[3H]digoxin [Ligand Id: 4725] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1751 (NSC-95100, Digoxin Pediatric, Vanoxin, Lanoxin-125, Lanoxicaps, Lanoxin-PG, Digoxin, Digamex, Lanoxin Pediatric, Lanoxin)
  • sodium/potassium-transporting ATPase subunit β-1/sodium/potassium-transporting ATPase subunit α-4/N+/K+ ATPase alpha-4/beta-1 in Rat [ChEMBL: CHEMBL4106165] [GtoPdb: 837836] [UniProtKB: P07340Q64541]
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  • RAR-related orphan receptor-γ/Nuclear receptor ROR-gamma in Human [ChEMBL: CHEMBL1741186] [GtoPdb: 600] [UniProtKB: P51449]
  • RAR-related orphan receptor-γ/Nuclear receptor ROR-gamma in Mouse [ChEMBL: CHEMBL1293231] [GtoPdb: 600] [UniProtKB: P51450]
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  • sodium/potassium-transporting ATPase subunit α-1/sodium/potassium-transporting ATPase subunit β-1/sodium/potassium-transporting ATPase subunit α-3/sodium/potassium-transporting ATPase subunit β-2/sodium/potassium-transporting ATPase subunit α-2/sodium/potassium-transporting ATPase subunit β-3/sodium/potassium-transporting ATPase subunit γ/sodium/potassium-transporting ATPase subunit α-4/Sodium/potassium-transporting ATPase in Human [ChEMBL: CHEMBL2095186] [GtoPdb: 8338378358388348392610836] [UniProtKB: P05023P05026P13637P14415P50993P54709P54710Q13733]
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  • sodium/potassium-transporting ATPase subunit α-1/Sodium/potassium-transporting ATPase alpha-1 chain in Human [ChEMBL: CHEMBL1807] [GtoPdb: 833] [UniProtKB: P05023]
  • Sodium/potassium-transporting ATPase alpha-1 chain in Dog [ChEMBL: CHEMBL4838] [UniProtKB: P50997]
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  • sodium/potassium-transporting ATPase subunit α-2/sodium/potassium-transporting ATPase subunit α-3/Sodium/potassium-transporting ATPase subunit alpha-2/alpha-3 in Rat [ChEMBL: CHEMBL3885640] [GtoPdb: 834835] [UniProtKB: P06686P06687]
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  • Solute carrier organic anion transporter family member 1A4 in Rat [ChEMBL: CHEMBL1781860] [UniProtKB: O35913]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
sodium/potassium-transporting ATPase subunit β-1/sodium/potassium-transporting ATPase subunit α-4/N+/K+ ATPase alpha-4/beta-1 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4106165] [GtoPdb: 837836] [UniProtKB: P07340Q64541]
ChEMBL Inhibition of recombinant rat Na+/K+-ATPase alpha4/beta1 expressed in baculovirus infected insect Sf9 cell membranes using [gamma-32P]ATP as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins in presence of Na+, K+ and Mg2+ by liquid scintillation counting B 8.26 pIC50 5.5 nM IC50 J Med Chem (2018) 61: 1800-1820 [PMID:29291372]
RAR-related orphan receptor-γ/Nuclear receptor ROR-gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1741186] [GtoPdb: 600] [UniProtKB: P51449]
ChEMBL Displacement of [3H]25-hydroxycholesterol from human RORc-LBD expressed in bacterial expression system after 3 hrs by scintillation counting analysis B 6.96 pKd 109 nM Kd Bioorg. Med. Chem. Lett. (2014) 24: 5769-5776 [PMID:25453817]
ChEMBL Displacement of fluorescein-labelled 25-HC from human RoRgamma-LBD by competitive binding assay B 5.39 pIC50 4100 nM IC50 J. Med. Chem. (2014) 57: 5871-5892 [PMID:24502334]
ChEMBL Displacement of fluorescein-labeled 25-hydroxycholesterol from human N-terminal 6xHis-tagged ROR gamma LBD (residues 262 to 518) expressed in Escherichia coli BL21-CodonPlus(DE3)-RIL cells by fluorescence polarization assay B 5.4 pIC50 4000 nM IC50 MedChemComm (2013) 4: 764-776
ChEMBL Antagonist activity at transactivation domain of RORgammat (unknown origin) expressed in Drosophila Schneider cells co-expressing Gal4-DNA binding domain B 5.7 pIC50 2000 nM IC50 ACS Med. Chem. Lett. (2013) 4: 79-84 [PMID:24040486]
ChEMBL Inhibition of thymus-specific isoform RORgamma (unknown origin) transcriptional activity by luciferase-based cotransfection assay B 5.7 pIC50 1980 nM IC50 J. Med. Chem. (2014) 57: 5871-5892 [PMID:24502334]
RAR-related orphan receptor-γ/Nuclear receptor ROR-gamma in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293231] [GtoPdb: 600] [UniProtKB: P51450]
ChEMBL Inhibition of mouse Gal4 DNA binding domain-fused ROR gamma expressed in Drosophila S2 cells assessed as inhibition of transcriptional activity by luciferase reporter assay B 5.7 pIC50 2000 nM IC50 MedChemComm (2013) 4: 764-776
