity. Belongs to the G-protein coupled receptor 1 family.

Isoforms (2)

UniProt ID	Names	Canonical?
P21731-3	1, Alpha, Placenta receptor	yes
P21731-2	2, Beta, Endothelial receptor

RefSeq proteins (2): NP_001051, NP_963998 (=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000276	GPCR_Rhodpsn	Family
IPR001105	Thbox_rcpt	Family
IPR008365	Prostanoid_rcpt	Family
IPR017452	GPCR_Rhodpsn_7TM	Domain

Pfam: PF00001

UniProt features (52 total): helix 12, topological domain 8, transmembrane region 7, sequence variant 7, mutagenesis site 4, turn 4, modified residue 2, glycosylation site 2, strand 2, chain 1, disulfide bond 1, splice variant 1, sequence conflict 1

Structure

Experimental structures (PDB)

6 structures.

PDB	Method	Resolution (Å)
6IIU	X-RAY DIFFRACTION	2.5
6IIV	X-RAY DIFFRACTION	3
8XJN	ELECTRON MICROSCOPY	3.06
8XJO	ELECTRON MICROSCOPY	3.11
9GGG	ELECTRON MICROSCOPY	3.25
9GG5	ELECTRON MICROSCOPY	3.26

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P21731-F1	86.08	0.63

Antibody-complex structures (SAbDab): 2 — 8XJN, 8XJO

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Post-translational modifications (2): 329, 331

Disulfide bonds (1): 105–183

Glycosylation sites (2): 4, 16

Mutagenesis-validated functional residues (4):

Position	Phenotype
291	suppresses antagonist binding.
295	reduces antagonist binding.
299	reduces antagonist binding.

Function

Pathways and Gene Ontology

Reactome pathways

13 pathways

ID	Pathway
R-HSA-391908	Prostanoid ligand receptors
R-HSA-416476	G alpha (q) signalling events
R-HSA-416482	G alpha (12/13) signalling events
R-HSA-428930	Thromboxane signalling through TP receptor
R-HSA-109582	Hemostasis
R-HSA-162582	Signal Transduction
R-HSA-372790	Signaling by GPCR
R-HSA-373076	Class A/1 (Rhodopsin-like receptors)
R-HSA-388396	GPCR downstream signalling
R-HSA-391903	Eicosanoid ligand-binding receptors
R-HSA-392518	Signal amplification
R-HSA-500792	GPCR ligand binding
R-HSA-76002	Platelet activation, signaling and aggregation

MSigDB gene sets: 272 (showing top): TONKS_TARGETS_OF_RUNX1_RUNX1T1_FUSION_MONOCYTE_UP, GOBP_RESPONSE_TO_ETHANOL, GOBP_REGULATION_OF_BLOOD_PRESSURE, GOBP_REGULATION_OF_WOUND_HEALING, GOBP_CIRCULATORY_SYSTEM_PROCESS, GOBP_INFLAMMATORY_RESPONSE, REACTOME_EICOSANOID_LIGAND_BINDING_RECEPTORS, GOBP_CELLULAR_RESPONSE_TO_LIPID, GOBP_REGULATION_OF_COAGULATION, GOCC_SECRETORY_GRANULE, REACTOME_PLATELET_ACTIVATION_SIGNALING_AND_AGGREGATION, GOBP_NEGATIVE_REGULATION_OF_BLOOD_VESSEL_ENDOTHELIAL_CELL_MIGRATION, GOBP_CELLULAR_RESPONSE_TO_BIOTIC_STIMULUS, XU_HGF_TARGETS_REPRESSED_BY_AKT1_DN, GRAESSMANN_APOPTOSIS_BY_SERUM_DEPRIVATION_UP

GO Biological Process (20): smooth muscle contraction (GO:0006939), inflammatory response (GO:0006954), G protein-coupled receptor signaling pathway (GO:0007186), adenylate cyclase-activating G protein-coupled receptor signaling pathway (GO:0007189), positive regulation of cytosolic calcium ion concentration (GO:0007204), response to nutrient (GO:0007584), response to xenobiotic stimulus (GO:0009410), positive regulation of blood coagulation (GO:0030194), response to testosterone (GO:0033574), response to ethanol (GO:0045471), positive regulation of angiogenesis (GO:0045766), positive regulation of blood pressure (GO:0045777), positive regulation of vasoconstriction (GO:0045907), positive regulation of smooth muscle contraction (GO:0045987), cellular response to lipopolysaccharide (GO:0071222), negative regulation of cell migration involved in sprouting angiogenesis (GO:0090051), signal transduction (GO:0007165), regulation of vasoconstriction (GO:0019229), response to lipopolysaccharide (GO:0032496), thromboxane A2 signaling pathway (GO:0038193)

GO Molecular Function (5): thromboxane A2 receptor activity (GO:0004961), guanyl-nucleotide exchange factor activity (GO:0005085), G protein-coupled receptor activity (GO:0004930), thromboxane receptor activity (GO:0004960), protein binding (GO:0005515)

GO Cellular Component (4): acrosomal vesicle (GO:0001669), plasma membrane (GO:0005886), nuclear speck (GO:0016607), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-9 pathways:

Category	Pathways
GPCR downstream signalling	2
Signaling by GPCR	2
Eicosanoid ligand-binding receptors	1
Signal amplification	1
Signal Transduction	1
GPCR ligand binding	1
Class A/1 (Rhodopsin-like receptors)	1
Platelet activation, signaling and aggregation	1
Hemostasis	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
response to chemical	2
response to lipid	2
vasoconstriction	2
G protein-coupled receptor signaling pathway	2
muscle contraction	1
defense response	1
G protein-coupled receptor activity	1
signal transduction	1
adenylate cyclase-modulating G protein-coupled receptor signaling pathway	1
adenylate cyclase activator activity	1
regulation of biological quality	1
response to nutrient levels	1
blood coagulation	1
regulation of blood coagulation	1
positive regulation of coagulation	1
positive regulation of wound healing	1
positive regulation of hemostasis	1
response to ketone	1
response to alcohol	1
angiogenesis	1
regulation of angiogenesis	1
positive regulation of vasculature development	1
regulation of blood pressure	1
regulation of vasoconstriction	1
positive regulation of multicellular organismal process	1
smooth muscle contraction	1
regulation of smooth muscle contraction	1
positive regulation of muscle contraction	1
response to lipopolysaccharide	1
cellular response to molecule of bacterial origin	1
cellular response to lipid	1
cellular response to oxygen-containing compound	1
cell migration involved in sprouting angiogenesis	1
negative regulation of blood vessel endothelial cell migration	1
regulation of cell migration involved in sprouting angiogenesis	1
cell communication	1
cellular process	1
signaling	1
regulation of cellular process	1
cellular response to stimulus	1

Protein interactions and networks

STRING

936 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
TBXA2R	HADHB	P55084	797
TBXA2R	GNAQ	P50148	737
TBXA2R	ADRA1B	P35368	692
TBXA2R	ADRA1D	P25100	665
TBXA2R	KCNMA1	Q12791	653
TBXA2R	PTGDR2	Q9Y5Y4	625
TBXA2R	CYSLTR1	Q9Y271	601
TBXA2R	TBXAS1	P24557	599
TBXA2R	PAH	P00439	591
TBXA2R	CYSLTR2	Q9NS75	550
TBXA2R	LHCGR	P22888	545
TBXA2R	P2RY12	Q9H244	525
TBXA2R	AAMP	Q13685	525
TBXA2R	LTB4R	Q15722	524
TBXA2R	TGM1	P22735	522

