P2RY13
geneOn this page
Also known as FKSG77P2Y13
Summary
P2RY13 (purinergic receptor P2Y13, HGNC:4537) is a protein-coding gene on chromosome 3q25.1, encoding P2Y purinoceptor 13 (Q9BPV8). Receptor for ADP.
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 activated by ADP.
Source: NCBI Gene 53829 — RefSeq curated summary.
At a glance
- Clinical variants (ClinVar): 1 total
- Druggable target: yes — 3 molecules with ChEMBL bioactivity
- MANE Select transcript:
NM_176894
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:4537 |
| Approved symbol | P2RY13 |
| Name | purinergic receptor P2Y13 |
| Location | 3q25.1 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | FKSG77, P2Y13 |
| Ensembl gene | ENSG00000181631 |
| Ensembl biotype | protein_coding |
| OMIM | 606380 |
| Entrez | 53829 |
Gene structure
Transcript identifiers
Ensembl transcripts: 1 — 1 protein_coding
ENST00000325602
RefSeq mRNA: 1 — MANE Select: NM_176894
NM_176894
CCDS: CCDS3158
Canonical transcript exons
ENST00000325602 — 2 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001619892 | 151326312 | 151329007 |
| ENSE00001876920 | 151329481 | 151329549 |
Expression profiles
Bgee: expression breadth ubiquitous, 192 present calls, max score 96.63.
FANTOM5 (CAGE): breadth broad, TPM avg 8.9817 / max 1081.8020, expressed in 356 samples.
FANTOM5 promoters (1 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 45149 | 8.9817 | 356 |
Top tissues by expression
272 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| monocyte | CL:0000576 | 96.63 | gold quality |
| mononuclear cell | CL:0000842 | 96.31 | gold quality |
| leukocyte | CL:0000738 | 96.28 | gold quality |
| blood | UBERON:0000178 | 94.59 | gold quality |
| granulocyte | CL:0000094 | 92.52 | gold quality |
| spleen | UBERON:0002106 | 90.03 | gold quality |
| bone marrow | UBERON:0002371 | 88.92 | gold quality |
| trabecular bone tissue | UBERON:0002483 | 87.64 | gold quality |
| bone marrow cell | CL:0002092 | 86.33 | gold quality |
| vermiform appendix | UBERON:0001154 | 84.83 | gold quality |
| lymph node | UBERON:0000029 | 81.36 | gold quality |
| male germ line stem cell (sensu Vertebrata) in testis | CL:0000089 ∩ UBERON:0000473 | 80.55 | silver quality |
| inferior vagus X ganglion | UBERON:0005363 | 78.59 | gold quality |
| palpebral conjunctiva | UBERON:0001812 | 77.53 | gold quality |
| caecum | UBERON:0001153 | 77.12 | gold quality |
| rectum | UBERON:0001052 | 76.61 | gold quality |
| periodontal ligament | UBERON:0008266 | 74.37 | gold quality |
| smooth muscle tissue | UBERON:0001135 | 73.24 | gold quality |
| right lung | UBERON:0002167 | 72.68 | gold quality |
| gall bladder | UBERON:0002110 | 72.28 | gold quality |
| corpus callosum | UBERON:0002336 | 70.95 | gold quality |
| spinal cord | UBERON:0002240 | 70.41 | gold quality |
| C1 segment of cervical spinal cord | UBERON:0006469 | 70.28 | gold quality |
| superior vestibular nucleus | UBERON:0007227 | 69.76 | gold quality |
| prefrontal cortex | UBERON:0000451 | 69.12 | gold quality |
| subthalamic nucleus | UBERON:0001906 | 67.66 | silver quality |
| ventral tegmental area | UBERON:0002691 | 67.54 | gold quality |
| midbrain | UBERON:0001891 | 67.53 | gold quality |
| substantia nigra | UBERON:0002038 | 67.51 | gold quality |
| upper lobe of left lung | UBERON:0008952 | 66.79 | gold quality |
Single-cell (SCXA)
Detected in 1 experiment(s), a significant marker in 1.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | yes | 4.92 |
Regulation
