asapiprant [Ligand Id: 11951] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3545043 (S-555739, Asapiprant)
  • DP1 receptor/Prostanoid DP receptor in Human [ChEMBL: CHEMBL4427] [GtoPdb: 338] [UniProtKB: Q13258]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
DP1 receptor/Prostanoid DP receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4427] [GtoPdb: 338] [UniProtKB: Q13258]
ChEMBL Displacement of [3H]-PGD2 from PGD2 receptor in human platelet membranes after 2 hrs by micro beta scintillation counting analysis B 6.62 pKi 240 nM Ki US-8153793-B2. Sulfonamide derivative having PGD2 receptor antagonistic activity (2012)
GtoPdb Displacement of [3H]-PGD2 from DP receptor in human platelet membranes - 6.62 pKi 240 nM Ki US8153793B2. Sulfonamide derivative having PGD2 receptor antagonistic activity (2012)
ChEMBL Antagonist activity at PGD2 receptor in human platelets assessed as inhibition of PGD2-mediated cAMP accumulation preincubated for 5 mins followed by PGD2 addition measured after 2 mins by HTRF assay B 6.28 pIC50 520 nM IC50 US-8153793-B2. Sulfonamide derivative having PGD2 receptor antagonistic activity (2012)

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]