ChEMBL ligand: CHEMBL1751 (Digamex, Digoxin, Digoxin pediatric, Digoxinum, Dynamos, Fargoxin, Lanocardin, Lanoxicaps, Lanoxin, Lanoxin-125, Lanoxin pediatric, Lanoxin-pg, Mapluxin, Natigoxin, NSC-95100, Rougoxin, Stillacor-, Toloxin, Vanoxin)
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: 837, 836] [UniProtKB: P07340, Q64541] There should be some charts here, you may need to enable JavaScript!
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] There should be some charts here, you may need to enable JavaScript!
ABCB1/P-glycoprotein 1 in Human [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183] P-glycoprotein 1 in Mouse [ChEMBL: CHEMBL3467] [UniProtKB: P06795] There should be some charts here, you may need to enable JavaScript!
ABCB1/P-glycoprotein 3 in Mouse [ChEMBL: CHEMBL2573] [GtoPdb: 768] [UniProtKB: P21447] There should be some charts here, you may need to enable JavaScript!
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: 833, 837, 835, 838, 834, 839, 2610, 836] [UniProtKB: P05023, P05026, P13637, P14415, P50993, P54709, P54710, Q13733] There should be some charts here, you may need to enable JavaScript!
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] There should be some charts here, you may need to enable JavaScript!
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: 834, 835] [UniProtKB: P06686, P06687] There should be some charts here, you may need to enable JavaScript!
Solute carrier organic anion transporter family member 1A4 in Rat [ChEMBL: CHEMBL1781860] [UniProtKB: O35913] There should be some charts here, you may need to enable JavaScript!

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: 837, 836] [UniProtKB: P07340, Q64541]
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	Competitive inverse agonist activity at human N-terminal His6-tagged RORgammat LBD (265 to 518 residues) expressed in Escherichia coli BL21 (DE3) assessed as inhibition of N-terminal biotinylated co-activator SRC1 box2 peptide recruitment measured after 30 mins in presence of 1 uM RORgamma agonist cholesterol by TR-FRET assay	B	4.07	pIC50	85400	nM	IC50	J Med Chem (2020) 63: 241-259 [PMID:31821760]
ChEMBL	Competitive inverse agonist activity at human N-terminal His6-tagged RORgammat LBD (265 to 518 residues) expressed in Escherichia coli BL21 (DE3) assessed as inhibition of N-terminal biotinylated co-activator SRC1 box2 peptide recruitment measured after 30 mins in presence of 0.25 uM RORgamma agonist cholesterol by TR-FRET assay	B	4.47	pIC50	33620	nM	IC50	J Med Chem (2020) 63: 241-259 [PMID:31821760]
ChEMBL	Orthosteric inverse agonist activity at 2-chloro-5-nitro-N-(2-(trifluoromethyl)phenyl)benzamide-ligated recombinant human N-terminal His6-tagged RORgammat ligand binding domain (265 to 518 residues) expressed in Escherichia coli BL21 (DE3) assessed as reduction in coactivator, N-terminal biotinylated SRC-1 box2 peptide recruitment in presence of 2-chloro-5-nitro-N-(2-(trifluoromethyl)phenyl)benzamide incubated for 60 mins by TR-FRET assay	B	5	pIC50	>10000	nM	IC50	ACS Med Chem Lett (2021) 12: 631-639 [PMID:33854703]
ChEMBL	Orthosteric inverse agonist activity at 2-chloro-N-(2,6-dimethylphenyl)-5-nitrobenzamide-ligated recombinant human N-terminal His6-tagged RORgammat ligand binding domain (265 to 518 residues) expressed in Escherichia coli BL21 (DE3) assessed as reduction in coactivator, N-terminal biotinylated SRC-1 box2 peptide recruitment in presence of 2-chloro-N-(2,6-dimethylphenyl)-5-nitrobenzamide incubated for 60 mins by TR-FRET assay	B	5	pIC50	>10000	nM	IC50	ACS Med Chem Lett (2021) 12: 631-639 [PMID:33854703]
ChEMBL	Orthosteric inverse agonist activity at 2-chloro-5-nitro-N-o-tolylbenzamide-ligated recombinant human N-terminal His6-tagged RORgammat ligand binding domain (265 to 518 residues) expressed in Escherichia coli BL21 (DE3) assessed as reduction in coactivator, N-terminal biotinylated SRC-1 box2 peptide recruitment in presence of 2-chloro-5-nitro-N-o-tolylbenzamide incubated for 60 mins by TR-FRET assay	B	5	pIC50	>10000	nM	IC50	ACS Med Chem Lett (2021) 12: 631-639 [PMID:33854703]
ChEMBL	Competitive inverse agonist activity at human N-terminal His6-tagged RORgammat LBD (265 to 518 residues) expressed in Escherichia coli BL21 (DE3) assessed as inhibition of N-terminal biotinylated co-activator SRC1 box2 peptide recruitment measured after 30 mins in absence of RORgamma agonist cholesterol by TR-FRET assay	B	5.15	pIC50	7012	nM	IC50	J Med Chem (2020) 63: 241-259 [PMID:31821760]
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	Orthosteric inverse agonist activity at recombinant human N-terminal His6-tagged RORgammat ligand binding domain (265 to 518 residues) expressed in Escherichia coli BL21 (DE3) assessed as reduction in coactivator, N-terminal biotinylated SRC-1 box2 peptide recruitment incubated for 60 mins by TR-FRET assay	B	5.64	pIC50	2307	nM	IC50	ACS Med Chem Lett (2021) 12: 631-639 [PMID:33854703]
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: 833, 837, 835, 838, 834, 839, 2610, 836] [UniProtKB: P05023, P05026, P13637, P14415, P50993, P54709, P54710, Q13733]
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: 834, 835] [UniProtKB: P06686, P06687]
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 31:

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]