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 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] |
| ChEMBL | Inhibition of human recombinant sEH | B | 8.1 | pIC50 | 8 | nM | IC50 | J Med Chem (2022) 65: 13660-13680 [PMID:36222708] |
| 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 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] |
| 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 soluble epoxide hydroxylase by kinetic fluorescent assay | B | 8.15 | pIC50 | 7 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 5212-5216 [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] |
| 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 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]
