KCNA10
geneOn this page
Also known as Kv1.8
Summary
KCNA10 (potassium voltage-gated channel subfamily A member 10, HGNC:6219) is a protein-coding gene on chromosome 1p13.3, encoding Potassium voltage-gated channel subfamily A member 10 (Q16322). Voltage-gated potassium ion channel that mediates K(+) permeability of excitable membranes. It is a selective cancer dependency (DepMap: 15.2% of cell lines).
Potassium channels represent the most complex class of voltage-gated ion channels from both functional and structural standpoints. Their diverse functions include regulating neurotransmitter release, heart rate, insulin secretion, neuronal excitability, epithelial electrolyte transport, smooth muscle contraction, and cell volume. Four sequence-related potassium channel genes - shaker, shaw, shab, and shal - have been identified in Drosophila, and each has been shown to have human homolog(s). This gene encodes a member of the potassium channel, voltage-gated, shaker-related subfamily. This member contains six membrane-spanning domains with a shaker-type repeat in the fourth segment. It is specifically regulated by cGMP and postulated to mediate the effects of substances that increase intracellular cGMP. This gene is intronless, and the gene is clustered with genes KCNA2 and KCNA3 on chromosome 1.
Source: NCBI Gene 3744 — RefSeq curated summary.
At a glance
- GWAS associations: 2
- Clinical variants (ClinVar): 93 total
- Druggable target: yes
- Cancer dependency (DepMap): dependent in 15.2% of screened cell lines
- MANE Select transcript:
NM_005549
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:6219 |
| Approved symbol | KCNA10 |
| Name | potassium voltage-gated channel subfamily A member 10 |
| Location | 1p13.3 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | Kv1.8 |
| Ensembl gene | ENSG00000143105 |
| Ensembl biotype | protein_coding |
| OMIM | 602420 |
| Entrez | 3744 |
Gene structure
Transcript identifiers
Ensembl transcripts: 1 — 1 protein_coding
ENST00000369771
RefSeq mRNA: 1 — MANE Select: NM_005549
NM_005549
CCDS: CCDS826
Canonical transcript exons
ENST00000369771 — 1 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001450849 | 110517217 | 110519175 |
Expression profiles
Bgee: expression breadth tissue_specific, 4 present calls, max score 72.76.
Top tissues by expression
225 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| buccal mucosa cell | CL:0002336 | 72.76 | gold quality |
| skeletal muscle tissue of rectus abdominis | UBERON:0004511 | 71.33 | gold quality |
| tendon of biceps brachii | UBERON:0008188 | 70.67 | gold quality |
| myocardium | UBERON:0002349 | 66.82 | gold quality |
| vena cava | UBERON:0004087 | 66.07 | gold quality |
| sperm | CL:0000019 | 65.47 | gold quality |
| skeletal muscle tissue of biceps brachii | UBERON:0004502 | 64.49 | gold quality |
| secondary oocyte | CL:0000655 | 64.24 | gold quality |
| biceps brachii | UBERON:0001507 | 63.79 | gold quality |
| oocyte | CL:0000023 | 63.63 | gold quality |
| nipple | UBERON:0002030 | 61.91 | gold quality |
| substantia nigra pars reticulata | UBERON:0001966 | 61.66 | gold quality |
| ventral tegmental area | UBERON:0002691 | 61.25 | gold quality |
| deltoid | UBERON:0001476 | 61.14 | gold quality |
| saphenous vein | UBERON:0007318 | 61.09 | gold quality |
| lateral globus pallidus | UBERON:0002476 | 60.95 | gold quality |
| substantia nigra pars compacta | UBERON:0001965 | 60.92 | gold quality |
| pharyngeal mucosa | UBERON:0000355 | 60.86 | gold quality |
| subthalamic nucleus | UBERON:0001906 | 60.59 | gold quality |
| pericardium | UBERON:0002407 | 60.40 | gold quality |
| nasal cavity epithelium | UBERON:0005384 | 60.24 | gold quality |
| inferior vagus X ganglion | UBERON:0005363 | 60.14 | gold quality |
| parotid gland | UBERON:0001831 | 60.11 | gold quality |
| cartilage tissue | UBERON:0002418 | 59.99 | gold quality |
| dorsal plus ventral thalamus | UBERON:0001897 | 59.97 | gold quality |
| cerebellar vermis | UBERON:0004720 | 59.95 | gold quality |
| thymus | UBERON:0002370 | 59.93 | gold quality |
| pylorus | UBERON:0001166 | 59.92 | gold quality |
| pons | UBERON:0000988 | 59.90 | gold quality |
| trigeminal ganglion | UBERON:0001675 | 59.88 | gold quality |
Single-cell (SCXA)
Detected in 1 experiment(s), a significant marker in 0.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | no | 0.82 |
Regulation
Is transcription factor: no
Functional genomics
DepMap (CRISPR cell-line fitness): dependent in 15.2% of screened cell lines.