IntAct

12 interactions, top by confidence:

A	B	Type	Score
PRDX4	TBXA2R	psi-mi:“MI:0915”(physical association)	0.590
PRDX4	TBXA2R	psi-mi:“MI:0407”(direct interaction)	0.590
	TBXA2R	psi-mi:“MI:0915”(physical association)	0.490
TBXA2R	GPRASP1	psi-mi:“MI:0407”(direct interaction)	0.440
TBXA2R	KCNMA1	psi-mi:“MI:0915”(physical association)	0.400
E5	ESYT2	psi-mi:“MI:0914”(association)	0.350
TBXA2R	UPK3BL1	psi-mi:“MI:0914”(association)	0.350
CANX	TBXA2R	psi-mi:“MI:0403”(colocalization)	0.270
	TBXA2R	psi-mi:“MI:0915”(physical association)	0.000

BioGRID (126): GNAQ (Affinity Capture-Western), GNA13 (Co-purification), GNAQ (Co-purification), TBXA2R (Co-purification), TBXA2R (Co-purification), TBXA2R (Synthetic Lethality), NOX1 (Two-hybrid), VRK2 (Two-hybrid), ZDHHC15 (Two-hybrid), SLC41A1 (Two-hybrid), EMP1 (Two-hybrid), ADIPOR1 (Two-hybrid), GJB2 (Two-hybrid), TM4SF4 (Two-hybrid), ARL6IP6 (Two-hybrid)

ESM2 similar proteins: A5D7K8, O35932, O95136, O95977, P21731, P30557, P30987, P34972, P34978, P34979, P34980, P35375, P35408, P37289, P43088, P43114, P43115, P43116, P43117, P43118, P43119, P43252, P43253, P46069, P47752, P47901, P47936, P50131, P52592, P56486, P70263, P70597, P79393, Q13258, Q28691, Q28905, Q5R949, Q62053, Q62928, Q8MJ08

Diamond homologs: O02662, P21731, P30557, P30987, P34978, P34979, P34980, P34995, P35375, P37289, P43088, P43115, P43117, P43118, P43119, P43141, P43252, P43253, P46069, P46626, P50131, P56486, P70597, P79393, Q28524, Q28550, Q28905, Q804Q2, Q804X9, Q8R456, Q95125, Q95252, Q9BGL8, Q9QXZ9, Q9TST4, Q9UHM6, Q9XT57, Q9XT58, P32240, P35408

SIGNOR signaling

9 interactions.

A	Effect	B	Mechanism
EGR1	“up-regulates quantity by expression”	TBXA2R	“transcriptional regulation”
SP1	“up-regulates quantity by expression”	TBXA2R	“transcriptional regulation”
TBXA2R	“up-regulates activity”	GNAI1	binding
TBXA2R	“up-regulates activity”	GNAQ	binding
TBXA2R	“up-regulates activity”	GNA14	binding
TBXA2R	“up-regulates activity”	GNA13	binding
“9,11-Methanoepoxy PGH2”	“up-regulates activity”	TBXA2R	“chemical activation”
PRKACA	unknown	TBXA2R	phosphorylation
thromboxane	“up-regulates activity”	TBXA2R	“chemical activation”

Disease & clinical

Clinical variants and AI predictions

ClinVar

260 variants total. Per-class counts are floors (≥ shown; pagination cap):

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	4
Uncertain significance	148
Likely benign	69
Benign	23

Top pathogenic / likely-pathogenic (4)

Variant ID	HGVS	Classification
1684472	NM_001060.6(TBXA2R):c.548G>A (p.Cys183Tyr)	Likely pathogenic
3376276	NM_001060.6(TBXA2R):c.416C>A (p.Ser139Ter)	Likely pathogenic
429346	NM_001060.6(TBXA2R):c.82C>T (p.Pro28Ser)	Likely pathogenic
627136	NM_001060.6(TBXA2R):c.787-2A>G	Likely pathogenic

SpliceAI

391 predictions. Top by Δscore:

Variant	Effect	Δscore
19:3595929:AAGAC:A	acceptor_gain	1.0000
19:3595930:AGAC:A	acceptor_gain	1.0000
19:3595931:GAC:G	acceptor_gain	1.0000
19:3595931:GACC:G	acceptor_loss	1.0000
19:3595932:AC:A	acceptor_gain	1.0000
19:3595933:CC:C	acceptor_gain	1.0000
19:3595934:C:CC	acceptor_gain	1.0000
19:3595935:T:C	acceptor_loss	1.0000
19:3599843:ACT:A	donor_loss	1.0000
19:3599844:CTC:C	donor_loss	1.0000
19:3599845:TCAC:T	donor_loss	1.0000
19:3599846:CACC:C	donor_loss	1.0000
19:3599847:A:AC	donor_gain	1.0000
19:3599848:C:CC	donor_gain	1.0000
19:3600715:CAC:C	acceptor_gain	1.0000
19:3595937:C:CT	acceptor_gain	0.9900
19:3597969:T:TA	donor_gain	0.9900
19:3599848:CCAGA:C	donor_gain	0.9900
19:3599878:C:CT	donor_gain	0.9900
19:3600713:CACAC:C	acceptor_gain	0.9900
19:3600717:CCTG:C	acceptor_loss	0.9900
19:3600726:C:CT	acceptor_gain	0.9900
19:3597980:AGGT:A	donor_gain	0.9800
19:3599847:AC:A	donor_gain	0.9800
19:3599848:CC:C	donor_gain	0.9800
19:3599848:CCAG:C	donor_gain	0.9800
19:3599879:C:CT	donor_gain	0.9800
19:3600718:C:CC	acceptor_gain	0.9800
19:3599848:CCA:C	donor_gain	0.9700
19:3599908:TCTCC:T	donor_gain	0.9700

AlphaMissense

2151 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
19:3595806:G:T	P305H	0.998
19:3595804:A:G	W306R	0.997
19:3595804:A:T	W306R	0.997
19:3599870:G:C	S255R	0.997
19:3599870:G:T	S255R	0.997
19:3599872:T:G	S255R	0.997
19:3595806:G:A	P305L	0.996
19:3599981:G:C	S218R	0.996
19:3599981:G:T	S218R	0.996
19:3599983:T:G	S218R	0.996
19:3600413:G:C	D74E	0.996
19:3600413:G:T	D74E	0.996
19:3600414:T:A	D74V	0.996
19:3600414:T:G	D74A	0.996
19:3600083:G:C	F184L	0.995
19:3600083:G:T	F184L	0.995
19:3600085:A:G	F184L	0.995
19:3600509:G:C	N42K	0.995
19:3600509:G:T	N42K	0.995
19:3595806:G:C	P305R	0.994
19:3595807:G:A	P305S	0.994
19:3595820:G:C	N300K	0.994
19:3595820:G:T	N300K	0.994
19:3600084:A:C	F184C	0.994
19:3600414:T:C	D74G	0.994
19:3600415:C:G	D74H	0.994
19:3595825:A:G	W299R	0.993
19:3595825:A:T	W299R	0.993
19:3599864:A:C	C257W	0.993
19:3599865:C:T	C257Y	0.993

dbSNP variants (sampled 300 via entrez): RS1000036783 (19:3597232 G>A,T), RS1000152723 (19:3597076 A>G), RS1000212986 (19:3606886 G>C,T), RS1000307414 (19:3597921 G>A), RS1000344072 (19:3602815 T>C,G), RS1000376669 (19:3602603 G>GGT), RS1000714302 (19:3607225 G>A,T), RS1000841564 (19:3595106 T>C,G), RS1000858412 (19:3598947 C>T), RS1000889896 (19:3602003 C>G,T), RS1000983624 (19:3607506 C>T), RS1001013298 (19:3607303 C>T), RS1001077412 (19:3594319 C>A), RS1001221725 (19:3608238 C>A,T), RS1001287053 (19:3603152 G>C)

Disease associations

OMIM: gene MIM:188070 | disease phenotypes: MIM:614009

GenCC curated gene-disease

Disease	Classification	Inheritance
bleeding diathesis due to thromboxane synthesis deficiency	Moderate	Autosomal dominant
bleeding disorder, platelet-type, 13, susceptibility to	Moderate	Autosomal dominant
schizophrenia	No Known Disease Relationship	Unknown

ClinGen Gene-Disease Validity (1)

Expert-panel classifications — Definitive > Strong > Moderate > Limited > Disputed > Refuted.

