ATP1B2

gene
On this page

Also known as AMOG

Summary

ATP1B2 (ATPase Na+/K+ transporting subunit beta 2, HGNC:805) is a protein-coding gene on chromosome 17p13.1, encoding Sodium/potassium-transporting ATPase subunit beta-2 (P14415). This is the non-catalytic component of the active enzyme, which catalyzes the hydrolysis of ATP coupled with the exchange of Na(+) and K(+) ions across the plasma membrane.

The protein encoded by this gene belongs to the family of Na+/K+ and H+/K+ ATPases beta chain proteins, and to the subfamily of Na+/K+ -ATPases. Na+/K+ -ATPase is an integral membrane protein responsible for establishing and maintaining the electrochemical gradients of Na and K ions across the plasma membrane. These gradients are essential for osmoregulation, for sodium-coupled transport of a variety of organic and inorganic molecules, and for electrical excitability of nerve and muscle. This enzyme is composed of two subunits, a large catalytic subunit (alpha) and a smaller glycoprotein subunit (beta). The beta subunit regulates, through assembly of alpha/beta heterodimers, the number of sodium pumps transported to the plasma membrane. The glycoprotein subunit of Na+/K+ -ATPase is encoded by multiple genes. This gene encodes a beta 2 subunit. Two transcript variants encoding different isoforms have been found for this gene.

Source: NCBI Gene 482 — RefSeq curated summary.

At a glance

  • GWAS associations: 18
  • Clinical variants (ClinVar): 49 total
  • Druggable target: yes — 5 molecules with ChEMBL bioactivity
  • MANE Select transcript: NM_001678

Identifiers

Gene identifiers

FieldValue
HGNC IDHGNC:805
Approved symbolATP1B2
NameATPase Na+/K+ transporting subunit beta 2
Location17p13.1
Locus typegene with protein product
StatusApproved
AliasesAMOG
Ensembl geneENSG00000129244
Ensembl biotypeprotein_coding
OMIM182331
Entrez482

Gene structure

Transcript identifiers

Ensembl transcripts: 6 — 6 protein_coding

ENST00000250111, ENST00000577026, ENST00000577113, ENST00000896722, ENST00000937621, ENST00000937622

RefSeq mRNA: 2 — MANE Select: NM_001678 NM_001303263, NM_001678

CCDS: CCDS32550

Canonical transcript exons

ENST00000250111 — 7 exons

ExonStartEnd
ENSE0000088738976533747653502
ENSE0000088739176540527654257
ENSE0000088739276546287654684
ENSE0000088739376555277655625
ENSE0000114737976557317657770
ENSE0000114738476509267651630
ENSE0000360827076538417653945

Expression profiles

Bgee: expression breadth ubiquitous, 221 present calls, max score 99.12.

FANTOM5 (CAGE): breadth broad, TPM avg 72.8918 / max 5778.8011, expressed in 674 samples.

FANTOM5 promoters (11 alternative TSS)

Promoter IDTPM avgSamples expressed
15928470.5111669
1592900.9638195
1592930.5920121
1592920.211072
1592910.153067
1592880.107962
1592890.090154
1593110.086430
1593090.082145
1593120.054414

Top tissues by expression

296 total, by Bgee expression score (0-100, higher = more expressed):

TissueAnatomy IDExpression scoreQuality
right hemisphere of cerebellumUBERON:001489099.12gold quality
cerebellar hemisphereUBERON:000224598.96gold quality
cerebellar cortexUBERON:000212998.89gold quality
right frontal lobeUBERON:000281098.35gold quality
caudate nucleusUBERON:000187398.28gold quality
nucleus accumbensUBERON:000188298.24gold quality
paraflocculusUBERON:000535198.23gold quality
cerebellumUBERON:000203798.18gold quality
amygdalaUBERON:000187697.91gold quality
putamenUBERON:000187497.88gold quality
dorsal motor nucleus of vagus nerveUBERON:000287097.79gold quality
ventricular zoneUBERON:000305397.65gold quality
middle frontal gyrusUBERON:000270297.26gold quality
inferior olivary complexUBERON:000212797.25gold quality
entorhinal cortexUBERON:000272897.01gold quality
cingulate cortexUBERON:000302797.01gold quality
anterior cingulate cortexUBERON:000983596.97gold quality
temporal lobeUBERON:000187196.93gold quality
medial globus pallidusUBERON:000247796.86gold quality
hypothalamusUBERON:000189896.58gold quality
Brodmann (1909) area 9UBERON:001354096.53gold quality
dorsolateral prefrontal cortexUBERON:000983496.34gold quality
lateral globus pallidusUBERON:000247696.25gold quality
postcentral gyrusUBERON:000258196.24gold quality
telencephalonUBERON:000189396.13gold quality
globus pallidusUBERON:000187595.97gold quality
Ammon’s hornUBERON:000195495.95gold quality
neocortexUBERON:000195095.76gold quality
frontal cortexUBERON:000187095.72gold quality
brainUBERON:000095595.70gold quality

Single-cell (SCXA)

Detected in 5 experiment(s), a significant marker in 5.

ExperimentMarker?Max mean expression
E-GEOD-84465yes599.31
E-GEOD-93593yes288.41
E-GEOD-135922yes13.61
E-HCAD-25yes4.23
E-ANND-3no0.00

