P2RY12

Summary

P2RY12 (purinergic receptor P2Y12, HGNC:18124) is a protein-coding gene on chromosome 3q25.1, encoding P2Y purinoceptor 12 (Q9H244). Receptor for ADP and ATP coupled to G-proteins that inhibit the adenylyl cyclase second messenger system.

The product of this gene belongs to the family of G-protein coupled receptors. This family has several receptor subtypes with different pharmacological selectivity, which overlaps in some cases, for various adenosine and uridine nucleotides. This receptor is involved in platelet aggregation, and is a potential target for the treatment of thromboembolisms and other clotting disorders. Mutations in this gene are implicated in bleeding disorder, platelet type 8 (BDPLT8). Alternative splicing results in multiple transcript variants of this gene.

Source: NCBI Gene 64805 — RefSeq curated summary.

At a glance

• Gene–disease (curated): platelet-type bleeding disorder 8 (Definitive, ClinGen)
• GWAS associations: 1
• Clinical variants (ClinVar): 24 total — 1 pathogenic, 3 likely-pathogenic
• Phenotypes (HPO): 8
• Druggable target: yes — 11 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_022788

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:18124
Approved symbol	P2RY12
Name	purinergic receptor P2Y12
Location	3q25.1
Locus type	gene with protein product
Status	Approved
Aliases	P2Y12, SP1999, HORK3
Ensembl gene	ENSG00000169313
Ensembl biotype	protein_coding
OMIM	600515
Entrez	64805

Gene structure

Transcript identifiers

Ensembl transcripts: 5 — 4 protein_coding, 1 retained_intron

ENST00000302632, ENST00000468596, ENST00000955805, ENST00000955806, ENST00000955807

RefSeq mRNA: 2 — MANE Select: NM_022788 NM_022788, NM_176876

CCDS: CCDS3159

Canonical transcript exons

ENST00000302632 — 3 exons

Exon	Start	End
ENSE00001157311	151336843	151338859
ENSE00001169257	151340596	151340760
ENSE00001813621	151384692	151384753

Expression profiles

Bgee: expression breadth ubiquitous, 204 present calls, max score 97.12.

FANTOM5 (CAGE): breadth broad, TPM avg 3.0864 / max 331.6989, expressed in 240 samples.

FANTOM5 promoters (11 alternative TSS)

Promoter ID	TPM avg	Samples expressed
45161	1.9173	233
45152	0.7420	86
45154	0.1138	52
45153	0.0927	54
45151	0.0773	42
45150	0.0675	37
45157	0.0288	1
45155	0.0149	1
202983	0.0134	5
45158	0.0094	1

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
inferior vagus X ganglion	UBERON:0005363	97.12	gold quality
superior vestibular nucleus	UBERON:0007227	96.60	gold quality
ventral tegmental area	UBERON:0002691	94.74	gold quality
subthalamic nucleus	UBERON:0001906	93.92	gold quality
medulla oblongata	UBERON:0001896	92.95	gold quality
Brodmann (1909) area 46	UBERON:0006483	92.22	gold quality
dorsal plus ventral thalamus	UBERON:0001897	91.45	gold quality
monocyte	CL:0000576	90.55	gold quality
corpus callosum	UBERON:0002336	89.35	gold quality
dorsal root ganglion	UBERON:0000044	89.32	gold quality
leukocyte	CL:0000738	89.22	gold quality
midbrain	UBERON:0001891	88.67	gold quality
spinal cord	UBERON:0002240	88.35	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	88.10	gold quality
substantia nigra	UBERON:0002038	87.86	gold quality
C1 segment of cervical spinal cord	UBERON:0006469	87.68	gold quality
trigeminal ganglion	UBERON:0001675	87.66	gold quality
substantia nigra pars reticulata	UBERON:0001966	86.40	gold quality
prefrontal cortex	UBERON:0000451	84.69	gold quality
amygdala	UBERON:0001876	81.85	gold quality
temporal lobe	UBERON:0001871	81.19	gold quality
epithelial cell of pancreas	CL:0000083	80.99	silver quality
entorhinal cortex	UBERON:0002728	80.69	gold quality
substantia nigra pars compacta	UBERON:0001965	80.65	gold quality
pons	UBERON:0000988	80.48	gold quality
Ammon’s horn	UBERON:0001954	80.16	gold quality
hypothalamus	UBERON:0001898	79.95	gold quality
caudate nucleus	UBERON:0001873	79.62	gold quality
dorsolateral prefrontal cortex	UBERON:0009834	79.19	gold quality
medial globus pallidus	UBERON:0002477	78.76	gold quality

Single-cell (SCXA)

Detected in 6 experiment(s), a significant marker in 4.

Experiment	Marker?	Max mean expression
E-GEOD-84465	yes	781.01
E-GEOD-100618	yes	118.58
E-HCAD-35	yes	32.50
E-HCAD-25	yes	15.76
E-HCAD-30	no	932.44
E-ANND-3	no	2.17

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

71 targeting P2RY12, 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-126-5P	100.00	72.71	3180
HSA-MIR-4795-3P	100.00	74.62	4024
HSA-MIR-3646	100.00	73.56	5283
HSA-MIR-5011-5P	100.00	83.46	5820
HSA-MIR-548C-3P	99.99	74.01	7587
HSA-MIR-4775	99.98	75.00	6394
HSA-MIR-4789-5P	99.98	70.76	2721
HSA-MIR-4803	99.98	71.99	3117
HSA-MIR-520D-5P	99.98	73.34	4883
HSA-MIR-524-5P	99.98	73.43	4882
HSA-MIR-548AT-5P	99.96	70.83	2666
HSA-MIR-651-3P	99.94	73.48	5177
HSA-MIR-335-3P	99.93	73.36	4958
HSA-MIR-6508-5P	99.92	70.67	2465
HSA-MIR-329-3P	99.91	66.56	1234
HSA-MIR-362-3P	99.91	66.38	1267
HSA-MIR-6809-3P	99.91	71.45	3814
HSA-MIR-4753-3P	99.90	71.03	3786
HSA-MIR-153-5P	99.89	73.86	6317
HSA-MIR-3140-3P	99.88	68.47	2069
HSA-MIR-8067	99.86	69.59	2260
HSA-MIR-6844	99.82	70.69	2423
HSA-MIR-4799-5P	99.82	70.60	2663
HSA-MIR-6875-3P	99.82	70.26	2983
HSA-MIR-4659A-3P	99.80	72.62	4248
HSA-MIR-4659B-3P	99.80	72.62	4248
HSA-MIR-4760-5P	99.80	69.88	1619
HSA-MIR-139-5P	99.80	69.50	1399
HSA-MIR-548AG	99.77	69.25	1492
HSA-MIR-5002-5P	99.76	70.84	1763

Literature-anchored findings (GeneRIF, showing 40)

