Uridine Triphosphate
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Also known as INS-316INS316Uridine 5'-triphosphateUtpUridine-5'-triphosphateUridine triphosphate (UTP)SID26756678
Summary
Uridine Triphosphate (CHEMBL336296) is a phase-3 clinical-stage small molecule targeting P2RY2, P2RY4, and P2RY6; indicated across 2 conditions including lung neoplasm and interstitial lung disease.
At a glance
- Status: Max clinical phase 3 (not approved)
- Modality: Small molecule
- Targets: 4 (P2RY2, P2RY4, P2RY6…)
- Indications: 2 conditions
- Clinical trials: 3
- Chemistry: 484.14 Da · C9H15N2O15P3
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL336296 |
| Name | Uridine Triphosphate |
| Type | Small molecule |
| Max phase | 3 |
| FDA approved | no |
| PubChem CID | 6133 |
| ChEBI | CHEBI:15713 |
| Molecular formula | C9H15N2O15P3 |
| Molecular weight | 484.14 |
| InChIKey | PGAVKCOVUIYSFO-XVFCMESISA-N |
SMILES: C1=CN(C(=O)NC1=O)[C@H]2[C@@H]([C@@H]([C@H](O2)COP(=O)(O)OP(=O)(O)OP(=O)(O)O)O)O
IUPAC name: [[(2R,3S,4R,5R)-5-(2,4-dioxopyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate
ChEBI definition: A pyrimidine ribonucleoside 5’-triphosphate having uracil as the nucleobase.
Other ChEBI roles (chemical / environmental): Escherichia coli metabolite, mouse metabolite.
Also known as: INS-316, INS316, Uridine 5’-triphosphate, Uridine triphosphate, Utp, Uridine-5’-triphosphate, Uridine triphosphate (UTP), UTP, uridine triphosphate, uridine 5’-triphosphate, SID26756678, URIDINE TRIPHOSPHATE
Parent form; salt/anhydrous children: CHEMBL5077459
Patent coverage: 7,183 distinct patent families (17,782 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.
Targets
Targets
Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).
| Gene | Target | Action | pAffinity | Cancer dependency | UniProt |
|---|---|---|---|---|---|
| P2RY2 | P2Y2 receptor | Full agonist | 8.1 | 1% | P41231 |
| P2RY4 | P2Y4 receptor | Full agonist | 6.3 | 0% | P51582 |
| P2RY6 | P2Y6 receptor | Partial agonist | 5.2 | 3.2% | Q15077 |
| P2RY11 | P2Y11 receptor | Full agonist | 5.2 | 0% | Q96G91 |
Broader ChEMBL bioactivity targets: 8 (assay-derived). Sample: Tyrosyl-DNA phosphodiesterase 1, P2Y purinoceptor 2, Inositol monophosphatase 1, P2Y purinoceptor 4, P2Y purinoceptor 4, P2Y purinoceptor 2, P2Y purinoceptor 2, P2Y purinoceptor 6.
Bioactivity
ChEMBL activities: 62 potent at pChembl ≥ 5 of 65 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| P2RY2 | 8.25 | EC50 | 5.61 | nM | CHEMBL_ACT_18092217 |
| P2RY2 | 8.15 | EC50 | 7 | nM | CHEMBL_ACT_2011533 |
| P2RY2 | 8.15 | EC50 | 7 | nM | CHEMBL_ACT_2013697 |
| P2RY2 | 7.75 | EC50 | 17.9 | nM | CHEMBL_ACT_6163205 |
| P2RY2 | 7.7 | EC50 | 20 | nM | CHEMBL_ACT_8045538 |
| P2RY2 | 7.52 | EC50 | 30 | nM | CHEMBL_ACT_1104765 |
| P2RY2 | 7.43 | EC50 | 37.2 | nM | CHEMBL_ACT_2513448 |
| P2RY4 | 7.41 | EC50 | 39 | nM | CHEMBL_ACT_2011552 |
| P2RY4 | 7.41 | EC50 | 39 | nM | CHEMBL_ACT_2013716 |
| P2RY2 | 7.37 | EC50 | 43 | nM | CHEMBL_ACT_1782117 |