Literature-anchored findings (GeneRIF, showing 2)
- KCNA10 in human proximal tubular cells, glomerular and vascular endothelial cells, and also in vascular smooth muscle cells. (PMID:12444201)
- Association of Single Nucleotide Polymorphisms in KCNA10 and SLC13A3 Genes with the Susceptibility to Chronic Kidney Disease of Unknown Etiology in Central Indian Patients. (PMID:36696070)
Cross-species orthologs
2 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| mus_musculus | Kcna10 | ENSMUSG00000042861 |
| rattus_norvegicus | Kcna10 | ENSRNOG00000050416 |
Paralogs (31): KCNG1 (ENSG00000026559), KCNQ1 (ENSG00000053918), KCNQ2 (ENSG00000075043), KCND1 (ENSG00000102057), KCNA7 (ENSG00000104848), KCNA1 (ENSG00000111262), KCNC4 (ENSG00000116396), KCNQ4 (ENSG00000117013), KCNS1 (ENSG00000124134), KCNC1 (ENSG00000129159), KCNA5 (ENSG00000130037), KCNC3 (ENSG00000131398), KCNA6 (ENSG00000151079), KCNS2 (ENSG00000156486), KCNB1 (ENSG00000158445), KCNF1 (ENSG00000162975), KCNV1 (ENSG00000164794), KCNC2 (ENSG00000166006), KCNV2 (ENSG00000168263), KCNG4 (ENSG00000168418), KCNS3 (ENSG00000170745), KCNG3 (ENSG00000171126), KCND3 (ENSG00000171385), KCNA3 (ENSG00000177272), KCNA2 (ENSG00000177301), KCNG2 (ENSG00000178342), KCNA4 (ENSG00000182255), KCNB2 (ENSG00000182674), KCNQ3 (ENSG00000184156), KCND2 (ENSG00000184408), KCNQ5 (ENSG00000185760)
Protein
Protein identifiers
Potassium voltage-gated channel subfamily A member 10 — Q16322 (reviewed: Q16322)
Alternative names: Voltage-gated potassium channel subunit Kv1.8
All UniProt accessions (1): Q16322
UniProt curated annotations — full annotation on UniProt →
Function. Voltage-gated potassium ion channel that mediates K(+) permeability of excitable membranes. When opened in response to the voltage difference across the membrane, KCNA10 channel selectively allows the flow of potassium ions across the membrane down their electrochemical gradient.
Subunit / interactions. Homotetramer. Interacts with KCN4B/POMP. Interaction with KCN4B/POMP is necessary for the modulation of channel activity by cAMP.
Subcellular location. Membrane.
Tissue specificity. Detected in kidney, in proximal tubules, glomerular endothelium, in vascular endothelium and in smooth muscle cells.
Activity regulation. The channel activity is up-regulated by cAMP.
Domain organisation. The N-terminus may be important in determining the rate of inactivation of the channel while the tail may play a role in modulation of channel activity and/or targeting of the channel to specific subcellular compartments. The segment S4 is probably the voltage-sensor and is characterized by a series of positively charged amino acids at every third position.
Similarity. Belongs to the potassium channel family. A (Shaker) (TC 1.A.1.2) subfamily. Kv1.8/KCNA10 sub-subfamily.