• Characterization and channel coupling of the nucleotide receptor in brain capillary endothelial cells (PMID:12080041)
• identification of the reactive cysteine residues on the human P2Y(12) receptor by site-directed mutagenesis using pCMBS as the thiol reagent (PMID:12560222)
• PI3-K activation is signaled by rapid feedback amplification that involves P2Y(12) receptor-mediated activation of Syk. (PMID:12606772)
• the P2Y(1) purinoceptor and the P2Y(12)receptor appear to be involved in ADP-induced platelet shape change, an early phase of platelet activation that precedes aggregation (PMID:12623443)
• Intercellular calcium communication is primarily mediated by a signaling mchanism operating between this protein, ITGA2B and ITGB3. (PMID:12668663)
• In healthy subjects ADP-induced platelet aggregation is associated with a haplotype of the P2Y12 receptor gene. Carriers of the H2 haplotype may have an increased risk of atherothrombosis and less response to platelet inhibitors (PMID:12912815)
• Supports P2Y(12) as a drug target compared with P2Y(1). (PMID:14644082)
• ADP-mediated P2Y1 and P2Y12 receptor activation supports LPA-induced platelet aggregation. (PMID:14645014)
• The P2Y12 H2 haplotype is associated with atherosclerosis. (PMID:14662702)
• stimulation of the human P2Y12 receptor stably expressed in Chinese hamster ovary cells activates two major intracellular signaling mechanisms leading either to cell proliferation or to actin cytoskeleton reorganization (PMID:14717977)
• Whereas P2RY1 antagonism did not affect collagen or thrombin-induced thrombin generation, P2RY12 antagonism did decrease both, suggesting that ADP potentiates thrombin generation primarily through the P2Y12 receptor (PMID:15099288)
• GIRK channels are important functional effectors of the P2Y(12) receptor in human platelets. (PMID:15142872)
• the Src family kinase inhibitor PP1 selectively potentiates the contribution to the calcium response by P2Y(12), although inhibition of adenylate cyclase by P2Y(12) is unaffected (PMID:15187029)
• both P2Y12 and P2Y1 contribute to ADP-potentiation of platelet-derived microparticles generation induced by collagen (PMID:15203713)
• ADP signaling through P2Y(1) may contribute to the initial stages of platelet adhesion and activation mediated by immobilized VWF, and through P2Y(12) to sustained thrombus formation. (PMID:15284110)
• platelet ADP receptor P2Y(12) and clusterin are downregulated in patients with systemic lupus erythematosus (PMID:15304052)
• Results describe the cloning of DNA sequences encoding the murine ortholog of the human P2Y12 receptor, and its expression in the mouse brain. (PMID:15464998)
• P2Y12 receptors could play a key role in the hypersensitivity of platelets in type 2 diabetic patients. (PMID:15483100)
• Absence of desensitization of the Gi protein-coupled P2Y12 receptor-dependent responses could represent a mechanism to preserve the hemostatic properties in platelets (PMID:15602005)
• both P2Y(1) and P2Y(12) desensitize in human platelets; P2Y(12), but not P2Y(1), desensitization is mediated by GRKs (PMID:15665114)
• Galpha(i) signaling downstream of P2Y12 activation, but not Galpha(q) or Galpha(z) signaling downstream of P2Y1 or alpha2A activation, respectively, has a requirement for lipid rafts that is necessary for its function in ADP-mediated platelet activation (PMID:15869601)
• P2Y12 ADP receptor has a role in tyrosine phosphorylation of proteins of 27 and 31 kDa in thrombin-stimulated human platelets (PMID:15886804)
• a P2Y12 34C>T polymorphism may have a role in development of ischemic cerebrovascular events in patients with peripheral artery disease (PMID:15933261)
• function in the platelet procoagulant response (PMID:15968399)
• There is no association between P2Y12 receptor gene polymorphism and platelet response to clopidogrel in patients with coronary artery disease. (PMID:16181985)
• Identification of 5-phosphoribosyl 1-pyrophosphate and leukotriene E4 as P2Y12 receptor agonists. (PMID:16185654)
• Results suggest that P2Y12 plays a potentiatory role in ADP-induced shape change through regulation of the Rho kinase pathway. (PMID:16236603)
• This study therefore is the first to reveal distinct roles for PKC isoforms in the regulation of platelet P2Y receptor function and trafficking. (PMID:16804093)
• Data show that at relatively high concentration of agonist, inhibition of the P2Y12 receptor and of calcium mobilization result in complete inhibition of PAR4-induced aggregation, with no effect on either thrombin or PAR1-mediated platelet aggregation. (PMID:16837456)
• Outside-in signaling via P2Y12 and both PI3Kbeta and PI3Kgamma isoforms is required for maintenance of a platelet aggregate. (PMID:16840732)
• No influence of the T744C polymorphism of the P2Y12 receptor gene on clopidogrel response in acute coronary syndrome (PMID:17337040)
• the haplotype H2 of purinergic receptor P2Y G-protein coupled 12 (P2RY12) was significantly associated with a lower risk of incident Deep vein thrombosis/pulmonary embolism as compared to the reference haplotype H1 (PMID:17707382)
• Gene sequence variations of the P2Y12 receptor gene are associated with the presence of significant coronary artery disease, particularly in non-smoking individuals (PMID:17803810)
• common variation in the P2Y12 gene predicts restenosis in percutaneous coronary intervention-treated patients (PMID:18175333)
• The P2Y(13) Met-158-Thr polymorphism is in tight linkage disequilibrium with the P2Y(12) locus but is not associated with acute myocardial infaction or classical cardiovascular risk factors (PMID:18213371)
• Use VerifyNow P2Y12 assay to measure platelet P2Y12 receptor blockade by prasugrel and clopidogrel. (PMID:18278193)
• Coexisting polymorphisms of the genes affecting clopiogrel resistance may influence platelet activation (PMID:18577829)
• present data clearly show that P2Y purinoceptor 11 and P2Y purinoceptor 12 are expressed in human pancreatic islets (PMID:18726826)
• the the G(i)-coupled P2Y12 receptor has a role in the regulation of diacylglycerol-mediated events in activated platelets (PMID:18755689)
• plays a critical role in the regulation of integrin alphaIIb beta3 functions. (review) (PMID:18800613)

Cross-species orthologs

3 orthologs

Organism	Symbol	Gene ID
danio_rerio	p2ry12	ENSDARG00000069945
mus_musculus	P2ry12	ENSMUSG00000036353
rattus_norvegicus	P2ry12	ENSRNOG00000013902

Paralogs (6): GPR87 (ENSG00000138271), PTAFR (ENSG00000169403), GPR34 (ENSG00000171659), P2RY14 (ENSG00000174944), GPR171 (ENSG00000174946), P2RY13 (ENSG00000181631)

Protein

Protein identifiers

P2Y purinoceptor 12 — Q9H244 (reviewed: Q9H244)

Alternative names: ADP-glucose receptor, P2T(AC), P2Y(AC), P2Y(cyc), P2Y12 platelet ADP receptor, SP1999

All UniProt accessions (1): Q9H244

UniProt curated annotations — full annotation on UniProt →

Function. Receptor for ADP and ATP coupled to G-proteins that inhibit the adenylyl cyclase second messenger system. Not activated by UDP and UTP. Required for normal platelet aggregation and blood coagulation.

Subcellular location. Cell membrane.

Tissue specificity. Highly expressed in the platelets, lower levels in the brain. Lowest levels in the lung, appendix, pituitary and adrenal gland. Expressed in the spinal cord and in the fetal brain.

Disease relevance. Bleeding disorder, platelet-type, 8 (BDPLT8) [MIM:609821] A condition characterized by mild to moderate mucocutaneous bleeding, and excessive bleeding after surgery or trauma. The defect is due to severe impairment of platelet response to ADP resulting in defective platelet aggregation. The disease is caused by variants affecting the gene represented in this entry.

Domain organisation. The transmembrane domain is composed of seven transmembrane helices; most of these are not strictly perpendicular to the plane of the membrane, but are tilted and/or kinked. Agonist binding promotes a conformation change in the extracellular loops that leads to an inward movement of the transmembrane helices. Antagonists such as AZD1283 can bind to an overlapping site, but block the inward movement of the transmembrane helices.

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

RefSeq proteins (2): NP_073625, NP_795345 (=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000276	GPCR_Rhodpsn	Family
IPR005394	P2Y12_rcpt	Family
IPR017452	GPCR_Rhodpsn_7TM	Domain

Pfam: PF00001

UniProt features (62 total): helix 13, binding site 10, mutagenesis site 9, topological domain 8, transmembrane region 7, sequence variant 4, modified residue 2, glycosylation site 2, disulfide bond 2, chain 1, region of interest 1, compositionally biased region 1, strand 1, turn 1

Structure

Experimental structures (PDB)

5 structures.

PDB	Method	Resolution (Å)
4PXZ	X-RAY DIFFRACTION	2.5
4NTJ	X-RAY DIFFRACTION	2.62
7PP1	X-RAY DIFFRACTION	2.78
7XXI	ELECTRON MICROSCOPY	3
4PY0	X-RAY DIFFRACTION	3.1

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9H244-F1	85.11	0.59

Functional residue map

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

Ligand- & substrate-binding residues (10): 93; 97; 105; 156–159; 175–179; 187; 191; 256–259; 263; 280

Post-translational modifications (2): 55, 57

Disulfide bonds (2): 17–270, 97–175

Glycosylation sites (2): 6, 13

Mutagenesis-validated functional residues (9):

Position	Phenotype
80	abolishes adp binding.
83	no effect on adp binding.
97	abolishes adp binding.
156	slightly decreases affinity for adp.
159	slightly decreases affinity for adp.
175	abolishes adp binding.
256	decreases affinity for adp.
280	abolishes adp binding.
281	abolishes adp binding.

Function

Pathways and Gene Ontology

Reactome pathways

3 pathways

ID	Pathway
R-HSA-392170	ADP signalling through P2Y purinoceptor 12
R-HSA-417957	P2Y receptors
R-HSA-418594	G alpha (i) signalling events

MSigDB gene sets: 256 (showing top): GOBP_G_PROTEIN_COUPLED_PURINERGIC_RECEPTOR_SIGNALING_PATHWAY, GOBP_RESPONSE_TO_NITROGEN_COMPOUND, GOBP_G_PROTEIN_COUPLED_PURINERGIC_NUCLEOTIDE_RECEPTOR_SIGNALING_PATHWAY, GOBP_MYELOID_LEUKOCYTE_MIGRATION, REACTOME_PLATELET_ACTIVATION_SIGNALING_AND_AGGREGATION, GOBP_PLATELET_ACTIVATION, REACTOME_P2Y_RECEPTORS, GOCC_CELL_SURFACE, GOBP_REGULATION_OF_RUFFLE_ASSEMBLY, GOBP_NEUROGENESIS, GOBP_RESPONSE_TO_AXON_INJURY, GOBP_REGULATION_OF_CELLULAR_COMPONENT_BIOGENESIS, GOBP_CELLULAR_RESPONSE_TO_OXYGEN_CONTAINING_COMPOUND, GOBP_REGULATION_OF_LEUKOCYTE_MIGRATION, GOBP_FOREBRAIN_DEVELOPMENT