Disease	Classification	Inheritance
qualitative platelet defect	Moderate	AD

Mondo (4): asthma (MONDO:0004979), bleeding disorder, platelet-type, 13, susceptibility to (MONDO:0800447), (MONDO:0013524), schizophrenia (MONDO:0005090)

Orphanet (0):

HPO phenotypes

8 total (9 of 8 shown, HPO-id order):

HPO	Term
HP:0000006	Autosomal dominant inheritance
HP:0000421	Epistaxis
HP:0000978	Bruising susceptibility
HP:0003593	Infantile onset
HP:0011870	Impaired arachidonic acid-induced platelet aggregation
HP:0011873	Abnormal platelet count
HP:0011894	Impaired thromboxane A2 agonist-induced platelet aggregation
HP:0031364	Ecchymosis
HP:0002099	Asthma

GWAS associations

0 associations (top):

MeSH disease descriptors (1)

Descriptor	Name	Tree numbers
D001249	Asthma	C08.127.108; C08.381.495.108; C08.674.095; C20.543.480.680.095

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL2069 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

210 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 565,394 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

Molecule	Name	Phase	Patents
CHEMBL1014	CANDESARTAN CILEXETIL	4	11,194
CHEMBL1017	TELMISARTAN	4	27,457
CHEMBL1023	BEXAROTENE	4	40,951
CHEMBL104	CLOTRIMAZOLE	4	56,325
CHEMBL1042	CHOLECALCIFEROL	4	64,162
CHEMBL1064	SIMVASTATIN	4	123,163
CHEMBL1065	METHYSERGIDE	4	8,455
CHEMBL1071	OXAPROZIN	4	51,044
CHEMBL1082407	ENZALUTAMIDE	4	9,652
CHEMBL110691	CHLORMADINONE ACETATE	4	9,747
CHEMBL111	RIMONABANT	4	15,726
CHEMBL1112	ARIPIPRAZOLE	4	24,205
CHEMBL1138	EZETIMIBE	4	29,509
CHEMBL1148	TORSEMIDE	4	15,151
CHEMBL1171837	PONATINIB	4	8,955
CHEMBL1172	DESLORATADINE	4	19,720
CHEMBL1200430	ESTRADIOL ACETATE	4	1,114
CHEMBL1200438	TIOCONAZOLE	4	15,162
CHEMBL1200500	BECLOMETHASONE DIPROPIONATE	4	29,239
CHEMBL1200853	DYDROGESTERONE	4	4,463
CHEMBL1200868	PHENYL AMINOSALICYLATE	4
CHEMBL1201146	NORETHINDRONE ACETATE	4
CHEMBL1201196	SERTACONAZOLE	4
CHEMBL1201245	BROMODIPHENHYDRAMINE	4
CHEMBL1201303	PYRVINIUM	4
CHEMBL1201304	INDOCYANINE GREEN ACID FORM	4
CHEMBL1201342	METHIXENE	4
CHEMBL1219	RABEPRAZOLE	4
CHEMBL1231	OXYBUTYNIN	4
CHEMBL1237021	LURASIDONE	4

PharmGKB: 1 entry (VIP=true, CPIC=false)

PharmGKB clinical annotations

3 annotations.

Variant	Type	Level	Drugs	Phenotypes
rs1131882	Toxicity	3	aspirin	Asthma
rs1131882	Efficacy,Toxicity	3	aspirin	Diabetes Mellitus;Type 2
rs4523	Efficacy	3	aspirin

PharmGKB variants

3 variants.

Variant	Genes	Level	Score	#Clin annots	Drugs
rs4523	TBXA2R	3	5.00	1	aspirin
rs5758	TBXA2R		0.00	0
rs1131882	TBXA2R	3	2.50	2	aspirin

GtoPdb / IUPHAR curated pharmacology

(IUPHAR/BPS Guide to Pharmacology — expert-curated)

Target class: gpcr — Prostanoid receptors

Most potent curated ligand interactions (43 total), top 25:

Ligand	Action	Affinity	Parameter
domitroban	Antagonist	9.6	pKi
vapiprost	Antagonist	9.4	pKi
I-SAP	Antagonist	9.33	pKd
I-BOP	Agonist	9.32	pKd
[125I]SAP	Antagonist	9.3	pKd
SQ-29548	Antagonist	9.1	pKi
SQ 26655	Full agonist	9.05	pEC50
KW-3635	Antagonist	8.9	pKi
[3H]S-145	Antagonist	8.9	pKd
ONO-3708	Antagonist	8.9	pKi
AGN192093	Agonist	8.9	pEC50
[125I]BOP	Full agonist	8.7	pKd
EP 171	Full agonist	8.5	pKi
U46609	Full agonist	8.4	pKi
ifetroban	Antagonist	8.4	pKi
[125I]SQ-29548	Antagonist	8.3	pKd
[3H]SQ-29548	Antagonist	8.2	pKd
ramatroban	Antagonist	8.0	pKi
[3H]U46619	Full agonist	7.8	pKd
AGN 191976	Full agonist	7.8	pEC50
[125I]PTA-OH	Antagonist	7.7	pKd
daltroban	Antagonist	7.7	pKi
S-5751	Antagonist	7.6	pKi
U46619	Full agonist	7.5	pKi
NTP42	Antagonist	7.25	pIC50

Binding affinities (BindingDB)