RefSeq proteins (1): NP_005540* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR000210 | BTB/POZ_dom | Domain |
| IPR003131 | T1-type_BTB | Domain |
| IPR003968 | K_chnl_volt-dep_Kv | Family |
| IPR003972 | K_chnl_volt-dep_Kv1 | Family |
| IPR005821 | Ion_trans_dom | Domain |
| IPR011333 | SKP1/BTB/POZ_sf | Homologous_superfamily |
| IPR027359 | Volt_channel_dom_sf | Homologous_superfamily |
| IPR028325 | VG_K_chnl | Family |
Pfam: PF00520, PF02214
Catalyzed reactions (Rhea), 1 shown:
- K(+)(in) = K(+)(out) (RHEA:29463)
UniProt features (17 total): transmembrane region 6, glycosylation site 3, sequence variant 3, region of interest 2, chain 1, lipid moiety-binding region 1, short sequence motif 1
Structure
Experimental structures (PDB)
0 structures.
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-Q16322-F1 | 77.53 | 0.53 |
Functional residue map
Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.
Post-translational modifications (1): 293
Glycosylation sites (3): 256, 334, 498
Function
Pathways and Gene Ontology
Reactome pathways
3 pathways
| ID | Pathway |
|---|---|
| R-HSA-1296072 | Voltage gated Potassium channels |
| R-HSA-112316 | Neuronal System |
| R-HSA-1296071 | Potassium Channels |
MSigDB gene sets: 54 (showing top):
GOBP_POTASSIUM_ION_TRANSPORT, REACTOME_VOLTAGE_GATED_POTASSIUM_CHANNELS, REACTOME_POTASSIUM_CHANNELS, GOBP_MONOATOMIC_CATION_TRANSPORT, GOBP_PROTEIN_HOMOOLIGOMERIZATION, GOBP_TRANSMEMBRANE_TRANSPORT, GOCC_POTASSIUM_CHANNEL_COMPLEX, GOBP_REGULATION_OF_MEMBRANE_POTENTIAL, GOCC_CATION_CHANNEL_COMPLEX, GOCC_TRANSPORTER_COMPLEX, GOCC_MEMBRANE_PROTEIN_COMPLEX, GOCC_PLASMA_MEMBRANE_PROTEIN_COMPLEX, GOMF_VOLTAGE_GATED_MONOATOMIC_CATION_CHANNEL_ACTIVITY, GOMF_METAL_ION_TRANSMEMBRANE_TRANSPORTER_ACTIVITY, GOMF_GATED_CHANNEL_ACTIVITY
GO Biological Process (7): action potential (GO:0001508), potassium ion transport (GO:0006813), protein homooligomerization (GO:0051260), potassium ion transmembrane transport (GO:0071805), monoatomic ion transport (GO:0006811), monoatomic ion transmembrane transport (GO:0034220), transmembrane transport (GO:0055085)
GO Molecular Function (6): intracellularly cyclic nucleotide-activated monoatomic cation channel activity (GO:0005221), voltage-gated potassium channel activity (GO:0005249), delayed rectifier potassium channel activity (GO:0005251), monoatomic ion channel activity (GO:0005216), potassium channel activity (GO:0005267), protein binding (GO:0005515)
GO Cellular Component (4): plasma membrane (GO:0005886), voltage-gated potassium channel complex (GO:0008076), membrane (GO:0016020), monoatomic ion channel complex (GO:0034702)
Reactome top-level categories
Rollup of top-2 pathways:
| Category | Pathways |
|---|---|
| Potassium Channels | 1 |
| Neuronal System | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| transport | 2 |
| regulation of membrane potential | 1 |
| metal ion transport | 1 |
| protein complex oligomerization | 1 |
| potassium ion transport | 1 |
| monoatomic cation transmembrane transport | 1 |
| monoatomic ion transport | 1 |
| transmembrane transport | 1 |
| cellular process | 1 |
| intracellularly ligand-gated monoatomic ion channel activity | 1 |