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

138 targeting ATP1B2, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNAMax scoreAvg scoremiRNA target_count
HSA-MIR-5011-5P100.0083.465820
HSA-MIR-4747-5P100.0067.902681
HSA-MIR-5196-5P100.0067.982761
HSA-MIR-190A-3P100.0080.355520
HSA-MIR-6867-5P100.0082.213464
HSA-MIR-3613-3P100.0076.367965
HSA-MIR-6758-5P100.0066.211470
HSA-MIR-4692100.0067.322066
HSA-MIR-6856-5P100.0065.471298
HSA-MIR-4510100.0066.602050
HSA-MIR-6127100.0066.762188
HSA-MIR-6129100.0066.462080
HSA-MIR-6130100.0066.692012
HSA-MIR-6133100.0066.482064
HSA-MIR-6748-5P100.0065.811057
HSA-MIR-4533100.0069.482758
HSA-MIR-12118100.0065.881270
HSA-MIR-4476100.0068.182030
HSA-MIR-6876-5P100.0067.682126
HSA-MIR-451499.9967.101870
HSA-MIR-548AW99.9972.573559
HSA-MIR-371B-5P99.9975.344759
HSA-MIR-453499.9966.581907
HSA-MIR-3173-3P99.9866.491217
HSA-MIR-6891-5P99.9866.531372
HSA-MIR-103A-3P99.9869.141595
HSA-MIR-10799.9869.141595
HSA-MIR-373-5P99.9875.364753
HSA-MIR-616-5P99.9875.584775
HSA-MIR-548AN99.9770.912817

Literature-anchored findings (GeneRIF, showing 11)

  • Results demonstrated that the sodium-potassium ATPase beta2 subunit (NKA1b2) was localized both in the neuronal cytoplasm and cellular membrane. (PMID:15294280)
  • We identified interesting novel candidate genes that likely contribute to glioma progression and provide first evidence for a role of epigenetic silencing of AMOG in malignant glioma cells. (PMID:16865689)
  • Common genetic variation in TP53 and its flanking genes (ATP1B2) found no significant overall associations between SNPs in TP53 and breast cancer risk (PMID:17683073)
  • The strong expression of AMOG within the precursor cells of gangliogliomas may represent an additional marker for the diagnostic evaluation of these glioneuronal lesions (PMID:19371356)
  • the ER quality control system allows export only of assembled alpha-beta complexes to the Golgi, whereas the number of alpha(1) subunits in the ER determines the amount of the alpha-beta complexes (PMID:19764716)
  • The AMOG expression pattern with altered cellular distribution observed in malformations of cortical development suggests that AMOG might contribute to abnormal cortical development via mTOR activation. (PMID:20656459)
  • analysis of pathways for maturation of the Na,K-ATPase beta1 and beta2 subunits in the endoplasmic reticulum (PMID:20937802)
  • Retinoschisin, the protein involved in the pathogenesis of X-linked juvenile retinoschisis, membrane association is severely impaired in the absence of ATP1A3 and ATP1B2. (PMID:21196491)
  • different members of the Na,K-ATPase beta subunit family may have specialized functions. (PMID:2538450)
  • AMOG and L1 interdependently regulate their expression levels not only in U-87 MG cells but also in U251 and SHG44 human glioma cell lines. The capacity of AMOG to reduce L1 expression suggests that methods for increasing AMOG expression may provide a therapeutic choice for the management of glial tumors with high expression of L1. (PMID:31510944)
  • The beta2-Subunit (AMOG) of Human Na(+), K(+)-ATPase Is a Homophilic Adhesion Molecule. (PMID:35887102)

Cross-species orthologs

4 orthologs

OrganismSymbolGene ID
danio_rerioatp1b2bENSDARG00000034424
danio_rerioatp1b2aENSDARG00000099203
mus_musculusAtp1b2ENSMUSG00000041329
rattus_norvegicusAtp1b2ENSRNOG00000011227

Paralogs (4): ATP1B3 (ENSG00000069849), ATP1B4 (ENSG00000101892), ATP1B1 (ENSG00000143153), ATP4B (ENSG00000186009)

Protein

Protein identifiers

Sodium/potassium-transporting ATPase subunit beta-2P14415 (reviewed: P14415)

Alternative names: Adhesion molecule in glia, Sodium/potassium-dependent ATPase subunit beta-2

All UniProt accessions (3): P14415, I3L1V9, I3L3J8

UniProt curated annotations — full annotation on UniProt →

Function. This is the non-catalytic component of the active enzyme, which catalyzes the hydrolysis of ATP coupled with the exchange of Na(+) and K(+) ions across the plasma membrane. The exact function of the beta-2 subunit is not known. Mediates cell adhesion of neurons and astrocytes, and promotes neurite outgrowth.

Subunit / interactions. The sodium/potassium-transporting ATPase is composed of a catalytic alpha subunit, an auxiliary non-catalytic beta subunit and an additional regulatory subunit. Interacts with isoform 2 of BSG.

Subcellular location. Cell membrane.

Domain organisation. The C-terminal lobe folds into an immunoglobulin-like domain and mediates cell adhesion properties.

Similarity. Belongs to the X(+)/potassium ATPases subunit beta family.

RefSeq proteins (2): NP_001290192, NP_001669* (*=MANE)

Domains & families (InterPro)

IDNameType
IPR000402Na/K_ATPase_sub_betaFamily
IPR038702Na/K_ATPase_sub_beta_sfHomologous_superfamily

Pfam: PF00287

UniProt features (21 total): glycosylation site 7, sequence conflict 4, disulfide bond 3, topological domain 2, sequence variant 2, chain 1, transmembrane region 1, region of interest 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-P14415-F190.040.66

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Disulfide bonds (3): 129–150, 160–177, 200–261

Glycosylation sites (7): 197, 238, 96, 118, 153, 159, 193

Function

Pathways and Gene Ontology

Reactome pathways

14 pathways

IDPathway
R-HSA-210991Basigin interactions
R-HSA-5578775Ion homeostasis
R-HSA-936837Ion transport by P-type ATPases
R-HSA-9679191Potential therapeutics for SARS
R-HSA-109582Hemostasis
R-HSA-1643685Disease
R-HSA-202733Cell surface interactions at the vascular wall
R-HSA-382551Transport of small molecules
R-HSA-397014Muscle contraction
R-HSA-5576891Cardiac conduction
R-HSA-5663205Infectious disease
R-HSA-9679506SARS-CoV Infections
R-HSA-9824446Viral Infection Pathways
R-HSA-983712Ion channel transport