| P2RY2 | 7.31 | EC50 | 49 | nM | CHEMBL_ACT_1820922 |
| P2RY2 | 7.3 | EC50 | 50.1 | nM | CHEMBL_ACT_2513451 |
| P2RY2 | 7.26 | EC50 | 55 | nM | CHEMBL_ACT_6214779 |
| P2RY2 | 7.23 | EC50 | 59 | nM | CHEMBL_ACT_2513449 |
| P2RY2 | 7.22 | EC50 | 60 | nM | CHEMBL_ACT_2350099 |
| P2RY2 | 7.22 | EC50 | 60 | nM | CHEMBL_ACT_3309948 |
| P2RY2 | 7.22 | EC50 | 60 | nM | CHEMBL_ACT_6214768 |
| P2RY2 | 7.15 | EC50 | 70.6 | nM | CHEMBL_ACT_18092219 |
| P2RY4 | 7.14 | EC50 | 73 | nM | CHEMBL_ACT_1820923 |
| P2RY4 | 7.1 | EC50 | 80 | nM | CHEMBL_ACT_6214809 |
| P2RY2 | 7.09 | EC50 | 80.4 | nM | CHEMBL_ACT_2513425 |
| P2RY4 | 7.06 | EC50 | 87 | nM | CHEMBL_ACT_1782118 |
| P2RY4 | 7.05 | EC50 | 90 | nM | CHEMBL_ACT_2350134 |
| P2RY4 | 7.05 | EC50 | 90 | nM | CHEMBL_ACT_3309938 |
| P2RY4 | 7.05 | EC50 | 88.4 | nM | CHEMBL_ACT_6163231 |
| P2RY4 | 7.05 | EC50 | 90 | nM | CHEMBL_ACT_6214776 |
| P2RY4 | 7 | EC50 | 100 | nM | CHEMBL_ACT_1104766 |
| P2RY2 | 7 | EC50 | 100 | nM | CHEMBL_ACT_18488165 |
| P2RY2 | 7 | EC50 | 100 | nM | CHEMBL_ACT_3105585 |
| P2RY2 | 6.97 | EC50 | 108 | nM | CHEMBL_ACT_2513456 |
| P2RY2 | 6.96 | EC50 | 109.7 | nM | CHEMBL_ACT_1998139 |
| P2RY2 | 6.92 | EC50 | 120 | nM | CHEMBL_ACT_18488170 |
| P2RY2 | 6.92 | EC50 | 121 | nM | CHEMBL_ACT_2513455 |
| P2RY2 | 6.91 | EC50 | 124 | nM | CHEMBL_ACT_2513450 |
| P41232 | 6.89 | EC50 | 130 | nM | CHEMBL_ACT_1690753 |
| P2RY2 | 6.86 | EC50 | 138 | nM | CHEMBL_ACT_2513452 |
| P2RY2 | 6.85 | EC50 | 140 | nM | CHEMBL_ACT_11011188 |
| P2RY2 | 6.85 | EC50 | 140 | nM | CHEMBL_ACT_18488160 |
| P2RY2 | 6.85 | EC50 | 140 | nM | CHEMBL_ACT_25089890 |
| P2RY2 | 6.85 | EC50 | 140 | nM | CHEMBL_ACT_38857 |
| P2RY2 | 6.8 | EC50 | 160 | nM | CHEMBL_ACT_18488167 |
| P2RY2 | 6.8 | EC50 | 157 | nM | CHEMBL_ACT_2513454 |
| P2RY6 | 6.37 | EC50 | 424 | nM | CHEMBL_ACT_2011557 |
| P2RY2 | 6.35 | EC50 | 450 | nM | CHEMBL_ACT_1690754 |
| P2RY4 | 6.32 | EC50 | 480 | nM | CHEMBL_ACT_2302276 |
| P2RY4 | 6.32 | EC50 | 480 | nM | CHEMBL_ACT_8031839 |
| P2RY4 | 6.3 | EC50 | 500 | nM | CHEMBL_ACT_3105588 |
| P2RY4 | 6.26 | EC50 | 550 | nM | CHEMBL_ACT_25089895 |
| P2RY2 | 6.19 | EC50 | 640 | nM | CHEMBL_ACT_2302275 |
| P2RY2 | 6.19 | EC50 | 640 | nM | CHEMBL_ACT_8031821 |
| P2RY2 | 6.11 | EC50 | 781 | nM | CHEMBL_ACT_2513556 |
| P2RY4 | 6.05 | EC50 | 900 | nM | CHEMBL_ACT_11011189 |
| P2RY2 | 6.04 | EC50 | 911 | nM | CHEMBL_ACT_18092221 |
| P2RY2 | 6 | EC50 | 996 | nM | CHEMBL_ACT_18092224 |
| P2RY2 | 5.9 | EC50 | 1250 | nM | CHEMBL_ACT_18488163 |
| P35383 | 5.9 | EC50 | 1260 | nM | CHEMBL_ACT_2918172 |
| P35383 | 5.82 | IC50 | 1510 | nM | CHEMBL_ACT_2918158 |
| P2RY2 | 5.68 | EC50 | 2090 | nM | CHEMBL_ACT_2513426 |
| P2RY4 | 5.6 | EC50 | 2500 | nM | CHEMBL_ACT_38858 |
| O35811 | 5.58 | EC50 | 2600 | nM | CHEMBL_ACT_38859 |
| P2RY6 | 5.22 | EC50 | 6000 | nM | CHEMBL_ACT_38860 |
| P2RY6 | 5.22 | EC50 | 6000 | nM | CHEMBL_ACT_6163257 |
Target pathways
Aggregated over 4 target gene(s): P2RY2, P2RY4, P2RY6, P2RY11.