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL Inhibition of P-glycoprotein using calcein-AM assay transfected in porcine PBCEC F 4.3 pIC50 >50000 nM IC50 J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389]
ChEMBL Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay F 4.3 pIC50 >50000 nM IC50 J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389]
ChEMBL TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells F 4.3 pIC50 >50000 nM IC50 J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389]
P-glycoprotein 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3467] [UniProtKB: P06795]
ChEMBL Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay F 4.3 pIC50 >50000 nM IC50 J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389]
ChEMBL TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1b-expressing LLC-PK1 cells F 4.3 pIC50 >50000 nM IC50 J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389]
ABCB1/P-glycoprotein 3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2573] [GtoPdb: 768] [UniProtKB: P21447]
ChEMBL Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay F 4.3 pIC50 >50000 nM IC50 J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389]
ChEMBL TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells F 4.3 pIC50 >50000 nM IC50 J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389]
sodium/potassium-transporting ATPase subunit α-1/sodium/potassium-transporting ATPase subunit β-1/sodium/potassium-transporting ATPase subunit α-3/sodium/potassium-transporting ATPase subunit β-2/sodium/potassium-transporting ATPase subunit α-2/sodium/potassium-transporting ATPase subunit β-3/sodium/potassium-transporting ATPase subunit γ/sodium/potassium-transporting ATPase subunit α-4/Sodium/potassium-transporting ATPase in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2095186] [GtoPdb: 8338378358388348392610836] [UniProtKB: P05023P05026P13637P14415P50993P54709P54710Q13733]
ChEMBL Inhibitory activity against Na+/K+ ATPase was determined B 6.4 pIC50 400 nM IC50 J. Med. Chem. (2003) 46: 3644-3654 [PMID:12904068]
ChEMBL Inhibition of human Na+/K+-ATPase assessed as reduction in inorganic phosphate release from ATP incubated for 15 mins followed by ATP addition measured over 15 mins in presence of Na+/K+ by colorimetric method B 6.57 pIC50 270 nM IC50 Bioorg Med Chem Lett (2018) 28: 2885-2889 [PMID:30049579]
sodium/potassium-transporting ATPase subunit α-1/Sodium/potassium-transporting ATPase alpha-1 chain in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1807] [GtoPdb: 833] [UniProtKB: P05023]
ChEMBL Inhibition of human kidney Na(+)/K(+) ATPase alpha-1 assessed as amount of Pi release after 1 hr by colorimetric method B 6.54 pIC50 290 nM IC50 Bioorg. Med. Chem. (2015) 23: 4397-4404 [PMID:26122772]
Sodium/potassium-transporting ATPase alpha-1 chain in Dog (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4838] [UniProtKB: P50997]
ChEMBL Inhibition of Na+/K+ ATPase from dog kidney B 6.3 pIC50 500 nM IC50 J. Med. Chem. (1997) 40: 3484-3488 [PMID:9341924]
ChEMBL In vitro inhibitory concentration against dog kidney Na+,K+-ATPase B 6.3 pIC50 500 nM IC50 J. Med. Chem. (2000) 43: 2332-2349 [PMID:10882359]
sodium/potassium-transporting ATPase subunit α-2/sodium/potassium-transporting ATPase subunit α-3/Sodium/potassium-transporting ATPase subunit alpha-2/alpha-3 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3885640] [GtoPdb: 834835] [UniProtKB: P06686P06687]
ChEMBL Inhibition of Wistar rat brain Na(+)/K(+) ATPase alpha-2/3 assessed as amount of Pi release after 1 hr by colorimetric method B 6.66 pIC50 220 nM IC50 Bioorg. Med. Chem. (2015) 23: 4397-4404 [PMID:26122772]
Solute carrier organic anion transporter family member 1A4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1781860] [UniProtKB: O35913]
ChEMBL TP_TRANSPORTER: inhibition of Taurocholate uptake in Oatp2-expressing LLC-PK1 cells F 6.24 pKi 580 nM Ki Drug Metab. Dispos. (2002) 30: 220-223 [PMID:11792694]
ChEMBL TP_TRANSPORTER: inhibition of E217betaG uptake in Oatp2-expressing LLC-PK1 cells F 7.43 pKi 37 nM Ki J. Pharmacol. Exp. Ther. (2001) 298: 316-322 [PMID:11408557]

ChEMBL data shown on this page come from version 26:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]