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Target
P2X purinoceptor 1
Ligand
BDBM50015276
Substrate
n/a
Meas. Tech.
ChEMBL_1365177 (CHEMBL3292927)
IC50
180±n/a nM
Citation
 Jeon, YT; Yang, W; Qiao, JX; Li, L; Ruel, R; Thibeault, C; Hiebert, S; Wang, TC; Wang, Y; Liu, Y; Clark, CG; Wong, HS; Zhu, J; Wu, DR; Sun, D; Chen, BC; Mathur, A; Chacko, SA; Malley, M; Chen, XQ; Shen, H; Huang, CS; Schumacher, WA; Bostwick, JS; Stewart, AB; Price, LA; Hua, J; Li, D; Levesque, PC; Seiffert, DA; Rehfuss, R; Wexler, RR; Lam, 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 Lett 24:1294-8 (2014) [PubMed]  Article 
Target
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:
MARRFQEELAAFLFEYDTPRMVLVRNKKVGVIFRLIQLVVLVYVIGWVFLYEKGYQTSSGLISSVSVKLKGLAVTQLPGLGPQVWDVADYVFPAQGDNSFVVMTNFIVTPKQTQGYCAEHPEGGICKEDSGCTPGKAKRKAQGIRTGKCVAFNDTVKTCEIFGWCPVEVDDDIPRPALLREAENFTLFIKNSISFPRFKVNRRNLVEEVNAAHMKTCLFHKTLHPLCPVFQLGYVVQESGQNFSTLAEKGGVVGITIDWHCDLDWHVRHCRPIYEFHGLYEEKNLSPGFNFRFARHFVENGTNYRHLFKVFGIRFDILVDGKAGKFDIIPTMTTIGSGIGIFGVATVLCDLLLLHILPKRHYYKQKKFKYAEDMGPGAAERDLAATSSTLGLQENMRTS
  
Inhibitor
Name:
BDBM50015276
Synonyms:
CHEMBL3263056 | US9428504, 166 | US9428504, 167
Type:
Small organic molecule
Emp. Form.:
C30H32Cl2N6O2S
Mol. Mass.:
611.585
SMILES:
CC(C)(C)CN1CCC2(CN(c3c2c(Cl)ccc3O)c2ccccc2NC(=O)Nc2nc3ccc(Cl)nc3s2)CC1
Structure:
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