Is transcription factor: no
Literature-anchored findings (GeneRIF, showing 11)
- (p2y13 purinoceptor) (PMID:11961076)
- results demonstrate a crosstalk between two metabotropic and one ionotropic purinergic receptor that regulates cAMP levels through adenylate cyclase 5 and modulates axonal elongation triggered by neurotropic factors and the PI3K-Akt-GSK3 pathway (PMID:22250198)
- The pattern of responsiveness to more selective P2-antagonists implies that both P2Y13 and P2X7 receptors are involved in Epsilon-toxin-of Clostridium perfringens induced hemolysis in human species. (PMID:30277122)
- Common p2y13 polymorphisms are associated with plasma inhibitory factor 1 and lipoprotein(a) concentrations, heart rate and body fat mass and may modulate cardiovascular risk. (PMID:30600215)
- P2Y13 and P2X7 receptors modulate mechanically induced adenosine triphosphate release from mast cells. (PMID:32155290)
- Nucleotides-Induced Changes in the Mechanical Properties of Living Endothelial Cells and Astrocytes, Analyzed by Atomic Force Microscopy. (PMID:33435130)
- Evaluation of tumor microenvironmental immune regulation and prognostic in lung adenocarcinoma from the perspective of purinergic receptor P2Y13. (PMID:34494914)
- Targeting the P2Y13 Receptor Suppresses IL-33 and HMGB1 Release and Ameliorates Experimental Asthma. (PMID:34860143)
- P2RY13 Exacerbates Intestinal Inflammation by Damaging the Intestinal Mucosal Barrier via Activating IL-6/STAT3 Pathway. (PMID:35982893)
- Erythrocytes from patients with ST-elevation myocardial infarction induce cardioprotection through the purinergic P2Y13 receptor and nitric oxide signaling. (PMID:36112326)
- P2Y13 receptor deficiency favors adipose tissue lipolysis and worsens insulin resistance and fatty liver disease. (PMID:38470490)
Cross-species orthologs
3 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | p2ry13 | ENSDARG00000069944 |
| mus_musculus | P2ry13 | ENSMUSG00000036362 |
| rattus_norvegicus | P2ry13 | ENSRNOG00000029756 |
Paralogs (6): GPR87 (ENSG00000138271), P2RY12 (ENSG00000169313), PTAFR (ENSG00000169403), GPR34 (ENSG00000171659), P2RY14 (ENSG00000174944), GPR171 (ENSG00000174946)
Protein
Protein identifiers
P2Y purinoceptor 13 — Q9BPV8 (reviewed: Q9BPV8)
Alternative names: G-protein coupled receptor 86, G-protein coupled receptor 94
All UniProt accessions (1): Q9BPV8
UniProt curated annotations — full annotation on UniProt →
Function. Receptor for ADP. Coupled to G(i)-proteins. May play a role in hematopoiesis and the immune system.
Subcellular location. Cell membrane.
Tissue specificity. Strong expression in spleen and adult brain. Lower expression in placenta, lung, liver, spinal cord, thymus, small intestine, uterus, stomach, testis, fetal brain, and adrenal gland. Not detected in pancreas, heart, kidney, skeletal muscle, ovary or fetal aorta. Clearly detected in lymph node and bone marrow, weakly detected in peripheral blood mononuclear cells (PBMC) and in peripheral blood leukocytes (PBL), but not detected in polymorphonuclear cells (PMN). In the brain, detected in all brain regions examined.
Miscellaneous. Stimulation by ADP in stably transfected CHO cells resulted in inhibition of adenylyl cyclase and the phosphorylation of the MAP kinases MAPK3 and MAPK1 in a pertussis toxin-sensitive way. Inhibition of adenylyl cyclase and phosphorylation of the MAP kinases are transduction mechanisms that involve G(i) proteins.
Similarity. Belongs to the G-protein coupled receptor 1 family.
