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 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]
