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Target
Prostaglandin E2 receptor EP4 subtype
Ligand
BDBM50107283
Substrate
n/a
Meas. Tech.
ChEMBL_1548142 (CHEMBL3754944)
IC50
1600±n/a nM
Citation
 Blanco, MJ; Vetman, T; Chandrasekhar, S; Fisher, MJ; Harvey, A; Chambers, M; Lin, C; Mudra, D; Oskins, J; Wang, XS; Yu, XP; Warshawsky, AM Discovery of potent aryl-substituted 3-[(3-methylpyridine-2-carbonyl) amino]-2,4-dimethyl-benzoic acid EP4 antagonists with improved pharmacokinetic profile. Bioorg Med Chem Lett 26:931-5 (2016) [PubMed]  Article 
Target
Name:
Prostaglandin E2 receptor EP4 subtype
Synonyms:
PE2R4_HUMAN | PGE receptor EP4 subtype | PGE2 receptor EP4 subtype | PTGER2 | PTGER4 | Prostaglandin E2 receptor | Prostanoid EP4 receptor
Type:
Enzyme
Mol. Mass.:
53134.53
Organism:
Homo sapiens (Human)
Description:
P35408
Residue:
488
Sequence:
MSTPGVNSSASLSPDRLNSPVTIPAVMFIFGVVGNLVAIVVLCKSRKEQKETTFYTLVCGLAVTDLLGTLLVSPVTIATYMKGQWPGGQPLCEYSTFILLFFSLSGLSIICAMSVERYLAINHAYFYSHYVDKRLAGLTLFAVYASNVLFCALPNMGLGSSRLQYPDTWCFIDWTTNVTAHAAYSYMYAGFSSFLILATVLCNVLVCGALLRMHRQFMRRTSLGTEQHHAAAAASVASRGHPAASPALPRLSDFRRRRSFRRIAGAEIQMVILLIATSLVVLICSIPLVVRVFVNQLYQPSLEREVSKNPDLQAIRIASVNPILDPWIYILLRKTVLSKAIEKIKCLFCRIGGSRRERSGQHCSDSQRTSSAMSGHSRSFISRELKEISSTSQTLLPDLSLPDLSENGLGGRNLLPGVPGMGLAQEDTTSLRTLRISETSDSSQGQDSESVLLVDEAGGSGRAGPAPKGSSLQVTFPSETLNLSEKCI
  
Inhibitor
Name:
BDBM50107283
Synonyms:
AAT-007 | CJ-023 | Grapiprant | MR-10A7 | RQ-00000007 | RQ-7
Type:
Small organic molecule
Emp. Form.:
C26H29N5O3S
Mol. Mass.:
491.605
SMILES:
CCc1nc2c(C)nc(C)cc2n1-c1ccc(CCNC(=O)NS(=O)(=O)c2ccc(C)cc2)cc1
Structure:
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