laropiprant [Ligand Id: 3356] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL426559 (Cordaptive, Laropiprant, MK-0524)
  • 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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  • FP receptor/Prostanoid FP receptor in Human [ChEMBL: CHEMBL1987] [GtoPdb: 344] [UniProtKB: P43088]
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  • IP receptor/Prostanoid IP receptor in Human [ChEMBL: CHEMBL1995] [GtoPdb: 345] [UniProtKB: P43119]
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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
DP2 receptor/G protein-coupled receptor 44 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5071] [GtoPdb: 339] [UniProtKB: Q9Y5Y4]
ChEMBL Activity at CRTH2 receptor B 6.13 pKi 745 nM Ki J. Med. Chem. (2007) 50: 794-806 [PMID:17300164]
DP1 receptor/Prostanoid DP receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4427] [GtoPdb: 338] [UniProtKB: Q13258]
ChEMBL Binding affinity to human DP receptor expressed in HEK293 cells B 10.52 pKd 0.03 nM Kd J. Med. Chem. (2007) 50: 794-806 [PMID:17300164]
ChEMBL Binding affinity to human DP receptor expressed in HEK293 cells B 9.24 pKi 0.57 nM Ki J. Med. Chem. (2007) 50: 794-806 [PMID:17300164]
ChEMBL Activity at human DP receptor in platelet rich plasma assessed as inhibition of PGD2-induced cAMP accumulation F 8.4 pIC50 4 nM IC50 J. Med. Chem. (2007) 50: 794-806 [PMID:17300164]
ChEMBL Activity at sheep DP receptor by PRP assay B 8.85 pIC50 1.4 nM IC50 J. Med. Chem. (2007) 50: 794-806 [PMID:17300164]
ChEMBL Activity at human DP receptor in washed platelets assessed as inhibition of PGD2-induced cAMP accumulation F 10.05 pIC50 0.09 nM IC50 J. Med. Chem. (2007) 50: 794-806 [PMID:17300164]
EP1 receptor/Prostanoid EP1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1811] [GtoPdb: 340] [UniProtKB: P34995]
ChEMBL Binding affinity to human EP1 receptor expressed in HEK293 cells B 5.94 pKi 1160 nM Ki J. Med. Chem. (2007) 50: 794-806 [PMID:17300164]
EP2 receptor/Prostanoid EP2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1881] [GtoPdb: 341] [UniProtKB: P43116]
ChEMBL Binding affinity to human EP2 receptor expressed in HEK293 cells B 6.87 pKi 136 nM Ki J. Med. Chem. (2007) 50: 794-806 [PMID:17300164]
EP3 receptor/Prostanoid EP3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3710] [GtoPdb: 342] [UniProtKB: P43115]
ChEMBL Binding affinity to human EP3 receptor expressed in HEK293 cells B 6.05 pKi 892 nM Ki J. Med. Chem. (2007) 50: 794-806 [PMID:17300164]
EP4 receptor/Prostanoid EP4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1836] [GtoPdb: 343] [UniProtKB: P35408]
ChEMBL Binding affinity to human EP4 receptor expressed in HEK293 cells B 4.82 pKi >15200 nM Ki J. Med. Chem. (2007) 50: 794-806 [PMID:17300164]
FP receptor/Prostanoid FP receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1987] [GtoPdb: 344] [UniProtKB: P43088]
ChEMBL Binding affinity to human FP receptor expressed in HEK293 cells B 5 pKi 9991 nM Ki J. Med. Chem. (2007) 50: 794-806 [PMID:17300164]
IP receptor/Prostanoid IP receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1995] [GtoPdb: 345] [UniProtKB: P43119]
ChEMBL Binding affinity to human IP receptor expressed in HEK293 cells B 5.18 pKi 6628 nM Ki J. Med. Chem. (2007) 50: 794-806 [PMID:17300164]
TP receptor/Thromboxane A2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2069] [GtoPdb: 346] [UniProtKB: P21731]
ChEMBL Binding affinity to human TP receptor expressed in HEK293 cells B 7.96 pKd 10.9 nM Kd J. Med. Chem. (2007) 50: 794-806 [PMID:17300164]
ChEMBL Binding affinity to human TP receptor expressed in HEK293 cells B 8.53 pKi 2.95 nM Ki J. Med. Chem. (2007) 50: 794-806 [PMID:17300164]
ChEMBL Activity at human TP receptor in platelet rich plasma assessed as inhibition U44619-induced platelet aggregation F 6.11 pIC50 770 nM IC50 J. Med. Chem. (2007) 50: 794-806 [PMID:17300164]

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]