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ChEMBL ligand: CHEMBL3342693 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
ChEMBL | Inhibition of human ERG | B | 4.38 | pKi | 41300 | nM | Ki | J Med Chem (2016) 59: 194-205 [PMID:26653180] |
ChEMBL | Inhibition of human ERG | B | 4.08 | pIC50 | 82600 | nM | IC50 | J Med Chem (2016) 59: 194-205 [PMID:26653180] |
mPGES1/Prostaglandin E synthase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5658] [GtoPdb: 1377] [UniProtKB: O14684] | ||||||||
ChEMBL | Inhibition of mPGES-1 in human A549 cells assessed as PEG2 formation preincubated for 30 mins followed by recombinant human interleukin 1beta addition measured after 18 hrs by LC/MS analysis | B | 7.92 | pIC50 | 12 | nM | IC50 | J Med Chem (2016) 59: 5970-5986 [PMID:26791385] |
ChEMBL | Inhibition of mPGES-1 in human A549 cells assessed as inhibition of IL-1beta-induced PGE2 production incubated for 30 mins prior to IL-1beta challenge measured after 18 hrs by plate reader analysis | B | 7.92 | pIC50 | 12 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 4838-4844 [PMID:25260492] |
ChEMBL | Inhibition of mPGES-1 in human whole blood assessed as inhibition of LPS-induced PGE2 production incubated for 30 mins prior to LPS challenge measured after 20 to 24 hrs by LC/MS/MS analysis | B | 7.92 | pIC50 | 12 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 4838-4844 [PMID:25260492] |
ChEMBL | Inhibition of mPGES1 in LPS-induced human whole blood assessed as suppression of PGE2 response after 20 to 24 hrs by LC-MS/MS analysis | B | 7.92 | pIC50 | 12 | nM | IC50 | J Med Chem (2016) 59: 194-205 [PMID:26653180] |
ChEMBL | Inhibition of mPGES-1 in human whole blood cells assessed as PEG2 formation by LC/MS analysis | B | 7.92 | pIC50 | 12 | nM | IC50 | J Med Chem (2016) 59: 5970-5986 [PMID:26791385] |
ChEMBL | Inhibition of mPGES1 in rhIL-1beta-stimulated human A549 cells assessed as PGE2 level treated for 18 hrs after 30 mins pre-incubation with rhIL-1beta by EIA method | B | 7.92 | pIC50 | 12 | nM | IC50 | J Med Chem (2016) 59: 194-205 [PMID:26653180] |
ChEMBL | Inhibition of human mPGES-1 expressed in 293E cell microsomes using PGH2 substrate by LC/MS analysis1 | B | 9.03 | pIC50 | 0.94 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 4838-4844 [PMID:25260492] |
GtoPdb | Potency for inhibition of human mPGES-1 expressed in 293E cell microsomes | - | 9.03 | pIC50 | 0.94 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 4838-44 [PMID:25260492] |
ChEMBL | Inhibition of human microsomal PGES1 expressed in 293E cells by LC/MS/MS analysis | B | 9.05 | pIC50 | 0.9 | nM | IC50 | J Med Chem (2016) 59: 194-205 [PMID:26653180] |
Prostaglandin E synthase in Dog (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3341581] [UniProtKB: A0SYQ0] | ||||||||
ChEMBL | Inhibition of mPGES1 in LPS-induced dog whole blood assessed as suppression of PGE2 response pre-incubated for 30 mins followed by LPS addition and measured after 5 hrs by LC-MS/MS analysis | B | 6.86 | pIC50 | 139 | nM | IC50 | J Med Chem (2016) 59: 194-205 [PMID:26653180] |
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]