| cyclic nucleotide-activated monoatomic ion channel activity | 1 |
| ligand-gated monoatomic cation channel activity | 1 |
| potassium channel activity | 1 |
| voltage-gated monoatomic cation channel activity | 1 |
| voltage-gated potassium channel activity | 1 |
| monoatomic ion transmembrane transporter activity | 1 |
| channel activity | 1 |
| monoatomic cation channel activity | 1 |
| potassium ion transmembrane transporter activity | 1 |
| binding | 1 |
| membrane | 1 |
| cell periphery | 1 |
| potassium channel complex | 1 |
| plasma membrane protein complex | 1 |
| cellular anatomical structure | 1 |
| transmembrane transporter complex | 1 |
Protein interactions and networks
STRING
1360 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| KCNA10 | ZNF705D | P0CH99 | 446 |
| KCNA10 | KCNA2 | P16389 | 397 |
| KCNA10 | KCNH5 | Q8NCM2 | 396 |
| KCNA10 | KCNH8 | Q96L42 | 393 |
| KCNA10 | IQCC | Q4KMZ1 | 372 |
| KCNA10 | TPBGL | P0DKB5 | 367 |
| KCNA10 | KCNAB2 | Q13303 | 360 |
| KCNA10 | OCM2 | P0CE71 | 359 |
| KCNA10 | KCNAB1 | Q14722 | 357 |
| KCNA10 | PROSER3 | Q2NL68 | 351 |
| KCNA10 | KCNH3 | Q9ULD8 | 343 |
| KCNA10 | KCNH4 | Q9UQ05 | 342 |
| KCNA10 | SLC26A5 | P58743 | 328 |
| KCNA10 | SLC13A3 | Q8WWT9 | 325 |
| KCNA10 | CCDC9B | Q6ZUT6 | 308 |
IntAct
20 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| KCNA10 | DOLK | psi-mi:“MI:0915”(physical association) | 0.560 |
| TMBIM6 | KCNA10 | psi-mi:“MI:0915”(physical association) | 0.560 |
| KCNA1 | KCNA10 | psi-mi:“MI:0915”(physical association) | 0.560 |
| MAL | KCNA10 | psi-mi:“MI:0915”(physical association) | 0.560 |
| SGTA | KCNA10 | psi-mi:“MI:0915”(physical association) | 0.560 |
| KCNA10 | GAPDHS | psi-mi:“MI:0914”(association) | 0.530 |
| DOLK | KCNA10 | psi-mi:“MI:0915”(physical association) | 0.000 |
| TMBIM6 | KCNA10 | psi-mi:“MI:0915”(physical association) | 0.000 |
| KCNA1 | KCNA10 | psi-mi:“MI:0915”(physical association) | 0.000 |
| MAL | KCNA10 | psi-mi:“MI:0915”(physical association) | 0.000 |
| SGTA | KCNA10 | psi-mi:“MI:0915”(physical association) | 0.000 |
BioGRID (37): REEP1 (Affinity Capture-MS), EXTL2 (Affinity Capture-MS), FAM63A (Affinity Capture-MS), SLMAP (Affinity Capture-MS), NAT14 (Affinity Capture-MS), CHSY1 (Affinity Capture-MS), GOLM1 (Affinity Capture-MS), C1orf43 (Affinity Capture-MS), SLC12A9 (Affinity Capture-MS), REEP4 (Affinity Capture-MS), KCNAB2 (Affinity Capture-MS), GAPDHS (Affinity Capture-MS), LEMD2 (Affinity Capture-MS), CASP3 (Affinity Capture-MS), B3GALT6 (Affinity Capture-MS)
ESM2 similar proteins: B2RQA1, D4ADX7, G5EFC3, O35119, O35174, O88759, P08510, P10499, P15384, P15385, P16388, P16389, P16390, P17658, P17659, P19024, P22001, P22459, P22462, P22739, P25122, P34586, P48994, P63141, P63142, P79100, Q05037, Q09081, Q09470, Q14B80, Q16322, Q25452, Q28293, Q28527, Q61423, Q61762, Q61923, Q7T199, Q7TSH7, Q8BQZ8
Diamond homologs: A4K2M4, A4K2P6, A4K2T1, A4K2Y2, A6H8H5, B2RQA1, G5EFC3, O18868, O35174, O43526, O88759, O88943, O97531, P08510, P10499, P15384, P15385, P15387, P15388, P16388, P16389, P16390, P17658, P17659, P17970, P17971, P17972, P19024, P22001, P22459, P22460, P22462, P22739, P25122, P48547, P50638, P56696, P59994, P59995, P63141
SIGNOR signaling
0 interactions.
