KCNA1
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Also known as Kv1.1RBK1HUK1MBK1
Summary
KCNA1 (potassium voltage-gated channel subfamily A member 1, HGNC:6218) is a protein-coding gene on chromosome 12p13.32, encoding Potassium voltage-gated channel subfamily A member 1 (Q09470). Voltage-gated potassium channel that mediates transmembrane potassium transport in excitable membranes, primarily in the brain and the central nervous system, but also in the kidney.
This gene encodes a voltage-gated delayed potassium channel that is phylogenetically related to the Drosophila Shaker channel. The encoded protein has six putative transmembrane segments (S1-S6), and the loop between S5 and S6 forms the pore and contains the conserved selectivity filter motif (GYGD). The functional channel is a homotetramer. The N-terminus of the channel is associated with beta subunits that can modify the inactivation properties of the channel as well as affect expression levels. The C-terminus of the channel is complexed to a PDZ domain protein that is responsible for channel targeting. Mutations in this gene have been associated with myokymia with periodic ataxia (AEMK).
Source: NCBI Gene 3736 — RefSeq curated summary.
At a glance
- Gene–disease (curated): episodic ataxia type 1 (Definitive, ClinGen) — +4 more curated relationships
- Clinical variants (ClinVar): 735 total — 25 pathogenic, 16 likely-pathogenic
- Phenotypes (HPO): 108
- Druggable target: yes — 5 molecules with ChEMBL bioactivity
- MANE Select transcript:
NM_000217
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:6218 |
| Approved symbol | KCNA1 |
| Name | potassium voltage-gated channel subfamily A member 1 |
| Location | 12p13.32 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | Kv1.1, RBK1, HUK1, MBK1 |
| Ensembl gene | ENSG00000111262 |
| Ensembl biotype | protein_coding |
| OMIM | 176260 |
| Entrez | 3736 |
Gene structure
Transcript identifiers
Ensembl transcripts: 4 — 2 protein_coding, 1 protein_coding_CDS_not_defined, 1 nonsense_mediated_decay
ENST00000382545, ENST00000543874, ENST00000639306, ENST00000639680
RefSeq mRNA: 1 — MANE Select: NM_000217
NM_000217
CCDS: CCDS8535
Canonical transcript exons
ENST00000382545 — 2 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001492547 | 4910840 | 4918256 |
| ENSE00001527108 | 4909905 | 4910472 |
Expression profiles
Bgee: expression breadth ubiquitous, 151 present calls, max score 96.12.
FANTOM5 (CAGE): breadth broad, TPM avg 1.1623 / max 73.9319, expressed in 199 samples.
FANTOM5 promoters (5 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 123593 | 0.8367 | 161 |
| 123594 | 0.1268 | 53 |
| 123595 | 0.1157 | 66 |
| 123599 | 0.0542 | 32 |
| 123598 | 0.0290 | 15 |
Top tissues by expression
275 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| endothelial cell | CL:0000115 | 96.12 | gold quality |
| Brodmann (1909) area 23 | UBERON:0013554 | 95.43 | gold quality |
| middle temporal gyrus | UBERON:0002771 | 94.17 | gold quality |
| cerebellar hemisphere | UBERON:0002245 | 93.78 | gold quality |
| cerebellar cortex | UBERON:0002129 | 93.77 | gold quality |
| primary visual cortex | UBERON:0002436 | 93.60 | gold quality |
| right hemisphere of cerebellum | UBERON:0014890 | 93.35 | gold quality |
| lateral nuclear group of thalamus | UBERON:0002736 | 92.92 | gold quality |
| cerebellum | UBERON:0002037 | 92.44 | gold quality |
| postcentral gyrus | UBERON:0002581 | 92.02 | gold quality |
| putamen | UBERON:0001874 | 91.42 | gold quality |
| parietal lobe | UBERON:0001872 | 90.97 | gold quality |
| caudate nucleus | UBERON:0001873 | 90.92 | gold quality |
| pons | UBERON:0000988 | 90.33 | gold quality |
| occipital lobe | UBERON:0002021 | 89.84 | gold quality |
| dorsal root ganglion | UBERON:0000044 | 89.25 | gold quality |
| lateral globus pallidus | UBERON:0002476 | 88.50 | gold quality |
| dorsolateral prefrontal cortex | UBERON:0009834 | 88.20 | gold quality |
| Brodmann (1909) area 9 | UBERON:0013540 | 88.19 | gold quality |
| nucleus accumbens | UBERON:0001882 | 88.15 | gold quality |
| superior frontal gyrus | UBERON:0002661 | 87.47 | gold quality |
| right frontal lobe | UBERON:0002810 | 87.13 | gold quality |
| cerebellar vermis | UBERON:0004720 | 85.61 | gold quality |
| Ammon’s horn | UBERON:0001954 | 85.47 | gold quality |
| prefrontal cortex | UBERON:0000451 | 85.30 | gold quality |
| telencephalon | UBERON:0001893 | 84.83 | gold quality |
| frontal cortex | UBERON:0001870 | 84.39 | gold quality |
| cerebral cortex | UBERON:0000956 | 84.15 | gold quality |
| cingulate cortex | UBERON:0003027 | 84.13 | gold quality |
| anterior cingulate cortex | UBERON:0009835 | 83.91 | gold quality |
Single-cell (SCXA)
Detected in 1 experiment(s), a significant marker in 1.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | yes | 3.93 |
Regulation
Is transcription factor: no
Upstream regulators (CollecTRI, top): IRF6, NFYA, NFYB, SPI1, YBX1, YBX3
miRNA regulators (miRDB)
278 targeting KCNA1, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):
| miRNA | Max score | Avg score | miRNA target_count |
|---|---|---|---|
| HSA-MIR-3163 | 100.00 | 77.23 | 8605 |
| HSA-MIR-4262 | 100.00 | 73.26 | 3931 |
| HSA-MIR-3646 | 100.00 | 73.56 | 5283 |
| HSA-MIR-4682 | 100.00 | 68.89 | 1258 |
| HSA-MIR-9-5P | 100.00 | 72.28 | 2361 |
| HSA-MIR-7110-3P | 100.00 | 73.18 | 2486 |
| HSA-MIR-6873-3P | 100.00 | 71.42 | 2626 |
| HSA-MIR-12118 | 100.00 | 65.88 | 1270 |
| HSA-MIR-6758-5P | 100.00 | 66.21 | 1470 |
| HSA-MIR-6856-5P | 100.00 | 65.47 | 1298 |
| HSA-MIR-181A-5P | 99.99 | 72.96 | 2995 |
| HSA-MIR-181B-5P | 99.99 | 72.97 | 2996 |
| HSA-MIR-181C-5P | 99.99 | 72.95 | 2996 |
| HSA-MIR-181D-5P | 99.99 | 73.04 | 2997 |
| HSA-MIR-4282 | 99.99 | 75.36 | 6408 |
| HSA-MIR-6077 | 99.99 | 68.04 | 2299 |
