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TargetP2X purinoceptor 1
LigandBDBM50015276
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1365177 (CHEMBL3292927)
IC50 180±n/a nM
Citation Jeon, YTYang, WQiao, JXLi, LRuel, RThibeault, CHiebert, SWang, TCWang, YLiu, YClark, CGWong, HSZhu, JWu, DRSun, DChen, BCMathur, AChacko, SAMalley, MChen, XQShen, HHuang, CSSchumacher, WABostwick, JSStewart, ABPrice, LAHua, JLi, DLevesque, PCSeiffert, DARehfuss, RWexler, RRLam, PY Identification of 1-{2-[4-chloro-1'-(2,2-dimethylpropyl)-7-hydroxy-1,2-dihydrospiro[indole-3,4'-piperidine]-1-yl]phenyl}-3-{5-chloro-[1,3]thiazolo[5,4-b]pyridin-2-yl}urea, a potent, efficacious and orally bioavailable P2Y(1) antagonist as an antiplatelet agent. Bioorg Med Chem Lett24:1294-8 (2014) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
P2X purinoceptor 1
Name:P2X purinoceptor 1
Synonyms:ATP receptor | P2RX1 | P2RX1_HUMAN | P2X1 | Purinergic receptor | Purinergic, P2X
Type:Enzyme Catalytic Domain
Mol. Mass.:44992.65
Organism:Homo sapiens (Human)
Description:Purinergic, P2X 0 HUMAN::P51575
Residue:399
Sequence:
MARRFQEELAAFLFEYDTPRMVLVRNKKVGVIFRLIQLVVLVYVIGWVFLYEKGYQTSSG
LISSVSVKLKGLAVTQLPGLGPQVWDVADYVFPAQGDNSFVVMTNFIVTPKQTQGYCAEH
PEGGICKEDSGCTPGKAKRKAQGIRTGKCVAFNDTVKTCEIFGWCPVEVDDDIPRPALLR
EAENFTLFIKNSISFPRFKVNRRNLVEEVNAAHMKTCLFHKTLHPLCPVFQLGYVVQESG
QNFSTLAEKGGVVGITIDWHCDLDWHVRHCRPIYEFHGLYEEKNLSPGFNFRFARHFVEN
GTNYRHLFKVFGIRFDILVDGKAGKFDIIPTMTTIGSGIGIFGVATVLCDLLLLHILPKR
HYYKQKKFKYAEDMGPGAAERDLAATSSTLGLQENMRTS
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50015276
n/a
NameBDBM50015276
Synonyms:CHEMBL3263056 | US9428504, 166 | US9428504, 167
TypeSmall organic molecule
Emp. Form.C30H32Cl2N6O2S
Mol. Mass.611.585
SMILESCC(C)(C)CN1CCC2(CN(c3c2c(Cl)ccc3O)c2ccccc2NC(=O)Nc2nc3ccc(Cl)nc3s2)CC1
Structure
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