Isoforms (2)
| UniProt ID | Names | Canonical? |
|---|---|---|
| Q9BPV8-1 | 1 | yes |
| Q9BPV8-2 | 2 |
RefSeq proteins (1): NP_795713* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR000276 | GPCR_Rhodpsn | Family |
| IPR008109 | P2Y13_rcpt | Family |
| IPR017452 | GPCR_Rhodpsn_7TM | Domain |
Pfam: PF00001
UniProt features (23 total): topological domain 8, transmembrane region 7, glycosylation site 3, chain 1, region of interest 1, disulfide bond 1, splice variant 1, sequence variant 1
Structure
Experimental structures (PDB)
0 structures.
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-Q9BPV8-F1 | 83.33 | 0.56 |
Functional residue map
Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.
Disulfide bonds (1): 116–194
Glycosylation sites (3): 23, 31, 285
Function
Pathways and Gene Ontology
Reactome pathways
2 pathways
| ID | Pathway |
|---|---|
| R-HSA-417957 | P2Y receptors |
| R-HSA-418594 | G alpha (i) signalling events |
MSigDB gene sets: 171 (showing top):
GOBP_G_PROTEIN_COUPLED_PURINERGIC_NUCLEOTIDE_RECEPTOR_SIGNALING_PATHWAY, REACTOME_P2Y_RECEPTORS, IVANOVA_HEMATOPOIESIS_MATURE_CELL, CEBPB_01, PICCALUGA_ANGIOIMMUNOBLASTIC_LYMPHOMA_UP, WTGAAAT_UNKNOWN, KEGG_NEUROACTIVE_LIGAND_RECEPTOR_INTERACTION, COATES_MACROPHAGE_M1_VS_M2_UP, AACTTT_UNKNOWN, GOBP_PURINERGIC_NUCLEOTIDE_RECEPTOR_SIGNALING_PATHWAY, REACTOME_CLASS_A_1_RHODOPSIN_LIKE_RECEPTORS, GOMF_TRANSMEMBRANE_SIGNALING_RECEPTOR_ACTIVITY, CHEN_METABOLIC_SYNDROM_NETWORK, GOMF_G_PROTEIN_COUPLED_RECEPTOR_ACTIVITY, chr3q25
GO Biological Process (4): G protein-coupled receptor signaling pathway (GO:0007186), signal transduction (GO:0007165), negative regulation of adenylate cyclase activity (GO:0007194), G protein-coupled purinergic nucleotide receptor signaling pathway (GO:0035589)
GO Molecular Function (3): G protein-coupled purinergic nucleotide receptor activity (GO:0045028), G protein-coupled receptor activity (GO:0004930), protein binding (GO:0005515)
GO Cellular Component (3): endoplasmic reticulum (GO:0005783), plasma membrane (GO:0005886), membrane (GO:0016020)
Reactome top-level categories
Rollup of top-2 pathways:
| Category | Pathways |
|---|---|
| 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 | 2 |
| signal transduction | 1 |
| cell communication | 1 |
| cellular process | 1 |
| signaling | 1 |
| regulation of cellular process | 1 |
| cellular response to stimulus | 1 |
| adenylate cyclase activity | 1 |
| negative regulation of catalytic activity | 1 |
| regulation of adenylate cyclase activity | 1 |
| purinergic nucleotide receptor signaling pathway | 1 |
| purinergic nucleotide receptor activity | 1 |
| G protein-coupled purinergic nucleotide receptor signaling pathway | 1 |
| transmembrane signaling receptor activity | 1 |
| G protein-coupled receptor signaling pathway | 1 |
| binding | 1 |
| cytoplasm | 1 |
| endomembrane system | 1 |
| intracellular membrane-bounded organelle | 1 |
| membrane | 1 |
| cell periphery | 1 |
| cellular anatomical structure | 1 |
Protein interactions and networks
STRING
1106 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| P2RY13 | P2RY11 | Q96G91 | 882 |