| HSA-MIR-3662 | 99.99 | 73.82 | 5684 |
| HSA-MIR-548AW | 99.99 | 72.57 | 3559 |
| HSA-MIR-8068 | 99.98 | 73.85 | 2376 |
| HSA-MIR-12136 | 99.98 | 72.81 | 5713 |
| HSA-MIR-32-5P | 99.98 | 75.21 | 1964 |
| HSA-MIR-92A-3P | 99.98 | 75.21 | 1960 |
| HSA-MIR-92B-3P | 99.98 | 75.25 | 1955 |
| HSA-MIR-520D-5P | 99.98 | 73.34 | 4883 |
| HSA-MIR-524-5P | 99.98 | 73.43 | 4882 |
| HSA-MIR-25-3P | 99.98 | 74.60 | 1817 |
| HSA-MIR-363-3P | 99.98 | 74.72 | 1821 |
| HSA-MIR-367-3P | 99.98 | 74.83 | 1819 |
| HSA-MIR-27A-3P | 99.98 | 72.13 | 2955 |
| HSA-MIR-27B-3P | 99.98 | 72.13 | 2955 |
Literature-anchored findings (GeneRIF, showing 40)
- Variable K(+) channel subunit dysfunction in inherited mutations of KCNA1 (PMID:11773313)
- missense mutation involved in episodic ataxia type 1 (PMID:11960817)
- I177N, mutation in S1 segment, alters the expression and gating properties of channel expressed in Xenopus oocytes. (PMID:12799903)
- Results describe an erbstatin (Erb) analogue as a small molecule inhibitor of the N-type inactivation in potassium channels Kv1.4 and Kv1.1+Kvbeta1. (PMID:15136567)
- This study report an unusual family in which the same point mutation in the voltage-gated potassium channel gene KCNA1 resulted in markedly different clinical phenotypes. (PMID:15351427)
- coupling between calcium influx and inactivation of voltage-gated A-type K+ channels occurs as a result of membrane depolarization and may contribute to afterhyperpolarization as negative feedback to control neuronal excitability (PMID:15486093)
- Results identify palmitoylation as a mechanism for K(+) channel interactions with plasma membrane lipids contributing to electric field-induced conformational alterations. (PMID:15837928)
- Myokymia is an autosomal dominant trait caused by mutations in KCNA1, encoding a voltage-gated potassium channel. (PMID:17136396)
- This study identified a novel 3-nucleotide deletion mutation in KCNA1 in the episodic ataxia with paroxysmal dyspnea. (PMID:17912752)
- The spectrum of neurologic manifestations and neoplasms associated with voltage-gated potassium channel (VGKC) autoimmunity is broader than previously recognized (PMID:18474843)
- A novel missense mutation (F414C) KCNA1 identified in an Italian family affected by episodic ataxia type 1. (PMID:18926884)
- Contribution of the central hydrophobic residue in the PXP motif of voltage-dependent K+ channels, KCNA1, to S6 flexibility and gating properties. (PMID:19202350)
- This study suggested that KCNA1 mutations are associated with a broader clinical phenotype, which may include persistent cerebellar dysfunction and cognitive delay. (PMID:19205071)
- studied a family with isolated autosomal dominant hypomagnesemia and used a positional cloning approach to identify an N255D mutation in KCNA1 (PMID:19307729)
- An asparagine at position 255 in Kv1.1 is required for normal voltage dependence and kinetics of channel gating. (PMID:19903818)
- The occurrence of epilepsy in 1 of 2 families with the F414S mutation suggests an interplay of KCNA1 with other genetic factors (PMID:20660867)
- integrative genomics approach to a large cohort of medulloblastomas has identified four disparate subgroups (KCNA1)with distinct demographics, clinical presentation, transcriptional profiles, genetic abnormalities, and clinical outcome. (PMID:20823417)
- Studies of nerve excitability can identify K(v)1.1 dysfunction in patients with episodic ataxia type 1 (PMID:21106501)
- Data suggest that episodic ataxia type 1 mutations affect fast inactivation of Kv1.1/1.4 channels by a reduction in either subunit surface expression or altered affinity for the inactivation domain. (PMID:21307345)
- Kv1.1 channels are expressed in the beta-cells of several species (PMID:21483673)
- This study suggested that kcna1 missense mutation have been related to Episodic ataxias 1. (PMID:21827920)
- Editing of K(V)1.1 channel mRNAs disrupts binding of the N-terminus tip at the intracellular cavity. (PMID:21847110)
- NRG1 increased the intrinsic excitability of FS-PV interneurons which was mediated by increasing the near-threshold responsiveness and decreasing the voltage threshold for action potentials through Kv1.1 (PMID:22158511)
- characterization of mutations in the potassium channel Kv1.1 (PMID:22609616)
- New mutations (R167M, C185W and I407M) were identified in three out of the four families. When expressed in human embryonic kidney cells, all three new mutations resulted in a loss of K(v)1.1 channel function. (PMID:23349320)
- Novel mutations in KCNA1 genes are associated with episodic ataxia type 1. (PMID:24275721)
- The combination of copy number variant and SNPs in KCNA1 (and SCN1A) genes increased the risk for both epilepsy and premature death. (PMID:24372310)
- Using mutagenesis and analysis of gating currents from gating pore mutations in the Shaker Kv channel, we identified statistically highly significant correlations between VSD function and physicochemical properties of gating pore residues. (PMID:24782544)
- Fine-tuning of Kv1.1 surface expression by RNA editing might contribute to the complexity of neuronal Kv channel regulation. (PMID:25100718)
- These findings provide evidence of an intrinsic cardiac role of Kv1.1 channels and indicate that they may contribute to atrial repolarization and atrial fibrillation susceptibility. (PMID:26162324)
- KCNA1 mutations should be considered in patients of all ages with episodic neurological phenotypes, even when ataxia is not present. (PMID:26395884)
- we demonstrate that the pathophysiological impact of the I262T mutation entails altered channel gating and defective protein biosynthesis, both of which raise imperative questions that call for further elucidation of the structural and functional roles of the S3 transmembrane segment in Kv1.1 channels. (PMID:26778656)