GO Biological Process (30): monoatomic ion transport (GO:0006811), substrate-dependent cell migration, cell extension (GO:0006930), G protein-coupled receptor signaling pathway (GO:0007186), adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway (GO:0007193), phospholipase C-activating G protein-coupled receptor signaling pathway (GO:0007200), hemostasis (GO:0007599), calcium-mediated signaling (GO:0019722), cerebral cortex radial glia-guided migration (GO:0021801), cell projection organization (GO:0030030), lamellipodium assembly (GO:0030032), platelet activation (GO:0030168), positive regulation of integrin activation by cell surface receptor linked signal transduction (GO:0033626), positive regulation of cell adhesion mediated by integrin (GO:0033630), positive regulation of monoatomic ion transport (GO:0043270), response to axon injury (GO:0048678), regulation of chemotaxis (GO:0050920), positive regulation of chemotaxis (GO:0050921), establishment of localization in cell (GO:0051649), positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction (GO:0051897), platelet aggregation (GO:0070527), cellular response to ATP (GO:0071318), visual system development (GO:0150063), positive regulation of ruffle assembly (GO:1900029), regulation of microglial cell migration (GO:1904139), positive regulation of microglial cell migration (GO:1904141), G protein-coupled adenosine receptor signaling pathway (GO:0001973), signal transduction (GO:0007165), adenylate cyclase-modulating G protein-coupled receptor signaling pathway (GO:0007188), blood coagulation (GO:0007596), G protein-coupled purinergic nucleotide receptor signaling pathway (GO:0035589)

GO Molecular Function (5): G protein-coupled adenosine receptor activity (GO:0001609), G protein-coupled ADP receptor activity (GO:0001621), guanyl-nucleotide exchange factor activity (GO:0005085), G protein-coupled purinergic nucleotide receptor activity (GO:0045028), G protein-coupled receptor activity (GO:0004930)

GO Cellular Component (5): plasma membrane (GO:0005886), cell surface (GO:0009986), membrane (GO:0016020), cell projection membrane (GO:0031253), cell body membrane (GO:0044298)

Reactome top-level categories

Rollup of top-3 pathways:

Category	Pathways
Signal amplification	1
Nucleotide-like (purinergic) receptors	1
GPCR downstream signalling	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
G protein-coupled receptor activity	3
cellular anatomical structure	3
plasma membrane bounded cell projection assembly	2
G protein-coupled receptor signaling pathway	2
chemotaxis	2
transport	1
substrate-dependent cell migration	1
signal transduction	1
adenylate cyclase-modulating G protein-coupled receptor signaling pathway	1
adenylate cyclase inhibitor activity	1
phospholipase C activator activity	1
regulation of body fluid levels	1
intracellular signaling cassette	1
cerebral cortex radially oriented cell migration	1
telencephalon glial cell migration	1
cellular component organization	1
lamellipodium organization	1
cell activation	1
blood coagulation	1
cell surface receptor signaling pathway	1
integrin activation	1
positive regulation of integrin activation	1
cell adhesion mediated by integrin	1
regulation of cell adhesion mediated by integrin	1
positive regulation of cell adhesion	1
monoatomic ion transport	1
regulation of monoatomic ion transport	1
positive regulation of transport	1
response to wounding	1
regulation of response to external stimulus	1
regulation of locomotion	1
positive regulation of response to external stimulus	1
positive regulation of locomotion	1
regulation of chemotaxis	1
establishment of localization	1
cellular localization	1
phosphatidylinositol 3-kinase/protein kinase B signal transduction	1
regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction	1
positive regulation of intracellular signal transduction	1
platelet activation	1

Protein interactions and networks

STRING

1694 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
P2RY12	P2RX1	P51575	976
P2RY12	P2RY1	P47900	957
P2RY12	CYP2C19	P33259	912
P2RY12	TMEM119	Q4V9L6	867
P2RY12	TREM2	Q9NZC2	867
P2RY12	GP6	Q9HCN6	853
P2RY12	SELP	P16109	819
P2RY12	PPIG	Q13427	792
P2RY12	P2RX4	Q99571	792
P2RY12	ITGA2B	P08514	774
P2RY12	VASP	P50552	772
P2RY12	F3	P13726	742
P2RY12	OLFML3	Q9NRN5	733
P2RY12	CYP3A5	P20815	726
P2RY12	P2RX7	Q99572	724

IntAct

4 interactions, top by confidence:

A	B	Type	Score
P2RY12	P2RY12	psi-mi:“MI:0915”(physical association)	0.400
P2RY12	GPR89A	psi-mi:“MI:0914”(association)	0.350

BioGRID (136): VKORC1L1 (Affinity Capture-MS), LMBR1 (Affinity Capture-MS), KIAA2013 (Affinity Capture-MS), ATP5B (Affinity Capture-MS), SAAL1 (Affinity Capture-MS), GEMIN4 (Affinity Capture-MS), TTYH3 (Affinity Capture-MS), ECSIT (Affinity Capture-MS), SACM1L (Affinity Capture-MS), XPO4 (Affinity Capture-MS), MPP6 (Affinity Capture-MS), TMEM161B (Affinity Capture-MS), IPO11 (Affinity Capture-MS), ACP2 (Affinity Capture-MS), NME2P1 (Affinity Capture-MS)

ESM2 similar proteins: B5X337, D4A4Q2, D4A7K7, O00398, O14626, O35881, P21556, P25105, P32249, P43657, P60019, Q15391, Q1RMI1, Q2NNR5, Q3SAG9, Q3SX17, Q3U507, Q3U6B2, Q3UJF0, Q3ZBK9, Q4G072, Q5ZI82, Q6XCF2, Q80Z39, Q8BFU7, Q8BG55, Q8BLG2, Q8BMC0, Q920A1, Q924T8, Q924T9, Q95KC3, Q95N02, Q95N03, Q99677, Q99JA4, Q99MT7, Q9BXC1, Q9BY21, Q9CPV9

Diamond homologs: D4A4Q2, O14626, O35881, P30992, P32250, Q15391, Q3SX17, Q3ZBK9, Q6GUG4, Q8BG55, Q95KC3, Q99MT7, Q9BE53, Q9BPV8, Q9BY21, Q9CPV9, Q9D8I2, Q9EPX4, Q9ESG6, Q9H244, O00254, P25105, Q28553, P60019, Q05394, Q3SAG9, Q6XCF2, Q9R1K6, Q9UPC5, A5PLE7, E7FEL0, E9QJ73, O00398, O46685, O77590, O88680, P21556, P25104, P30555, P30560

SIGNOR signaling

5 interactions.

A	Effect	B	Mechanism
P2RY12	“up-regulates activity”	GNAI1	binding
P2RY12	“up-regulates activity”	GNAI3	binding
P2RY12	“up-regulates activity”	GNAO1	binding
P2RY12	“up-regulates activity”	GNAZ	binding
ADP	“up-regulates activity”	P2RY12	“chemical activation”

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	1
Likely pathogenic	3
Uncertain significance	8
Likely benign	2
Benign	2

Top pathogenic / likely-pathogenic (4)

Variant ID	HGVS	Classification
592166	NM_001393769.1(MED12L):c.4791-1G>A	Pathogenic
2572656	NM_022788.5(P2RY12):c.662dup (p.Arg222fs)	Likely pathogenic
3391828	GRCh37/hg19 3q24-25.1(chr3:146504503-151662391)x1	Likely pathogenic
4529923	NM_001393769.1(MED12L):c.2394_2395del (p.Val800fs)	Likely pathogenic

SpliceAI

2848 predictions. Top by Δscore:

Variant	Effect	Δscore
3:151338856:TTAC:T	acceptor_gain	1.0000
3:151338857:TAC:T	acceptor_gain	1.0000
3:151338858:AC:A	acceptor_gain	1.0000
3:151338859:CC:C	acceptor_gain	1.0000
3:151338860:C:CC	acceptor_gain	1.0000
3:151338861:T:A	acceptor_loss	1.0000
3:151340590:CATTA:C	donor_loss	1.0000
3:151340591:ATTAC:A	donor_loss	1.0000
3:151340592:TTACC:T	donor_loss	1.0000
3:151340593:TACCT:T	donor_loss	1.0000
3:151340595:CCTG:C	donor_loss	1.0000
3:151340759:CT:C	acceptor_gain	1.0000
3:151350053:TTTCA:T	acceptor_loss	1.0000
3:151350055:TCAG:T	acceptor_loss	1.0000
3:151350056:CAG:C	acceptor_loss	1.0000
3:151350057:A:AG	acceptor_gain	1.0000
3:151350057:A:AT	acceptor_loss	1.0000
3:151350057:AG:A	acceptor_gain	1.0000
3:151350057:AGGAT:A	acceptor_gain	1.0000
3:151350058:G:GA	acceptor_gain	1.0000
3:151350058:GG:G	acceptor_gain	1.0000
3:151350058:GGA:G	acceptor_gain	1.0000
3:151350058:GGAT:G	acceptor_gain	1.0000
3:151350058:GGATG:G	acceptor_gain	1.0000
3:151350203:GGGG:G	donor_gain	1.0000
3:151350204:G:GT	donor_gain	1.0000
3:151350204:GGG:G	donor_gain	1.0000
3:151350205:GG:G	donor_gain	1.0000
3:151350205:GGG:G	donor_gain	1.0000
3:151350206:GG:G	donor_gain	1.0000