Disease & clinical
Clinical variants and AI predictions
ClinVar
93 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 86 |
| Likely benign | 2 |
| Benign | 5 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
117 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 1:110517884:T:A | donor_gain | 0.6300 |
| 1:110517919:A:T | donor_gain | 0.5400 |
| 1:110517969:C:CT | acceptor_gain | 0.5200 |
| 1:110517922:C:CT | donor_gain | 0.5100 |
| 1:110517964:TC:T | donor_gain | 0.5000 |
| 1:110517965:CC:C | donor_gain | 0.5000 |
| 1:110518040:C:CT | donor_gain | 0.4700 |
| 1:110517923:G:T | donor_gain | 0.4500 |
| 1:110517945:C:CT | donor_gain | 0.4500 |
| 1:110518041:C:CT | donor_gain | 0.4500 |
| 1:110517752:CCAGG:C | donor_gain | 0.4200 |
| 1:110517921:CCGGA:C | donor_gain | 0.4100 |
| 1:110517543:TGCC:T | donor_gain | 0.4000 |
| 1:110517601:G:C | donor_gain | 0.4000 |
| 1:110517764:T:TA | donor_gain | 0.3900 |
| 1:110517523:A:AC | donor_gain | 0.3700 |
| 1:110517524:C:CC | donor_gain | 0.3700 |
| 1:110517634:C:G | acceptor_gain | 0.3700 |
| 1:110517692:G:A | donor_gain | 0.3700 |
| 1:110517922:CGGAG:C | donor_gain | 0.3600 |
| 1:110518037:TGAC:T | donor_gain | 0.3600 |
| 1:110517636:A:T | acceptor_gain | 0.3500 |
| 1:110517486:C:A | donor_gain | 0.3400 |
| 1:110517751:A:AC | donor_gain | 0.3400 |
| 1:110517752:C:CC | donor_gain | 0.3400 |
| 1:110517822:CT:C | acceptor_gain | 0.3400 |
| 1:110517824:C:CC | acceptor_gain | 0.3400 |
| 1:110517836:T:C | acceptor_gain | 0.3400 |
| 1:110517966:C:CT | acceptor_gain | 0.3400 |
| 1:110517706:AGCC:A | donor_gain | 0.3300 |
AlphaMissense
3406 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 1:110517408:G:C | F460L | 1.000 |
| 1:110517408:G:T | F460L | 1.000 |
| 1:110517409:A:C | F460C | 1.000 |
| 1:110517409:A:G | F460S | 1.000 |
| 1:110517410:A:G | F460L | 1.000 |
| 1:110517433:G:C | P452R | 1.000 |
| 1:110517433:G:T | P452H | 1.000 |
| 1:110517436:A:G | L451P | 1.000 |
| 1:110517436:A:T | L451H | 1.000 |
| 1:110517439:G:T | A450D | 1.000 |
| 1:110517448:A:G | L447P | 1.000 |
| 1:110517448:A:T | L447H | 1.000 |
| 1:110517454:C:A | G445V | 1.000 |
| 1:110517454:C:T | G445E | 1.000 |
| 1:110517455:C:A | G445W | 1.000 |
| 1:110517455:C:G | G445R | 1.000 |
| 1:110517455:C:T | G445R | 1.000 |
| 1:110517463:G:T | A442D | 1.000 |
| 1:110517465:A:C | C441W | 1.000 |
| 1:110517466:C:T | C441Y | 1.000 |
| 1:110517467:A:G | C441R | 1.000 |
| 1:110517475:C:T | G438D | 1.000 |
| 1:110517476:C:G | G438R | 1.000 |
| 1:110517488:C:A | G434W | 1.000 |
| 1:110517502:G:T | P429Q | 1.000 |
| 1:110517514:C:A | G425V | 1.000 |
| 1:110517514:C:T | G425E | 1.000 |
| 1:110517520:C:T | G423D | 1.000 |
| 1:110517521:C:G | G423R | 1.000 |
| 1:110517535:G:A | T418I | 1.000 |
dbSNP variants (sampled 300 via entrez): RS1001793431 (1:110520962 T>G), RS1002396549 (1:110519465 C>G), RS1002743758 (1:110518494 C>G), RS1002774806 (1:110518670 G>A), RS1003193236 (1:110516767 C>G,T), RS1003747394 (1:110519781 A>C,G), RS1004826949 (1:110520916 G>C), RS1005706348 (1:110519984 G>A), RS1006190506 (1:110520801 A>G), RS1006634910 (1:110521117 A>C), RS1007410943 (1:110516948 C>T), RS1007658476 (1:110518344 A>G), RS1008344597 (1:110518040 C>A,G,T), RS1009704492 (1:110520048 G>A,T), RS1011272947 (1:110520974 C>G)
Disease associations
OMIM: gene MIM:602420 | disease phenotypes: MIM:192500
GenCC curated gene-disease
