grapiprant [Ligand Id: 5858] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3039498 (423, AAT-007, CJ-023, Cj-023,423, CJ 023423, CJ-023423, Galliprant, Grapiprant, MR-10A7, MR10A7, RQ-00000007, RQ-7)
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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]
  • EP4 receptor/Prostanoid EP4 receptor in Mouse [ChEMBL: CHEMBL2489] [GtoPdb: 343] [UniProtKB: P32240]
  • EP4 receptor/Prostanoid EP4 receptor in Rat [ChEMBL: CHEMBL4086] [GtoPdb: 343] [UniProtKB: P43114]
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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
Prostaglandin E receptor 4 in Dog (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105910] [UniProtKB: Q9TU16]
ChEMBL Antagonist activity at dog recombinant EP4 receptor B 7.62 pKi 24 nM Ki Bioorg Med Chem Lett (2017) 27: 1186-1192 [PMID:28169162]
EP1 receptor/Prostanoid EP1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1811] [GtoPdb: 340] [UniProtKB: P34995]
ChEMBL Antagonist activity at human EP1 receptor B 5.3 pKi >5000 nM Ki Bioorg Med Chem Lett (2017) 27: 1186-1192 [PMID:28169162]
EP2 receptor/Prostanoid EP2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1881] [GtoPdb: 341] [UniProtKB: P43116]
ChEMBL Antagonist activity at human EP2 receptor B 5.3 pKi >5000 nM Ki Bioorg Med Chem Lett (2017) 27: 1186-1192 [PMID:28169162]
EP3 receptor/Prostanoid EP3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3710] [GtoPdb: 342] [UniProtKB: P43115]
ChEMBL Antagonist activity at human EP3 receptor B 5.3 pKi >5000 nM Ki Bioorg Med Chem Lett (2017) 27: 1186-1192 [PMID:28169162]
EP4 receptor/Prostanoid EP4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1836] [GtoPdb: 343] [UniProtKB: P35408]
ChEMBL Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay F 8.32 pKd 4.79 nM Kd Bioorg Med Chem Lett (2017) 27: 1186-1192 [PMID:28169162]
ChEMBL Displacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis B 6.35 pKi 449 nM Ki Bioorg Med Chem Lett (2015) 25: 3176-3178 [PMID:26091726]
ChEMBL Antagonist activity at human EP4 receptor B 6.35 pKi 448 nM Ki Bioorg Med Chem Lett (2016) 26: 105-109 [PMID:26608552]
ChEMBL Displacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranes B 7.89 pKi 13 nM Ki Bioorg Med Chem Lett (2017) 27: 1186-1192 [PMID:28169162]
GtoPdb - - 7.89 pKi 13 nM Ki J Pharmacol Exp Ther (2007) 322: 686-94 [PMID:17495127]
ChEMBL Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISA B 5.79 pIC50 1614 nM IC50 Bioorg Med Chem Lett (2015) 25: 3176-3178 [PMID:26091726]
ChEMBL Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassay B 5.8 pIC50 1600 nM IC50 Bioorg Med Chem Lett (2016) 26: 931-935 [PMID:26764191]
ChEMBL Antagonist activity at EP4 receptor in human whole blood assessed as reversal of inhibition of PGE2 mediated LPS-induced TNF alpha production pretreated for 30 mins using 3,3',5,5' tetramethylbiphenyl-4,4'-diamine substrate measured after 20 to 24 hrs by immunoassay B 5.82 pIC50 1520 nM IC50 Bioorg Med Chem Lett (2016) 26: 105-109 [PMID:26608552]
ChEMBL Antagonist activity against EP4 in human whole blood assessed as reversal of PGE2-mediated suppression of LPS-induced TNF-alpha production preincubated for 30 mins followed by LPS stimulation measured after 20 to 24 hrs by enzyme immunoassay B 5.82 pIC50 1520 nM IC50 Bioorg Med Chem Lett (2016) 26: 2303-2307 [PMID:27020304]
ChEMBL Displacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis B 6.16 pIC50 689 nM IC50 Bioorg Med Chem Lett (2015) 25: 3176-3178 [PMID:26091726]
ChEMBL Antagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMP F 7.93 pIC50 11.7 nM IC50 Bioorg Med Chem Lett (2015) 25: 3176-3178 [PMID:26091726]
ChEMBL Antagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assay F 7.93 pIC50 11.7 nM IC50 Bioorg Med Chem Lett (2016) 26: 2303-2307 [PMID:27020304]
ChEMBL Antagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation F 7.93 pIC50 11.7 nM IC50 Bioorg Med Chem Lett (2016) 26: 105-109 [PMID:26608552]
EP4 receptor/Prostanoid EP4 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2489] [GtoPdb: 343] [UniProtKB: P32240]
ChEMBL Antagonist activity at mouse recombinant EP4 receptor assessed as inhibition of PGE2-induced cAMP level by cell based assay F 8.11 pKd 7.76 nM Kd Bioorg Med Chem Lett (2017) 27: 1186-1192 [PMID:28169162]
EP4 receptor/Prostanoid EP4 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4086] [GtoPdb: 343] [UniProtKB: P43114]
ChEMBL Antagonist activity at rat recombinant EP4 receptor assessed as inhibition of PGE2-induced cAMP level by cell based assay F 8.19 pKd 6.46 nM Kd Bioorg Med Chem Lett (2017) 27: 1186-1192 [PMID:28169162]
ChEMBL Antagonist activity at rat recombinant EP4 receptor B 7.7 pKi 20 nM Ki Bioorg Med Chem Lett (2017) 27: 1186-1192 [PMID:28169162]
FP receptor/Prostanoid FP receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1987] [GtoPdb: 344] [UniProtKB: P43088]
ChEMBL Antagonist activity at human FP receptor B 5.3 pKi >5000 nM Ki Bioorg Med Chem Lett (2017) 27: 1186-1192 [PMID:28169162]
IP receptor/Prostanoid IP receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1995] [GtoPdb: 345] [UniProtKB: P43119]
ChEMBL Antagonist activity at human IP receptor B 5.3 pKi >5000 nM Ki Bioorg Med Chem Lett (2017) 27: 1186-1192 [PMID:28169162]
TP receptor/Thromboxane A2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2069] [GtoPdb: 346] [UniProtKB: P21731]
ChEMBL Antagonist activity at human platelet TP receptor B 5.3 pKi >5000 nM Ki Bioorg Med Chem Lett (2017) 27: 1186-1192 [PMID:28169162]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]