Reaction Details |
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Target | Sphingosine 1-phosphate receptor 2 |
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Ligand | BDBM50585280 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_2161846 (CHEMBL5046707) |
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IC50 | 3.4±n/a nM |
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Citation | Mammoliti, O; Jansen, K; El Bkassiny, S; Palisse, A; Triballeau, N; Bucher, D; Allart, B; Jaunet, A; Tricarico, G; De Wachter, M; Menet, C; Blanc, J; Letfus, V; Rup?i?, R; ?mehil, M; Poljak, T; Coornaert, B; Sonck, K; Duys, I; Waeckel, L; Lecru, L; Marsais, F; Jagerschmidt, C; Auberval, M; Pujuguet, P; Oste, L; Borgonovi, M; Wakselman, E; Christophe, T; Houvenaghel, N; Jans, M; Heckmann, B; Sanière, L; Brys, R Discovery and Optimization of Orally Bioavailable Phthalazone and Cinnolone Carboxylic Acid Derivatives as S1P2 Antagonists against Fibrotic Diseases. J Med Chem64:14557-14586 (2021) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Sphingosine 1-phosphate receptor 2 |
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Name: | Sphingosine 1-phosphate receptor 2 |
Synonyms: | EDG5 | S1P2 | S1PR2 | S1PR2_HUMAN | Sphingosine 1-phosphate receptor | Sphingosine 1-phosphate receptor Edg-5 | Sphingosine-1-phosphate receptor 2 | ndothelial differentiation G-protein coupled receptor 5 |
Type: | G Protein-Coupled Receptor (GPCR) |
Mol. Mass.: | 38883.16 |
Organism: | Homo sapiens (Human) |
Description: | Membranes isolated from S1P2-transfected CHO cells were used in ligand binding assay. |
Residue: | 353 |
Sequence: | MGSLYSEYLNPNKVQEHYNYTKETLETQETTSRQVASAFIVILCCAIVVENLLVLIAVAR
NSKFHSAMYLFLGNLAASDLLAGVAFVANTLLSGSVTLRLTPVQWFAREGSAFITLSASV
FSLLAIAIERHVAIAKVKLYGSDKSCRMLLLIGASWLISLVLGGLPILGWNCLGHLEACS
TVLPLYAKHYVLCVVTIFSIILLAIVALYVRIYCVVRSSHADMAAPQTLALLKTVTIVLG
VFIVCWLPAFSILLLDYACPVHSCPILYKAHYFFAVSTLNSLLNPVIYTWRSRDLRREVL
RPLQCWRPGVGVQGRRRGGTPGHHLLPLRSSSSLERGMHMPTSPTFLEGNTVV
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BDBM50585280 |
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n/a |
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Name | BDBM50585280 |
Synonyms: | CHEMBL5090966 |
Type | Small organic molecule |
Emp. Form. | C24H21F3N4O4 |
Mol. Mass. | 486.4431 |
SMILES | CC(C(O)=O)c1nn(Cc2cn3cc(OCC4CC4)c(cc3n2)C(F)(F)F)c2ccccc2c1=O |
Structure |
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