| P2RY13 | A0A0B4J1V8 | A0A0B4J1V8 | 881 |
| P2RY13 | P2RX1 | P51575 | 785 |
| P2RY13 | P2RX6 | O15547 | 784 |
| P2RY13 | P2RX5 | Q93086 | 708 |
| P2RY13 | P2RX2 | Q9UBL9 | 701 |
| P2RY13 | P2RX3 | P56373 | 696 |
| P2RY13 | ALDH18A1 | P54886 | 638 |
| P2RY13 | TMEM119 | Q4V9L6 | 627 |
| P2RY13 | P2RX4 | Q99571 | 622 |
| P2RY13 | ADORA3 | P0DMS8 | 602 |
| P2RY13 | TREM2 | Q9NZC2 | 590 |
| P2RY13 | P2RX7 | Q99572 | 559 |
| P2RY13 | P2RY4 | P51582 | 545 |
| P2RY13 | ENTPD1 | P49961 | 542 |
IntAct
4 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| GJA8 | P2RY13 | psi-mi:“MI:0915”(physical association) | 0.560 |
| GJA8 | P2RY13 | psi-mi:“MI:0915”(physical association) | 0.000 |
| P2RY13 | GJA8 | psi-mi:“MI:0915”(physical association) | 0.000 |
BioGRID (2): P2RY13 (Two-hybrid), P2RY13 (Affinity Capture-MS)
ESM2 similar proteins: A5A4K9, B0F9W3, B2ZI34, F7EQ49, O08878, O35881, O54799, O93361, P21729, P24053, P28336, P30550, P32250, P33534, P34975, P35372, P41144, P41145, P42866, P43657, P46663, P52500, P55085, P55086, P79350, Q15391, Q2HJA4, Q2KIP6, Q3SX17, Q4G072, Q5IS39, Q63645, Q6GUG4, Q8BLG2, Q8BMC0, Q8BMP4, Q95254, Q95KC3, Q95M54, Q98907
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, B0UXR0, C8YUV0, E9QJ73, O02213, O08786, O09047, O16020, O42179, O55197, O57422, O70129
SIGNOR signaling
7 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| P2RY13 | “up-regulates activity” | GNAO1 | binding |
| P2RY13 | “up-regulates activity” | GNAQ | binding |
| P2RY13 | “up-regulates activity” | GNA14 | binding |
| P2RY13 | “up-regulates activity” | GNA15 | binding |
| P2RY13 | “up-regulates activity” | GNA12 | binding |
| P2RY13 | “up-regulates activity” | GNA13 | binding |
| ADP | “up-regulates activity” | P2RY13 | “chemical activation” |
Disease & clinical
Clinical variants and AI predictions
ClinVar
1 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 0 |
| Likely benign | 0 |
| Benign | 0 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
158 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 3:151329016:A:T | acceptor_gain | 0.9900 |
| 3:151329023:A:C | acceptor_gain | 0.9900 |
| 3:151329027:A:C | acceptor_gain | 0.9900 |
| 3:151329476:TTCA:T | donor_loss | 0.9900 |
| 3:151329008:C:CA | acceptor_loss | 0.9800 |
| 3:151329009:T:A | acceptor_loss | 0.9800 |
| 3:151329015:CAA:C | acceptor_gain | 0.9800 |
| 3:151329497:A:AC | donor_gain | 0.9800 |
| 3:151329498:G:C | donor_gain | 0.9800 |
| 3:151329005:CAC:C | acceptor_gain | 0.9700 |
| 3:151329209:TTTA:T | donor_gain | 0.9700 |
| 3:151329008:C:CC | acceptor_gain | 0.9600 |
| 3:151329025:A:C | acceptor_gain | 0.9600 |
| 3:151329014:CCAA:C | acceptor_gain | 0.9400 |
| 3:151329219:CCA:C | donor_gain | 0.9400 |
| 3:151329497:AGTT:A | donor_gain | 0.9400 |
| 3:151328535:A:C | acceptor_gain | 0.9300 |
| 3:151329011:T:TC | acceptor_gain | 0.9300 |
| 3:151329233:T:TA | donor_gain | 0.9300 |
| 3:151329011:T:C | acceptor_gain | 0.9200 |
| 3:151329015:C:T | acceptor_gain | 0.9200 |
| 3:151329017:A:AC | acceptor_gain | 0.9100 |
| 3:151329004:TCAC:T | acceptor_gain | 0.9000 |