- Herein, we critically evaluate the molecular and biophysical characteristics of the KV1.1 protein in comparison with others and discuss their role in the greater penetrance of KCNA1 mutations in humans leading to the neurological signs of episodic ataxia type 1 (PMID:26825872)
- Study reports a novel KCNA1 mutation associated with an episodic ataxia type 1 phenotype and a possible association with malignant hyperthermia (MH). The current report broadens the phenotypes associated with KCNA1 mutations to include possible susceptibility to MH. (PMID:27271339)
- Mutation p.Arg324Thr in the KCNA1 gene is pathogenic and results in episodic ataxia type 1 through a dominant-negative effect. (PMID:27477325)
- Pharmacogenetic and case-control study evaluated the role of the variants of KCNA1, KCNA2, and KCNV2 in the susceptibility and drug resistance of genetic generalized epilepsies and revealed no significant association between 8 variants of KCNA1, KCNA2, and KCNV2 genes and risk or drug resistance of genetic generalized epilepsies after a Bonferroni correction for multiple comparisons. (PMID:28658141)
- A novel Kv1.1 mutation E283K is associated with a broader EA1 phenotype. Mutant channels show slower activation and positively shifted voltage dependence. (PMID:28666963)
- we found a new mutation in KCNA1 (F303V) and demonstrated that the reduced current amplitudes and altered gating properties of the channel account for its pathophysiological impact. (PMID:28676720)
- Pathogenic mutation in KCNA1 gene is associated with Episodic Ataxia. (PMID:29062094)
- study suggests that these mutations in KCNA1 cause the Kv1.1 channel dysfunction, which leads to familial paroxysmal kinesigenic dyskinesia (PMID:29294000)
Cross-species orthologs
4 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | kcna1b | ENSDARG00000017108 |
| danio_rerio | kcna1a | ENSDARG00000062942 |
| mus_musculus | Kcna1 | ENSMUSG00000047976 |
| rattus_norvegicus | Kcna1 | ENSRNOG00000064052 |
Paralogs (31): KCNG1 (ENSG00000026559), KCNQ1 (ENSG00000053918), KCNQ2 (ENSG00000075043), KCND1 (ENSG00000102057), KCNA7 (ENSG00000104848), KCNC4 (ENSG00000116396), KCNQ4 (ENSG00000117013), KCNS1 (ENSG00000124134), KCNC1 (ENSG00000129159), KCNA5 (ENSG00000130037), KCNC3 (ENSG00000131398), KCNA10 (ENSG00000143105), 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 1 — Q09470 (reviewed: Q09470)
Alternative names: Voltage-gated K(+) channel HuKI, Voltage-gated potassium channel HBK1, Voltage-gated potassium channel subunit Kv1.1
All UniProt accessions (3): Q09470, A0A1W2PQM4, A0A1W2PRI2
UniProt curated annotations — full annotation on UniProt →
Function. Voltage-gated potassium channel that mediates transmembrane potassium transport in excitable membranes, primarily in the brain and the central nervous system, but also in the kidney. Contributes to the regulation of the membrane potential and nerve signaling, and prevents neuronal hyperexcitability. Forms tetrameric potassium-selective channels through which potassium ions pass in accordance with their electrochemical gradient. The channel alternates between opened and closed conformations in response to the voltage difference across the membrane. Can form functional homotetrameric channels and heterotetrameric channels that contain variable proportions of KCNA1, KCNA2, KCNA4, KCNA5, KCNA6, KCNA7, and possibly other family members as well; channel properties depend on the type of alpha subunits that are part of the channel. Channel properties are modulated by cytoplasmic beta subunits that regulate the subcellular location of the alpha subunits and promote rapid inactivation of delayed rectifier potassium channels. In vivo, membranes probably contain a mixture of heteromeric potassium channel complexes, making it difficult to assign currents observed in intact tissues to any particular potassium channel family member. Homotetrameric KCNA1 forms a delayed-rectifier potassium channel that opens in response to membrane depolarization, followed by slow spontaneous channel closure. In contrast, a heterotetrameric channel formed by KCNA1 and KCNA4 shows rapid inactivation. Regulates neuronal excitability in hippocampus, especially in mossy fibers and medial perforant path axons, preventing neuronal hyperexcitability. Response to toxins that are selective for KCNA1, respectively for KCNA2, suggests that heteromeric potassium channels composed of both KCNA1 and KCNA2 play a role in pacemaking and regulate the output of deep cerebellar nuclear neurons. May function as down-stream effector for G protein-coupled receptors and inhibit GABAergic inputs to basolateral amygdala neurons. May contribute to the regulation of neurotransmitter release, such as gamma-aminobutyric acid (GABA) release. Plays a role in regulating the generation of action potentials and preventing hyperexcitability in myelinated axons of the vagus nerve, and thereby contributes to the regulation of heart contraction. Required for normal neuromuscular responses. Regulates the frequency of neuronal action potential firing in response to mechanical stimuli, and plays a role in the perception of pain caused by mechanical stimuli, but does not play a role in the perception of pain due to heat stimuli. Required for normal responses to auditory stimuli and precise location of sound sources, but not for sound perception. The use of toxins that block specific channels suggest that it contributes to the regulation of the axonal release of the neurotransmitter dopamine. Required for normal postnatal brain development and normal proliferation of neuronal precursor cells in the brain. Plays a role in the reabsorption of Mg(2+) in the distal convoluted tubules in the kidney and in magnesium ion homeostasis, probably via its effect on the membrane potential.
