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Target
Sphingosine 1-phosphate receptor 2
Ligand
BDBM50576242
Substrate
n/a
Meas. Tech.
ChEMBL_2126724 (CHEMBL4836069)
IC50
0.610000±n/a nM
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 Chem 64:6037-6058 (2021) [PubMed]  Article 
Target
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:
MGSLYSEYLNPNKVQEHYNYTKETLETQETTSRQVASAFIVILCCAIVVENLLVLIAVARNSKFHSAMYLFLGNLAASDLLAGVAFVANTLLSGSVTLRLTPVQWFAREGSAFITLSASVFSLLAIAIERHVAIAKVKLYGSDKSCRMLLLIGASWLISLVLGGLPILGWNCLGHLEACSTVLPLYAKHYVLCVVTIFSIILLAIVALYVRIYCVVRSSHADMAAPQTLALLKTVTIVLGVFIVCWLPAFSILLLDYACPVHSCPILYKAHYFFAVSTLNSLLNPVIYTWRSRDLRREVLRPLQCWRPGVGVQGRRRGGTPGHHLLPLRSSSSLERGMHMPTSPTFLEGNTVV
  
Inhibitor
Name:
BDBM50576242
Synonyms:
CHEMBL4850513
Type:
Small organic molecule
Emp. Form.:
C21H19Cl2N5O
Mol. Mass.:
428.314
SMILES:
Cc1nn(C)cc1-c1cnc(CNC(=O)c2cc3c(Cl)cc(Cl)cc3[nH]2)cc1C
Structure:
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