AlphaMissense

2264 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
3:151338401:A:G	W149R	0.998
3:151338401:A:T	W149R	0.998
3:151337962:G:T	P295Q	0.997
3:151338079:C:G	R256P	0.997
3:151338099:A:C	F249L	0.997
3:151338099:A:T	F249L	0.997
3:151338101:A:G	F249L	0.997
3:151338252:G:C	F198L	0.997
3:151338252:G:T	F198L	0.997
3:151338254:A:G	F198L	0.997
3:151338481:C:G	R122P	0.997
3:151338556:C:G	C97S	0.997
3:151338557:A:T	C97S	0.997
3:151338094:G:C	P251R	0.996
3:151338094:G:T	P251H	0.996
3:151338251:A:G	W199R	0.996
3:151338251:A:T	W199R	0.996
3:151338309:T:A	K179N	0.996
3:151338309:T:G	K179N	0.996
3:151338322:C:G	C175S	0.996
3:151338323:A:T	C175S	0.996
3:151338500:C:G	G116R	0.996
3:151338500:C:T	G116R	0.996
3:151338513:A:C	S111R	0.996
3:151338513:A:T	S111R	0.996
3:151338515:T:G	S111R	0.996
3:151338658:A:G	L63P	0.996
3:151337962:G:C	P295R	0.995
3:151337972:A:G	C292R	0.995
3:151337993:A:G	W285R	0.995

dbSNP variants (sampled 300 via entrez): RS1000069760 (3:151359348 CTT>C), RS1000097247 (3:151353863 C>A,T), RS1000149512 (3:151353542 A>G), RS1000168546 (3:151340643 A>G), RS1000200629 (3:151372954 C>T), RS1000202312 (3:151384376 G>A,C), RS1000390935 (3:151359532 C>A), RS1000514511 (3:151363876 G>T), RS1000675105 (3:151364409 A>G), RS1000808269 (3:151377549 G>A), RS1000878881 (3:151351033 G>A), RS1000929386 (3:151350747 T>TA), RS1001037648 (3:151341251 T>C), RS1001069973 (3:151370717 T>C), RS1001088514 (3:151340989 T>G)

Disease associations

OMIM: gene MIM:600515 | disease phenotypes: MIM:609821, MIM:618872

GenCC curated gene-disease

Disease	Classification	Inheritance
platelet-type bleeding disorder 8	Strong	Autosomal recessive

ClinGen Gene-Disease Validity (2)

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

Disease	Classification	Inheritance
platelet-type bleeding disorder 8	Definitive	AR
platelet-type bleeding disorder 8	Moderate	AD

Mondo (4): platelet-type bleeding disorder 8 (MONDO:0012354), intellectual disability (MONDO:0001071), Nizon-Isidor syndrome (MONDO:0030030), thrombocytopenia (MONDO:0002049)

Orphanet (2): Bleeding disorder due to P2Y12 defect (Orphanet:36355), NON RARE IN EUROPE: Unexplained intellectual disability (Orphanet:319658)

HPO phenotypes

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

HPO	Term
HP:0000007	Autosomal recessive inheritance
HP:0000421	Epistaxis
HP:0000978	Bruising susceptibility
HP:0001892	Abnormal bleeding
HP:0001934	Persistent bleeding after trauma
HP:0004846	Prolonged bleeding after surgery
HP:0004866	Impaired ADP-induced platelet aggregation
HP:0031364	Ecchymosis

GWAS associations

1 associations (top):

Study	Trait	p-value
GCST006479_120	Diverticular disease	9.000000e-11

EFO canonical traits (1, from GWAS)

EFO ID	Trait name
EFO:0009959	diverticular disease

MeSH disease descriptors (3)

Descriptor	Name	Tree numbers
D008607	Intellectual Disability	C10.597.606.360; C23.888.592.604.646; F01.700.687; F03.625.539
D013921	Thrombocytopenia	C15.378.140.855; C15.378.243.937
C565220	Bleeding Disorder Due To P2RY12 Defect (supp.)

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL2001 (SINGLE PROTEIN), CHEMBL4524011 (PROTEIN FAMILY)

Molecules with ChEMBL bioactivity

11 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 70,174 (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
CHEMBL1097279	CANGRELOR TETRASODIUM	4	108
CHEMBL1201772	PRASUGREL	4	844
CHEMBL1771	CLOPIDOGREL	4	40,370
CHEMBL334966	CANGRELOR	4	900
CHEMBL398435	TICAGRELOR	4	2,956
CHEMBL760	ANAGRELIDE	4	23,754
CHEMBL4297589	SELATOGREL	3	53
CHEMBL1162175	REGRELOR	2	10
CHEMBL2103828	ELINOGREL	2	273
CHEMBL261244	REGRELOR DISODIUM	2	3
CHEMBL69139	LIXAZINONE	2	903

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

PharmGKB clinical annotations

8 annotations.

Variant	Type	Level	Drugs	Phenotypes
rs2046934	Efficacy	3	clopidogrel	Major Adverse Cardiac Events (MACE)
rs2046934	Efficacy	4	clopidogrel	Acute coronary syndrome;Angina Pectoris
rs3732759	Efficacy	3	clopidogrel	Coronary Disease
rs6785930	Efficacy,Toxicity	4	clopidogrel
rs6787801	Efficacy	3	clopidogrel
rs6787801	Efficacy	3	cangrelor
rs6809699	Efficacy	3	clopidogrel	Coronary Artery Disease
rs9859552	Efficacy	3	cangrelor

PharmGKB variants

21 variants.

Variant	Genes	Level	Score	#Clin annots	Drugs
rs2046934	MED12L, P2RY12	3	1.75	2	clopidogrel
rs5853517	MED12L, P2RY12		0.00	0
rs6785930	MED12L, P2RY12	4	-2.25	1	clopidogrel
rs6787801	MED12L, P2RY12	3	2.50	2	cangrelor;clopidogrel
rs6801273	MED12L, P2RY12		0.00	0
rs6809699	MED12L, P2RY12	3	2.25	1	clopidogrel
rs9859552	MED12L, P2RY12	3	0.50	1	cangrelor
rs10935838	MED12L, P2RY12		0.00	0
rs16846673	MED12L, P2RY12		0.00	0
rs10935842	MED12L, P2RY12		0.00	0
rs4603933	MED12L, P2RY12		0.00	0
rs1491974	MED12L, P2RY12		0.00	0
rs9859538	MED12L, P2RY12		0.00	0
rs7634096	MED12L, P2RY12		0.00	0
rs12487835	MED12L, P2RY12		0.00	0
rs16863336	MED12L, P2RY12		0.00	0
rs12497330	MED12L, P2RY12		0.00	0
rs12637988	MED12L, P2RY12		0.00	0
rs16863323	MED12L, P2RY12		0.00	0
rs7428575	MED12L, P2RY12		0.00	0
rs3732759	MED12L, P2RY12	3	2.00	1	clopidogrel

GtoPdb / IUPHAR curated pharmacology

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

Target class: gpcr — P2Y receptors

Most potent curated ligand interactions (29 total), top 25:

Ligand	Action	Affinity	Parameter
[3H]2MeSADP	Full agonist	9.6	pIC50
2MeSADP	Full agonist	9.2	pKi
selatogrel	Antagonist	8.7	pKd
ADPβS	Full agonist	8.6	pIC50
[3H]AZ12464237	Antagonist	8.5	pKd
[3H]PSB-0413	Antagonist	8.5	pKd
[3H]PSB-22219	Antagonist	8.34	pKd
PSB-22219	Antagonist	8.3	pKi
AR-C67085	Antagonist	8.2	pKd
compound 20o [PMID: 22984835]	Antagonist	8.1	pKi
cangrelor	Antagonist	8.0	pIC50
AZD1283	Antagonist	8.0	pKi
regrelor	Antagonist	7.95	pIC50
ARL66096	Antagonist	7.95	pIC50
ticagrelor	Antagonist	7.85	pKi
PSB-0702	Antagonist	7.7	pIC50
PSB-0739	Antagonist	7.6	pKi
BX 667	Antagonist	7.0	pIC50
clopidogrel (active metabolite)	Antagonist	6.9	pKi
compound 4 [PMID: 22984835]	Antagonist	6.9	pKi
compound 4 [PMID: 23083103]	Antagonist	6.9	pIC50
compound 58l [PMID: 30843696]	Antagonist	6.53	pIC50
BX 048	Antagonist	6.5	pIC50
INS49266	Antagonist	6.28	pIC50
Ap4A	Antagonist	6.0	pIC50

Binding affinities (BindingDB)