Mondo (1): familial long QT syndrome (MONDO:0019171)
Orphanet (2): Romano-Ward syndrome (Orphanet:101016), Congenital long QT syndrome (Orphanet:768)
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
2 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST003800_3 | Response to bupropion in depression | 5.000000e-07 |
| GCST008019_4 | Bitter taste perception (phenylthiocarbamide) in obesity with metabolic syndrome | 5.000000e-07 |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (2): CHEMBL2362996 (PROTEIN FAMILY), CHEMBL2363001 (SINGLE PROTEIN)
PharmGKB: 1 entry (VIP=true, CPIC=false)
GtoPdb / IUPHAR curated pharmacology
(IUPHAR/BPS Guide to Pharmacology — expert-curated)
Target class: vgic — Voltage-gated potassium channels (Kv)
Most potent curated ligand interactions (7 total), top 7:
| Ligand | Action | Affinity | Parameter |
|---|---|---|---|
| charybdotoxin | Channel blocker | 7.0 | pIC50 |
| pimozide | Channel blocker | 6.5 | pIC50 |
| ketoconazole | Channel blocker | 6.3 | pIC50 |
| verapamil | Channel blocker | 4.3 | pIC50 |
| fampridine | Channel blocker | 2.8 | pIC50 |
| Ba2+ | Channel blocker | 2.3 | pIC50 |
| tetraethylammonium | Channel blocker | 1.3 | pIC50 |
ChEMBL bioactivities
2 potent at pChembl≥5 of 2 total, top 2 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 9.82 | Ki | 0.15 | nM | CHEMBL5722941 |
| 9.74 | IC50 | 0.18 | nM | CHEMBL5722941 |
PubChem BioAssay actives
2 with measured affinity, of 35 total; 1 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.
| Compound | Assay | Type | Value | Unit |
|---|---|---|---|---|
| 3-[(1R,2aS,4S,5aS,8aS,10S,11aR,14aS,16S,17aS,19S,20aS,22S,23aS,25S,26aS,28S,29aS,31R,32aS,35aS,36R,38aS,39S,41aS,42S,44aS,45S,48R,50aS,51S,53aS,54S,56aS,57S,59aS,60S,63S,66S,69S,72S,75S,78S,87R,93S,96S,99S)-17a,20a,23a,53a,63-pentakis(4-aminobutyl)-31-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-5-carbamimidamido-2-[[(2S)-5-carbamimidamido-2-[[(2S)-1-[(2S)-5-oxopyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]pentanoyl]amino]pentanoyl]amino]hexanoyl]amino]-4-methylpentanoyl]amino]-16,29a,72,78-tetrakis(2-amino-2-oxoethyl)-14a,26a-bis(3-amino-3-oxopropyl)-2a,38a,66-tribenzyl-28,50a,57-tris[(2S)-butan-2-yl]-4,5a,19,42,45,69-hexakis(3-carbamimidamidopropyl)-51,54-bis(2-carboxyethyl)-56a,99-bis(carboxymethyl)-36-[[(2S,3S)-1-(carboxymethylamino)-3-methyl-1-oxopentan-2-yl]carbamoyl]-39,60-bis[(1R)-1-hydroxyethyl]-75,93-bis(hydroxymethyl)-32a,35a,59a-tris[(4-hydroxyphenyl)methyl]-22-(1H-imidazol-4-ylmethyl)-96-(1H-indol-3-ylmethyl)-41a-methyl-25-(2-methylpropyl)-1a,3,4a,6,7a,9,10a,13a,15,16a,18,19a,21,22a,24,25a,27,28a,30,31a,34a,37a,38,40a,41,43a,44,47,49a,50,52a,53,55a,56,58a,59,61a,62,65,68,71,74,77,80,83,86,89,92,95,98-pentacontaoxo-33,34,63a,64a,67a,68a-hexathia-a,2,3a,5,6a,8,9a,12a,14,15a,17,18a,20,21a,23,24a,26,27a,29,30a,33a,36a,37,39a,40,42a,43,46,48a,49,51a,52,54a,55,57a,58,60a,61,64,67,70,73,76,79,82,85,88,91,94,97-pentacontazapentacyclo[85.74.4.448,111.010,14.0144,148]nonahexacontahectan-8a-yl]propanoic acid | 2198828: Binding affinity to KV channel (unknown origin) assessed as inhibition constant | ki | 0.0001 | uM |
CTD chemical–gene interactions
14 total (human), top 14 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| sodium arsenite | affects methylation | 1 |
| 4-O-methyl-12-O-tetradecanoylphorbol 13-acetate | increases transport, decreases reaction | 1 |