87 measured of 94 human assays (101 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
3-(2-{3-[4-(6-Cyclohexyl-hexanoyl)-oxazol-2-yl]-7-oxa-bicyclo[2.2.1]hept-2-ylmethyl}-phenyl)-propionic acid	KD	0.05 nM
3-(2-{3-[4-(4-Cyclohexyl-butylcarbamoyl)-oxazol-2-yl]-7-oxa-bicyclo[2.2.1]hept-2-ylmethyl}-phenyl)-propionic acid	KD	0.1 nM
3-[2-(3-{4-[4-(4-Chloro-phenyl)-butylcarbamoyl]-oxazol-2-yl}-7-oxa-bicyclo[2.2.1]hept-2-ylmethyl)-phenyl]-propionic acid	KD	0.2 nM
3-{2-[3-(4-Heptylcarbamoyl-oxazol-2-yl)-7-oxa-bicyclo[2.2.1]hept-2-ylmethyl]-phenyl}-propionic acid	KD	0.2 nM
3-[2-(3-{4-[4-(4-Methoxy-phenyl)-butylcarbamoyl]-oxazol-2-yl}-7-oxa-bicyclo[2.2.1]hept-2-ylmethyl)-phenyl]-propionic acid	KD	0.3 nM
3-(2-{3-[4-(4-Phenyl-butylcarbamoyl)-oxazol-2-yl]-7-oxa-bicyclo[2.2.1]hept-2-ylmethyl}-phenyl)-propionic acid	KD	0.3 nM
CHEMBL2096756	KD	0.4 nM
2-Chlor-11-(2-dimethylaminoaethoxy)-dibenzo(b,f)-thiepin	KI	0.5 nM
3-[2-(3-{4-[4-(4-Hydroxy-phenyl)-butylcarbamoyl]-oxazol-2-yl}-7-oxa-bicyclo[2.2.1]hept-2-ylmethyl)-phenyl]-propionic acid	KD	0.5 nM
3-(2-{3-[4-(5,5-Dimethyl-hexylcarbamoyl)-oxazol-2-yl]-7-oxa-bicyclo[2.2.1]hept-2-ylmethyl}-phenyl)-propionic acid	KD	0.6 nM
3-{2-[3-(4-Phenethylcarbamoyl-oxazol-2-yl)-7-oxa-bicyclo[2.2.1]hept-2-ylmethyl]-phenyl}-propionic acid	KD	0.7 nM
3-(2-{3-[4-(2-Cyclohexyl-ethylcarbamoyl)-oxazol-2-yl]-7-oxa-bicyclo[2.2.1]hept-2-ylmethyl}-phenyl)-propionic acid	KD	0.7 nM
3-(2-{3-[4-(1,1-Dimethyl-propylcarbamoyl)-oxazol-2-yl]-7-oxa-bicyclo[2.2.1]hept-2-ylmethyl}-phenyl)-propionic acid	KD	0.8 nM
BM 573	KI	0.8 nM
4-(2-{3-[4-(4-Cyclohexyl-butylcarbamoyl)-oxazol-2-yl]-7-oxa-bicyclo[2.2.1]hept-2-ylmethyl}-phenyl)-butyric acid	KD	0.85 nM
3-[2-(5-oxabicyclo[2.2.1],3-formaldehyde (anilinocarbonyl)hydrazonehept-2-ylmethyl)phenyl]propanoic acid	KD	1 nM
2-{3-[2-(2-Carboxy-ethyl)-benzyl]-7-oxa-bicyclo[2.2.1]hept-2-yl}-oxazole-4-carboxylic acid 4-cyclohexyl-butyl ester	KD	1 nM
7-(3-{[2-(4-Cyclohexyl-butyrylamino)-acetylamino]-methyl}-7-oxa-bicyclo[2.2.1]hept-2-yl)-hept-5-enoic acid	KD	1.1 nM
(3-{3-[4-(4-Cyclohexyl-butylcarbamoyl)-oxazol-2-yl]-7-oxa-bicyclo[2.2.1]hept-2-ylmethyl}-phenyl)-acetic acid	KD	1.2 nM
3-[2-(3-{4-[2-(4-Chloro-phenyl)-ethylcarbamoyl]-oxazol-2-yl}-7-oxa-bicyclo[2.2.1]hept-2-ylmethyl)-phenyl]-propionic acid	KD	1.3 nM
2-{3-[2-(3-Methanesulfonylamino-3-oxo-propyl)-benzyl]-7-oxa-bicyclo[2.2.1]hept-2-yl}-oxazole-4-carboxylic acid (4-cyclohexyl-butyl)-amide	KD	1.6 nM
CHEMBL176714	KD	1.6 nM
5-[2-(4-Benzo[d]isothiazol-3-yl-piperazin-1-yl)-ethyl]-6-chloro-1,3-dihydro-indol-2-one	KI	1.9 nM
7-(3-{[2-(5-Cyclohexyl-pentanoylamino)-acetylamino]-methyl}-7-oxa-bicyclo[2.2.1]hept-2-yl)-hept-5-enoic acid	KD	2.6 nM
3-[2-(3-{4-[4-(4-Methylsulfanyl-phenyl)-butylcarbamoyl]-oxazol-2-yl}-7-oxa-bicyclo[2.2.1]hept-2-ylmethyl)-phenyl]-propionic acid	KD	2.9 nM
3-(2-{3-[4-(3,3-Dimethyl-butylcarbamoyl)-oxazol-2-yl]-7-oxa-bicyclo[2.2.1]hept-2-ylmethyl}-phenyl)-propionic acid	KD	2.9 nM
4-[4-(4-Chloro-phenyl)-4-hydroxy-piperidin-1-yl]-1-(4-fluoro-phenyl)-butan-1-one;propionate(HCl)	KI	2.92 nM
BDBM50188614	KI	3.1 nM
(2-{3-[4-(4-Cyclohexyl-butylcarbamoyl)-oxazol-2-yl]-7-oxa-bicyclo[2.2.1]hept-2-ylmethyl}-phenoxy)-acetic acid	KD	3.2 nM
CAS_128719-90-4	KI	3.7 nM
3-[2-(3-{4-[4-(4-Fluoro-phenyl)-butylcarbamoyl]-oxazol-2-yl}-7-oxa-bicyclo[2.2.1]hept-2-ylmethyl)-phenyl]-propionic acid	KD	3.9 nM
BMS-180291	KD	4 nM
7-[3-({2-[2-(4-tert-Butyl-phenylsulfanyl)-acetylamino]-acetylamino}-methyl)-7-oxa-bicyclo[2.2.1]hept-2-yl]-hept-5-enoic acid	KD	4.2 nM
3-{2-[3-(4-Cyclohexylcarbamoyl-oxazol-2-yl)-7-oxa-bicyclo[2.2.1]hept-2-ylmethyl]-phenyl}-propionic acid	KD	4.5 nM
3-{2-[3-(4-Hept-6-ynylcarbamoyl-oxazol-2-yl)-7-oxa-bicyclo[2.2.1]hept-2-ylmethyl]-phenyl}-propionic acid	KD	4.7 nM
3-(2-{3-[4-(5,5,5-Trifluoro-pentylcarbamoyl)-oxazol-2-yl]-7-oxa-bicyclo[2.2.1]hept-2-ylmethyl}-phenyl)-propionic acid	KD	4.8 nM
3-{2-[3-(4-Decylcarbamoyl-oxazol-2-yl)-7-oxa-bicyclo[2.2.1]hept-2-ylmethyl]-phenyl}-propionic acid	KD	5.8 nM
[2-(5-oxabicyclo[2.2.1],3-formaldehyde (anilinocarbonyl)hydrazone-hept-2-ylmethyl)phenoxy]acetic acid	KD	6 nM
NSC_114865	KI	7.1 nM
GR 32191	KI	7.8 nM
7-{3-[(2-Nonanoylamino-acetylamino)-methyl]-7-oxa-bicyclo[2.2.1]hept-2-yl}-hept-5-enoic acid	KD	8.3 nM
4-[2-[(1R,2R)-2-[(E)-4-(3-fluorophenyl)-3-hydroxybut-1-enyl]-5-oxocyclopentyl]ethyl]benzoic acid	EC50	10 nM	US-9394273: Therapeutic prostaglandin receptor agonists
3-{2-[3-(4-Propylcarbamoyl-oxazol-2-yl)-7-oxa-bicyclo[2.2.1]hept-2-ylmethyl]-phenyl}-propionic acid	KD	10 nM
4-[2-[(1R,2R)-2-[(E)-4-(4-fluorophenyl)-3-hydroxybut-1-enyl]-5-oxocyclopentyl]ethyl]benzoic acid	EC50	11 nM	US-9394273: Therapeutic prostaglandin receptor agonists
3-(2-{3-[4-(Methyl-pentyl-carbamoyl)-oxazol-2-yl]-7-oxa-bicyclo[2.2.1]hept-2-ylmethyl}-phenyl)-propionic acid	KD	11 nM
3-(2-{3-[4-(4-Cyclohexyl-butylthiocarbamoyl)-oxazol-2-yl]-7-oxa-bicyclo[2.2.1]hept-2-ylmethyl}-phenyl)-propionic acid	KD	11 nM
(daltroban){4-[2-(4-Chloro-benzenesulfonylamino)-ethyl]-phenyl}-acetic acid	KI	11.3 nM
7-{3-[(2-Heptanethioylamino-acetylamino)-methyl]-7-oxa-bicyclo[2.2.1]hept-2-yl}-hept-5-enoic acid	KD	12 nM
[3-(2-{3-[4-(4-Cyclohexyl-butylcarbamoyl)-oxazol-2-yl]-7-oxa-bicyclo[2.2.1]hept-2-yl}-ethyl)-phenyl]-acetic acid	KD	16 nM
3-(2-{3-[4-(4-Cyclohexyl-butylcarbamoyl)-oxazol-2-yl]-7-oxa-bicyclo[2.2.1]hept-2-yl}-ethyl)-benzoic acid	KD	18 nM