Subunit / interactions. Homotetramer and heterotetramer with other channel-forming alpha subunits, such as KCNA2, KCNA4, KCNA5, KCNA6 and KCNA7. Channel activity is regulated by interaction with the beta subunits KCNAB1 and KCNAB2. Identified in a complex with KCNA2 and KCNAB2. Interacts (via C-terminus) with the PDZ domains of DLG1, DLG2 and DLG4. Interacts with LGI1 within a complex containing LGI1, KCNA4 and KCNAB1. Interacts (via N-terminus) with STX1A; this promotes channel inactivation. Interacts (via N-terminus) with the heterodimer formed by GNB1 and GNG2; this promotes channel inactivation. Can interact simultaneously with STX1A and the heterodimer formed by GNB1 and GNG2. Interacts (via cytoplasmic N-terminal domain) with KCNRG; this inhibits channel activity. Interacts with ANK3; this inhibits channel activity. Interacts with ADAM11.
Subcellular location. Cell membrane. Membrane. Cell projection. Axon. Cytoplasmic vesicle. Perikaryon. Endoplasmic reticulum. Dendrite. Cell junction. Synapse. Presynaptic cell membrane. Presynapse.
Tissue specificity. Detected adjacent to nodes of Ranvier in juxtaparanodal zones in spinal cord nerve fibers, but also in paranodal regions in some myelinated spinal cord axons (at protein level). Detected in the islet of Langerhans.
Post-translational modifications. N-glycosylated. Palmitoylated on Cys-243; which may be required for membrane targeting. Phosphorylated on tyrosine residues. Phosphorylation increases in response to NRG1; this inhibits channel activity. Phosphorylation at Ser-446 regulates channel activity by down-regulating expression at the cell membrane.
Disease relevance. Episodic ataxia 1 (EA1) [MIM:160120] An autosomal dominant disorder characterized by brief episodes of ataxia and dysarthria. Neurological examination during and between the attacks demonstrates spontaneous, repetitive discharges in the distal musculature (myokymia) that arise from peripheral nerve. Nystagmus is absent. The disease is caused by variants affecting the gene represented in this entry. Myokymia isolated 1 (MK1) [MIM:160120] A condition characterized by spontaneous involuntary contraction of muscle fiber groups that can be observed as vermiform movement of the overlying skin. Electromyography typically shows continuous motor unit activity with spontaneous oligo- and multiplet-discharges of high intraburst frequency (myokymic discharges). Isolated spontaneous muscle twitches occur in many persons and have no grave significance. The disease is caused by variants affecting the gene represented in this entry.
Activity regulation. Inhibited by 1.1 mM 4-aminopyridine (4-AP) and by 20 mM tetraethylammonium (TEA), but not by charybdotoxin (CTX). Inhibited by dendrotoxin (DTX).
Domain organisation. The cytoplasmic N-terminus is important for tetramerization and for interaction with the beta subunits that promote rapid channel closure. The transmembrane segment S4 functions as a voltage-sensor and is characterized by a series of positively charged amino acids at every third position. Channel opening and closing is effected by a conformation change that affects the position and orientation of the voltage-sensor paddle formed by S3 and S4 within the membrane. A transmembrane electric field that is positive inside would push the positively charged S4 segment outwards, thereby opening the pore, while a field that is negative inside would pull the S4 segment inwards and close the pore. Changes in the position and orientation of S4 are then transmitted to the activation gate formed by the inner helix bundle via the S4-S5 linker region.
Miscellaneous. The delay or D-type current observed in hippocampus pyramidal neurons is probably mediated by potassium channels containing KCNA2 plus KCNA1 or other family members. It is activated at about -50 mV, i.e. below the action potential threshold, and is characterized by slow inactivation, extremely slow recovery from inactivation, sensitivity to dendrotoxin (DTX) and to 4-aminopyridine (4-AP).
Similarity. Belongs to the potassium channel family. A (Shaker) (TC 1.A.1.2) subfamily. Kv1.1/KCNA1 sub-subfamily.
