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Target
Prostacyclin receptor
Ligand
BDBM50372058
Substrate
n/a
Meas. Tech.
ChEMBL_464718 (CHEMBL933061)
Ki
2000±n/a nM
Citation
 Burch, JD; Belley, M; Fortin, R; Deschênes, D; Girard, M; Colucci, J; Farand, J; Therien, AG; Mathieu, MC; Denis, D; Vigneault, E; Lévesque, JF; Gagné, S; Wrona, M; Xu, D; Clark, P; Rowland, S; Han, Y Structure-activity relationships and pharmacokinetic parameters of quinoline acylsulfonamides as potent and selective antagonists of the EP(4) receptor. Bioorg Med Chem Lett 18:2048-54 (2008) [PubMed]  Article
Target
Name:
Prostacyclin receptor
Synonyms:
PGI receptor | PI2R_HUMAN | PRIPR | PTGIR | Prostacyclin (IP) Receptor | Prostacyclin receptor | Prostaglandin I | Prostaglandin I2 | Prostaglandin I2 receptor | Prostanoid IP receptor
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
40968.22
Organism:
Homo sapiens (Human)
Description:
The membranes prepared from human platelet were used in binding assay.
Residue:
386
Sequence:
MADSCRNLTYVRGSVGPATSTLMFVAGVVGNGLALGILSARRPARPSAFAVLVTGLAATDLLGTSFLSPAVFVAYARNSSLLGLARGGPALCDAFAFAMTFFGLASMLILFAMAVERCLALSHPYLYAQLDGPRCARLALPAIYAFCVLFCALPLLGLGQHQQYCPGSWCFLRMRWAQPGGAAFSLAYAGLVALLVAAIFLCNGSVTLSLCRMYRQQKRHQGSLGPRPRTGEDEVDHLILLALMTVVMAVCSLPLTIRCFTQAVAPDSSSEMGDLLAFRFYAFNPILDPWVFILFRKAVFQRLKLWVCCLCLGPAHGDSQTPLSQLASGRRDPRAPSAPVGKEGSCVPLSAWGEGQVEPLPPTQQSSGSAVGTSSKAEASVACSLC
  
Inhibitor
Name:
BDBM50372058
Synonyms:
CHEMBL404199
Type:
Small organic molecule
Emp. Form.:
C35H31F6N3O8S
Mol. Mass.:
767.691
SMILES:
COc1cccc(OC)c1C1(CC1)C(=O)NS(=O)(=O)Cc1ccc(N2Cc3c(C2=O)c(OCC(F)(F)F)c2cccnc2c3OCC(F)(F)F)c(C)c1
Structure:
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