Top Reactome pathways
6 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| P2Y receptors | 4 | P2RY11, P2RY2, P2RY4, P2RY6 |
| G alpha (q) signalling events | 3 | P2RY11, P2RY2, P2RY6 |
| G alpha (s) signalling events | 1 | P2RY11 |
| G alpha (i) signalling events | 1 | P2RY4 |
| Surfactant metabolism | 1 | P2RY2 |
| High laminar flow shear stress activates signaling by PIEZO1 and PECAM1:CDH5:KDR in endothelial cells | 1 | P2RY2 |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| G protein-coupled receptor signaling pathway | 4 |
| phospholipase C-activating G protein-coupled receptor signaling pathway | 4 |
| G protein-coupled purinergic nucleotide receptor signaling pathway | 4 |
| signal transduction | 4 |
| cellular response to ATP | 3 |
| transepithelial chloride transport | 2 |
| cellular response to prostaglandin E stimulus | 2 |
| intracellular monoatomic ion homeostasis | 1 |
| positive regulation of mucus secretion | 1 |
| blood vessel diameter maintenance | 1 |
| positive regulation of cytosolic calcium ion concentration | 1 |
| phagocytosis | 1 |
| positive regulation of inositol trisphosphate biosynthetic process | 1 |
| positive regulation of release of sequestered calcium ion into cytosol | 1 |
| positive regulation of ERK1 and ERK2 cascade | 1 |
Indications & clinical
Indications
2 diseases in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.
| Disease (in trials) | Phase | MONDO | EFO |
|---|---|---|---|
| lung neoplasm | 3 | MONDO:0021117 | MONDO:0008903 |
| interstitial lung disease | 2 | MONDO:0015925 | EFO:0004244 |
Clinical trials
Total trials: 3.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 1 |
| EARLY_PHASE1 | 1 |
| Not specified | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT00008255 | PHASE2 | COMPLETED | INS316 in Diagnosing Lung Cancer in Patients With Untreated Lung Cancer |
| NCT03738943 | EARLY_PHASE1 | COMPLETED | Pyridoxine, P2 Receptor Antagonism, and ATP-mediated Vasodilation in Young Adults |
| NCT00033527 | Not specified | UNKNOWN | INS316 Compared With Saline for Sputum Collection in Diagnosing Lung Cancer |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No PharmGKB pharmacogenomic data curated for this drug.
Related molecules
Related molecules
Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.
9 molecules share ≥1 primary target. Top 9 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| ADENOSINE | ChEMBL + PubChem | Phase 4 (approved) | P2RY11, P2RY2, P2RY4 |
| DIQUAFOSOL | ChEMBL | Phase 4 (approved) | P2RY2, P2RY4, P2RY6 |
| DIQUAFOSOL TETRASODIUM | ChEMBL | Phase 4 (approved) | P2RY2, P2RY4, P2RY6 |
| DENUFOSOL | ChEMBL | Phase 3 | P2RY2, P2RY4, P2RY6 |
| SURAMIN | ChEMBL | Phase 3 | P2RY11, P2RY2, P2RY6 |
| ADENOSINE TRIPHOSPHATE | ChEMBL | Phase 2 | P2RY11, P2RY2, P2RY4 |
| DENUFOSOL TETRASODIUM | ChEMBL | Phase 3 | P2RY2, P2RY4 |
| Carbachol | PubChem | Approved | P2RY2 |
| Indomethacin | PubChem | Approved | P2RY2 |
Related Atlas pages
- Genes: P2RY2, P2RY4, P2RY6, P2RY11
- In clinical trials for: lung neoplasm, interstitial lung disease
- Drugs: Adenosine, Diquafosol, Denufosol, Suramin, Carbachol, Indomethacin