RefSeq proteins (1): NP_000208* (*=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 |
| IPR004048 | K_chnl_volt-dep_Kv1.1 | 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 (61 total): sequence variant 20, mutagenesis site 9, topological domain 8, transmembrane region 6, modified residue 5, region of interest 3, sequence conflict 3, intramembrane region 2, short sequence motif 2, chain 1, lipid moiety-binding region 1, glycosylation site 1
Structure
Experimental structures (PDB)
0 structures.
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-Q09470-F1 | 78.74 | 0.55 |
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 (6): 23, 322, 437, 439, 446, 243
Glycosylation sites (1): 207
Mutagenesis-validated functional residues (9):
| Position | Phenotype |
|---|---|
| 35–36 | no effect on palmitoylation, no effect on current kinetics. |
| 177 | slows down n-type inactivation of heteromeric channels formed by kcna1 and kcna4. |
| 243 | strongly decreases palmitoylation and alters current kinetics. |
| 255 | slightly increases channel activity, but does not affect expression at the cell membrane. |
| 255 | abolishes channel activity, but does not affect expression at the cell membrane. |
| 255 | strongly reduces channel activity, but does not affect expression at the cell membrane. |
| 255 | no effect on channel activity. |
| 446 | impairs phosphorylation by pka. |
| 446 | impairs expression at the cell membrane. |
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: 473 (showing top):
GSE37336_LY6C_POS_VS_NEG_NAIVE_CD4_TCELL_DN, GOBP_POTASSIUM_ION_TRANSPORT, RRAGTTGT_UNKNOWN, BENPORATH_ES_WITH_H3K27ME3, REACTOME_VOLTAGE_GATED_POTASSIUM_CHANNELS, GOBP_SENSORY_PERCEPTION_OF_MECHANICAL_STIMULUS, REACTOME_POTASSIUM_CHANNELS, GOBP_DETECTION_OF_MECHANICAL_STIMULUS_INVOLVED_IN_SENSORY_PERCEPTION, BIOCARTA_BARRESTIN_SRC_PATHWAY, GOCC_CELL_SURFACE, GOBP_NEUROGENESIS, AP2_Q3, GGGTGGRR_PAX4_03, EFC_Q6, GOBP_FOREBRAIN_DEVELOPMENT
GO Biological Process (22): action potential (GO:0001508), startle response (GO:0001964), regulation of muscle contraction (GO:0006937), neuroblast proliferation (GO:0007405), cell communication by electrical coupling (GO:0010644), magnesium ion homeostasis (GO:0010960), neuronal action potential (GO:0019228), hippocampus development (GO:0021766), neuronal signal transduction (GO:0023041), regulation of membrane potential (GO:0042391), neuromuscular process (GO:0050905), detection of mechanical stimulus involved in sensory perception of pain (GO:0050966), detection of mechanical stimulus involved in sensory perception of touch (GO:0050976), protein homooligomerization (GO:0051260), cellular response to magnesium ion (GO:0071286), potassium ion transmembrane transport (GO:0071805), membrane repolarization during action potential (GO:0086011), monoatomic ion transport (GO:0006811), potassium ion transport (GO:0006813), brain development (GO:0007420), monoatomic ion transmembrane transport (GO:0034220), transmembrane transport (GO:0055085)
GO Molecular Function (6): voltage-gated potassium channel activity (GO:0005249), delayed rectifier potassium channel activity (GO:0005251), disordered domain specific binding (GO:0097718), monoatomic ion channel activity (GO:0005216), potassium channel activity (GO:0005267), protein binding (GO:0005515)
GO Cellular Component (22): endoplasmic reticulum (GO:0005783), cytosol (GO:0005829), plasma membrane (GO:0005886), voltage-gated potassium channel complex (GO:0008076), cell surface (GO:0009986), membrane (GO:0016020), cell junction (GO:0030054), dendrite (GO:0030425), cytoplasmic vesicle (GO:0031410), paranode region of axon (GO:0033270), presynaptic membrane (GO:0042734), neuronal cell body (GO:0043025), axon initial segment (GO:0043194), perikaryon (GO:0043204), axon terminus (GO:0043679), juxtaparanode region of axon (GO:0044224), synapse (GO:0045202), anchoring junction (GO:0070161), axon (GO:0030424), monoatomic ion channel complex (GO:0034702), cell projection (GO:0042995), presynapse (GO:0098793)
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 |
|---|---|
| cellular anatomical structure | 8 |
| cytoplasm | 3 |
| main axon | 3 |
| action potential | 2 |
| detection of mechanical stimulus involved in sensory perception | 2 |
| neuron projection | 2 |
| presynapse | 2 |
| cell junction | 2 |
| regulation of membrane potential | 1 |
| response to external stimulus | 1 |
| neuromuscular process | 1 |
| muscle contraction | 1 |
| regulation of muscle system process | 1 |