| 3:151329005:CACC:C | acceptor_gain | 0.9000 |
| 3:151329022:CATA:C | acceptor_gain | 0.8900 |
| 3:151329027:A:AC | acceptor_gain | 0.8900 |
| 3:151328528:C:CT | acceptor_gain | 0.8800 |
| 3:151329017:A:C | acceptor_gain | 0.8800 |
| 3:151329221:A:AC | donor_gain | 0.8700 |
| 3:151329025:A:AC | acceptor_gain | 0.8600 |
AlphaMissense
2347 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 3:151328252:A:C | F268L | 0.995 |
| 3:151328252:A:T | F268L | 0.995 |
| 3:151328254:A:G | F268L | 0.995 |
| 3:151328405:G:C | F217L | 0.993 |
| 3:151328405:G:T | F217L | 0.993 |
| 3:151328407:A:G | F217L | 0.993 |
| 3:151328257:A:G | C267R | 0.992 |
| 3:151328811:A:G | L82P | 0.991 |
| 3:151328475:C:G | C194S | 0.990 |
| 3:151328476:A:T | C194S | 0.990 |
| 3:151328476:A:G | C194R | 0.989 |
| 3:151328084:G:C | F324L | 0.988 |
| 3:151328084:G:T | F324L | 0.988 |
| 3:151328086:A:G | F324L | 0.988 |
| 3:151328247:G:C | P270R | 0.988 |
| 3:151328462:C:A | K198N | 0.988 |
| 3:151328462:C:G | K198N | 0.988 |
| 3:151328653:C:G | G135R | 0.988 |
| 3:151328653:C:T | G135R | 0.988 |
| 3:151328709:C:G | C116S | 0.988 |
| 3:151328710:A:T | C116S | 0.988 |
| 3:151328242:G:C | H272D | 0.987 |
| 3:151328247:G:T | P270Q | 0.987 |
| 3:151328443:A:G | W205R | 0.987 |
| 3:151328443:A:T | W205R | 0.987 |
| 3:151328554:A:G | W168R | 0.987 |
| 3:151328554:A:T | W168R | 0.987 |
| 3:151328710:A:G | C116R | 0.987 |
| 3:151328884:C:G | G58R | 0.986 |
| 3:151328160:T:A | K299I | 0.985 |
dbSNP variants (sampled 300 via entrez): RS1000024182 (3:151329251 A>G), RS1000193151 (3:151329982 T>C,G), RS1000530433 (3:151328283 A>G), RS1001850633 (3:151327244 G>A), RS1002219977 (3:151326598 G>A), RS1002614891 (3:151326876 A>C,G), RS1003334575 (3:151330113 C>A), RS1005001415 (3:151328669 C>A,T), RS1005338738 (3:151327212 G>C,T), RS1005348804 (3:151326976 A>G), RS1006223421 (3:151326955 G>T), RS1006287847 (3:151327673 G>A), RS1006624364 (3:151326046 C>A), RS1006991854 (3:151326580 G>A), RS1007218444 (3:151330805 G>A)
Disease associations
OMIM: gene MIM:606380 | disease phenotypes:
GenCC curated gene-disease
Mondo (0):
Orphanet (0):
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
0 associations (top):
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (2): CHEMBL3321651 (SINGLE PROTEIN), CHEMBL4524011 (PROTEIN FAMILY)
Molecules with ChEMBL bioactivity
3 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 6,599 (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 |
|---|---|---|---|
| CHEMBL334966 | CANGRELOR | 4 | 900 |
| CHEMBL398435 | TICAGRELOR | 4 | 2,956 |
| CHEMBL413376 | SURAMIN HEXASODIUM | 3 | 2,743 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
GtoPdb / IUPHAR curated pharmacology
(IUPHAR/BPS Guide to Pharmacology — expert-curated)
Target class: gpcr — P2Y receptors
Most potent curated ligand interactions (15 total), top 15:
| Ligand | Action | Affinity | Parameter |
|---|---|---|---|
| [33P]2MeSADP | Full agonist | 9.6 | pKd |
| 2MeSADP | Full agonist | 9.0 | pIC50 |
| cangrelor | Antagonist | 8.3 | pIC50 |
| 2MeSATP | Full agonist | 7.7 | pIC50 |
| Ap4A | Antagonist | 6.7 | pIC50 |
