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, Grapiprant, MR-10A7, MR10A7, RQ-00000007, RQ-7) |
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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 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]