| generation of neurons | 1 |
| neural precursor cell proliferation | 1 |
| cell communication | 1 |
| monoatomic cation homeostasis | 1 |
| inorganic ion homeostasis | 1 |
| transmission of nerve impulse | 1 |
| pallium development | 1 |
| limbic system development | 1 |
| anatomical structure development | 1 |
| signal transduction | 1 |
| monoatomic ion transmembrane transport | 1 |
| regulation of biological quality | 1 |
| nervous system process | 1 |
| sensory perception of pain | 1 |
| sensory perception of touch | 1 |
| protein complex oligomerization | 1 |
| response to magnesium ion | 1 |
| cellular response to metal ion | 1 |
| potassium ion transport | 1 |
| monoatomic cation transmembrane transport | 1 |
| membrane repolarization | 1 |
| transport | 1 |
| metal ion transport | 1 |
| central nervous system development | 1 |
| animal organ development | 1 |
| head development | 1 |
| potassium channel activity | 1 |
Protein interactions and networks
STRING
2963 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| KCNA1 | LGI1 | O95970 | 989 |
| KCNA1 | KCNAB1 | Q14722 | 987 |
| KCNA1 | KCNAB2 | Q13303 | 985 |
| KCNA1 | KCNA2 | P16389 | 982 |
| KCNA1 | CNTNAP2 | Q9UHC6 | 978 |
| KCNA1 | KCNA6 | P17658 | 976 |
| KCNA1 | KCNA4 | P22459 | 969 |
| KCNA1 | CNTN2 | P78432 | 948 |
| KCNA1 | STX1A | Q16623 | 904 |
| KCNA1 | CACNA1A | P78510 | 866 |
| KCNA1 | KCNA3 | P22001 | 859 |
| KCNA1 | SCN8A | Q9UQD0 | 826 |
| KCNA1 | ADAM22 | Q9P0K1 | 823 |
| KCNA1 | SHPK | Q9UHJ6 | 792 |
| KCNA1 | SCN2A | Q99250 | 791 |
IntAct
168 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| KCNA1 | DLG4 | psi-mi:“MI:0407”(direct interaction) | 0.680 |
| DLG4 | KCNA1 | psi-mi:“MI:0407”(direct interaction) | 0.680 |
| MAL | KCNA1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| KCNA1 | IER3IP1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| KCNA1 | TMEM14B | psi-mi:“MI:0915”(physical association) | 0.560 |
| KCNA1 | TMEM86A | psi-mi:“MI:0915”(physical association) | 0.560 |
| KCNA1 | DOLK | psi-mi:“MI:0915”(physical association) | 0.560 |
| KCNA1 | JAGN1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| SGTA | KCNA1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| KCNA1 | KCNA10 | psi-mi:“MI:0915”(physical association) | 0.560 |
| KCNA3 | KCNA1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| KCNA1 | psi-mi:“MI:0915”(physical association) | 0.560 | |
| GPR42 | KCNA1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| KCNA1 | GPR152 | psi-mi:“MI:0915”(physical association) | 0.560 |
| KCNA1 | APOL2 | psi-mi:“MI:0915”(physical association) | 0.560 |
| KCNA1 | MAST2 | psi-mi:“MI:0407”(direct interaction) | 0.440 |
| KCNA1 | DLG3 | psi-mi:“MI:0407”(direct interaction) | 0.440 |
| KCNA1 | ARHGEF12 | psi-mi:“MI:0407”(direct interaction) | 0.440 |
| KCNA1 | DLG1 | psi-mi:“MI:0407”(direct interaction) | 0.440 |
| PDZD7 | KCNA1 | psi-mi:“MI:0407”(direct interaction) | 0.440 |
| KCNA1 | MAST1 | psi-mi:“MI:0407”(direct interaction) | 0.440 |
| DLG2 | KCNA1 | psi-mi:“MI:0407”(direct interaction) | 0.440 |
| KCNA1 | ARHGEF11 | psi-mi:“MI:0407”(direct interaction) | 0.440 |
| TAX1BP3 | KCNA1 | psi-mi:“MI:0407”(direct interaction) | 0.440 |
| KCNA1 | MAGI1 | psi-mi:“MI:0407”(direct interaction) | 0.440 |
| MAGI3 | KCNA1 | psi-mi:“MI:0407”(direct interaction) | 0.440 |
| DLG1 | KCNA1 | psi-mi:“MI:0407”(direct interaction) | 0.440 |
| KCNA1 | PDZD2 | psi-mi:“MI:0407”(direct interaction) | 0.440 |
BioGRID (26): KCNA1 (Affinity Capture-Western), KCNA1 (Affinity Capture-Western), KCNA1 (Affinity Capture-MS), KCNA1 (Two-hybrid), GPR42 (Two-hybrid), APOL2 (Two-hybrid), IER3IP1 (Two-hybrid), TMEM14B (Two-hybrid), KCNA10 (Two-hybrid), TMEM86A (Two-hybrid), FCER1G (Two-hybrid), JAGN1 (Two-hybrid), MAL (Two-hybrid), DOLK (Two-hybrid), GPR152 (Two-hybrid)
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: A2BDX4, A4K2M4, A4K2N8, A4K2P6, A4K2Q6, A4K2R3, A4K2S2, A4K2T1, A4K2V2, A4K2W6, A4K2X4, A4K2Y2, A6H8H5, D4AD53, D4ADX7, G5EFC3, O18868, O35173, O35174, O73606, O88758, O88759, P10499, P15384, P15385, P15387, P15388, P16388, P16390, P17970, P17971, P17972, P22001, P22459, P22739, P25122, P48547, P59053, P59994, P59995
SIGNOR signaling
1 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| PKA | “down-regulates quantity” | KCNA1 | phosphorylation |
Enriched among interaction partners
Reactome pathways and GO biological processes over-represented among this gene’s 93 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.