17 measured of 17 human assays (17 total across all organisms); most potent 17 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
3,3,3-trifluoropropyl 4-[2-[[4-[2-[(2S)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-7-methylquinoline-2-carbonyl]amino]acetyl]piperazine-1-carboxylate	IC50	3 nM	US-8669266: Quinoline-carboxamide derivatives as P2Y12 antagonists
butyl 4-[(2S)-2-[[4-[2-[(2S)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-7-methylquinoline-2-carbonyl]amino]-4-hydroxybutanoyl]piperazine-1-carboxylate	IC50	4 nM	US-8669266: Quinoline-carboxamide derivatives as P2Y12 antagonists
butyl 4-[(2S)-2-[[4-[2-[(2S)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-7-methylquinoline-2-carbonyl]amino]-3-hydroxypropanoyl]piperazine-1-carboxylate	IC50	4 nM	US-8669266: Quinoline-carboxamide derivatives as P2Y12 antagonists
(4S)-4-[[4-[(2R)-1-[(2S)-2-(cyclopropylmethylcarbamoyl)pyrrolidin-1-yl]-1-oxopropan-2-yl]oxy-7-methylquinoline-2-carbonyl]amino]-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxopentanoic acid	IC50	5 nM	US-8669266: Quinoline-carboxamide derivatives as P2Y12 antagonists
propyl 4-[(2S)-2-[[4-[2-[(2S)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-7-methylquinoline-2-carbonyl]amino]-5-methoxy-5-oxopentanoyl]piperazine-1-carboxylate	IC50	5 nM	US-8669266: Quinoline-carboxamide derivatives as P2Y12 antagonists
butyl 4-[2-[[4-[2-[(2S)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]quinoline-2-carbonyl]amino]acetyl]piperazine-1-carboxylate	IC50	5 nM	US-8669266: Quinoline-carboxamide derivatives as P2Y12 antagonists
butyl 4-[(2S)-2-[[4-[2-[(2S)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-7-methylquinoline-2-carbonyl]amino]-4-(2H-tetrazol-5-yl)butanoyl]piperazine-1-carboxylate	IC50	8 nM	US-8669266: Quinoline-carboxamide derivatives as P2Y12 antagonists
(3S)-3-[[4-[2-[(2S)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-6-fluoro-7-methylquinoline-2-carbonyl]amino]-4-(4-ethoxycarbonylpiperazin-1-yl)-4-oxobutanoic acid	IC50	9 nM	US-8669266: Quinoline-carboxamide derivatives as P2Y12 antagonists
(4S)-5-(4-ethoxycarbonylpiperazin-1-yl)-4-[[7-methyl-4-[(2R)-1-oxo-1-[(2S)-2-(piperidine-1-carbonyl)pyrrolidin-1-yl]propan-2-yl]oxyquinoline-2-carbonyl]amino]-5-oxopentanoic acid	IC50	12 nM	US-8669266: Quinoline-carboxamide derivatives as P2Y12 antagonists
(4S)-5-(4-ethoxycarbonylpiperazin-1-yl)-4-[[7-methyl-4-[2-oxo-2-[(2S)-2-(pyrrolidine-1-carbonyl)pyrrolidin-1-yl]ethoxy]quinoline-2-carbonyl]amino]-5-oxopentanoic acid	IC50	17 nM	US-8669266: Quinoline-carboxamide derivatives as P2Y12 antagonists
ethyl 4-[(2S)-2-[[4-[2-[(2S)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-7-methylquinoline-2-carbonyl]amino]-5-(2-methylpropoxy)-5-oxopentanoyl]piperazine-1-carboxylate	IC50	28 nM	US-8669266: Quinoline-carboxamide derivatives as P2Y12 antagonists
(4S)-4-[[4-[2-[(2S)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-6,7-difluoroquinoline-2-carbonyl]amino]-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxopentanoic acid	IC50	65 nM	US-8669266: Quinoline-carboxamide derivatives as P2Y12 antagonists
(4S)-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxo-4-[[4-[2-oxo-2-[(2S)-2-(2,2,2-trifluoroethylcarbamoyl)pyrrolidin-1-yl]ethoxy]quinoline-2-carbonyl]amino]pentanoic acid	IC50	67 nM	US-8669266: Quinoline-carboxamide derivatives as P2Y12 antagonists
ethyl 4-[(2S)-2-[[4-[2-[(2S)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-7-methylquinoline-2-carbonyl]amino]-5-(cyclopentylmethoxy)-5-oxopentanoyl]piperazine-1-carboxylate	IC50	71 nM	US-8669266: Quinoline-carboxamide derivatives as P2Y12 antagonists
ethyl 4-[(2S)-5-amino-2-[[4-[2-[(2S)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-7-methylquinoline-2-carbonyl]amino]-5-oxopentanoyl]piperazine-1-carboxylate	IC50	83 nM	US-8669266: Quinoline-carboxamide derivatives as P2Y12 antagonists
(4S)-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxo-4-[[4-[2-oxo-2-(2-phenylpyrrolidin-1-yl)ethoxy]quinoline-2-carbonyl]amino]pentanoic acid	IC50	102 nM	US-8669266: Quinoline-carboxamide derivatives as P2Y12 antagonists
(4S)-5-(4-ethoxycarbonylpiperazin-1-yl)-4-[[4-[2-[(2S)-2-ethoxycarbonylpyrrolidin-1-yl]-2-oxoethoxy]-7-methylquinoline-2-carbonyl]amino]-5-oxopentanoic acid	IC50	132 nM	US-8669266: Quinoline-carboxamide derivatives as P2Y12 antagonists

ChEMBL bioactivities

1610 potent at pChembl≥5 of 1726 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
9.80	Kd	0.1585	nM	CHEMBL455536
9.60	Ki	0.2512	nM	CHEMBL251041
9.52	Ki	0.3	nM	CHEMBL5181634
9.50	IC50	0.3162	nM	CHEMBL251024
9.48	IC50	0.33	nM	CHEMBL5176593
9.42	Ki	0.38	nM	CHEMBL570295
9.40	IC50	0.3981	nM	CANGRELOR
9.40	IC50	0.4	nM	CANGRELOR
9.40	Ki	0.4	nM	CHEMBL567915
9.35	IC50	0.45	nM	CANGRELOR
9.34	Ki	0.46	nM	CHEMBL567561
9.30	IC50	0.5012	nM	CHEMBL437204
9.24	Ki	0.58	nM	CHEMBL601696
9.22	Ki	0.6	nM	CHEMBL567740
9.21	Ki	0.61	nM	CHEMBL565974
9.20	Ki	0.631	nM	CHEMBL249790
9.19	Ki	0.64	nM	CHEMBL601489
9.17	Ki	0.67	nM	CHEMBL565836
9.17	Ki	0.68	nM	CHEMBL570295
9.16	Ki	0.69	nM	CHEMBL568059
9.15	EC50	0.7	nM	CHEMBL90804
9.15	Ki	0.7	nM	CHEMBL567133
9.15	Ki	0.71	nM	CHEMBL567709
9.15	IC50	0.7	nM	CANGRELOR TETRASODIUM
9.10	Ki	0.8	nM	CHEMBL2172149
9.10	IC50	0.7943	nM	CHEMBL1160364
9.10	Ki	0.79	nM	CHEMBL568211
9.10	Ki	0.79	nM	CHEMBL601695
9.08	Ki	0.83	nM	CHEMBL566913
9.05	IC50	0.9	nM	CHEMBL3326907
9.05	Ki	0.9	nM	CHEMBL565409
9.04	Ki	0.92	nM	CHEMBL571599
9.01	Ki	0.98	nM	CHEMBL601698
9.00	EC50	1	nM	CHEMBL431799
9.00	EC50	1	nM	CHEMBL90237
9.00	IC50	1	nM	CHEMBL3288123
9.00	IC50	1	nM	CHEMBL5179719
9.00	IC50	1	nM	CHEMBL5184268
9.00	IC50	1	nM	CHEMBL5195237
9.00	IC50	1	nM	CHEMBL5173489
9.00	IC50	1	nM	CHEMBL5192953
9.00	IC50	1	nM	CHEMBL5203416
9.00	Ki	0.99	nM	CHEMBL570275
9.00	Ki	1	nM	CHEMBL569914
9.00	Ki	1	nM	CHEMBL569097
8.96	Ki	1.1	nM	CHEMBL601903
8.96	Ki	1.1	nM	CHEMBL601692
8.92	Ki	1.2	nM	CHEMBL567416
8.92	Ki	1.2	nM	CHEMBL570128
8.92	Ki	1.2	nM	CHEMBL566745