ChEMBL bioactivities

1280 potent at pChembl≥5 of 1518 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
10.82	IC50	0.015	nM	CHEMBL3354618
10.30	Kd	0.05	nM	CHEMBL31146
10.28	IC50	0.052	nM	CHEMBL3354616
10.00	Kd	0.1	nM	CHEMBL31765
9.89	IC50	0.13	nM	CHEMBL435382
9.70	Kd	0.2	nM	CHEMBL30743
9.70	Kd	0.2	nM	CHEMBL30615
9.52	EC50	0.3	nM	CHEMBL3967284
9.52	Kd	0.3	nM	CHEMBL283923
9.52	Kd	0.3	nM	CHEMBL281959
9.50	Kd	0.3162	nM	CHEMBL263442
9.40	Kd	0.3981	nM	CHEMBL30024
9.40	Kd	0.4	nM	CHEMBL2096756
9.34	IC50	0.46	nM	CHEMBL209168
9.30	Kd	0.5	nM	CHEMBL25657
9.30	Kd	0.5	nM	CHEMBL29429
9.25	IC50	0.56	nM	CHEMBL209306
9.24	IC50	0.58	nM	CHEMBL209134
9.24	Ki	0.58	nM	RAMATROBAN
9.22	Kd	0.6	nM	CHEMBL30972
9.20	Kd	0.631	nM	CHEMBL49535
9.19	IC50	0.65	nM	CHEMBL274415
9.17	IC50	0.68	nM	CHEMBL209168
9.15	IC50	0.7	nM	CHEMBL209406
9.15	IC50	0.71	nM	CHEMBL379736
9.15	IC50	0.7	nM	CHEMBL379659
9.15	Kd	0.7	nM	CHEMBL410732
9.15	Kd	0.7	nM	CHEMBL31922
9.14	IC50	0.72	nM	CHEMBL208818
9.13	IC50	0.74	nM	CHEMBL209406
9.11	IC50	0.78	nM	CHEMBL210602
9.11	IC50	0.77	nM	CHEMBL380274
9.11	IC50	0.78	nM	CHEMBL209306
9.10	IC50	0.79	nM	CHEMBL208543
9.10	Kd	0.8	nM	CHEMBL281726
9.08	Ki	0.84	nM	CHEMBL426387
9.07	Kd	0.85	nM	CHEMBL31154
9.04	Ki	0.91	nM	CHEMBL431075
9.00	Kd	1	nM	CHEMBL95872
9.00	IC50	1.01	nM	CHEMBL208115
9.00	Kd	1	nM	CHEMBL352040
9.00	Kd	1	nM	CHEMBL116852
9.00	Kd	1	nM	CHEMBL286978
8.98	IC50	1.05	nM	CHEMBL210602
8.97	IC50	1.07	nM	CHEMBL379736
8.97	IC50	1.08	nM	CHEMBL379659
8.96	Kd	1.1	nM	CHEMBL310406
8.96	IC50	1.1	nM	CHEMBL7353
8.93	IC50	1.17	nM	CHEMBL209245
8.92	Kd	1.2	nM	CHEMBL285596

PubChem BioAssay actives

949 with measured affinity, of 4924 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