MSigDB gene sets: 307 (showing top): GOBP_POTASSIUM_ION_TRANSPORT, GOBP_HINDBRAIN_DEVELOPMENT, RRAGTTGT_UNKNOWN, GOBP_BEHAVIOR, GOBP_CIRCULATORY_SYSTEM_PROCESS, GGGNRMNNYCAT_UNKNOWN, RORA1_01, GOBP_SODIUM_ION_TRANSMEMBRANE_TRANSPORT, MODULE_45, GOCC_CELL_SURFACE, GOBP_POTASSIUM_ION_HOMEOSTASIS, GOBP_NEUROGENESIS, MEF2_02, GOBP_POSITIVE_REGULATION_OF_SODIUM_ION_TRANSPORT, MODULE_16

GO Biological Process (24): retina homeostasis (GO:0001895), intracellular sodium ion homeostasis (GO:0006883), positive regulation of neuron projection development (GO:0010976), lateral ventricle development (GO:0021670), third ventricle development (GO:0021678), neuronal-glial interaction involved in hindbrain glial-mediated radial cell migration (GO:0021944), intracellular potassium ion homeostasis (GO:0030007), cell-substrate adhesion (GO:0031589), sodium ion export across plasma membrane (GO:0036376), photoreceptor cell maintenance (GO:0045494), protein stabilization (GO:0050821), motor behavior (GO:0061744), membrane repolarization (GO:0086009), cell communication by electrical coupling involved in cardiac conduction (GO:0086064), plasma membrane bounded cell projection organization (GO:0120036), transport across blood-brain barrier (GO:0150104), positive regulation of sodium ion export across plasma membrane (GO:1903278), positive regulation of potassium ion import across plasma membrane (GO:1903288), negative regulation of glial cell migration (GO:1903976), potassium ion import across plasma membrane (GO:1990573), monoatomic ion transport (GO:0006811), potassium ion transport (GO:0006813), sodium ion transport (GO:0006814), cell adhesion (GO:0007155)

GO Molecular Function (6): ATPase activator activity (GO:0001671), protein-macromolecule adaptor activity (GO:0030674), protein heterodimerization activity (GO:0046982), ATPase binding (GO:0051117), transporter activator activity (GO:0141109), protein binding (GO:0005515)

GO Cellular Component (14): photoreceptor inner segment (GO:0001917), cytoplasm (GO:0005737), plasma membrane (GO:0005886), sodium:potassium-exchanging ATPase complex (GO:0005890), external side of plasma membrane (GO:0009897), membrane (GO:0016020), apical plasma membrane (GO:0016324), lateral plasma membrane (GO:0016328), cell projection membrane (GO:0031253), cell body membrane (GO:0044298), cell periphery (GO:0071944), astrocyte projection (GO:0097449), astrocyte end-foot (GO:0097450), neuron to neuron synapse (GO:0098984)

Reactome top-level categories

Rollup of top-10 pathways:

CategoryPathways
Cell surface interactions at the vascular wall1
Cardiac conduction1
Ion channel transport1
SARS-CoV Infections1
Hemostasis1
Muscle contraction1
Disease1
Viral Infection Pathways1
Infectious disease1
Transport of small molecules1

GO top-level categories

Rollup of top GO terms by namespace:

CategoryTerms
cellular anatomical structure6
plasma membrane3
intracellular monoatomic cation homeostasis2
ventricular system development2
anatomical structure development2
molecular function activator activity2
plasma membrane region2
tissue homeostasis1
sodium ion homeostasis1
regulation of neuron projection development1
neuron projection development1
positive regulation of cell projection organization1
telencephalon development1
hindbrain radial glia guided cell migration1
cell-cell adhesion1
potassium ion homeostasis1
cell adhesion1
sodium ion transmembrane transport1
export across plasma membrane1
retina homeostasis1
multicellular organismal process1
regulation of protein stability1
behavior1
regulation of membrane potential1
cell communication by electrical coupling1
cardiac conduction1
cell communication involved in cardiac conduction1
cell projection organization1
vascular transport1
sodium ion export across plasma membrane1
positive regulation of sodium ion transmembrane transport1
regulation of sodium ion export across plasma membrane1
positive regulation of potassium ion transmembrane transport1
regulation of potassium ion import1
potassium ion import across plasma membrane1
glial cell migration1
negative regulation of cell migration1
regulation of glial cell migration1
potassium ion transmembrane transport1
inorganic cation import across plasma membrane1

Protein interactions and networks

STRING

1508 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
ATP1B2ATP1A2P50993888
ATP1B2ATP1A3P13637801
ATP1B2ZNF3P13683769
ATP1B2ATP1A4Q13733769
ATP1B2ASGR2P07307765
ATP1B2ATP1A1P05023763
ATP1B2ASGR1P07306749
ATP1B2PIGQQ9BRB3710
ATP1B2ATP1B1P05026690
ATP1B2ST3GAL4Q11206497
ATP1B2ATP2B1P20020492
ATP1B2ATP1B3P54709419
ATP1B2KCNJ10P78508404
ATP1B2NNATQ16517385
ATP1B2CD59P13987383

IntAct

11 interactions, top by confidence:

ABTypeScore
ATP1B2RTN4psi-mi:“MI:0915”(physical association)0.400
RS1ATP1A3psi-mi:“MI:0914”(association)0.350
APBB1SSPOPpsi-mi:“MI:0914”(association)0.350
MAPTSHTN1psi-mi:“MI:0914”(association)0.350
CANXHLA-Apsi-mi:“MI:0914”(association)0.350
ATP1A3TMEM223psi-mi:“MI:0914”(association)0.350
TSPAN31TMEM120Bpsi-mi:“MI:0914”(association)0.350
ATP1B2CLGNpsi-mi:“MI:0914”(association)0.350

