fevipiprant [Ligand Id: 8995] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3137332 (Fevipiprant, NVP-QAW039, QAW-039, QAW039) |
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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] | ||||||||
| GtoPdb | - | - | 8.99 | pKd | 1.02 | nM | Kd |
Eur Respir J (2014) 44: 4074; Mol Pharmacol (2016) 89: 593-605 [PMID:26916831] |
| ChEMBL | Displacement of [3H]NVP-QAW039 from human DP2 receptor expressed in CHO cell membranes by TopCount scintillation assay | B | 8.99 | pKd | 1.02 | nM | Kd | ACS Med Chem Lett (2017) 8: 582-586 [PMID:28523115] |
| ChEMBL | Displacement of [3H]-PGD2 from human CRTh2 expressed in CHO-K1 cell membranes incubated for 1 hr by SPA binding assay | B | 8.4 | pKi | 4 | nM | Ki | US-7666878-B2. Pyrrolopyridine derivatives and their use as Crth2 antagonists (2010) |
| ChEMBL | Displacement of [3H]PGD2 from human DP2 receptor expressed in CHO cell membranes after 60 mins by scintillation proximity assay | B | 8.4 | pKi | 4 | nM | Ki | ACS Med Chem Lett (2017) 8: 582-586 [PMID:28523115] |
| ChEMBL | Antagonist activity against human CRTh2 expressed in CHO-K1 cells assessed as inhibition of PGD2-mediated attenuation of forskolin-induced cAMP accumulation incubated for 60 mins by scintillation counting method | F | 7.72 | pIC50 | 19 | nM | IC50 | US-7666878-B2. Pyrrolopyridine derivatives and their use as Crth2 antagonists (2010) |
| ChEMBL | Antagonist activity at DP2 receptor in CD4-positive human TH2 cells assessed as inhibition of PGD2-induced IL-4 production preincubated for 30 mins followed by PGD2 addition measured after 6 hrs | B | 8.51 | pIC50 | 3.1 | nM | IC50 | ACS Med Chem Lett (2017) 8: 582-586 [PMID:28523115] |
| ChEMBL | Antagonist activity at DP2 receptor in CD4-positive human TH2 cells assessed as inhibition of DK-PGD2-induced IL-5 production after 6 to 8 hrs | B | 8.59 | pIC50 | 2.6 | nM | IC50 | ACS Med Chem Lett (2017) 8: 582-586 [PMID:28523115] |
| ChEMBL | Antagonist activity at DP2 receptor in CD4-positive human TH2 cells assessed as inhibition of DK-PGD2-induced IL-13 production after 6 to 8 hrs | B | 8.85 | pIC50 | 1.4 | nM | IC50 | ACS Med Chem Lett (2017) 8: 582-586 [PMID:28523115] |
| ChEMBL | Antagonist activity at DP2 receptor in human whole assessed as inhibition of DK-PGD2-induced eosinophils shape change preincubated for 5 mins followed by DK-PGD2 addition measured after 5 mins by flow cytometry | B | 9.4 | pIC50 | 0.4 | nM | IC50 | ACS Med Chem Lett (2017) 8: 582-586 [PMID:28523115] |
| ChEMBL | Antagonist activity at DP2 receptor in human isolated eosinophils assessed as inhibition of DK-PGD2-induced shape change preincubated for 5 mins followed by DK-PGD2 addition measured after 5 mins by flow cytometry | B | 9.4 | pIC50 | 0.4 | nM | IC50 | ACS Med Chem Lett (2017) 8: 582-586 [PMID:28523115] |
| DP1 receptor/Prostanoid DP receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4427] [GtoPdb: 338] [UniProtKB: Q13258] | ||||||||
| ChEMBL | Antagonist activity at DP1 receptor (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | ACS Med Chem Lett (2017) 8: 582-586 [PMID:28523115] |
| EP2 receptor/Prostanoid EP2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1881] [GtoPdb: 341] [UniProtKB: P43116] | ||||||||
| ChEMBL | Antagonist activity at EP2 receptor (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | ACS Med Chem Lett (2017) 8: 582-586 [PMID:28523115] |
| EP3 receptor/Prostanoid EP3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3710] [GtoPdb: 342] [UniProtKB: P43115] | ||||||||
| ChEMBL | Antagonist activity at EP3 receptor (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | ACS Med Chem Lett (2017) 8: 582-586 [PMID:28523115] |
| ChEMBL | Agonist activity at EP3 receptor (unknown origin) | B | 5 | pEC50 | >10000 | nM | EC50 | ACS Med Chem Lett (2017) 8: 582-586 [PMID:28523115] |
| EP4 receptor/Prostanoid EP4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1836] [GtoPdb: 343] [UniProtKB: P35408] | ||||||||
| ChEMBL | Antagonist activity at EP4 receptor (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | ACS Med Chem Lett (2017) 8: 582-586 [PMID:28523115] |
| FP receptor/Prostanoid FP receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1987] [GtoPdb: 344] [UniProtKB: P43088] | ||||||||
| ChEMBL | Antagonist activity at FP receptor (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | ACS Med Chem Lett (2017) 8: 582-586 [PMID:28523115] |
| IP receptor/Prostanoid IP receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1995] [GtoPdb: 345] [UniProtKB: P43119] | ||||||||
| ChEMBL | Antagonist activity at IP receptor (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | ACS Med Chem Lett (2017) 8: 582-586 [PMID:28523115] |
| ChEMBL | Agonist activity at IP receptor (unknown origin) | B | 5 | pEC50 | >10000 | nM | EC50 | ACS Med Chem Lett (2017) 8: 582-586 [PMID:28523115] |
| TP receptor/Thromboxane A2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2069] [GtoPdb: 346] [UniProtKB: P21731] | ||||||||
| ChEMBL | Antagonist activity at TP receptor (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | ACS Med Chem Lett (2017) 8: 582-586 [PMID:28523115] |
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]