Compound	Assay	Type	Value	Unit
4-chloro-N-[5-[[3-(2,6-dimethylphenyl)-2-hydroxy-4-oxocyclopent-2-en-1-yl]methyl]-1,2,3,4-tetrahydronaphthalen-2-yl]benzenesulfonamide	1164309: Antagonist activity against human thromboxane A2 receptor alpha expressed in QBI-HEK293A cells assessed as reduction in I-BOP-induced inositol monophosphate production incubated for 15 to 60 mins before I-BOP addition by HTRF assay	ic50	<0.0001	uM
(Z)-7-[(1R,2S,3S,4S)-3-(naphthalen-2-ylsulfonylamino)-2-bicyclo[2.2.1]heptanyl]hept-5-enoic acid	210334: Inhibition of [3H]- (+)-S-145 specific binding to human platelet membranes in TXA2 receptor (TP) assay	ic50	0.0001	uM
4-chloro-N-[5-[[2-hydroxy-3-(4-methoxyphenyl)-4-oxocyclopent-2-en-1-yl]methyl]-1,2,3,4-tetrahydronaphthalen-2-yl]benzenesulfonamide	1164309: Antagonist activity against human thromboxane A2 receptor alpha expressed in QBI-HEK293A cells assessed as reduction in I-BOP-induced inositol monophosphate production incubated for 15 to 60 mins before I-BOP addition by HTRF assay	ic50	0.0001	uM
3-[2-[[3-[4-(4-cyclohexylbutylcarbamoyl)-1,3-oxazol-2-yl]-7-oxabicyclo[2.2.1]heptan-2-yl]methyl]phenyl]propanoic acid	215618: Inhibitory binding activity against TXA2 receptor in human platelet membrane, using [3H]-SQ 29548 as the radioligand	kd	0.0001	uM
3-[2-[[3-[4-(6-cyclohexylhexanoyl)-1,3-oxazol-2-yl]-7-oxabicyclo[2.2.1]heptan-2-yl]methyl]phenyl]propanoic acid	215618: Inhibitory binding activity against TXA2 receptor in human platelet membrane, using [3H]-SQ 29548 as the radioligand	kd	0.0001	uM
3-[2-[[3-[4-(heptylcarbamoyl)-1,3-oxazol-2-yl]-7-oxabicyclo[2.2.1]heptan-2-yl]methyl]phenyl]propanoic acid	215618: Inhibitory binding activity against TXA2 receptor in human platelet membrane, using [3H]-SQ 29548 as the radioligand	kd	0.0002	uM
3-[2-[[3-[4-[4-(4-chlorophenyl)butylcarbamoyl]-1,3-oxazol-2-yl]-7-oxabicyclo[2.2.1]heptan-2-yl]methyl]phenyl]propanoic acid	215618: Inhibitory binding activity against TXA2 receptor in human platelet membrane, using [3H]-SQ 29548 as the radioligand	kd	0.0002	uM
3-[2-[[3-[4-[4-(4-methoxyphenyl)butylcarbamoyl]-1,3-oxazol-2-yl]-7-oxabicyclo[2.2.1]heptan-2-yl]methyl]phenyl]propanoic acid	215618: Inhibitory binding activity against TXA2 receptor in human platelet membrane, using [3H]-SQ 29548 as the radioligand	kd	0.0003	uM
3-[2-[[3-[4-(4-phenylbutylcarbamoyl)-1,3-oxazol-2-yl]-7-oxabicyclo[2.2.1]heptan-2-yl]methyl]phenyl]propanoic acid	215618: Inhibitory binding activity against TXA2 receptor in human platelet membrane, using [3H]-SQ 29548 as the radioligand	kd	0.0003	uM
(Z)-7-[3-[[(Z)-hex-3-enyl]sulfanylmethyl]-7-oxabicyclo[2.2.1]heptan-2-yl]hept-5-enoic acid	80572: Compound was evaluated for inhibition of specific binding of HSQ (5,6-di-3H-SQ 29,548) in washed platelets	kd	0.0004	uM
N-[2-(4-methylanilino)-5-nitrophenyl]sulfonylpiperidine-1-carboxamide	266289: Displacement of [3H]SQ29,548 from TPalpha receptor (short isoform) expressed in COS7 cells at 1 uM	ic50	0.0005	uM
3-[2-[[3-[4-[4-(4-hydroxyphenyl)butylcarbamoyl]-1,3-oxazol-2-yl]-7-oxabicyclo[2.2.1]heptan-2-yl]methyl]phenyl]propanoic acid	215618: Inhibitory binding activity against TXA2 receptor in human platelet membrane, using [3H]-SQ 29548 as the radioligand	kd	0.0005	uM
1-[2-(4-methylphenoxy)-5-nitrophenyl]sulfonyl-3-pentylurea	266290: Displacement of [3H]SQ-29548 from TPbeta receptor (long isoform) expressed in COS7 cells at 1 uM	ic50	0.0006	uM
1-[2-(4-bromo-3-methylanilino)-5-nitrophenyl]sulfonyl-3-pentylurea	266290: Displacement of [3H]SQ-29548 from TPbeta receptor (long isoform) expressed in COS7 cells at 1 uM	ic50	0.0006	uM
1-tert-butyl-3-[2-(2,6-dimethylanilino)-5-nitrophenyl]sulfonylurea	266290: Displacement of [3H]SQ-29548 from TPbeta receptor (long isoform) expressed in COS7 cells at 1 uM	ic50	0.0006	uM
3-[(3R)-3-[(4-fluorophenyl)sulfonylamino]-1,2,3,4-tetrahydrocarbazol-9-yl]propanoic acid	551275: Binding affinity to thromboxane receptor	ki	0.0006	uM
3-[2-[[3-[4-(5,5-dimethylhexylcarbamoyl)-1,3-oxazol-2-yl]-7-oxabicyclo[2.2.1]heptan-2-yl]methyl]phenyl]propanoic acid	215618: Inhibitory binding activity against TXA2 receptor in human platelet membrane, using [3H]-SQ 29548 as the radioligand	kd	0.0006	uM
(Z)-7-[(2R,3R)-3-[[2-(phenylcarbamoyl)hydrazinyl]methyl]-7-oxabicyclo[2.2.1]heptan-2-yl]hept-5-enoic acid	212260: Antagonistic activity against Thromboxane A2 receptor in guinea pig trachea in the presence of 11,9-epoxymethano-PGH2	kd	0.0006	uM
1-butyl-3-[2-(4-methylphenoxy)-5-nitrophenyl]sulfonylurea	266289: Displacement of [3H]SQ29,548 from TPalpha receptor (short isoform) expressed in COS7 cells at 1 uM	ic50	0.0007	uM
1-[2-(cyclohexylamino)-5-nitrophenyl]sulfonyl-3-hexylurea	266289: Displacement of [3H]SQ29,548 from TPalpha receptor (short isoform) expressed in COS7 cells at 1 uM	ic50	0.0007	uM
1-[2-(3,5-dimethylanilino)-5-nitrophenyl]sulfonyl-3-pentylurea	266290: Displacement of [3H]SQ-29548 from TPbeta receptor (long isoform) expressed in COS7 cells at 1 uM	ic50	0.0007	uM
1-hexyl-3-[2-(4-methylphenoxy)-5-nitrophenyl]sulfonylurea	266289: Displacement of [3H]SQ29,548 from TPalpha receptor (short isoform) expressed in COS7 cells at 1 uM	ic50	0.0007	uM
3-[2-[[3-[4-(2-cyclohexylethylcarbamoyl)-1,3-oxazol-2-yl]-7-oxabicyclo[2.2.1]heptan-2-yl]methyl]phenyl]propanoic acid	215618: Inhibitory binding activity against TXA2 receptor in human platelet membrane, using [3H]-SQ 29548 as the radioligand	kd	0.0007	uM
3-[2-[[3-[4-(2-phenylethylcarbamoyl)-1,3-oxazol-2-yl]-7-oxabicyclo[2.2.1]heptan-2-yl]methyl]phenyl]propanoic acid	215618: Inhibitory binding activity against TXA2 receptor in human platelet membrane, using [3H]-SQ 29548 as the radioligand	kd	0.0007	uM
2-[(3R)-5-bromo-4-[(4-chlorophenyl)methyl]-7-fluoro-2,3-dihydro-1H-cyclopenta[b]indol-3-yl]acetic acid	277845: Binding affinity to human TP receptor expressed in HEK293 cells	ki	0.0008	uM
1-tert-butyl-3-[2-(4-methylphenyl)sulfanyl-5-nitrophenyl]sulfonylurea	266289: Displacement of [3H]SQ29,548 from TPalpha receptor (short isoform) expressed in COS7 cells at 1 uM	ic50	0.0008	uM
1-cyclohexyl-3-[2-(4-methylphenoxy)-5-nitrophenyl]sulfonylurea	266290: Displacement of [3H]SQ-29548 from TPbeta receptor (long isoform) expressed in COS7 cells at 1 uM	ic50	0.0008	uM
3-[2-[[3-[4-(2-methylbutan-2-ylcarbamoyl)-1,3-oxazol-2-yl]-7-oxabicyclo[2.2.1]heptan-2-yl]methyl]phenyl]propanoic acid	215618: Inhibitory binding activity against TXA2 receptor in human platelet membrane, using [3H]-SQ 29548 as the radioligand	kd	0.0008	uM
4-[2-[[3-[4-(4-cyclohexylbutylcarbamoyl)-1,3-oxazol-2-yl]-7-oxabicyclo[2.2.1]heptan-2-yl]methyl]phenyl]butanoic acid	215618: Inhibitory binding activity against TXA2 receptor in human platelet membrane, using [3H]-SQ 29548 as the radioligand	kd	0.0008	uM
1-tert-butyl-3-[2-(4-methylanilino)-5-nitrophenyl]sulfonylurea	266290: Displacement of [3H]SQ-29548 from TPbeta receptor (long isoform) expressed in COS7 cells at 1 uM	ic50	0.0008	uM
(11E)-11-[2-[5-(benzylcarbamoyl)benzimidazol-1-yl]ethylidene]-6H-benzo[c][1]benzoxepine-2-carboxylic acid	210494: Binding affinity at TXA2/PGH2 receptor by measuring its ability to displace [3H]U-46619 from guinea pig platelets	ki	0.0009	uM
1-[2-(3-methylanilino)-5-nitrophenyl]sulfonyl-3-pentylurea	266289: Displacement of [3H]SQ29,548 from TPalpha receptor (short isoform) expressed in COS7 cells at 1 uM	ic50	0.0010	uM
3-[2-[[3-[(E)-(phenylcarbamoylhydrazinylidene)methyl]-7-oxabicyclo[2.2.1]heptan-2-yl]methyl]phenyl]propanoic acid	212281: The compound was tested for inhibition of specific binding of [3H]-SQ 29,548 to thromboxane A2 receptor in human platelet membranes	kd	0.0010	uM
3-[2-[[3-[4-(4-cyclohexylbutoxycarbonyl)-1,3-oxazol-2-yl]-7-oxabicyclo[2.2.1]heptan-2-yl]methyl]phenyl]propanoic acid	215618: Inhibitory binding activity against TXA2 receptor in human platelet membrane, using [3H]-SQ 29548 as the radioligand	kd	0.0010	uM
(E)-7-[3-[[[2-(4-cyclohexylbutanoylamino)acetyl]amino]methyl]-7-oxabicyclo[2.2.1]heptan-2-yl]hept-5-enoic acid	212278: Binding affinity was determined from the inhibition of [3H]-SQ 29,548 binding to Thromboxane A2 receptor in human platelet membranes.	kd	0.0011	uM
1-[2-(cyclohexylamino)-5-nitrophenyl]sulfonyl-3-pentylurea	210345: In vitro inhibitory concentration of compound against thromboxane A2 receptor	ic50	0.0011	uM
1-benzyl-3-[2-(4-methylanilino)-5-nitrophenyl]sulfonylurea	266290: Displacement of [3H]SQ-29548 from TPbeta receptor (long isoform) expressed in COS7 cells at 1 uM	ic50	0.0012	uM
2-[3-[[3-[4-(4-cyclohexylbutylcarbamoyl)-1,3-oxazol-2-yl]-7-oxabicyclo[2.2.1]heptan-2-yl]methyl]phenyl]acetic acid	215618: Inhibitory binding activity against TXA2 receptor in human platelet membrane, using [3H]-SQ 29548 as the radioligand	kd	0.0012	uM
1-tert-butyl-3-[2-(4-methylphenoxy)-5-nitrophenyl]sulfonylurea	266289: Displacement of [3H]SQ29,548 from TPalpha receptor (short isoform) expressed in COS7 cells at 1 uM	ic50	0.0013	uM
3-[2-[[3-[4-[2-(4-chlorophenyl)ethylcarbamoyl]-1,3-oxazol-2-yl]-7-oxabicyclo[2.2.1]heptan-2-yl]methyl]phenyl]propanoic acid	215618: Inhibitory binding activity against TXA2 receptor in human platelet membrane, using [3H]-SQ 29548 as the radioligand	kd	0.0013	uM
1-[2-(2,6-dimethylanilino)-5-nitrophenyl]sulfonyl-3-pentylurea	266289: Displacement of [3H]SQ29,548 from TPalpha receptor (short isoform) expressed in COS7 cells at 1 uM	ic50	0.0015	uM
(Z)-7-[(1R,2S,3R)-3-(hexylsulfanylmethyl)-7-oxabicyclo[2.2.1]heptan-2-yl]hept-5-enoic acid	80572: Compound was evaluated for inhibition of specific binding of HSQ (5,6-di-3H-SQ 29,548) in washed platelets	kd	0.0016	uM
N-(4-cyclohexylbutyl)-2-[3-[[2-[3-(methanesulfonamido)-3-oxopropyl]phenyl]methyl]-7-oxabicyclo[2.2.1]heptan-2-yl]-1,3-oxazole-4-carboxamide	215618: Inhibitory binding activity against TXA2 receptor in human platelet membrane, using [3H]-SQ 29548 as the radioligand	kd	0.0016	uM
2-[9-[(4-chlorophenyl)methyl]-6,8-difluoro-1,2,3,4-tetrahydrocarbazol-1-yl]acetic acid	266352: Binding affinity to TP receptor	ki	0.0017	uM
(11E)-11-[2-(5-nitrobenzimidazol-1-yl)ethylidene]-6H-benzo[c][1]benzoxepine-2-carboxylic acid	210494: Binding affinity at TXA2/PGH2 receptor by measuring its ability to displace [3H]U-46619 from guinea pig platelets	ki	0.0018	uM
(11E)-11-[2-[5-(trifluoromethyl)benzimidazol-1-yl]ethylidene]-6H-benzo[c][1]benzoxepine-2-carboxylic acid	210494: Binding affinity at TXA2/PGH2 receptor by measuring its ability to displace [3H]U-46619 from guinea pig platelets	ki	0.0022	uM
2-[8-bromo-9-[(4-chlorophenyl)methyl]-1,2,3,4-tetrahydrocarbazol-1-yl]acetic acid	266352: Binding affinity to TP receptor	ki	0.0022	uM
2-[9-[(4-chlorophenyl)methyl]-1,2,3,4-tetrahydrocarbazol-1-yl]acetic acid	266352: Binding affinity to TP receptor	ki	0.0024	uM
3-acetamido-5-[2-[5-bromo-2-[(2,4-difluorophenyl)methoxy]phenyl]-5-methylpyrrol-1-yl]benzoic acid	292924: Inhibition of TP receptor	ic50	0.0025	uM
2-[9-[(4-chlorophenyl)methyl]-6-fluoro-8-methylsulfonyl-1,2,3,4-tetrahydrocarbazol-1-yl]acetic acid	538658: Antagonist activity at prostanoid TP receptor	ki	0.0025	uM

