AR-9281 [Ligand Id: 13112] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL436774 (Ar9281) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| epoxide hydrolase 2/Epoxide hydratase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2409] [GtoPdb: 2970] [UniProtKB: P34913] | ||||||||
| ChEMBL | Binding affinity to purified recombinant human sEH by FRET-displacement assay | B | 7.71 | pKi | 19.5 | nM | Ki | J Med Chem (2021) 64: 1856-1872 [PMID:33550801] |
| ChEMBL | Inhibition of soluble epoxide hydrolase in HUVEC assessed inhibition of as conversion of 14, 15-EET to 14, 15-DHET | B | 7.24 | pIC50 | 57 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 983-988 [PMID:21211973] |
| ChEMBL | Inhibition of human sEH by fluorescent assay | B | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (2007) 50: 3825-3840 [PMID:17616115] |
| ChEMBL | Inhibition of human recombinant sEH using PHOME as substrate measured after 10 mins by fluorescent based assay | B | 7.86 | pIC50 | 13.8 | nM | IC50 | Eur J Med Chem (2021) 223: 113678-113678 [PMID:34218083] |
| ChEMBL | Inhibition of human recombinant sEH using CMNPC as substrate incubated for 5 mins by fluorescent based assay | B | 8.1 | pIC50 | 8 | nM | IC50 | J Med Chem (2021) 64: 5429-5446 [PMID:33945278] |
| ChEMBL | Inhibition of human soluble epoxide hydrolase | B | 8.1 | pIC50 | 8 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 983-988 [PMID:21211973] |
| ChEMBL | Inhibition of recombinant human liver soluble epoxide hydrolase expressed in baculovirus infected Sf21 cells using NEPC as substrate by fluorescence based assay | B | 8.1 | pIC50 | 8 | nM | IC50 | Bioorg Med Chem (2019) 27: 115078-115078 [PMID:31488357] |
| ChEMBL | Inhibition of recombinant human soluble epoxide hydrolase using CMNPC as substrate preincubated for 5 mins followed by substrate addition and measured at 30 secs interval for 10 mins by fluorescence assay | B | 8.1 | pIC50 | 8 | nM | IC50 | J Med Chem (2020) 63: 9237-9257 [PMID:32787085] |
| GtoPdb | - | - | 8.1 | pIC50 | 8 | nM | IC50 | J Med Chem (2020) 63: 9237-9257 [PMID:32787085] |
| GtoPdb | - | - | 8.15 | pIC50 | 7 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 5212-6 [PMID:16870439] |
| ChEMBL | Inhibition of human soluble epoxide hydrolase using CMNPC as substrate after 5 mins by fluorescent assay | B | 8.15 | pIC50 | 7 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 601-605 [PMID:22079754] |
| ChEMBL | Inhibition of soluble epoxide hydroxylase by kinetic fluorescent assay | B | 8.15 | pIC50 | 7 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 5212-5216 [PMID:16870439] |
| epoxide hydrolase 2/Epoxide hydratase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4140] [GtoPdb: 2970] [UniProtKB: P34914] | ||||||||
| ChEMBL | Inhibition of mouse recombinant soluble epoxide hydrolase by fluorescent assay | B | 8.05 | pIC50 | 9 | nM | IC50 | J Med Chem (2007) 50: 3825-3840 [PMID:17616115] |
| ChEMBL | Inhibition of mouse soluble epoxide hydrolase | B | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 983-988 [PMID:21211973] |
| ChEMBL | Inhibition of murine soluble epoxide hydrolase expressed in baculovirus infected Sf21 cells using NEPC as substrate by fluorescence based assay | B | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem (2019) 27: 115078-115078 [PMID:31488357] |
| ChEMBL | Inhibition of mouse recombinant sEH using PHOME as substrate measured after 10 mins by fluorescent based assay | B | 8.77 | pIC50 | 1.7 | nM | IC50 | Eur J Med Chem (2021) 223: 113678-113678 [PMID:34218083] |
| GtoPdb | - | - | 8.77 | pIC50 | 1.7 | nM | IC50 | Eur J Med Chem (2021) 223: 113678 [PMID:34218083] |
| Epoxide hydrolase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1968] [UniProtKB: P07099] | ||||||||
| ChEMBL | Inhibition Assay: Inhibition assay of human soluble epoxide hydrolases. | B | 7.84 | pIC50 | 14.5 | nM | IC50 | US-8501783-B2. Conformationally restricted urea inhibitors of soluble epoxide hydrolase (2013) |
| epoxide hydrolase 2 in Human [GtoPdb: 2970] [UniProtKB: P34913] | ||||||||
| GtoPdb | - | - | 8.1 | pIC50 | 8 | nM | IC50 | J Med Chem (2020) 63: 9237-9257 [PMID:32787085] |
| GtoPdb | - | - | 8.15 | pIC50 | 7 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 5212-6 [PMID:16870439] |
| epoxide hydrolase 2 in Mouse [GtoPdb: 2970] [UniProtKB: P34914] | ||||||||
| GtoPdb | - | - | 8.77 | pIC50 | 1.7 | nM | IC50 | Eur J Med Chem (2021) 223: 113678 [PMID:34218083] |
| epoxide hydrolase 2/Epoxide hydrolase 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5669] [GtoPdb: 2970] [UniProtKB: P80299] | ||||||||
| ChEMBL | Inhibition of rat recombinant soluble epoxide hydrolase by fluorescent assay | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (2007) 50: 3825-3840 [PMID:17616115] |
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]
