osthole [Ligand Id: 10302] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL52229 (Osthole)
  • 5-LOX/Arachidonate 5-lipoxygenase in Human [ChEMBL: CHEMBL215] [GtoPdb: 1385] [UniProtKB: P09917]
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  • GABAA receptor α1 subunit/GABAA receptor γ2 subunit/GABAA receptor β2 subunit/GABA-A receptor; alpha-1/beta-2/gamma-2 in Human [ChEMBL: CHEMBL2095172] [GtoPdb: 404, 414, 411] [UniProtKB: P14867, P18507, P47870]
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  • TRPV3 in Human [GtoPdb: 509] [UniProtKB: Q8NET8]
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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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]