CTD chemical–gene interactions

52 total (human), top 30 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
Valproic Acid	increases methylation, affects expression, increases expression	4
Aspirin	affects response to substance, decreases response to substance	3
SQ 29548	decreases activity, increases activity, affects binding	2
7-(3-(3-hydroxy-4-(4’-iodophenoxy)-1-butenyl)-7-oxabicyclo(2.2.1)heptan-2-yl)-5-heptenoic acid	affects binding, increases activity, decreases reaction	2
15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid	affects binding, increases activity, decreases reaction	2
aristolochic acid I	increases expression	1
FR900359	increases phosphorylation	1
triphenyl phosphate	affects expression	1
propionaldehyde	increases expression	1
bisphenol A	affects cotreatment, increases methylation	1
cinnamaldehyde	affects binding, decreases activity	1
hydroxyhydroquinone	decreases expression	1
sulforaphane	decreases expression	1
11-nor-delta(9)-tetrahydrocannabinol-9-carboxylic acid	affects methylation, increases abundance	1
sodium arsenite	decreases expression	1
butyraldehyde	increases expression	1
S-(1,2-dichlorovinyl)cysteine	decreases expression, affects response to substance, increases expression, affects cotreatment	1
diallyl trisulfide	increases expression	1
pentanal	increases expression	1
di-n-butylphosphoric acid	affects expression	1
8-epi-prostaglandin F2alpha	affects binding, increases activity	1
perfluorooctane sulfonic acid	decreases expression	1
15-deoxy-delta(12,14)-prostaglandin J2	affects reaction, decreases expression	1
entinostat	increases expression	1
nutlin 3	affects cotreatment, increases expression	1
quercetin 3,7,3’,4’-tetrasulfate	affects binding, decreases reaction, increases activity	1
quercetin 3-acetyl-7,3’,4’-trisulfate	increases activity, affects binding, decreases reaction	1
Rosiglitazone	decreases activity, decreases expression, decreases reaction, increases transport	1
Resveratrol	affects cotreatment, decreases expression	1
Fulvestrant	affects cotreatment, increases methylation	1