| ADP | Full agonist | 6.5 | pIC50 |
| MRS2603 | Antagonist | 6.18 | pIC50 |
| MRS2211 | Antagonist | 5.97 | pIC50 |
| reactive blue-2 | Antagonist | 5.7 | pIC50 |
| ADPβS | Full agonist | 5.7 | pIC50 |
| suramin | Antagonist | 5.6 | pIC50 |
| 2MeSAMP | Antagonist | 5.6 | pIC50 |
| ATPγS | Full agonist | 5.5 | pIC50 |
| ATP | Full agonist | 5.4 | pIC50 |
| PPADS | Antagonist | 4.9 | pIC50 |
Binding affinities (BindingDB)
9 measured of 9 human assays (9 total across all organisms); most potent 9 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value | Patent |
|---|---|---|---|
| ARL 69931MX | EC50 | 6320 nM | US-10220040: Compounds, compositions and methods useful for cholesterol mobilization |
| N-(2,3-dihydro-1,4-benzodioxin-6-yl)-2-(2-methoxyethylamino)acetamide | EC50 | 48900 nM | US-10220040: Compounds, compositions and methods useful for cholesterol mobilization |
| 4-[1-[(3-hydroxy-4-methoxyphenyl)methyl]piperidin-4-yl]-2-piperidin-1-yl-1H-pyrimidin-6-one | EC50 | 299000 nM | US-10220040: Compounds, compositions and methods useful for cholesterol mobilization |
| 4-[1-[[2-(methylamino)pyrimidin-5-yl]methyl]piperidin-4-yl]-2-piperidin-1-yl-1H-pyrimidin-6-one | EC50 | 6.63e+06 nM | US-10220040: Compounds, compositions and methods useful for cholesterol mobilization |
| ethyl (7S)-7-(2-chlorophenyl)-7-(6,7-dihydro-4H-thieno[3,2-c]pyridin-5-yl)-2,2-dimethylheptanoate | EC50 | 3.37e+07 nM | US-10220040: Compounds, compositions and methods useful for cholesterol mobilization |
| 4-[1-[[2-(dimethylamino)pyrimidin-5-yl]methyl]piperidin-4-yl]-2-morpholin-4-yl-1H-pyrimidin-6-one | EC50 | 4.03e+07 nM | US-10220040: Compounds, compositions and methods useful for cholesterol mobilization |
| 3,4-dihydro-1H-isochromen-1-yl(spiro[5H-pyrrolo[1,2-a]quinoxaline-4,4’-piperidine]-1’-yl)methanone | EC50 | 4.03e+07 nM | US-10220040: Compounds, compositions and methods useful for cholesterol mobilization |
| ethyl (7R)-7-(2-chlorophenyl)-7-(6,7-dihydro-4H-thieno[3,2-c]pyridin-5-yl)-2,2-dimethylheptanoate | EC50 | 4.24e+07 nM | US-10220040: Compounds, compositions and methods useful for cholesterol mobilization |
| 8-[(3E)-3-(carboxymethylidene)-4-hydroxypiperidin-1-yl]-8-(2-chlorophenyl)-2,2-dimethyloctanoic acid | EC50 | 5.52e+07 nM | US-10220040: Compounds, compositions and methods useful for cholesterol mobilization |
ChEMBL bioactivities
6 potent at pChembl≥5 of 8 total, top 6 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 6.18 | IC50 | 660.7 | nM | CHEMBL5281019 |
| 5.97 | IC50 | 1072 | nM | CHEMBL2219665 |
| 5.85 | IC50 | 1398 | nM | TICAGRELOR |
| 5.72 | IC50 | 1900 | nM | RB 2 |
| 5.64 | IC50 | 2300 | nM | SURAMIN HEXASODIUM |
| 5.20 | EC50 | 6322 | nM | CANGRELOR |
PubChem BioAssay actives
5 with measured affinity, of 23 total; 5 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 |
|---|---|---|---|---|
| [2-[(4-chloro-3-nitrophenyl)diazenyl]-4-formyl-5-hydroxy-6-methyl-3-pyridinyl]methyl dihydrogen phosphate | 1953765: Antagonist activity at human P2Y13 | ic50 | 0.6607 | uM |