Reactome pathways:
| Pathway | Partners | Fold | FDR |
|---|---|---|---|
| Ras activation upon Ca2+ influx through NMDA receptor | 5 | 50.1× | 2e-06 |
| Unblocking of NMDA receptors, glutamate binding and activation | 5 | 47.7× | 2e-06 |
| Negative regulation of NMDA receptor-mediated neuronal transmission | 5 | 47.7× | 2e-06 |
| Long-term potentiation | 5 | 41.7× | 3e-06 |
| Assembly and cell surface presentation of NMDA receptors | 9 | 40.1× | 8e-11 |
| Neurexins and neuroligins | 10 | 34.5× | 4e-11 |
| Protein-protein interactions at synapses | 6 | 28.0× | 2e-06 |
| RHOB GTPase cycle | 5 | 13.5× | 6e-04 |
GO biological processes:
| GO term | Partners | Fold | FDR |
|---|---|---|---|
| establishment or maintenance of epithelial cell apical/basal polarity | 11 | 72.6× | 8e-16 |
| protein localization to synapse | 6 | 52.2× | 2e-07 |
| receptor clustering | 7 | 49.6× | 2e-08 |
| regulation of postsynaptic membrane neurotransmitter receptor levels | 7 | 39.4× | 8e-08 |
| protein-containing complex assembly | 9 | 11.7× | 5e-06 |
| cell-cell adhesion | 10 | 11.5× | 1e-06 |
| regulation of small GTPase mediated signal transduction | 5 | 8.2× | 8e-03 |
| chemical synaptic transmission | 7 | 6.2× | 4e-03 |
Disease & clinical
Clinical variants and AI predictions
ClinVar
735 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 25 |
| Likely pathogenic | 16 |
| Uncertain significance | 433 |
| Likely benign | 176 |
| Benign | 40 |
Top pathogenic / likely-pathogenic (30)
| Variant ID | HGVS | Classification |
|---|---|---|
| 13480 | NM_000217.3(KCNA1):c.1223T>C (p.Val408Ala) | Pathogenic |
| 13481 | NM_000217.3(KCNA1):c.715C>A (p.Arg239Ser) | Pathogenic |
| 13482 | NM_000217.3(KCNA1):c.520G>T (p.Val174Phe) | Pathogenic |
| 13483 | NM_000217.3(KCNA1):c.745T>A (p.Phe249Ile) | Pathogenic |
| 13484 | NM_000217.3(KCNA1):c.551T>G (p.Phe184Cys) | Pathogenic |
| 13485 | NM_000217.3(KCNA1):c.975G>C (p.Glu325Asp) | Pathogenic |
| 13486 | NM_000217.3(KCNA1):c.676A>G (p.Thr226Ala) | Pathogenic |
| 13487 | NM_000217.3(KCNA1):c.1210G>A (p.Val404Ile) | Pathogenic |
| 13488 | NM_000217.3(KCNA1):c.530T>A (p.Ile177Asn) | Pathogenic |
| 13489 | NM_000217.3(KCNA1):c.724G>C (p.Ala242Pro) | Pathogenic |
| 13490 | NM_000217.3(KCNA1):c.731C>A (p.Pro244His) | Pathogenic |
| 13491 | NM_000217.3(KCNA1):c.1249C>T (p.Arg417Ter) | Pathogenic |
| 13492 | NM_000217.3(KCNA1):c.677C>G (p.Thr226Arg) | Pathogenic |
| 13493 | NM_000217.3(KCNA1):c.677C>A (p.Thr226Lys) | Pathogenic |
| 13494 | NM_000217.3(KCNA1):c.763A>G (p.Asn255Asp) | Pathogenic |
| 1411967 | NM_000217.3(KCNA1):c.1126G>A (p.Gly376Ser) | Pathogenic |
| 1452721 | NM_000217.3(KCNA1):c.850C>T (p.Gln284Ter) | Pathogenic |
| 1697293 | NM_000217.3(KCNA1):c.847G>A (p.Glu283Lys) | Pathogenic |
| 1879222 | NM_000217.3(KCNA1):c.781G>A (p.Ala261Thr) | Pathogenic |
| 21127 | NM_000217.3(KCNA1):c.677C>T (p.Thr226Met) | Pathogenic |
| 2500186 | NM_000217.3(KCNA1):c.1102G>C (p.Val368Leu) | Pathogenic |
| 2910304 | NM_000217.3(KCNA1):c.1207C>T (p.Pro403Ser) | Pathogenic |
| 3340603 | NM_000217.3(KCNA1):c.932G>A (p.Gly311Asp) | Pathogenic |
| 4057247 | NM_000217.3(KCNA1):c.941T>A (p.Ile314Asn) | Pathogenic |
| 447609 | NM_000217.3(KCNA1):c.1214C>T (p.Pro405Leu) | Pathogenic |
| 1098715 | NM_000217.3(KCNA1):c.1186G>C (p.Gly396Arg) | Likely pathogenic |
| 1176598 | NM_000217.3(KCNA1):c.893G>C (p.Arg298Thr) | Likely pathogenic |
| 1805796 | NM_000217.3(KCNA1):c.985C>A (p.Leu329Ile) | Likely pathogenic |
| 1994858 | NM_000217.3(KCNA1):c.985C>T (p.Leu329Phe) | Likely pathogenic |
| 2576584 | NM_000217.3(KCNA1):c.863T>A (p.Leu288Gln) | Likely pathogenic |
SpliceAI
201 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 12:4910469:CCAGG:C | donor_loss | 0.9500 |
| 12:4910470:CAGG:C | donor_loss | 0.9500 |
| 12:4910471:AG:A | donor_loss | 0.9500 |
| 12:4910472:GGTAG:G | donor_loss | 0.9500 |
| 12:4910473:GTAGG:G | donor_loss | 0.9500 |
| 12:4910474:T:A | donor_loss | 0.9500 |
| 12:4915854:T:TA | acceptor_gain | 0.7600 |
| 12:4915850:ACCGT:A | acceptor_gain | 0.7500 |
| 12:4913723:T:G | donor_gain | 0.6600 |
| 12:4910242:A:T | donor_gain | 0.6400 |
| 12:4910473:G:GG | donor_gain | 0.6300 |
| 12:4916196:G:A | acceptor_gain | 0.6200 |