BioGRID (21): COPG2 (Affinity Capture-MS), ATP1A1 (Co-fractionation), ATP5F1 (Co-fractionation), RPL26 (Co-fractionation), RPLP2 (Co-fractionation), RPS18 (Co-fractionation), RPS8 (Co-fractionation), RTN4 (Affinity Capture-MS), ATP1B2 (Affinity Capture-MS), ATP1B2 (Two-hybrid), GNMT (Affinity Capture-MS), ATP1B2 (Affinity Capture-MS), RTN4 (Affinity Capture-MS), ATP1B2 (Affinity Capture-MS), CLGN (Affinity Capture-MS)

ESM2 similar proteins: A5A6J8, P05026, P05027, P05028, P05029, P06583, P07340, P08251, P13638, P14094, P14231, P14415, P18434, P18597, P18598, P21188, P30715, P30716, P33704, P33879, P43002, P50992, P51164, P51165, P51575, P51577, P54709, Q17QL5, Q202B1, Q24048, Q28030, Q2HZ96, Q4R4V5, Q5E9U1, Q5F362, Q5J583, Q5R6C0, Q5R8S8, Q6AY41, Q8L8W0

Diamond homologs: A5A6J8, A7MB71, P05026, P05027, P05028, P05029, P06583, P07340, P08251, P13638, P14094, P14231, P14415, P18434, P18597, P18598, P21188, P25169, P30715, P30716, P33704, P33879, P43002, P51165, P54709, P97370, Q202B1, Q24046, Q28030, Q2HZ96, Q3T0C6, Q4R4V5, Q5J583, Q5R8S8, Q60489, Q63377, Q8WMG3, Q99ME6, Q9BDK6, Q9GLC3

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

49 variants total. Per-class counts are floors (≥ shown; pagination cap):

ClassificationCount (floor)
Pathogenic0
Likely pathogenic0
Uncertain significance43
Likely benign0
Benign0

Top pathogenic / likely-pathogenic (0)

SpliceAI

1274 predictions. Top by Δscore:

VariantEffectΔscore
17:7651593:G:GTdonor_gain1.0000
17:7651628:GGG:Gdonor_gain1.0000
17:7651629:GG:Gdonor_gain1.0000
17:7651629:GGG:Gdonor_gain1.0000
17:7651630:GG:Gdonor_gain1.0000
17:7653372:A:AGacceptor_gain1.0000
17:7653373:G:GGacceptor_gain1.0000
17:7653373:GC:Gacceptor_gain1.0000
17:7653373:GCCT:Gacceptor_gain1.0000
17:7653373:GCCTT:Gacceptor_gain1.0000
17:7653404:AT:Aacceptor_gain1.0000
17:7653404:ATG:Aacceptor_gain1.0000
17:7653405:T:Gacceptor_gain1.0000
17:7653405:T:TAacceptor_gain1.0000
17:7653406:G:Aacceptor_gain1.0000
17:7653501:GG:Gdonor_gain1.0000
17:7653501:GGGT:Gdonor_loss1.0000
17:7653502:GG:Gdonor_gain1.0000
17:7653502:GGTG:Gdonor_loss1.0000
17:7653503:G:Cdonor_loss1.0000
17:7653503:G:GGdonor_gain1.0000
17:7653504:T:Adonor_loss1.0000
17:7653832:T:Aacceptor_gain1.0000
17:7653838:TAGGC:Tacceptor_loss1.0000
17:7653839:A:AGacceptor_gain1.0000
17:7653840:G:GGacceptor_gain1.0000
17:7653840:G:GTacceptor_loss1.0000
17:7653840:GGCTT:Gacceptor_gain1.0000
17:7653941:GGAGC:Gdonor_gain1.0000
17:7653942:GAGC:Gdonor_gain1.0000

AlphaMissense

1954 scored. Top likely-pathogenic:

VariantProtein changeam_pathogenicity
17:7654153:T:AC150S1.000
17:7654154:G:CC150S1.000
17:7654673:T:AC200S1.000
17:7654674:G:CC200S1.000
17:7655803:T:AC261S1.000
17:7655803:T:CC261R1.000
17:7655804:G:CC261S1.000
17:7655851:T:CF277L1.000
17:7655853:C:AF277L1.000
17:7655853:C:GF277L1.000
17:7651612:C:AR32S0.999
17:7653424:T:CF55L0.999
17:7653426:C:AF55L0.999
17:7653426:C:GF55L0.999
17:7653473:C:AP71H0.999
17:7654090:T:AC129S0.999
17:7654090:T:CC129R0.999
17:7654091:G:AC129Y0.999
17:7654091:G:CC129S0.999
17:7654092:C:GC129W0.999
17:7654153:T:CC150R0.999
17:7654154:G:AC150Y0.999
17:7654154:G:TC150F0.999
17:7654155:C:GC150W0.999
17:7654159:T:CF152L0.999
17:7654160:T:CF152S0.999
17:7654160:T:GF152C0.999
17:7654161:C:AF152L0.999
17:7654161:C:GF152L0.999
17:7654183:T:AC160S0.999

dbSNP variants (sampled 300 via entrez): RS1000141906 (17:7656112 A>G), RS1000745886 (17:7654971 G>A), RS1000851438 (17:7649934 T>C), RS1000861094 (17:7649405 T>A,C), RS1000873891 (17:7645101 C>T), RS1001012398 (17:7655724 G>A,C,T), RS1001528461 (17:7655992 G>T), RS1001627161 (17:7652750 T>G), RS1001700981 (17:7653638 T>C), RS1001759346 (17:7646161 A>G,T), RS1001968964 (17:7651400 C>T), RS1002131423 (17:7657403 C>T), RS1002418755 (17:7657153 A>C), RS1002930865 (17:7654058 A>G,T), RS1003169580 (17:7646432 A>G,T)

Disease associations

OMIM: gene MIM:182331 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

0 total (0 of 0 shown, HPO-id order):

GWAS associations

18 associations (top):

