QAV680 [Ligand Id: 8996] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2442750 (Nvp-qav-680, NVP-QAV680, Qav-680, Qav680, QAV680, Qav-690 free acid, QAV690 FREE ACID) |
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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 | Displacement of [3H]NVP-QAW039 from human DP2 receptor expressed in CHO cell membranes by TopCount scintillation assay | B | 7.82 | pKd | 15.14 | nM | Kd | ACS Med Chem Lett (2017) 8: 582-586 [PMID:28523115] |
| GtoPdb | - | - | 7.82 | pKd | 15.1 | nM | Kd | Eur Respir J (2014) 44: 4074 |
| ChEMBL | Displacement of [3H]-prostaglandin D2 from human CRTh2 receptor expressed in CHO cells after 2 hrs | B | 7.44 | pKi | 36 | nM | Ki | Bioorg Med Chem (2013) 21: 6582-6591 [PMID:24021582] |
| ChEMBL | Displacement of [3H]PGD2 from human DP2 receptor expressed in CHO cell membranes after 60 mins by scintillation proximity assay | B | 7.44 | pKi | 36 | nM | Ki | 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 | 7.54 | pKi | 29 | nM | Ki | US-7666878-B2. Pyrrolopyridine derivatives and their use as Crth2 antagonists (2010) |
| ChEMBL | Antagonist activity at CRTh2 receptor in human isolated eosinophil assessed as inhibition of eotaxin-induced shape change after 5 mins by flow cytometry | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem (2013) 21: 6582-6591 [PMID:24021582] |
| ChEMBL | Antagonist activity at CRTh2 receptor in human whole blood assessed as inhibition of PGD2-induced eosinophil shape change after 5 mins by flow cytometry | B | 6.99 | pIC50 | 102 | nM | IC50 | Bioorg Med Chem (2013) 21: 6582-6591 [PMID:24021582] |
| 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 | 7.23 | pIC50 | 59 | nM | IC50 | ACS Med Chem Lett (2017) 8: 582-586 [PMID:28523115] |
| ChEMBL | Antagonist activity at human CRTh2 receptor expressed in CHO cells assessed as inhibition of prostaglandin D2 and forskolin-induced cAMP accumulation after 45 mins | F | 7.43 | pIC50 | 37 | nM | IC50 | Bioorg Med Chem (2013) 21: 6582-6591 [PMID:24021582] |
| ChEMBL | Antagonist activity at CRTh2 receptor in human whole blood assessed as inhibition of DK-PGD2-induced eosinophil shape change after 5 mins by flow cytometry | B | 7.51 | pIC50 | 31 | nM | IC50 | Bioorg Med Chem (2013) 21: 6582-6591 [PMID:24021582] |
| 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 | 7.51 | pIC50 | 31 | 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 | 7.6 | pIC50 | 25 | nM | IC50 | 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 | 7.68 | pIC50 | 21 | nM | IC50 | US-7666878-B2. Pyrrolopyridine derivatives and their use as Crth2 antagonists (2010) |
| ChEMBL | Antagonist activity at CRTh2 receptor in human isolated eosinophil assessed as inhibition of DK-PGD2-induced shape change after 5 mins by flow cytometry | B | 8.3 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem (2013) 21: 6582-6591 [PMID:24021582] |
| 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 | 8.3 | pIC50 | 5 | nM | IC50 | ACS Med Chem Lett (2017) 8: 582-586 [PMID:28523115] |
| ChEMBL | Antagonist activity at CRTh2 receptor in human isolated eosinophil assessed as inhibition of 11-Dehydro-TXB2-induced shape change after 5 mins by flow cytometry | B | 8.4 | pIC50 | 4 | nM | IC50 | Bioorg Med Chem (2013) 21: 6582-6591 [PMID:24021582] |
| ChEMBL | Antagonist activity at CRTh2 receptor in human isolated eosinophil assessed as inhibition of delta12-PGD2-induced shape change after 5 mins by flow cytometry | B | 8.4 | pIC50 | 4 | nM | IC50 | Bioorg Med Chem (2013) 21: 6582-6591 [PMID:24021582] |
| ChEMBL | Antagonist activity at CRTh2 receptor in human isolated eosinophil assessed as inhibition of delta12-PGJ2-induced shape change after 5 mins by flow cytometry | B | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem (2013) 21: 6582-6591 [PMID:24021582] |
| DP2 receptor/G protein-coupled receptor 44 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2291] [GtoPdb: 339] [UniProtKB: Q9Z2J6] | ||||||||
| ChEMBL | Displacement of [3H]-prostaglandin D2 from mouse CRTh2 receptor expressed in CHO cells after 2 hrs | B | 8 | pKi | 10 | nM | Ki | Bioorg Med Chem (2013) 21: 6582-6591 [PMID:24021582] |
| ChEMBL | Antagonist activity at mouse CRTh2 receptor expressed in CHO-K1 cells assessed as inhibition of [125S]-GTP-gamma-S binding after 50 mins by liquid scintillation counting | F | 7.03 | pIC50 | 94 | nM | IC50 | Bioorg Med Chem (2013) 21: 6582-6591 [PMID:24021582] |
| DP1 receptor/Prostanoid DP receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4427] [GtoPdb: 338] [UniProtKB: Q13258] | ||||||||
| ChEMBL | Inhibition of prostanoid DP1 receptor (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem (2013) 21: 6582-6591 [PMID:24021582] |
| EP2 receptor/Prostanoid EP2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1881] [GtoPdb: 341] [UniProtKB: P43116] | ||||||||
| ChEMBL | Inhibition of prostanoid EP2 receptor (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem (2013) 21: 6582-6591 [PMID:24021582] |
| EP3 receptor/Prostanoid EP3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3710] [GtoPdb: 342] [UniProtKB: P43115] | ||||||||
| ChEMBL | Inhibition of prostanoid EP3 receptor (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem (2013) 21: 6582-6591 [PMID:24021582] |
| EP4 receptor/Prostanoid EP4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1836] [GtoPdb: 343] [UniProtKB: P35408] | ||||||||
| ChEMBL | Inhibition of prostanoid EP4 receptor (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem (2013) 21: 6582-6591 [PMID:24021582] |
| FP receptor/Prostanoid FP receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1987] [GtoPdb: 344] [UniProtKB: P43088] | ||||||||
| ChEMBL | Inhibition of prostanoid FP receptor (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem (2013) 21: 6582-6591 [PMID:24021582] |
| IP receptor/Prostanoid IP receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1995] [GtoPdb: 345] [UniProtKB: P43119] | ||||||||
| ChEMBL | Inhibition of prostanoid IP receptor (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem (2013) 21: 6582-6591 [PMID:24021582] |
| TP receptor/Thromboxane A2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2069] [GtoPdb: 346] [UniProtKB: P21731] | ||||||||
| ChEMBL | Inhibition of prostanoid TP receptor (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem (2013) 21: 6582-6591 [PMID:24021582] |
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]
