Target Information
| Target General Information | Top | |||||
|---|---|---|---|---|---|---|
| Target ID |
T90782
(Former ID: TTDR00731)
|
|||||
| Target Name |
P2Y purinoceptor 6 (P2RY6)
|
|||||
| Synonyms |
P2Y6; P2RY6; Adenosine P2Y6 receptor
|
|||||
| Gene Name |
P2RY6
|
|||||
| Target Type |
Clinical trial target
|
[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Alzheimer disease [ICD-11: 8A20] | |||||
| Function |
Receptor for extracellular UDP > UTP > ATP. The activity of this receptor is mediated by G proteins which activate a phosphatidylinositol-calcium second messenger system.
Click to Show/Hide
|
|||||
| BioChemical Class |
GPCR rhodopsin
|
|||||
| UniProt ID | ||||||
| Sequence |
MEWDNGTGQALGLPPTTCVYRENFKQLLLPPVYSAVLAAGLPLNICVITQICTSRRALTR
TAVYTLNLALADLLYACSLPLLIYNYAQGDHWPFGDFACRLVRFLFYANLHGSILFLTCI SFQRYLGICHPLAPWHKRGGRRAAWLVCVAVWLAVTTQCLPTAIFAATGIQRNRTVCYDL SPPALATHYMPYGMALTVIGFLLPFAALLACYCLLACRLCRQDGPAEPVAQERRGKAARM AVVVAAAFAISFLPFHITKTAYLAVRSTPGVPCTVLEAFAAAYKGTRPFASANSVLDPIL FYFTQKKFRRRPHELLQKLTAKWQRQGR Click to Show/Hide
|
|||||
| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Clinical Trial Drug(s) | [+] 1 Clinical Trial Drugs | + | ||||
| 1 | GC021109 | Drug Info | Phase 1 | Alzheimer disease | [1], [2] | |
| Discontinued Drug(s) | [+] 1 Discontinued Drugs | + | ||||
| 1 | INS 316 | Drug Info | Discontinued in Phase 3 | Lung cancer | [3] | |
| Mode of Action | [+] 3 Modes of Action | + | ||||
| Agonist | [+] 13 Agonist drugs | + | ||||
| 1 | GC021109 | Drug Info | [1], [2] | |||
| 2 | INS 316 | Drug Info | [4] | |||
| 3 | 2MeSATP | Drug Info | [4] | |||
| 4 | 3-phenacyl-UDP | Drug Info | [5] | |||
| 5 | 5BrUTP | Drug Info | [4] | |||
| 6 | adenosine diphosphate | Drug Info | [4] | |||
| 7 | INS48823 | Drug Info | [6] | |||
| 8 | MRS2693 | Drug Info | [8] | |||
| 9 | MRS2782 | Drug Info | [9] | |||
| 10 | MRS2957 | Drug Info | [10] | |||
| 11 | Rp-5-OMe-UDPalphaB | Drug Info | [12] | |||
| 12 | UDP-beta-S | Drug Info | [6] | |||
| 13 | Up3U | Drug Info | [6] | |||
| Antagonist | [+] 2 Antagonist drugs | + | ||||
| 1 | MRS2567 | Drug Info | [7] | |||
| 2 | MRS2578 | Drug Info | [7] | |||
| Inhibitor | [+] 2 Inhibitor drugs | + | ||||
| 1 | PSB-0952 | Drug Info | [11] | |||
| 2 | RB 2 | Drug Info | [11] | |||
| Chemical Structure based Activity Landscape of Target | Top |
|---|---|
| Drug Property Profile of Target | Top | |
|---|---|---|
| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
|
|
||
| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
|
|
||
| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
|
|
||
| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Target Poor or Non Binders | Top | |||||
|---|---|---|---|---|---|---|
| Target Poor or Non Binders | ||||||
| Target Affiliated Biological Pathways | Top | |||||
|---|---|---|---|---|---|---|
| KEGG Pathway | [+] 1 KEGG Pathways | + | ||||
| 1 | Neuroactive ligand-receptor interaction | |||||
| Reactome | [+] 2 Reactome Pathways | + | ||||
| 1 | G alpha (q) signalling events | |||||
| 2 | P2Y receptors | |||||
| WikiPathways | [+] 5 WikiPathways | + | ||||
| 1 | Nucleotide GPCRs | |||||
| 2 | GPCRs, Class A Rhodopsin-like | |||||
| 3 | Gastrin-CREB signalling pathway via PKC and MAPK | |||||
| 4 | GPCR ligand binding | |||||
| 5 | GPCR downstream signaling | |||||
| Target-Related Models and Studies | Top | |||||
|---|---|---|---|---|---|---|
| Target Validation | ||||||
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 2 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 3 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008257) | |||||
| REF 4 | Cloning, functional expression and tissue distribution of the human P2Y6 receptor. Biochem Biophys Res Commun. 1996 May 15;222(2):303-8. | |||||
| REF 5 | Synthesis and structure-activity relationships of uracil nucleotide derivatives and analogues as agonists at human P2Y2, P2Y4, and P2Y6 receptors. J Med Chem. 2006 Nov 30;49(24):7076-87. | |||||
| REF 6 | P2 receptors activated by uracil nucleotides--an update. Curr Med Chem. 2006;13(3):289-312. | |||||
| REF 7 | Diisothiocyanate derivatives as potent, insurmountable antagonists of P2Y6 nucleotide receptors. Biochem Pharmacol. 2004 May 1;67(9):1763-70. | |||||
| REF 8 | Structure-activity relationships of uridine 5'-diphosphate analogues at the human P2Y6 receptor. J Med Chem. 2006 Sep 7;49(18):5532-43. | |||||
| REF 9 | Synthesis and potency of novel uracil nucleotides and derivatives as P2Y2 and P2Y6 receptor agonists. Bioorg Med Chem. 2008 Jun 15;16(12):6319-32. | |||||
| REF 10 | Pyrimidine ribonucleotides with enhanced selectivity as P2Y(6) receptor agonists: novel 4-alkyloxyimino, (S)-methanocarba, and 5'-triphosphate gamma-ester modifications. J Med Chem. 2010 Jun 10;53(11):4488-501. | |||||
| REF 11 | Development of potent and selective inhibitors of ecto-5'-nucleotidase based on an anthraquinone scaffold. J Med Chem. 2010 Mar 11;53(5):2076-86. | |||||
| REF 12 | 5-OMe-uridine-5'-O-(alpha-boranodiphosphate), a novel nucleotide derivative highly active at the human P2Y(6) receptor protects against death-receptor mediated glial apoptosis. Neurosci Lett. 2014 Aug 22;578:80-4. | |||||
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.