StudyTraitp-value
GCST001554_1Sex hormone-binding globulin levels2.000000e-16
GCST002568_2Esophageal squamous cell carcinoma3.000000e-13
GCST006190_4Diastolic blood pressure x smoking status (ever vs never) interaction (2df test)3.000000e-10
GCST006190_54Diastolic blood pressure x smoking status (ever vs never) interaction (2df test)3.000000e-08
GCST006192_52Systolic blood pressure x smoking status (ever vs never) interaction (2df test)8.000000e-11
GCST006192_75Systolic blood pressure x smoking status (ever vs never) interaction (2df test)2.000000e-12
GCST006193_37Diastolic blood pressure x smoking status (current vs non-current) interaction (2df test)9.000000e-11
GCST006193_75Diastolic blood pressure x smoking status (current vs non-current) interaction (2df test)9.000000e-09
GCST006195_19Systolic blood pressure x smoking status (current vs non-current) interaction (2df test)3.000000e-11
GCST006195_69Systolic blood pressure x smoking status (current vs non-current) interaction (2df test)1.000000e-12
GCST009380_7Type 2 diabetes (adjusted for BMI)1.000000e-10
GCST009380_8Type 2 diabetes (adjusted for BMI)5.000000e-06
GCST010002_119Refractive error3.000000e-22
GCST010703_158Brain morphology (MOSTest)3.000000e-09
GCST90002402_436Platelet count2.000000e-13
GCST90002404_349Red cell distribution width1.000000e-17
GCST90020029_827Waist circumference adjusted for body mass index6.000000e-12
GCST90020029_828Waist circumference adjusted for body mass index5.000000e-10

EFO canonical traits (8, from GWAS)

EFO IDTrait name
EFO:0004696sex hormone-binding globulin measurement
EFO:0006336diastolic blood pressure
EFO:0006527smoking status measurement
EFO:0006335systolic blood pressure
EFO:0004346neuroimaging measurement
EFO:0004309platelet count
EFO:0009188Red cell distribution width
EFO:0007789BMI-adjusted waist circumference

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL2095186 (PROTEIN COMPLEX GROUP), CHEMBL6066561 (PROTEIN COMPLEX)

Molecules with ChEMBL bioactivity

5 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 160,774 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

MoleculeNamePhasePatents
CHEMBL1503OMEPRAZOLE452,284
CHEMBL1751DIGOXIN467,342
CHEMBL254219DIGITOXIN416,757
CHEMBL480LANSOPRAZOLE424,317
CHEMBL2068971ROSTAFUROXIN274

PharmGKB: 1 entry (VIP=true, CPIC=false)

GtoPdb / IUPHAR curated pharmacology

(IUPHAR/BPS Guide to Pharmacology — expert-curated)

Target class: transporter — Na+/K+-ATPases

ChEMBL bioactivities

235 potent at pChembl≥5 of 287 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChemblTypeValueUnitMolecule
8.52IC503nMCHEMBL2092909
8.32IC504.79nMCHEMBL1651648
8.29Ki5.1nMCHEMBL5876237
8.28Ki5.3nMCHEMBL5879229
8.27Ki5.4nMCHEMBL5765464
8.22Ki6nMCHEMBL5879229
8.17Ki6.8nMCHEMBL5832044
8.17IC506.79nMCHEMBL1651648
8.15IC507nMCHEMBL2092738
8.15IC507.04nMCHEMBL1651624
8.10IC508nMCHEMBL3085467
8.10IC508nMCHEMBL3085497
8.10Ki8nMCHEMBL5765464
8.10IC508nMDIGITOXIGENIN
8.10IC508nMDIGITOXIN
8.05IC509nMCHEMBL3085468
8.00Ki10nMCHEMBL5748673
7.98Ki10.5nMCHEMBL5957388
7.98IC5010.5nMCHEMBL3349024
7.97IC5010.7nMCHEMBL3350144
7.92Ki12.1nMCHEMBL6026321
7.92IC5012nMCHEMBL2069010
7.89Ki13nMCHEMBL6056661
7.84Ki14.3nMCHEMBL5851200
7.82Ki15.3nMCHEMBL5910596
7.80IC5016nMCHEMBL2068887
7.80IC5016nMCHEMBL3349024
7.79Ki16.4nMCHEMBL6031986
7.78Ki16.7nMCHEMBL5791351
7.75IC5017.8nMCHEMBL1159613
7.74Ki18.1nMCHEMBL6030183
7.74Ki18.4nMCHEMBL5780414
7.70IC5020nMDIGITOXIGENIN
7.70IC5020nMCHEMBL2068894
7.70IC5020nMCHEMBL2068887
7.69Ki20.4nMCHEMBL5768226
7.66IC5022nMBUFALIN
7.60IC5025nMCHEMBL2068888
7.55IC5028.2nMCHEMBL3350144
7.52IC5030nMCHEMBL2068896
7.52IC5030nMCHEMBL2068909
7.50Ki31.7nMCHEMBL6005633
7.50Ki31.5nMCHEMBL5814784
7.47Ki33.5nMCHEMBL5961305
7.41IC5038.9nMCHEMBL3349024
7.40IC5040nMCHEMBL126930
7.40IC5040nMCHEMBL2069036
7.39Ki40.7nMDIGITOXIN
7.35IC5045nMCHEMBL2069112
7.30IC5050nMCHEMBL2069053

PubChem BioAssay actives

210 with measured affinity, of 373 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