| [2-[(2-chloro-5-nitrophenyl)diazenyl]-4-formyl-5-hydroxy-6-methyl-3-pyridinyl]methyl dihydrogen phosphate | 1953765: Antagonist activity at human P2Y13 | ic50 | 1.0715 | uM |
| Ticagrelor | 1896871: Antagonist activity at human P2Y13R expressed in HEK293 cells assessed as inhibition of 2MeSADP-induced cAMP production preincubated for 0.5 hrs followed by 2MeSADP stimulation by cAMP-glo assay | ic50 | 1.3980 | uM |
| trisodium;1-amino-4-[4-[[4-chloro-6-(3-sulfonatoanilino)-1,3,5-triazin-2-yl]amino]-3-sulfonatoanilino]-9,10-dioxoanthracene-2-sulfonate | 1953764: Antagonist activity at P2Y13 (unknown origin) | ic50 | 1.9000 | uM |
| hexasodium;8-[[4-methyl-3-[[3-[[3-[[2-methyl-5-[(4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl]phenyl]carbamoyl]phenyl]carbamoylamino]benzoyl]amino]benzoyl]amino]naphthalene-1,3,5-trisulfonate | 1953764: Antagonist activity at P2Y13 (unknown origin) | ic50 | 2.3000 | uM |
CTD chemical–gene interactions
16 total (human), top 16 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Nickel | decreases expression, increases expression | 3 |
| Air Pollutants | increases abundance, decreases expression, affects expression | 2 |
| triphenyl phosphate | affects expression | 1 |
| di-n-butylphosphoric acid | affects expression | 1 |
| MRS 2211 | affects binding, decreases activity, decreases reaction, decreases response to substance, increases reaction | 1 |
| Arsenic Trioxide | increases expression | 1 |
| Adenosine Triphosphate | increases reaction, decreases reaction, decreases response to substance | 1 |
| Air Pollutants, Occupational | decreases expression | 1 |
| Cadmium | decreases expression, increases abundance | 1 |
| Hydrogen Peroxide | decreases reaction, decreases response to substance, increases reaction | 1 |
| Ozone | affects expression, increases abundance | 1 |
| Tetrachlorodibenzodioxin | decreases expression | 1 |
| Tretinoin | increases expression | 1 |
| Antirheumatic Agents | decreases expression | 1 |
| Cadmium Chloride | decreases expression, increases abundance | 1 |
| Particulate Matter | decreases expression, increases abundance | 1 |
ChEMBL screening assays
12 unique, capped per target: 11 binding, 1 functional
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1070721 | Binding | Inhibition of P2Y13 at 10 uM | Part II: piperazinyl-glutamate-pyridines as potent orally bioavailable P2Y12 antagonists for inhibition of platelet aggregation. — Bioorg Med Chem Lett |
| CHEMBL5153133 | Functional | Antagonist activity at human P2Y13R expressed in HEK293 cells assessed as inhibition of 2MeSADP-induced cAMP production preincubated for 0.5 hrs followed by 2MeSADP stimulation by cAMP-glo assay | Discovery of a Series of 5-Amide-1H-pyrazole-3-carboxyl Derivatives as Potent P2Y14R Antagonists with Anti-Inflammatory Characters. — J Med Chem |
Cellosaurus cell lines
1 cell lines: 1 cancer cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_ZD96 | 1321N1-HA-P2Y13 | Cancer cell line | Male |
Clinical trials (associated diseases)
0 trials via MONDO — disease-level, not drug-specific.
Related Atlas pages
- Targeted by drugs: Cangrelor, Suramin, Triphosphate