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 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]
