Reaction Details |
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Target | Sphingosine 1-phosphate receptor 2 |
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Ligand | BDBM50576227 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_2126722 (CHEMBL4836067) |
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IC50 | 5.3±n/a nM |
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Citation | Mammoliti, O; Palisse, A; Joannesse, C; El Bkassiny, S; Allart, B; Jaunet, A; Menet, C; Coornaert, B; Sonck, K; Duys, I; Clément-Lacroix, P; Oste, L; Borgonovi, M; Wakselman, E; Christophe, T; Houvenaghel, N; Jans, M; Heckmann, B; Sanière, L; Brys, R Discovery of the S1P2 Antagonist GLPG2938 (1-[2-Ethoxy-6-(trifluoromethyl)-4-pyridyl]-3-[[5-methyl-6-[1-methyl-3-(trifluoromethyl)pyrazol-4-yl]pyridazin-3-yl]methyl]urea), a Preclinical Candidate for the Treatment of Idiopathic Pulmonary Fibrosis. J Med Chem64:6037-6058 (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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BDBM50576227 |
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n/a |
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Name | BDBM50576227 |
Synonyms: | CHEMBL4871414 |
Type | Small organic molecule |
Emp. Form. | C14H16Cl2N6O |
Mol. Mass. | 355.222 |
SMILES | CN(C)c1cnc(NNC(=O)Nc2cc(Cl)nc(Cl)c2)cc1C |
Structure |
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