setipiprant [Ligand Id: 10180] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2386081 (ACT-129968, KYTH-105, Setipiprant)
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  • DP2 receptor/G protein-coupled receptor 44 in Human [ChEMBL: CHEMBL5071] [GtoPdb: 339] [UniProtKB: Q9Y5Y4]
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  • DP1 receptor/Prostanoid DP receptor in Human [ChEMBL: CHEMBL4427] [GtoPdb: 338] [UniProtKB: Q13258]
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  • EP1 receptor/Prostanoid EP1 receptor in Human [ChEMBL: CHEMBL1811] [GtoPdb: 340] [UniProtKB: P34995]
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  • EP2 receptor/Prostanoid EP2 receptor in Human [ChEMBL: CHEMBL1881] [GtoPdb: 341] [UniProtKB: P43116]
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  • EP3 receptor/Prostanoid EP3 receptor in Human [ChEMBL: CHEMBL3710] [GtoPdb: 342] [UniProtKB: P43115]
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  • EP4 receptor/Prostanoid EP4 receptor in Human [ChEMBL: CHEMBL1836] [GtoPdb: 343] [UniProtKB: P35408]
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  • TP receptor/Thromboxane A2 receptor in Human [ChEMBL: CHEMBL2069] [GtoPdb: 346] [UniProtKB: P21731]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Cyclooxygenase-1 in Sheep (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2949] [UniProtKB: P05979]
ChEMBL Antagonist activity at ovine COX-1 B 5 pIC50 >10000 nM IC50 J Med Chem (2013) 56: 4899-4911 [PMID:23721423]
DP2 receptor/G protein-coupled receptor 44 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5071] [GtoPdb: 339] [UniProtKB: Q9Y5Y4]
ChEMBL Displacement of [3H]PGD2 from recombinant human CRTH2 receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting analysis in presence of human serum albumin B 6.47 pIC50 340 nM IC50 J Med Chem (2013) 56: 4899-4911 [PMID:23721423]
ChEMBL Antagonist activity at CRTH2 receptor in human eosinophils assessed as inhibition of PGD2-induced cell shape change incubated for 1 hr prior to PGD2 induction measured after 5 mins by FACS flow cytometric analysis in presence of human plasma B 6.63 pIC50 235 nM IC50 J Med Chem (2013) 56: 4899-4911 [PMID:23721423]
ChEMBL Antagonist activity at human CRTH2 receptor expressed in HEK293 cells assessed as inhibition of PGD2/forskolin-induced intracellular cAMP production after 20 mins by ELISA F 7.1 pIC50 80 nM IC50 J Med Chem (2013) 56: 4899-4911 [PMID:23721423]
ChEMBL Antagonist activity at human CRTH2 receptor expressed in HEK293 cells assessed as inhibition of PGD2-induced calcium flux after 5 mins by FLIPR assay F 7.52 pIC50 30 nM IC50 J Med Chem (2013) 56: 4899-4911 [PMID:23721423]
GtoPdb - - 8.22 pIC50 6 nM IC50 J Med Chem (2013) 56: 4899-911 [PMID:23721423]
ChEMBL Displacement of [3H]PGD2 from recombinant human CRTH2 receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting analysis B 8.22 pIC50 6 nM IC50 J Med Chem (2013) 56: 4899-4911 [PMID:23721423]
DP1 receptor/Prostanoid DP receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4427] [GtoPdb: 338] [UniProtKB: Q13258]
ChEMBL Displacement of [3H]PGD2 from recombinant human prostanoid DP1 receptor expressed in CHO cells after 90 mins by scintillation counting analysis B 5.89 pIC50 1290 nM IC50 J Med Chem (2013) 56: 4899-4911 [PMID:23721423]
EP1 receptor/Prostanoid EP1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1811] [GtoPdb: 340] [UniProtKB: P34995]
ChEMBL Antagonist activity at human prostanoid EP1 receptor expressed in CHOK1 cells assessed as inhibition of PGE2-induced calcium flux after 60 mins by FLIPR assay F 4.6 pIC50 >25000 nM IC50 J Med Chem (2013) 56: 4899-4911 [PMID:23721423]
EP2 receptor/Prostanoid EP2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1881] [GtoPdb: 341] [UniProtKB: P43116]
ChEMBL Inhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assay B 5.59 pIC50 2600 nM IC50 J Med Chem (2013) 56: 4899-4911 [PMID:23721423]
EP3 receptor/Prostanoid EP3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3710] [GtoPdb: 342] [UniProtKB: P43115]
ChEMBL Antagonist activity at human prostanoid EP3 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced calcium flux after 60 mins by FLIPR assay F 4.6 pIC50 >25000 nM IC50 J Med Chem (2013) 56: 4899-4911 [PMID:23721423]
EP4 receptor/Prostanoid EP4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1836] [GtoPdb: 343] [UniProtKB: P35408]
ChEMBL Inhibition of beta-arrestin binding to recombinant human prostanoid EP4 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assay B 5 pIC50 >10000 nM IC50 J Med Chem (2013) 56: 4899-4911 [PMID:23721423]
ChEMBL Displacement of [3H]PGE2 from recombinant human prostanoid EP4 receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting analysis B 5 pIC50 >10000 nM IC50 J Med Chem (2013) 56: 4899-4911 [PMID:23721423]
TP receptor/Thromboxane A2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2069] [GtoPdb: 346] [UniProtKB: P21731]
ChEMBL Antagonist activity at human prostanoid TP2 receptor expressed in HEK293 cells assessed as inhibition of calcium flux after 30 to 40 mins by FLIPR assay F 4.6 pIC50 >25000 nM IC50 J Med Chem (2013) 56: 4899-4911 [PMID:23721423]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]