PubChem BioAssay actives

1590 with measured affinity, of 2389 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
disodium;1-amino-4-(4-anilino-3-sulfonatoanilino)-9,10-dioxoanthracene-2-sulfonate	1443659: Competitive antagonist activity at human P2Y12 receptor expressed in CHO cells assessed as forskolin/ 2-methylthio-ADP-induced cAMP production preincubated for 10 mins followed 2-methylthio-ADP addition measured after 3.5 hrs by luciferase reporter gene assay	kd	0.0002	uM
(1S,2R,3S,4R)-2,3-dihydroxy-4-[7-[[(1R,2S)-2-phenylcyclopropyl]amino]-5-propylsulfanyltriazolo[4,5-d]pyrimidin-3-yl]cyclopentane-1-carboxylic acid	309606: Displacement of [125I] labeled ligand from human P2Y12 receptor in human platelets	ki	0.0003	uM
ethyl 5-cyano-2-methyl-6-[4-(3-phenyl-1H-1,2,4-triazol-5-yl)piperidin-1-yl]pyridine-3-carboxylate	1871493: Inhibition of 2-MeS-ADP induced P2Y12 (unknown origin) signalling expressed in CHO cells membrane incubated for 45 mins by 35S-GTPgammaS assay	ic50	0.0003	uM
(2S)-2-[[(E)-3-[(2R,3S,4R,5R)-5-[7-(butylamino)-5-propylsulfanyltriazolo[4,5-d]pyrimidin-3-yl]-3,4-dihydroxyoxolan-2-yl]prop-2-enoyl]amino]butanedioic acid	1953760: Antagonist activity at human P2Y12 by aggregation assay	ic50	0.0003	uM
2-(2-fluoroethoxy)-6-propyl-4-[3-(trifluoromethyl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]thieno[2,3-d]pyrimidine	1850678: Displacement of [3H]-2MesADP from human P2Y12 in HEK cell membrane assessed as inhibition constant incubated for 1 hr by scintillation counter method	ki	0.0003	uM
(4S)-5-oxo-5-(4-pentoxycarbonylpiperazin-1-yl)-4-[[2-phenyl-6-[4-(pyrrolidin-1-ylmethyl)piperidin-1-yl]pyrimidine-4-carbonyl]amino]pentanoic acid	443858: Binding affinity at human recombinant P2Y12 receptor expressed in CHO cells by radioligand binding assay	ki	0.0004	uM
(4S)-5-(4-butoxycarbonylpiperazin-1-yl)-4-[[4-[4-(ethylcarbamoyl)piperidin-1-yl]-6-phenylpyridine-2-carbonyl]amino]-5-oxopentanoic acid	443858: Binding affinity at human recombinant P2Y12 receptor expressed in CHO cells by radioligand binding assay	ki	0.0004	uM
Cangrelor	1298771: Antagonist activity at P2Y12 receptor in human platelets assessed as inhibition of ADP-induced platelet aggregation by turbidimetric method	ic50	0.0004	uM
(2S)-2-[[(E)-3-[(1R,2R,3S,4R)-4-[7-(butylamino)-5-propylsulfanyltriazolo[4,5-d]pyrimidin-3-yl]-2,3-dihydroxycyclopentyl]prop-2-enoyl]amino]butanedioic acid	1953760: Antagonist activity at human P2Y12 by aggregation assay	ic50	0.0005	uM
(4S)-5-oxo-5-(4-pentoxycarbonylpiperazin-1-yl)-4-[[2-phenyl-6-[4-(pyrrolidine-1-carbonyl)piperidin-1-yl]pyrimidine-4-carbonyl]amino]pentanoic acid	443858: Binding affinity at human recombinant P2Y12 receptor expressed in CHO cells by radioligand binding assay	ki	0.0005	uM
(1S,2S,3R,5S)-3-[7-[[(1R,2S)-2-(3,4-difluorophenyl)cyclopropyl]amino]-5-(3,3,3-trifluoropropylsulfanyl)triazolo[4,5-d]pyrimidin-3-yl]-5-(2-hydroxyethoxy)cyclopentane-1,2-diol	309606: Displacement of [125I] labeled ligand from human P2Y12 receptor in human platelets	ki	0.0006	uM
(4S)-4-[[6-[4-(diethylaminomethyl)piperidin-1-yl]-2-phenylpyrimidine-4-carbonyl]amino]-5-oxo-5-(4-pentoxycarbonylpiperazin-1-yl)pentanoic acid	443858: Binding affinity at human recombinant P2Y12 receptor expressed in CHO cells by radioligand binding assay	ki	0.0006	uM
(4S)-4-[[6-[4-(ethylcarbamoyl)piperidin-1-yl]-2-phenylpyrimidine-4-carbonyl]amino]-5-oxo-5-(4-pentoxycarbonylpiperazin-1-yl)pentanoic acid	443858: Binding affinity at human recombinant P2Y12 receptor expressed in CHO cells by radioligand binding assay	ki	0.0006	uM
(4S)-4-[[4-[4-(ethylcarbamoyl)piperidin-1-yl]-6-phenylpyridine-2-carbonyl]amino]-5-oxo-5-(4-pentoxycarbonylpiperazin-1-yl)pentanoic acid	457976: Inhibition of human P2Y12 receptor expressed in CHO cells	ki	0.0006	uM
(4S)-4-[[4-(3-carbamoylazetidin-1-yl)-6-phenylpyridine-2-carbonyl]amino]-5-oxo-5-(4-pentoxycarbonylpiperazin-1-yl)pentanoic acid	457976: Inhibition of human P2Y12 receptor expressed in CHO cells	ki	0.0006	uM
tetrasodium;[dichloro(phosphonato)methyl]-[[(2R,3S,4R,5R)-3,4-dihydroxy-5-[6-(2-methylsulfanylethylamino)-2-(3,3,3-trifluoropropylsulfanyl)purin-9-yl]oxolan-2-yl]methoxy-oxidophosphoryl]oxyphosphinate	480267: Antagonist activity at P2Y12 receptor by [35S]GTPgammaS binding assay	ic50	0.0007	uM
methyl 2-[cyclohexyl-[4-[(2-oxo-1,3-dihydroimidazo[4,5-b]quinolin-7-yl)oxy]butanoyl]amino]acetate	92528: Inhibition of platelet aggregation using adenosine diphosphate (ADP) as activating agent in human platelet rich plasma (PRP)	ec50	0.0007	uM
(4S)-4-[[6-(4-aminopiperidin-1-yl)-2-phenylpyrimidine-4-carbonyl]amino]-5-oxo-5-(4-pentoxycarbonylpiperazin-1-yl)pentanoic acid	443858: Binding affinity at human recombinant P2Y12 receptor expressed in CHO cells by radioligand binding assay	ki	0.0007	uM
(4S)-4-[[6-[4-(2-hydroxyethoxy)piperidin-1-yl]-2-phenylpyrimidine-4-carbonyl]amino]-5-oxo-5-(4-pentoxycarbonylpiperazin-1-yl)pentanoic acid	443858: Binding affinity at human recombinant P2Y12 receptor expressed in CHO cells by radioligand binding assay	ki	0.0007	uM
(4S)-5-(4-butoxycarbonylpiperazin-1-yl)-5-oxo-4-[[2-phenyl-6-[4-(pyrrolidine-1-carbonyl)piperidin-1-yl]pyrimidine-4-carbonyl]amino]pentanoic acid	443858: Binding affinity at human recombinant P2Y12 receptor expressed in CHO cells by radioligand binding assay	ki	0.0007	uM
(4S)-4-[[6-[4-[2-(ethylamino)-2-oxoethyl]piperidin-1-yl]-2-phenylpyrimidine-4-carbonyl]amino]-5-oxo-5-(4-pentoxycarbonylpiperazin-1-yl)pentanoic acid	443858: Binding affinity at human recombinant P2Y12 receptor expressed in CHO cells by radioligand binding assay	ki	0.0007	uM
[dichloro-[[[(2R,3S,4R,5R)-3,4-dihydroxy-5-[6-(2,2,2-trifluoroethylamino)-2-(3,3,3-trifluoropropylsulfanyl)purin-9-yl]oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-hydroxyphosphoryl]methyl]phosphonic acid	1298771: Antagonist activity at P2Y12 receptor in human platelets assessed as inhibition of ADP-induced platelet aggregation by turbidimetric method	ic50	0.0008	uM
(4S)-5-(4-butoxycarbonylpiperazin-1-yl)-4-[[5-[2-[(2S)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-oxopentanoic acid	703441: Displacement of [33P]2-MeS-ADP from human recombinant P2Y12 receptor expressed in CHO cell membranes by scintillation counting method	ki	0.0008	uM
(4S)-5-(4-butoxycarbonylpiperazin-1-yl)-4-[[6-[4-(diethylcarbamoyl)piperidin-1-yl]-2-phenylpyrimidine-4-carbonyl]amino]-5-oxopentanoic acid	443858: Binding affinity at human recombinant P2Y12 receptor expressed in CHO cells by radioligand binding assay	ki	0.0008	uM
