Ligand Id: 1881
Ligand name PGD2

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 5
Hydrogen bond donors 3
Rotatable bonds 12
Topological polar surface area 94.83
Molecular weight 352.22
XLogP 2.9
No. Lipinski's rules broken 1

Molecular properties generated using the CDK


Summary Biological activity References Structure Similar ligands Radio analogues
References
1. Wright, D. H., Nantel, F., Metters, K. M. and Ford-Hutchinson, A. W. (1999)
A novel biological role for prostaglandin D2 is suggested by distribution studies of the rat DP prostanoid receptor.
Eur J Pharmacol377: 101-115. [PMID:10448933]
2. Boie, Y., Sawyer, N., Slipetz, D. M., Metters, K. M. and Abramovitz, M. (1995)
Molecular cloning and characterization of the human prostanoid DP receptor.
J. Biol. Chem.270: 18910-18916. [PMID:7642548]
3. Wright, D. H., Metters, K. M., Abramovitz, M. and Ford-Hutchinson, A. W. (1998)
Characterization of the recombinant human prostaglandin DP-receptor identifies L-644,698 a novel, DP-selective agonist.
Br. J. Pharmacol.123: 1317-1324. [PMID:9579725]
4. Kiriyama, M., Ushikubi, F., Kobayashi, T., Hirata, M., Sugimoto, Y. and Narumiya, S. (1997)
Ligand binding specificities of the eight types and subtypes of the mouse prostanoid receptors expressed in Chinese hamster ovary cells.
Br. J. Pharmacol.122: 217-224. [PMID:9313928]
5. Wilson, R. J., Giblin, G. M., Roomans, S., Rhodes, S. A., Cartwright, K. A., Shield, V. J., Brown, J., Wise, A., Chowdhury, J., Pritchard, S., Coote, J., Noel, L. S., Kenakin, T., Burns-Kurtis, C. L., Morrison, V., Gray, D. W. and Giles, H. (2006)
GW627368X ((N-{2-[4-(4,9-diethoxy-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl)phenyl]acetyl} benzene sulphonamide): a novel, potent and selective prostanoid EP4 receptor antagonist.
Br J Pharmacol148: 326-339. [PMID:16604093]
6. Shichijo, M., Sugimoto, H., Nagao, K., Inbe, H., Encinas, J. A., Takeshita, K., Bacon, K. B. and Gantner, F. (2003)
Chemoattractant receptor-homologous molecule expressed on Th2 cells activation in vivo increases blood leukocyte counts and its blockade abrogates 13,14-dihydro-15-keto-prostaglandin D2-induced eosinophilia in rats.
J Pharmacol Exp Ther307: 518-525. [PMID:12975488]
7. Hata, A. N., Zent, R., Breyer, M. D. and Breyer, R. M. (2003)
Expression and molecular pharmacology of the mouse CRTH2 receptor.
J Pharmacol Exp Ther306: 463-470. [PMID:12721327]
8. Sawyer, N., Cauchon, E., Chateauneuf, A., Cruz, R. P., Nicholson, D. W., Metters, K. M., O'Neill, G. P. and Gervais, F. G. (2002)
Molecular pharmacology of the human prostaglandin D2 receptor, CRTH2.
Br J Pharmacol137: 1163-1172. [PMID:12466225]
9. Sugimoto, H., Shichijo, M., Okano, M. and Bacon, K. B. (2005)
CRTH2-specific binding characteristics of [3H]ramatroban and its effects on PGD2-, 15-deoxy-Delta12, 14-PGJ2- and indomethacin-induced agonist responses.
Eur J Pharmacol524: 30-37. [PMID:16256979]
10. Hata, A. N., Lybrand, T. P. and Breyer, R. M. (2005)
Identification of determinants of ligand binding affinity and selectivity in the prostaglandin D2 receptor CRTH2.
J Biol Chem280: 32442-32451. [PMID:16030019]
11. Boie, Y., Stocco, R., Sawyer, N., Slipetz, D. M., Ungrin, M. D., Neuschafer-Rube, F., Puschel, G. P., Metters, K. M. and Abramovitz, M. (1997)
Molecular cloning and characterisation of the four rat prostaglandin E2 prostanoid receptor subtypes.
Eur. J. Pharmacol.304: 227-241. [PMID:9537820]
12. Sharif, N. A. and Davis, T. L. (2002)
Cloned human EP1 prostanoid receptor pharmacology characterized using radioligand binding techniques.
J Pharm Pharmacol54: 539-547. [PMID:11999132]
13. Stillman, B. A., Breyer, M. D. and Breyer, R. M. (1999)
Importance of the extracellular domain for prostaglandin EP(2) receptor function.
Mol Pharmacol56: 545-551. [PMID:10462542]
14. Davis, T. L. and Sharif, N. A. (2000)
Pharmacological characterization of [(3)H]-prostaglandin E(2) binding to the cloned human EP(4) prostanoid receptor.
Br J Pharmacol130: 1919-1926. [PMID:10952683]
15. Neuschäfer-Rube, F., Engemaier, E., Koch, S., Böer, U. and Püschel, G. P. (2003)
Identification by site-directed mutagenesis of amino acids contributing to ligand-binding specificity or signal transduction properties of the human FP prostanoid receptor.
Biochem J371: 443-449. [PMID:12519077]
16. Leduc, M; Breton, B; Galés, C; Le Gouill, C; Bouvier, M; Chemtob, S; Heveker, N. (2009)
Functional selectivity of natural and synthetic prostaglandin EP4 receptor ligands.
J. Pharmacol. Exp. Ther.331 (1): 297-307. [PMID:19584306]