oroxylin A [Ligand Id: 13522] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL183513
  • fms related receptor tyrosine kinase 3/Receptor-type tyrosine-protein kinase FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
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  • OATP2B1/Solute carrier organic anion transporter family member 2B1 in Human [ChEMBL: CHEMBL1743124] [GtoPdb: 1224] [UniProtKB: O94956]
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  • sequestosome 1 in Human [GtoPdb: 3213] [UniProtKB: Q13501]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
fms related receptor tyrosine kinase 3/Receptor-type tyrosine-protein kinase FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
ChEMBL Inhibition of recombinant FLT3 (unknown origin) by TR-FRET assay B 5.83 pIC50 1480 nM IC50 Bioorg Med Chem Lett (2013) 23: 1768-1770 [PMID:23411073]
OATP2B1/Solute carrier organic anion transporter family member 2B1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743124] [GtoPdb: 1224] [UniProtKB: O94956]
ChEMBL Inhibition of human OATP2B1 expressed in Flp-In-CHO cells assessed as inhibition of OATP2B1 mediated DBF uptake using DBF as fluorescent substrate incubated for 2 mins by BCA assay B 5.15 pIC50 7100 nM IC50 RSC Med Chem (2023) 14: 890-898 [PMID:37252098]
ChEMBL Inhibition of human OATP2B1 expressed in Flp-In-CHO cells assessed as inhibition of OATP2B1 mediated DBF uptake using DBF as fluorescent substrate incubated for 2 mins by BCA assay B 5.15 pIC50 7079.46 nM IC50 RSC Med Chem (2023) 14: 890-898 [PMID:37252098]
sequestosome 1 in Human [GtoPdb: 3213] [UniProtKB: Q13501]
GtoPdb Binding affinity determined using microscale thermophoresis (MST). - 5.88 pKd 1308 nM Kd Br J Pharmacol (2024) 181: 5110-5132 [PMID:39313956]

ChEMBL data shown on this page come from version 36:

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]