CompoundAssayTypeValueUnit
3-[(3S,8R,9S,10S,13R,14R,17S)-14-hydroxy-10,13-dimethyl-3-[[(2R,3S,4S,5R,6S)-3,4,5,6-tetrahydroxyoxan-2-yl]methoxy]-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthren-17-yl]-2H-furan-5-one49025: Inhibition of [3H]ouabain binding to Na/K ATP-ase in dog heart muscleic500.0030uM
3-[(3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-[(2R,3R,4R,5R,6S)-3,4,5-trihydroxy-6-methyloxan-2-yl]oxy-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthren-17-yl]-2H-furan-5-one146845: Inhibition of hog kidney Na+, K+-dependent ATPaseic500.0048uM
3-[(3S,5R,8R,9S,10S,13R,14S,17R)-3-[(2R,4S,5S,6R)-4,5-dihydroxy-6-methyloxan-2-yl]oxy-14-hydroxy-10,13-dimethyl-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthren-17-yl]-2H-furan-5-one146845: Inhibition of hog kidney Na+, K+-dependent ATPaseic500.0070uM
3-[(3S,8R,9S,10S,13R,14R,17R)-14-hydroxy-10,13-dimethyl-3-[[(2R,3S,4S,5R,6S)-3,4,5,6-tetrahydroxyoxan-2-yl]methoxy]-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthren-17-yl]-2H-furan-5-one49025: Inhibition of [3H]ouabain binding to Na/K ATP-ase in dog heart muscleic500.0070uM
3-[(3S,5R,8R,9S,10S,13R,14S,17R)-3,14-dihydroxy-10,13-dimethyl-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthren-17-yl]-2H-furan-5-one56911: Inhibition of [3H]- ouabain binding to digitalis receptoric500.0080uM
3-[(3S,5R,8R,9S,10S,13R,14S,17R)-3-[(2R,4S,5S,6R)-5-[(2S,4S,5S,6R)-5-[(2S,4S,5S,6R)-4,5-dihydroxy-6-methyloxan-2-yl]oxy-4-hydroxy-6-methyloxan-2-yl]oxy-4-hydroxy-6-methyloxan-2-yl]oxy-14-hydroxy-10,13-dimethyl-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthren-17-yl]-2H-furan-5-one56911: Inhibition of [3H]- ouabain binding to digitalis receptoric500.0080uM
3-[(3S,5S,8R,9S,10S,13R,14R,17R)-3-[[(2S,3R,4R,6S)-3,4-dihydroxy-6-[[(2S,3R,4R,6S)-3,4,6-trihydroxyoxan-2-yl]methoxy]oxan-2-yl]methoxy]-14-hydroxy-10,13-dimethyl-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthren-17-yl]-2H-furan-5-one49025: Inhibition of [3H]ouabain binding to Na/K ATP-ase in dog heart muscleic500.0080uM
3-[(3S,5S,8R,9S,10S,13R,14R,17R)-3-[[(2S,3R,4R,6S)-6-[[(2S,3R,4R,6S)-3,4-dihydroxy-6-[[(2S,3R,4R,6S)-3,4,6-trihydroxyoxan-2-yl]methoxy]oxan-2-yl]methoxy]-3,4-dihydroxyoxan-2-yl]methoxy]-14-hydroxy-10,13-dimethyl-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthren-17-yl]-2H-furan-5-one49025: Inhibition of [3H]ouabain binding to Na/K ATP-ase in dog heart muscleic500.0080uM
3-[(3S,5S,8R,9S,10S,13R,14R,17R)-14-hydroxy-10,13-dimethyl-3-[[(2S,3R,4R,6S)-3,4,6-trihydroxyoxan-2-yl]methoxy]-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthren-17-yl]-2H-furan-5-one49025: Inhibition of [3H]ouabain binding to Na/K ATP-ase in dog heart muscleic500.0090uM
3-[(3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthren-17-yl]-2H-furan-5-one146845: Inhibition of hog kidney Na+, K+-dependent ATPaseic500.0105uM
3-[(3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-[(2R,3S,4S,5S,6S)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthren-17-yl]-2H-furan-5-one146845: Inhibition of hog kidney Na+, K+-dependent ATPaseic500.0107uM
(2R,4S,5R)-2-[[(3S,5R,8R,9S,10S,13R,14S,17S)-14-hydroxy-10,13-dimethyl-17-(nitromethyl)-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthren-3-yl]oxy]-6-methyloxane-3,4,5-triol56911: Inhibition of [3H]- ouabain binding to digitalis receptoric500.0120uM
(3S,5R,8R,9S,10S,13R,14S,17R)-17-[(E,3E)-3-(2-aminoethoxyimino)prop-1-enyl]-10,13-dimethyl-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthrene-3,14-diol146853: 50% displacement of the specific [3H]ouabain binding from the dog kidney Na+/K+ ATPaseic500.0160uM
3-[(13R)-14-hydroxy-10,13-dimethyl-3-[(2S,3R,4S,5R,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthren-17-yl]-2H-furan-5-one146845: Inhibition of hog kidney Na+, K+-dependent ATPaseic500.0178uM
(3S,5R,8R,9S,10S,13R,14S,17S)-17-[(E)-3-aminopropoxyiminomethyl]-10,13-dimethyl-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthrene-3,14-diol;oxalic acid146858: In vitro inhibitory concentration against dog kidney Na+/K+ ATPaseic500.0200uM
5-[(3S,5R,8R,9S,10S,13R,14S,17R)-3,14-dihydroxy-10,13-dimethyl-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthren-17-yl]pyran-2-one1941870: Inhibition of NA+/K+ ATPase (unknown origin) activityic500.0220uM
(3S,5R,8R,9S,10S,13R,14S,17R)-17-[(E,3E)-3-[2-(dimethylamino)ethoxyimino]prop-1-enyl]-10,13-dimethyl-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthrene-3,14-diol146853: 50% displacement of the specific [3H]ouabain binding from the dog kidney Na+/K+ ATPaseic500.0250uM
(3S,5R,8R,9S,10S,13R,14S,17R)-17-[(E,3E)-3-[2-(dimethylamino)ethoxyimino]prop-1-enyl]-10,13-dimethyl-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthrene-3,14-diol;oxalic acid146858: In vitro inhibitory concentration against dog kidney Na+/K+ ATPaseic500.0300uM
(3S,5R,8R,9S,10S,13R,14S,17R)-17-[(E,3E)-3-(2-aminoethoxyimino)-2-methylprop-1-enyl]-10,13-dimethyl-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthrene-3,14-diol;(E)-but-2-enedioic acid146858: In vitro inhibitory concentration against dog kidney Na+/K+ ATPaseic500.0300uM
(2R,4bS,7S,8aR)-2-[(1E,3S)-1-(2-aminoethoxyimino)pentan-3-yl]-7-hydroxy-2,4b-dimethyl-4,4a,5,6,7,8,8a,9,10,10a-decahydro-3H-phenanthren-1-one146843: Binding affinity towards Na+,K+ -ATPase isolated from dog kidney.ic500.0400uM
(3S,5R,8R,9S,10S,13R,14S,17S)-17-[(E)-2-(dimethylamino)ethoxyiminomethyl]-10,13-dimethyl-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthrene-3,14-diol146853: 50% displacement of the specific [3H]ouabain binding from the dog kidney Na+/K+ ATPaseic500.0400uM
(2R,4S,5R)-2-[[(3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-nitroethyl)-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthren-3-yl]oxy]-6-methyloxane-3,4,5-triol56911: Inhibition of [3H]- ouabain binding to digitalis receptoric500.0450uM
(3S,5R,8R,9S,10S,13R,14S,17S)-17-[(2E)-2-(2-aminoethoxyimino)ethyl]-10,13-dimethyl-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthrene-3,14-diol146843: Binding affinity towards Na+,K+ -ATPase isolated from dog kidney.ic500.0500uM
(E)-but-2-enedioic acid;(3S,5R,8R,9S,10S,13R,14S,17R)-17-[(E,3E)-3-[2-(dimethylamino)ethoxyimino]-2-methylprop-1-enyl]-10,13-dimethyl-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthrene-3,14-diol146858: In vitro inhibitory concentration against dog kidney Na+/K+ ATPaseic500.0600uM