| CGP 52608 | affects binding, increases reaction | 1 |
| Resveratrol | affects cotreatment, decreases expression | 1 |
| Arsenic | affects methylation | 1 |
| Barium | decreases reaction, increases transport | 1 |
| Benzo(a)pyrene | increases methylation | 1 |
| Pimozide | decreases reaction, increases transport | 1 |
| Plant Extracts | affects cotreatment, decreases expression | 1 |
| Potassium | decreases reaction, increases transport | 1 |
| Verapamil | decreases reaction, increases transport | 1 |
| 4-Aminopyridine | decreases reaction, increases transport | 1 |
| Aflatoxin B1 | increases methylation | 1 |
| Okadaic Acid | increases expression | 1 |
ChEMBL screening assays
22 unique, capped per target: 20 binding, 1 toxicity, 1 admet
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1787442 | Binding | Inhibition of human recombinant Kv channel at 10 uM by radioligand binding assay | Structure-activity relationships of pyrrole based S-nitrosoglutathione reductase inhibitors: pyrrole regioisomers and propionic acid replacement. — Bioorg Med Chem Lett |
| CHEMBL5522525 | Toxicity | Inhibition of human K+ channel by automated electrophysiology | Discovery of Clinical Candidate AZD5462, a Selective Oral Allosteric RXFP1 Agonist for Treatment of Heart Failure. — J Med Chem |
| CHEMBL4407437 | ADMET | Inhibition of Kv1.8 (unknown origin) at 3 uM relative to control | Discovery of 3,4,6-Trisubstituted Piperidine Derivatives as Orally Active, Low hERG Blocking Akt Inhibitors via Conformational Restriction and Structure-Based Design. — J Med Chem |
Cellosaurus cell lines
1 cell lines: 1 spontaneously immortalized cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_D1K0 | PrecisION hKv1.8-CHO | Spontaneously immortalized cell line | Female |
Clinical trials (associated diseases)
66 trials via MONDO — disease-level, not drug-specific.
| Trial | Phase | Status | Title |
|---|---|---|---|
| NCT02513940 | PHASE4 | COMPLETED | Influence of Testosterone Administration on Drug-Induced QT Interval Prolongation and Torsades de Pointes |
| NCT03834883 | PHASE4 | COMPLETED | Reducing the Risk of Drug-Induced QT Interval Lengthening in Women |
| NCT04169100 | PHASE4 | UNKNOWN | Novel Form of Acquired Long QT Syndrome |
| NCT04675788 | PHASE4 | COMPLETED | Novel Approaches for Minimizing Drug-Induced QT Interval Lengthening |
| NCT01648205 | PHASE2 | COMPLETED | Long-term Efficacy Study of Sodium Channel Blocker in LQT3 Patients |
| NCT02412709 | PHASE2 | UNKNOWN | Long QT Syndrome Screening in Newborns |
| NCT04581408 | PHASE2 | COMPLETED | Mutation-specific Therapy for the Long QT Syndrome |
| NCT00316459 | PHASE1 | COMPLETED | Study Evaluating the Effects of Multiple Oral Doses of ERB-041 on Cardiac Repolarization in Healthy Subjects |
| NCT01849003 | PHASE1 | COMPLETED | Study of the Effect of GS-6615 in Subjects With LQT-3 |
| NCT02365532 | PHASE1 | COMPLETED | Effect of Oral GS-6615 on Dofetilide-Induced QT Prolongation, Safety, and Tolerability in Healthy Adults |
| NCT02412098 | PHASE1 | COMPLETED | Pharmacokinetics of Eleclazine in Adults With Normal and Impaired Hepatic Function |
| NCT02441829 | PHASE1 | COMPLETED | Pharmacokinetics of Eleclazine in Adults With Normal and Impaired Renal Function |
| NCT05759962 | PHASE1 | COMPLETED | Phase 1 Study of LQT-1213 in Healthy Adults |
