Reaction Details |
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Target | Prostaglandin E2 receptor EP1 subtype |
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Ligand | BDBM50205276 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_425872 (CHEMBL856876) |
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Ki | >9000±n/a nM |
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Citation | Sturino, CF; O'Neill, G; Lachance, N; Boyd, M; Berthelette, C; Labelle, M; Li, L; Roy, B; Scheigetz, J; Tsou, N; Aubin, Y; Bateman, KP; Chauret, N; Day, SH; Lévesque, JF; Seto, C; Silva, JH; Trimble, LA; Carriere, MC; Denis, D; Greig, G; Kargman, S; Lamontagne, S; Mathieu, MC; Sawyer, N; Slipetz, D; Abraham, WM; Jones, T; McAuliffe, M; Piechuta, H; Nicoll-Griffith, DA; Wang, Z; Zamboni, R; Young, RN; Metters, KM Discovery of a potent and selective prostaglandin D2 receptor antagonist, [(3R)-4-(4-chloro-benzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]-acetic acid (MK-0524). J Med Chem50:794-806 (2007) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Prostaglandin E2 receptor EP1 subtype |
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Name: | Prostaglandin E2 receptor EP1 subtype |
Synonyms: | PE2R1_HUMAN | PGE receptor, EP1 subtype | PTGER1 | Prostaglandin E2 receptor | Prostaglandin E2 receptor EP1 subtype | Prostaglandin E2 receptor EP1 subtype (EP1) | Prostanoid EP1 receptor |
Type: | Enzyme |
Mol. Mass.: | 41834.57 |
Organism: | Homo sapiens (Human) |
Description: | P34995 |
Residue: | 402 |
Sequence: | MSPCGPLNLSLAGEATTCAAPWVPNTSAVPPSGASPALPIFSMTLGAVSNLLALALLAQA
AGRLRRRRSAATFLLFVASLLATDLAGHVIPGALVLRLYTAGRAPAGGACHFLGGCMVFF
GLCPLLLGCGMAVERCVGVTRPLLHAARVSVARARLALAAVAAVALAVALLPLARVGRYE
LQYPGTWCFIGLGPPGGWRQALLAGLFASLGLVALLAALVCNTLSGLALLRARWRRRSRR
PPPASGPDSRRRWGAHGPRSASASSASSIASASTFFGGSRSSGSARRARAHDVEMVGQLV
GIMVVSCICWSPMLVLVALAVGGWSSTSLQRPLFLAVRLASWNQILDPWVYILLRQAVLR
QLLRLLPPRAGAKGGPAGLGLTPSAWEASSLRSSRHSGLSHF
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BDBM50205276 |
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n/a |
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Name | BDBM50205276 |
Synonyms: | CHEMBL385126 | [(3R)-4-(4-chlorobenzyl)-7-fluoro-5-acetyl-1,2,3,4-tetrahydrocyclopenta-[b]indol-3-yl]acetic acid |
Type | Small organic molecule |
Emp. Form. | C22H19ClFNO3 |
Mol. Mass. | 399.843 |
SMILES | CC(=O)c1cc(F)cc2c3CC[C@H](CC(O)=O)c3n(Cc3ccc(Cl)cc3)c12 |
Structure |
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