6-[[(3S,8R,9S,10S,13R,14R,17S)-14-hydroxy-17-[(1S)-1-hydroxyethyl]-10,13-dimethyl-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthren-3-yl]oxy]-2-(hydroxymethyl)oxane-3,4-diol146854: Compound is evaluated for inhibition of specific binding of [3H]ouabain to membranes from dog heartic500.0600uM
3-[(5R,8R,9S,10S,13R,14R,17R)-14-hydroxy-10,13-dimethyl-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthren-17-yl]-2H-furan-5-one49025: Inhibition of [3H]ouabain binding to Na/K ATP-ase in dog heart muscleic500.0700uM
(2R,3R,4R,5R,6R)-6-[[(3R)-14-hydroxy-17-(1-hydroxyethyl)-10,13-dimethyl-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthren-3-yl]oxymethyl]oxane-2,3,4,5-tetrol49025: Inhibition of [3H]ouabain binding to Na/K ATP-ase in dog heart muscleic500.0750uM
(3S,5R,8R,9S,10S,13R,14S,17R)-17-[(1E,3E)-6-aminohexa-1,3-dienyl]-10,13-dimethyl-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthrene-3,14-diol146858: In vitro inhibitory concentration against dog kidney Na+/K+ ATPaseic500.0800uM
(3S,5R,8R,9S,10S,13R,14S,17S)-17-[(3Z)-3-(2-aminoethoxyimino)propyl]-10,13-dimethyl-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthrene-3,14-diol146858: In vitro inhibitory concentration against dog kidney Na+/K+ ATPaseic500.0800uM
3-[(3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-[(2R,3R,4R,5R,6S)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthren-17-yl]-2H-furan-5-one146845: Inhibition of hog kidney Na+, K+-dependent ATPaseic500.0870uM
(3S,4R,6R)-6-[[(3S,5R,8R,9S,10S,13R,14S,17S)-14-hydroxy-10,13-dimethyl-17-(nitromethyl)-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthren-3-yl]oxy]-2-methyloxane-3,4-diol56911: Inhibition of [3H]- ouabain binding to digitalis receptoric500.0880uM
(2R,4S,5R)-2-[[(3S,5R,8R,9S,10S,13R,14S,17S)-17-(aminomethyl)-14-hydroxy-10,13-dimethyl-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthren-3-yl]oxy]-6-methyloxane-3,4,5-triol;hydrochloride56911: Inhibition of [3H]- ouabain binding to digitalis receptoric500.0990uM
(2R,4bS,7S,8aR)-2-[(1E,3S)-1-[2-(dimethylamino)ethoxyimino]pentan-3-yl]-7-hydroxy-2,4b-dimethyl-4,4a,5,6,7,8,8a,9,10,10a-decahydro-3H-phenanthren-1-one146843: Binding affinity towards Na+,K+ -ATPase isolated from dog kidney.ic500.1000uM
(2R,4bS,7S,8aR)-2-[(2S,4E)-4-(2-aminoethoxyimino)butan-2-yl]-7-hydroxy-2,4b-dimethyl-4,4a,5,6,7,8,8a,9,10,10a-decahydro-3H-phenanthren-1-one146843: Binding affinity towards Na+,K+ -ATPase isolated from dog kidney.ic500.1000uM
2-[(E)-[(3S,5R,8R,9S,10S,13R,14S,17S)-3,14-dihydroxy-10,13-dimethyl-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthren-17-yl]methylideneamino]guanidine;hydrochloride146856: Displacement of [3H]ouabain from dog kidney Na+/K+ ATPaseic500.1000uM
(3S,5R,8R,9S,10S,13R,14S,17S)-17-[(3Z)-3-[2-(dimethylamino)ethoxyimino]propyl]-10,13-dimethyl-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthrene-3,14-diol;oxalic acid146858: In vitro inhibitory concentration against dog kidney Na+/K+ ATPaseic500.1000uM
(2R,4bS,7S,8aR)-2-[(2S,4E)-4-[2-(dimethylamino)ethoxyimino]butan-2-yl]-7-hydroxy-2,4b-dimethyl-4,4a,5,6,7,8,8a,9,10,10a-decahydro-3H-phenanthren-1-one146843: Binding affinity towards Na+,K+ -ATPase isolated from dog kidney.ic500.1300uM
2-(dimethylamino)ethyl (E)-4-[(2R,4bS,7S,8aR)-7-hydroxy-2,4b-dimethyl-1-oxo-4,4a,5,6,7,8,8a,9,10,10a-decahydro-3H-phenanthren-2-yl]hex-2-enoate146843: Binding affinity towards Na+,K+ -ATPase isolated from dog kidney.ic500.1300uM
1-[(3R)-14-hydroxy-10,13-dimethyl-3-[[(2R,3R,4R,5R,6R)-3,4,5,6-tetrahydroxyoxan-2-yl]methoxy]-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthren-17-yl]ethanone49025: Inhibition of [3H]ouabain binding to Na/K ATP-ase in dog heart muscleic500.1500uM
Digoxin1970782: Inhibition of NA+/K+ ATPase (unknown origin) activity incubated for 15 mins in presence of ATP by ADP-Glo assayic500.1600uM
(2R,4bS,7S,8aS)-2-[(1E,3S)-1-(2-aminoethoxyimino)pentan-3-yl]-7-hydroxy-2,4b-dimethyl-4,4a,5,6,7,8,8a,9,10,10a-decahydro-3H-phenanthren-1-one146843: Binding affinity towards Na+,K+ -ATPase isolated from dog kidney.ic500.1600uM
(3S,5R,8R,9S,10S,13R,14S,17S)-17-[(E)-2-aminoethoxyiminomethyl]-10,13-dimethyl-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthrene-3,14-diol;(E)-but-2-enedioic acid146858: In vitro inhibitory concentration against dog kidney Na+/K+ ATPaseic500.1600uM
2-[(E)-1-[(3S,5R,8R,9S,10S,13R,14S,17S)-3,14-dihydroxy-10,13-dimethyl-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthren-17-yl]ethylideneamino]guanidine146856: Displacement of [3H]ouabain from dog kidney Na+/K+ ATPaseic500.1995uM
(3S,5R,8R,9S,10S,13R,14S,17S)-17-[(E)-(4,5-dihydro-1H-imidazol-2-ylhydrazinylidene)methyl]-10,13-dimethyl-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthrene-3,14-diol146856: Displacement of [3H]ouabain from dog kidney Na+/K+ ATPaseic500.1995uM
(3S,5R,8R,9S,10S,13R,14S,17S)-17-[(2E)-2-(3-aminopropoxyimino)ethyl]-10,13-dimethyl-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthrene-3,14-diol146843: Binding affinity towards Na+,K+ -ATPase isolated from dog kidney.ic500.2000uM
3-[(1R)-1-[(2R,4bS,7S,8aR)-7-hydroxy-2,4b-dimethyl-1-oxo-4,4a,5,6,7,8,8a,9,10,10a-decahydro-3H-phenanthren-2-yl]propyl]-2H-furan-5-one146843: Binding affinity towards Na+,K+ -ATPase isolated from dog kidney.ic500.2000uM
(2R,4bS,7S,8aR)-2-[(1E,3S)-1-(2-aminoethoxyimino)hexan-3-yl]-7-hydroxy-2,4b-dimethyl-4,4a,5,6,7,8,8a,9,10,10a-decahydro-3H-phenanthren-1-one146843: Binding affinity towards Na+,K+ -ATPase isolated from dog kidney.ic500.2000uM
(3S,5R,8R,9S,10S,13R,14S,17R)-17-[(E,3E)-3-(3-aminopropoxyimino)-2-methylprop-1-enyl]-10,13-dimethyl-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthrene-3,14-diol;oxalic acid146858: In vitro inhibitory concentration against dog kidney Na+/K+ ATPaseic500.2000uM
(3S,5R,8R,9S,10S,13R,14S,17S)-17-[(2E)-2-[2-(dimethylamino)ethoxyimino]ethyl]-10,13-dimethyl-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthrene-3,14-diol146843: Binding affinity towards Na+,K+ -ATPase isolated from dog kidney.ic500.2500uM
2-(dimethylamino)ethyl (E,4R)-4-[(2R,4bS,7S,8aR)-7-hydroxy-2,4b-dimethyl-1-oxo-4,4a,5,6,7,8,8a,9,10,10a-decahydro-3H-phenanthren-2-yl]hex-2-enoate146843: Binding affinity towards Na+,K+ -ATPase isolated from dog kidney.ic500.2500uM