ChEMBL screening assays

307 unique, capped per target: 199 binding, 107 functional, 1 admet

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1000196	Binding	Binding affinity to thromboxane A2 receptor	Synthesis and evaluation of dibenzothiazepines: a novel class of selective cannabinoid-1 receptor inverse agonists. — J Med Chem
CHEMBL1292331	Functional	Antagonist activity at prostanoid TP receptor	Potent and highly selective DP1 antagonists with 2,3,4,9-tetrahydro-1H-carbazole as pharmacophore. — Bioorg Med Chem Lett
CHEMBL4810225	ADMET	Inhibition of human thromboxane A2 at 0.1 to 1 uM	Discovery of Pemigatinib: A Potent and Selective Fibroblast Growth Factor Receptor (FGFR) Inhibitor. — J Med Chem

Cellosaurus cell lines

7 cell lines: 5 cancer cell line, 2 transformed cell line

First 10 cell lines (id-ordered, not curated):

Cellosaurus	Name	Category	Sex
CVCL_D8WW	Ubigene HCT 116 TBXA2R KO	Cancer cell line	Male
CVCL_D9U0	Ubigene HEK293 TBXA2R KO	Transformed cell line	Female
CVCL_E0QL	Ubigene HeLa TBXA2R KO	Cancer cell line	Female
CVCL_H375	293/TP	Transformed cell line	Female
CVCL_LB38	PathHunter U2OS TBXA2R Activated GPCR Internalization	Cancer cell line	Female
CVCL_LB39	PathHunter U2OS TBXA2R beta-arrestin	Cancer cell line	Female
CVCL_ZK26	Tango TBXA2R-bla U2OS	Cancer cell line	Female

Clinical trials (associated diseases)

600 trials via MONDO — disease-level, not drug-specific.

Trial	Phase	Status	Title
NCT00000374	PHASE4	COMPLETED	Treatment for First-Episode Schizophrenia
NCT00001656	PHASE4	COMPLETED	Comparison of Clozapine vs Olanzapine in Childhood-Onset Psychotic Disorders
NCT00007774	PHASE4	COMPLETED	To Determine if Olanzapine is More Cost Effective Than Haloperidol for the Treatment of Schizophrenia
NCT00014001	PHASE4	COMPLETED	CATIE- Schizophrenia Trial
NCT00018668	PHASE4	COMPLETED	Antipsychotic Response in Schizophrenia
NCT00034801	PHASE4	COMPLETED	Olanzapine Versus Active Comparator in the Treatment of Depression in Patients With Schizophrenia
NCT00034905	PHASE4	COMPLETED	A Comparison of Seroquel vs. Risperidone in Schizophrenia
NCT00036088	PHASE4	COMPLETED	Olanzapine Versus An Active Comparator in the Treatment of Schizophrenia
NCT00044187	PHASE4	COMPLETED	The Assessment of a Weight-Gain Agent for the Treatment of Olanzapine-Associated Anti-Obesity Agent in Patients With Schizophrenia, Schizophreniform Disorder, Schizoaffective Disorder, and Bipolar I Disorder
NCT00044655	PHASE4	COMPLETED	Switching Medication to Treat Schizophrenia
NCT00048828	PHASE4	COMPLETED	Treating Drug-Resistant Childhood Schizophrenia
NCT00053703	PHASE4	COMPLETED	Treatment of Early Onset Schizophrenia Spectrum Disorders (TEOSS)
NCT00056498	PHASE4	COMPLETED	Risperidone Treatment in Schizophrenia Patients Who Are Currently Taking Clozapine
NCT00061802	PHASE4	COMPLETED	Efficacy and Safety of Two Atypical Antipsychotics vs. Placebo in Patients With an Acute Exacerbation of Either Schizophrenia or Schizoaffective Disorder
NCT00080327	PHASE4	COMPLETED	Study of Three Doses of Aripiprazole in Patients With Acute Schizophrenia
NCT00088049	PHASE4	COMPLETED	Study of Olanzapine vs. Aripiprazole in the Treatment of Schizophrenia
NCT00090012	PHASE4	COMPLETED	Comparison of Continuing Olanzapine to Switching to Quetiapine in Overweight or Obese Patients With Schizophrenia and Schizoaffective Disorder
NCT00100776	PHASE4	COMPLETED	Efficacy of High Dose Olanzapine for the Treatment of Schizophrenia and Schizoaffective Disorder
NCT00103571	PHASE4	COMPLETED	Olanzapine Versus Aripiprazole in the Treatment of Acutely Ill Patients With Schizophrenia
NCT00108368	PHASE4	COMPLETED	The Effects of Risperidone and Olanzapine on Thinking
NCT00114595	PHASE4	COMPLETED	Ethyl-Eicosapentaenoic Acid and Tardive Dyskinesia
NCT00130923	PHASE4	COMPLETED	Risperidone Long-acting Versus Oral Risperidone in Patients With Schizophrenia and Alcohol Use Disorder
NCT00137020	PHASE4	COMPLETED	Clinical Effect Of Cross Titration Of Antipsychotics With Ziprasidone In Schizophrenia Or Schizoaffective Disorder
NCT00140166	PHASE4	COMPLETED	Treatment of Acute Schizophrenia With Vitamin Therapy
NCT00145847	PHASE4	COMPLETED	Naltrexone Treatment of Alcohol Abuse in Schizophrenia
NCT00148564	PHASE4	COMPLETED	Energy Homeostasis Under Treatment With Atypical Antipsychotics
NCT00156715	PHASE4	COMPLETED	Efficacy of Quetiapine in the Treatment of Patients With Schizophrenia and a Comorbid Substance Use Disorder
NCT00158223	PHASE4	COMPLETED	Effectiveness of Pimozide in Augmenting the Effects of Clozapine in the Treatment of Schizophrenia
NCT00159081	PHASE4	COMPLETED	One Year Drug Treatment in First-Episode Schizophrenia
NCT00159120	PHASE4	COMPLETED	Maintenance Treatment vs. Stepwise Drug Discontinuation in First-Episode Schizophrenia
NCT00159133	PHASE4	COMPLETED	Prodrome-Based Early Intervention With Antipsychotics vs. Benzodiazepines in First-Episode Schizophrenia
NCT00159757	PHASE4	TERMINATED	12 Week Open, Non-Comparative Switch Study Of Oral Ziprazidone In Previously Treated Schizophrenic Patients
NCT00167817	PHASE4	COMPLETED	Effect of Switch to Aripiprazole on Health and Smoking Parameters in Patients With Schizophrenia: A Pilot Study
NCT00169026	PHASE4	TERMINATED	Alcoholism and Schizophrenia: Effects of Clozapine
NCT00169039	PHASE4	TERMINATED	Clozapine Versus Chlorpromazine for Treatment-Unresponsive Schizophrenia
NCT00169065	PHASE4	COMPLETED	Effectiveness of Clozapine Versus Olanzapine for Treatment-resistant Schizophrenia
NCT00169091	PHASE4	TERMINATED	Clozapine Versus Haloperidol for Treating the First Episode of Schizophrenia
NCT00176423	PHASE4	COMPLETED	Efficacy Study of Galantamine for Cognitive Impairments in Schizophrenia
NCT00176436	PHASE4	COMPLETED	Atomoxetine for Treatment of Weight Gain in Olanzapine or Clozapine Patients
NCT00177008	PHASE4	COMPLETED	Aripiprazole for the Treatment of Schizophrenia With Co-Morbid Social Anxiety