(4S)-4-[[6-[4-(azetidine-1-carbonyl)piperidin-1-yl]-2-phenylpyrimidine-4-carbonyl]amino]-5-oxo-5-(4-pentoxycarbonylpiperazin-1-yl)pentanoic acid	443858: Binding affinity at human recombinant P2Y12 receptor expressed in CHO cells by radioligand binding assay	ki	0.0008	uM
(4S)-5-(4-butoxycarbonylpiperazin-1-yl)-5-oxo-4-[[4-[4-[(2-oxopyrrolidin-1-yl)methyl]piperidin-1-yl]-6-phenylpyridine-2-carbonyl]amino]pentanoic acid	457976: Inhibition of human P2Y12 receptor expressed in CHO cells	ki	0.0008	uM
(4S)-4-[[6-[4-[2-(methylamino)-2-oxoethyl]piperidin-1-yl]-2-phenylpyrimidine-4-carbonyl]amino]-5-oxo-5-(4-pentoxycarbonylpiperazin-1-yl)pentanoic acid	443858: Binding affinity at human recombinant P2Y12 receptor expressed in CHO cells by radioligand binding assay	ki	0.0009	uM
(4S)-4-[[6-[4-[2-(azetidin-1-yl)-2-oxoethyl]piperidin-1-yl]-2-phenylpyrimidine-4-carbonyl]amino]-5-oxo-5-(4-pentoxycarbonylpiperazin-1-yl)pentanoic acid	443858: Binding affinity at human recombinant P2Y12 receptor expressed in CHO cells by radioligand binding assay	ki	0.0009	uM
2-[3-[[4-(4-butanoyl-5-methylpyrazol-1-yl)phenyl]carbamoyl]-5-methylindol-1-yl]acetic acid	1186074: Displacement of [33P]2MeS-ADP from P2Y12 receptor (unknown origin) transfected in CHO cells after 30 mins by scintillation counting analysis	ic50	0.0009	uM
N-cyclohexyl-N-methyl-5-[(2-oxo-1,3-dihydroimidazo[4,5-b]quinolin-7-yl)oxy]pentanamide	92528: Inhibition of platelet aggregation using adenosine diphosphate (ADP) as activating agent in human platelet rich plasma (PRP)	ec50	0.0010	uM
N-cycloheptyl-N-methyl-5-[(2-oxo-1,3-dihydroimidazo[4,5-b]quinolin-7-yl)oxy]pentanamide	92528: Inhibition of platelet aggregation using adenosine diphosphate (ADP) as activating agent in human platelet rich plasma (PRP)	ec50	0.0010	uM
1-(5-butanoyl-3-cyano-6-methylsulfanyl-2-pyridinyl)-N-(1-phenylcyclopropyl)sulfonylpiperidine-4-carboxamide	1153640: Antagonist activity P2Y12 receptor in human washed platelets assessed as inhibition of ADP-induced platelet aggregation after 5 to 90 mins by spectrophotometric analysis	ic50	0.0010	uM
(4S)-4-[[4-[3-(dimethylamino)propyl]-6-phenylpyridine-2-carbonyl]amino]-5-oxo-5-(4-pentoxycarbonylpiperazin-1-yl)pentanoic acid	461227: Displacement of [33P]ADP from human recombinant P2Y12 receptor expressed in CHO cells	ki	0.0010	uM
(4S)-4-[(6-morpholin-4-yl-2-phenylpyrimidine-4-carbonyl)amino]-5-oxo-5-(4-pentoxycarbonylpiperazin-1-yl)pentanoic acid	443858: Binding affinity at human recombinant P2Y12 receptor expressed in CHO cells by radioligand binding assay	ki	0.0010	uM
(4S)-5-oxo-4-[[6-[4-[(2-oxopyrrolidin-1-yl)methyl]piperidin-1-yl]-2-phenylpyrimidine-4-carbonyl]amino]-5-(4-pentoxycarbonylpiperazin-1-yl)pentanoic acid	443858: Binding affinity at human recombinant P2Y12 receptor expressed in CHO cells by radioligand binding assay	ki	0.0010	uM
(4S)-4-[[4-[4-(dimethylcarbamoyl)piperidin-1-yl]-6-phenylpyridine-2-carbonyl]amino]-5-oxo-5-(4-pentoxycarbonylpiperazin-1-yl)pentanoic acid	457976: Inhibition of human P2Y12 receptor expressed in CHO cells	ki	0.0010	uM
[4-[(2S)-3-(4-butoxycarbonylpiperazin-1-yl)-3-oxo-2-[(2-phenyl-1,3-thiazole-4-carbonyl)amino]propyl]phenyl]phosphonic acid	1871489: Displacement of tritium-labeled 2MeSADP from human P2Y12 expressed in CHO cells measured after 2 hrs by scintillation counting method	ic50	0.0010	uM
[(2R)-3-(4-butoxycarbonylpiperazin-1-yl)-2-[[5-(4-methylpiperazin-1-yl)-2-phenyl-1,3-thiazole-4-carbonyl]amino]-3-oxopropyl]phosphonic acid	1871489: Displacement of tritium-labeled 2MeSADP from human P2Y12 expressed in CHO cells measured after 2 hrs by scintillation counting method	ic50	0.0010	uM
[(2R)-3-(4-butoxycarbonylpiperazin-1-yl)-2-[[5-[butyl(methyl)amino]-2-phenyl-1,3-thiazole-4-carbonyl]amino]-3-oxopropyl]phosphonic acid	1871489: Displacement of tritium-labeled 2MeSADP from human P2Y12 expressed in CHO cells measured after 2 hrs by scintillation counting method	ic50	0.0010	uM
[(2R)-3-(4-butoxycarbonylpiperazin-1-yl)-3-oxo-2-[(2-phenyl-1,3-thiazole-4-carbonyl)amino]propyl]phosphonic acid	1871489: Displacement of tritium-labeled 2MeSADP from human P2Y12 expressed in CHO cells measured after 2 hrs by scintillation counting method	ic50	0.0010	uM
[4-[(2S)-3-(4-ethoxycarbonylpiperazin-1-yl)-3-oxo-2-[(2-phenyl-1,3-thiazole-4-carbonyl)amino]propyl]phenyl]phosphonic acid	1871489: Displacement of tritium-labeled 2MeSADP from human P2Y12 expressed in CHO cells measured after 2 hrs by scintillation counting method	ic50	0.0010	uM
(4S)-5-(4-butoxycarbonylpiperazin-1-yl)-4-[[5-[(3S)-3-methoxypyrrolidin-1-yl]-2-phenyl-1,3-thiazole-4-carbonyl]amino]-5-oxopentanoic acid	1871489: Displacement of tritium-labeled 2MeSADP from human P2Y12 expressed in CHO cells measured after 2 hrs by scintillation counting method	ic50	0.0010	uM
(4S)-5-oxo-5-(4-pentoxycarbonylpiperazin-1-yl)-4-[[6-phenyl-4-[4-(pyrrolidin-1-ylmethyl)piperidin-1-yl]pyridine-2-carbonyl]amino]pentanoic acid	457976: Inhibition of human P2Y12 receptor expressed in CHO cells	ki	0.0011	uM
(4S)-5-(4-butoxycarbonylpiperazin-1-yl)-4-[[4-[4-(diethylcarbamoyl)piperidin-1-yl]-6-phenylpyridine-2-carbonyl]amino]-5-oxopentanoic acid	457976: Inhibition of human P2Y12 receptor expressed in CHO cells	ki	0.0011	uM
(4S)-4-[[6-(2-methoxyethoxy)-2-phenylpyrimidine-4-carbonyl]amino]-5-oxo-5-(4-pentoxycarbonylpiperazin-1-yl)pentanoic acid	443858: Binding affinity at human recombinant P2Y12 receptor expressed in CHO cells by radioligand binding assay	ki	0.0012	uM
(4S)-4-[[4-(2-methoxyethoxy)-6-phenylpyrimidine-2-carbonyl]amino]-5-oxo-5-(4-pentoxycarbonylpiperazin-1-yl)pentanoic acid	443858: Binding affinity at human recombinant P2Y12 receptor expressed in CHO cells by radioligand binding assay	ki	0.0012	uM
(4S)-4-[[6-(2-methoxyethylamino)-2-phenylpyrimidine-4-carbonyl]amino]-5-oxo-5-(4-pentoxycarbonylpiperazin-1-yl)pentanoic acid	443858: Binding affinity at human recombinant P2Y12 receptor expressed in CHO cells by radioligand binding assay	ki	0.0012	uM
(4S)-4-[[6-(3-ethoxyazetidin-1-yl)-2-phenylpyrimidine-4-carbonyl]amino]-5-oxo-5-(4-pentoxycarbonylpiperazin-1-yl)pentanoic acid	443858: Binding affinity at human recombinant P2Y12 receptor expressed in CHO cells by radioligand binding assay	ki	0.0012	uM
(4S)-4-[[6-(4-carbamoylpiperazin-1-yl)-2-phenylpyrimidine-4-carbonyl]amino]-5-oxo-5-(4-pentoxycarbonylpiperazin-1-yl)pentanoic acid	443858: Binding affinity at human recombinant P2Y12 receptor expressed in CHO cells by radioligand binding assay	ki	0.0012	uM
(4S)-4-[[6-[4-(methylaminomethyl)piperidin-1-yl]-2-phenylpyrimidine-4-carbonyl]amino]-5-oxo-5-(4-pentoxycarbonylpiperazin-1-yl)pentanoic acid	443858: Binding affinity at human recombinant P2Y12 receptor expressed in CHO cells by radioligand binding assay	ki	0.0012	uM