CTD chemical–gene interactions

41 total (human), top 30 by PubMed support.

ChemicalActions (top 5)PubMed papers
Valproic Acidaffects expression, increases expression3
sodium arsenitedecreases expression, increases expression2
entinostatincreases expression, affects cotreatment2
(+)-JQ1 compoundincreases expression2
Benzo(a)pyreneincreases expression, increases methylation2
bisphenol Faffects cotreatment, increases expression1
methylmercuric chloridedecreases expression1
propionaldehydeincreases expression1
pirinixic acidaffects binding, decreases expression, increases activity1
2-methyl-4-isothiazolin-3-oneincreases expression1
trichostatin Aaffects cotreatment, affects expression1
butyraldehydeincreases expression1
S-(1,2-dichlorovinyl)cysteineaffects response to substance, increases expression, affects cotreatment1
pentanalincreases expression1
Y 27632increases expression1
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamideaffects cotreatment, increases expression1
abrineincreases expression1
dorsomorphinincreases expression, affects cotreatment1
Resveratrolaffects cotreatment, decreases expression1
Decitabineaffects cotreatment, affects expression1
Sunitinibdecreases expression1
Aldehydesincreases expression1
Atrazineincreases expression1
Dexamethasoneaffects cotreatment, increases expression1
Diethylhexyl Phthalatedecreases expression1
Drugs, Chinese Herbalincreases expression1
Indomethacinaffects cotreatment, increases expression1
Leadaffects expression1
Lipopolysaccharidesaffects response to substance, increases expression, affects cotreatment1
Naphthoquinonesincreases expression1

ChEMBL screening assays

46 unique, capped per target: 46 binding

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL1691887BindingInhibition of human Na+/ K+ ATPase at up to 10 uMLersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1. — Antimicrob Agents Chemother

Clinical trials (associated diseases)

0 trials via MONDO — disease-level, not drug-specific.

  • Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): esophageal squamous cell carcinoma