osthole [Ligand Id: 10302] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL52229 (Osthole) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 5-LOX/Arachidonate 5-lipoxygenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL215] [GtoPdb: 1385] [UniProtKB: P09917] | ||||||||
| ChEMBL | Inhibition of 5-lipoxygenase | B | 4.44 | pIC50 | 36200 | nM | IC50 | J Nat Prod (1998) 61: 347-350 [PMID:9544564] |
| Cyclooxygenase-1 in Sheep (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2949] [UniProtKB: P05979] | ||||||||
| ChEMBL | Inhibition of ovine COX1 using arachidonic acid as substrate pretreated for 3 mins followed by substrate addition measured immediately | B | 4.28 | pIC50 | 52500 | nM | IC50 | J Nat Prod (2017) 80: 2472-2477 [PMID:28885836] |
| COX-2 /Cyclooxygenase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL230] [GtoPdb: 1376] [UniProtKB: P35354] | ||||||||
| ChEMBL | Inhibition of human COX2 expressed in insect cells using arachidonic acid as substrate pretreated for 3 mins followed by substrate addition measured immediately | B | 4.09 | pIC50 | 81100 | nM | IC50 | J Nat Prod (2017) 80: 2472-2477 [PMID:28885836] |
| exportin 1/Exportin-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5661] [GtoPdb: 3014] [UniProtKB: O14980] | ||||||||
| ChEMBL | Inhibition of CRM1-mediated hemagglutininin-tagged HIV1 Rev protein nuclear export in human HeLa cells assessed as nucleus localization after 12 hrs by indirect fluorescent antibody technique | B | 5.8 | pIC50 | 1600 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 3717-3720 [PMID:20493693] |
| GABAA receptor α1 subunit/GABAA receptor γ2 subunit/GABAA receptor β2 subunit/GABA-A receptor; alpha-1/beta-2/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095172] [GtoPdb: 404, 414, 411] [UniProtKB: P14867, P18507, P47870] | ||||||||
| ChEMBL | Positive allosteric modulation of human GABA-A alpha1beta2gamma2S receptor expressed in Xenopus laevis oocytes assessed as increase in GABA-induced chloride channel current by two-electrode voltage clamp method relative to control | B | 4.85 | pEC50 | 14000 | nM | EC50 | Eur J Med Chem (2019) 171: 434-461 [PMID:30928713] |
| ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183] | ||||||||
| ChEMBL | Inhibition of P-gp in human LS180 cells after 90 mins by rhodamine123 cell exclusion method | B | 4.47 | pIC50 | 34000 | nM | IC50 | Medchemcomm (2014) 5: 1540-1547 |
| TRPV3 in Human [GtoPdb: 509] [UniProtKB: Q8NET8] | ||||||||
| GtoPdb | - | - | 4.4 | pIC50 | - | - | - | Mol Pharmacol (2018) 94: 1164-1173 [PMID:30108138] |
ChEMBL data shown on this page come from version 35:
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]