CTD chemical–gene interactions

15 total (human), top 15 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
Clopidogrel	affects binding, decreases activity, affects response to substance, affects reaction	6
cangrelor	decreases phosphorylation, affects response to substance, affects binding, decreases abundance, decreases activity	3
Adenosine Diphosphate	affects reaction, increases expression, affects response to substance	3
triphenyl phosphate	affects expression	1
S-(1,2-dichlorovinyl)cysteine	affects response to substance, increases expression, affects cotreatment, decreases expression	1
phosphatidylinositol 3,4,5-triphosphate	affects binding, decreases abundance, decreases activity	1
CGP 52608	affects binding, increases reaction	1
CT 50547	decreases activity, affects binding	1
Ticagrelor	affects binding, decreases activity	1
Anthraquinones	decreases activity	1
Benzo(a)pyrene	increases methylation	1
Diethylhexyl Phthalate	decreases expression	1
Lipopolysaccharides	affects response to substance, increases expression, affects cotreatment, decreases expression	1
Aflatoxin B1	increases methylation	1
Antirheumatic Agents	decreases expression	1

ChEMBL screening assays

160 unique, capped per target: 102 binding, 58 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1042521	Binding	Binding affinity at human recombinant P2Y12 receptor expressed in CHO cells by radioligand binding assay	Piperazinyl-glutamate-pyrimidines as potent P2Y12 antagonists for inhibition of platelet aggregation. — Bioorg Med Chem Lett
CHEMBL1042522	Functional	Antagonist activity at P2Y12 receptor in human platelet rich plasma assessed as inhibition of ADP-induced platelet aggregation by light transmission aggregometry	Piperazinyl-glutamate-pyrimidines as potent P2Y12 antagonists for inhibition of platelet aggregation. — Bioorg Med Chem Lett

Cellosaurus cell lines

6 cell lines: 5 cancer cell line, 1 spontaneously immortalized cell line

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

Cellosaurus	Name	Category	Sex
CVCL_D1Y1	Abcam A-549 P2RY12 KO	Cancer cell line	Male
CVCL_D2NT	Abcam THP-1 P2RY12 KO	Cancer cell line	Male
CVCL_H357	1321N1/P2Y12/Galpha15	Cancer cell line	Male
CVCL_KY75	PathHunter CHO-K1 P2RY12 beta-arrestin	Spontaneously immortalized cell line	Female
CVCL_LB07	PathHunter U2OS P2RY12 Total GPCR Internalization	Cancer cell line	Female
CVCL_ZD95	1321N1-HA-P2Y12	Cancer cell line	Male

Clinical trials (associated diseases)

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

Trial	Phase	Status	Title
NCT05657860	PHASE4	COMPLETED	Guanfacine Extended Release for the Reduction of Aggression and Self-injurious Behavior Associated With Prader-Willi Syndrome
NCT05744479	PHASE4	RECRUITING	Metformin for Antipsychotic-induced Weight Gain in Adults With Intellectual Disability
NCT06107829	PHASE4	WITHDRAWN	Valbenazine Treatment of Tardive Dyskinesia in Adults With Intellectual/Developmental Disabilities
NCT06997198	PHASE4	NOT_YET_RECRUITING	Deutetrabenazine Treatment for Tardive Dyskinesia in Intellectual/Developmental Disabilities
NCT00039858	PHASE4	COMPLETED	Evaluation of Argatroban Injection in Pediatric Patients Requiring Anticoagulant Alternatives to Heparin
NCT00239733	PHASE4	TERMINATED	Anti-D for Treating Thrombocytopenia in Adults Infected With Hepatitis C Virus With or Without HIV Co-Infection
NCT00907478	PHASE4	COMPLETED	Study on Bone Marrow Morphology in Adults Receiving Romiplostim for Treatment of Thrombocytopenia Associated With Immune Thrombocytopenia Purpura (ITP)
NCT01727401	PHASE4	TERMINATED	Thromboprophylaxis of Venous Thromboembolism in Acutely-ill Medical Inpatients With Thrombocytopenia
NCT02032134	PHASE4	TERMINATED	Protocol for the Infusion of Buffy Coat-derived Cryopreserved Platelets in Patients With Severe Thrombocytopenia
NCT02267993	PHASE4	COMPLETED	Efficacy and Safety of rhTPO for the Treatment of Thrombocytopenia After Chemotherapy in AML Patients
NCT03633019	PHASE4	UNKNOWN	High-dose Use of rhTPO in CIT Patients
NCT03688191	PHASE4	UNKNOWN	Study of Sirolimus in CTD-TP in China
NCT04906083	PHASE4	UNKNOWN	Avatrombopag in Patients With End-stage Liver Disease and Thrombocytopenia
NCT05217719	PHASE4	UNKNOWN	Effects of Recombinant Human Thrombopoietin on Platelet Levels in ICU Patients
NCT05255003	PHASE4	RECRUITING	STrategies for Anticoagulation in Patients With thRombocytopenia and Cancer-associated Thrombosis
NCT05382013	PHASE4	UNKNOWN	Efficacy and Safety of Avatrombopag for Treating TCP in HBV-ACLF Patients Receiving ALSS Treatment
NCT05944458	PHASE4	COMPLETED	Efficacy of Intravenous N-Acetylcysteine in Preventing Linezolid-Induced Thrombocytopenia in Critically Ill Patients
NCT06562738	PHASE4	RECRUITING	Clinical Study on Efficacy and Safety of Hetrombopag in the Preoperative Patients of Thrombocytopenia
NCT02270736	PHASE3	COMPLETED	Clinical Study to Investigate the Efficacy and Safety of NT 201 Compared to Placebo in the Treatment of Chronic Troublesome Drooling Associated With Neurological Disorders and/or Intellectual Disability
NCT00037791	PHASE3	COMPLETED	Safety and Efficacy of (PN-152,243)/PN-196,444 in the Prevention of Thrombocytopenia
NCT00039910	PHASE3	COMPLETED	Safety and Efficacy of (PN-152,243)/PN-196,444 in the Prevention of Thrombocytopenia
NCT00073580	PHASE3	COMPLETED	Angiomax in Patients With HIT/HITTS Type II Undergoing Off-Pump Coronary Artery Bypass Grafting (CABG) (CHOOSE)
NCT00102323	PHASE3	COMPLETED	AMG 531 Treatment of Thrombocytopenic Subjects With Immune (Idiopathic) Thrombocytopenic Purpura (ITP) Refractory to Splenectomy
NCT00102336	PHASE3	COMPLETED	AMG 531 Treatment of Thrombocytopenic Subjects With Immune (Idiopathic) Thrombocytopenic Purpura (ITP) Prior to Splenectomy
NCT00116688	PHASE3	COMPLETED	Open Label Extension Study of Romiplostim (AMG 531) in Thrombocytopenic Patients With Immune (Idiopathic) Thrombocytopenic Purpura (ITP)
NCT00128713	PHASE3	COMPLETED	Optimal Platelet Dose Strategy for Management of Thrombocytopenia
NCT00151866	PHASE3	COMPLETED	Efficacy of Transfusions With Platelets Stored in Platelet Additive Solution II Versus Plasma
NCT00261924	PHASE3	COMPLETED	Efficacy and Safety Study of Platelets Treated for Pathogen Inactivation and Stored for Up to Seven Days
NCT00415532	PHASE3	COMPLETED	Romiplostim (AMG 531) Versus Medical Standard of Care for Immune (Idiopathic) Thrombocytopenic Purpura
NCT00420914	PHASE3	TERMINATED	Strategies for Transfusion of Platelets (SToP)
NCT00501345	PHASE3	TERMINATED	Aspirin in Patients With Myocardial Infarction and Thrombocytopenia
NCT00508820	PHASE3	COMPLETED	An Open Label Study of Romiplostim in Adult Thrombocytopenic Subjects With ITP
NCT00678587	PHASE3	TERMINATED	Eltrombopag To Reduce The Need For Platelet Transfusion In Subjects With Chronic Liver Disease And Thrombocytopenia Undergoing Elective Invasive Procedures
NCT01438840	PHASE3	COMPLETED	Efficacy and Safety of Oral E5501 Plus Standard of Care for the Treatment of Thrombocytopenia in Adults With Chronic Immune Thrombocytopenia (Amendment 02)
NCT01444417	PHASE3	COMPLETED	Safety and Efficacy Study of Romiplostim to Treat Immune Thrombocytopenia (ITP) in Pediatric Patients
NCT01805648	PHASE3	UNKNOWN	Efficacy and Safety Study of Maintenance Treatment With rhTPO in Thrombocytopenic Subjects With ITP
NCT02244658	PHASE3	UNKNOWN	Recombinant Human Thrombopoietin (rhTPO) in Management of Chemotherapy-induced Thrombocytopenia in Acute Myelocytic Leukemia
NCT02389621	PHASE3	COMPLETED	Safety and Efficacy Study of Lusutrombopag for Thrombocytopenia in Patients With Chronic Liver Disease Undergoing Elective Invasive Procedures
NCT02444728	PHASE3	TERMINATED	Cyclophosphamide and Hydroxychloroquine for Thrombocytopenia in SLE
NCT02487563	PHASE3	COMPLETED	Prospective Study of Patients With Thrombocytopenia Following HSCT