Reaction Details
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Sphingosine 1-phosphate receptor 3
Ligand
BDBM22225
Substrate
BDBM10852
Meas. Tech.
Ligand-Induced Uptake of [35S]-GTP-gamma-S
pH
7.4±n/a
Temperature
295.15±n/a K
EC50
184±n/a nM
Citation
Yan, L; Huo, P; Hale, JJ; Mills, SG; Hajdu, R; Keohane, CA; Rosenbach, MJ; Milligan, JA; Shei, GJ; Chrebet, G; Bergstrom, J; Card, D; Mandala, SM SAR studies of 3-arylpropionic acids as potent and selective agonists of sphingosine-1-phosphate receptor-1 (S1P1) with enhanced pharmacokinetic properties. Bioorg Med Chem Lett 17:828-31 (2007) [PubMed] Article More Info.:
Target
Name:
Sphingosine 1-phosphate receptor 3
Synonyms:
C9orf108 | C9orf47 | EDG3 | Endothelial differentiation G-protein coupled receptor 3 | S1P receptor 3 | S1P receptor Edg-3 | S1P3 | S1PR3 | S1PR3_HUMAN | Sphingosine 1-phosphate receptor | Sphingosine 1-phosphate receptor 3 (S1P3) | Sphingosine 1-phosphate receptor Edg-3
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
42278.13
Organism:
Homo sapiens (Human)
Description:
Q99500
Residue:
378
Sequence:
MATALPPRLQPVRGNETLREHYQYVGKLAGRLKEASEGSTLTTVLFLVICSFIVLENLMVLIAIWKNNKFHNRMYFFIGNLALCDLLAGIAYKVNILMSGKKTFSLSPTVWFLREGSMFVALGASTCSLLAIAIERHLTMIKMRPYDANKRHRVFLLIGMCWLIAFTLGALPILGWNCLHNLPDCSTILPLYSKKYIAFCISIFTAILVTIVILYARIYFLVKSSSRKVANHNNSERSMALLRTVVIVVSVFIACWSPLFILFLIDVACRVQACPILFKAQWFIVLAVLNSAMNPVIYTLASKEMRRAFFRLVCNCLVRGRGARASPIQPALDPSRSKSSSSNNSSHSPKVKEDLPHTAPSSCIMDKNAALQNGIFCN
Inhibitor
Name:
BDBM22225
Synonyms:
3-(3-methyl-4-{5-[4-(propan-2-yloxy)-3-(trifluoromethyl)phenyl]-1,2,4-oxadiazol-3-yl}phenyl)butanoic acid | 3-arylpropionic acid derivative, 7b
Type:
Small organic molecule
Emp. Form.:
C23H23F3N2O4
Mol. Mass.:
448.4349
SMILES:
CC(C)Oc1ccc(cc1C(F)(F)F)-c1nc(no1)-c1ccc(cc1C)C(C)CC(O)=O
Structure:
Substrate