| NCT05906732 | PHASE1/PHASE2 | TERMINATED | Study of LQT-1213 on QTc-induced Prolongation in Healthy Adult Subjects (Part1) and on Congenital Long QT in Patients Diagnosed With Type 2 or 3 Long QT Syndrome (Part 2). |
| NCT00005176 | Not specified | COMPLETED | Long QT Syndrome-Population Genetics and Cardiac Studies |
| NCT00005250 | Not specified | COMPLETED | Linkage Study of Long QT Syndrome In An Amish Kindred |
| NCT00005367 | Not specified | COMPLETED | Epidemiology of Long QTand Asian Sudden Death in Sleep |
| NCT00221832 | Not specified | UNKNOWN | Molecular Genetic Screening and Identification of Congenital Arrhythmogenic Diseases |
| NCT00292032 | Not specified | COMPLETED | Registry of Unexplained Cardiac Arrest |
| NCT00335036 | Not specified | TERMINATED | Pediatric Lead Extractability and Survival Evaluation (PLEASE) |
| NCT00399412 | Not specified | COMPLETED | ECG Signal Collection From Long QT Syndrome, Wide QRS Complexes, Heart Failure, and Cardiac Resynchronization Patients |
| NCT00488254 | Not specified | COMPLETED | The Long QT Syndrome in Pregnancy |
| NCT00588965 | Not specified | COMPLETED | Effect of Beta-blocker Therapy on QTc Response in Exercise and Recovery in Normal Subjects |
| NCT01705925 | Not specified | COMPLETED | Multicenter Evaluation of Children and Young Adults With Genotype Positive Long QT Syndrome |
| NCT01903564 | Not specified | COMPLETED | Fetal and Neonatal Magnetophysiology |
| NCT02082431 | Not specified | COMPLETED | Determine the Incidence of Long QT Amongst a Large Cohort of Subjects Diagnosed With Unilateral or Bilateral Sensorineural Hearing Loss. |
| NCT02413450 | Not specified | ENROLLING_BY_INVITATION | Derivation of Human Induced Pluripotent Stem (iPS) Cells to Heritable Cardiac Arrhythmias |
| NCT02425189 | Not specified | COMPLETED | The Canadian National Long QT Syndrome Registry |
| NCT02439645 | Not specified | TERMINATED | A Registry to Determine the Clinical and Genetic Risk Factors for Torsade De Pointes |
| NCT02439658 | Not specified | UNKNOWN | Genetics of QT Prolongation With Antiarrhythmics |
| NCT02549664 | Not specified | COMPLETED | Exercise in Genetic Cardiovascular Conditions |
| NCT02581241 | Not specified | COMPLETED | Abnormal QT-Response to the Sudden Tachycardia Provoked by Standing in Individuals With Drug-induced Long QT Syndrome |
| NCT02680080 | Not specified | COMPLETED | Effect of Grapefruit on QT Interval in Healthy Volunteers and Patients With Congenital Long QT Syndrome |
| NCT02775513 | Not specified | UNKNOWN | Metabolism of Patients With Genetically Caused Cardiac Arrhythmia |
| NCT02814981 | Not specified | UNKNOWN | Hydroxyzine and Risk of Prolongation of QT Interval |
| NCT02876380 | Not specified | COMPLETED | Prospective Identification of Long QT Syndrome in Fetal Life |
| NCT03182777 | Not specified | COMPLETED | Safety of Local Dental Anesthesia in Patients With Cardiac Channelopathies |
| NCT03544918 | Not specified | COMPLETED | Prevalence of Congenital Long QT Syndrome and Acquired QT Prolongation in a Hospital Cohort |
| NCT03642405 | Not specified | UNKNOWN | Drug-induced Repolarization ECG Changes |
| NCT03678311 | Not specified | COMPLETED | Long QT Syndrome and Sleep Apnea |
Related Atlas pages
- Targeted by drugs: Barium, Dalfampridine, Ketoconazole, Pimozide, Verapamil
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): familial long QT syndrome