| 12:4910241:G:GT | donor_gain | 0.6100 |
| 12:4915036:TAGGC:T | acceptor_gain | 0.6100 |
| 12:4910468:GCCAG:G | donor_gain | 0.5700 |
| 12:4913729:C:T | donor_gain | 0.5700 |
| 12:4915852:C:A | acceptor_gain | 0.5700 |
| 12:4911348:T:TA | acceptor_gain | 0.5600 |
| 12:4912207:G:GT | donor_gain | 0.5600 |
| 12:4915035:CTAGG:C | acceptor_gain | 0.5600 |
| 12:4910156:G:GA | donor_gain | 0.5500 |
| 12:4910224:T:TA | donor_gain | 0.5200 |
| 12:4911383:C:CA | acceptor_gain | 0.5200 |
| 12:4915482:T:G | acceptor_gain | 0.5200 |
| 12:4915037:AGGCC:A | acceptor_gain | 0.5100 |
| 12:4913724:G:GG | donor_gain | 0.5000 |
| 12:4915099:TGGCA:T | acceptor_gain | 0.5000 |
| 12:4915100:GGCAG:G | acceptor_gain | 0.5000 |
| 12:4910475:A:C | donor_loss | 0.4900 |
| 12:4910647:A:T | donor_gain | 0.4900 |
AlphaMissense
3306 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 12:4911504:C:A | N42K | 1.000 |
| 12:4911504:C:G | N42K | 1.000 |
| 12:4911511:G:A | G45R | 1.000 |
| 12:4911511:G:C | G45R | 1.000 |
| 12:4911511:G:T | G45W | 1.000 |
| 12:4911512:G:A | G45E | 1.000 |
| 12:4911520:T:C | F48L | 1.000 |
| 12:4911522:C:A | F48L | 1.000 |
| 12:4911522:C:G | F48L | 1.000 |
| 12:4911566:T:A | L63Q | 1.000 |
| 12:4911568:G:C | G64R | 1.000 |
| 12:4911569:G:A | G64D | 1.000 |
| 12:4911569:G:T | G64V | 1.000 |
| 12:4911616:T:G | Y80D | 1.000 |
| 12:4911619:T:C | F81L | 1.000 |
| 12:4911621:C:A | F81L | 1.000 |
| 12:4911621:C:G | F81L | 1.000 |
| 12:4911628:C:A | R84S | 1.000 |
| 12:4911629:G:C | R84P | 1.000 |
| 12:4911640:A:C | S88R | 1.000 |
| 12:4911642:C:A | S88R | 1.000 |
| 12:4911642:C:G | S88R | 1.000 |
| 12:4911643:T:C | F89L | 1.000 |
| 12:4911645:C:A | F89L | 1.000 |
| 12:4911645:C:G | F89L | 1.000 |
| 12:4911653:T:A | I92N | 1.000 |
| 12:4911656:T:C | L93P | 1.000 |
| 12:4911664:T:G | Y96D | 1.000 |
| 12:4911668:A:C | Q97P | 1.000 |
| 12:4911670:T:C | S98P | 1.000 |
dbSNP variants (sampled 300 via entrez): RS1000033638 (12:4917098 C>T), RS1000246159 (12:4911275 C>A,T), RS1000438964 (12:4918359 C>G), RS1001780454 (12:4911036 C>T), RS1002075398 (12:4914267 G>A), RS1002085146 (12:4913992 A>T), RS1002176215 (12:4917488 G>A), RS1003049385 (12:4912431 A>G), RS1003607904 (12:4908790 T>G), RS1003736791 (12:4915548 C>T), RS1003769404 (12:4915268 C>G), RS1004158014 (12:4914945 C>G,T), RS1004210225 (12:4914742 C>G), RS1004259311 (12:4910126 G>A), RS1004546607 (12:4915852 C>G,T)
Disease associations
OMIM: gene MIM:176260 | disease phenotypes: MIM:160120, MIM:128200, MIM:609446, MIM:612240, MIM:308350
GenCC curated gene-disease
| Disease | Classification | Inheritance |
|---|---|---|
| episodic ataxia type 1 | Definitive | Autosomal dominant |
| epilepsy | Strong | Autosomal dominant |
| genetic developmental and epileptic encephalopathy | Supportive | Autosomal dominant |
| isolated autosomal dominant hypomagnesemia, Glaudemans type | Supportive | Autosomal dominant |
| episodic kinesigenic dyskinesia 1 | Supportive | Autosomal dominant |
ClinGen Gene-Disease Validity (1)
Expert-panel classifications — Definitive > Strong > Moderate > Limited > Disputed > Refuted.
| Disease | Classification | Inheritance |
|---|---|---|
| episodic ataxia type 1 | Definitive | AD |
Mondo (10): episodic ataxia type 1 (MONDO:0008047), episodic kinesigenic dyskinesia (MONDO:0044202), generalized epilepsy-paroxysmal dyskinesia syndrome (MONDO:0012276), breast ductal adenocarcinoma (MONDO:0005590), atrial fibrillation, familial, 7 (MONDO:0012828), hereditary ataxia (MONDO:0100309), genetic developmental and epileptic encephalopathy (MONDO:0100062), isolated autosomal dominant hypomagnesemia, Glaudemans type (MONDO:0016048), (MONDO:0007494), epilepsy (MONDO:0005027)
Orphanet (5): Episodic ataxia type 1 (Orphanet:37612), Hereditary continuous muscle fiber activity (Orphanet:972), Paroxysmal kinesigenic dyskinesia (Orphanet:98809), Generalized epilepsy-paroxysmal dyskinesia syndrome (Orphanet:79137), Hereditary ataxia (Orphanet:183518)
HPO phenotypes
108 total (30 of 108 shown, HPO-id order):
| HPO | Term |
|---|---|
| HP:0000006 | Autosomal dominant inheritance |
| HP:0000054 | Micropenis |
| HP:0000070 | Ureterocele |
| HP:0000110 | Renal dysplasia |
| HP:0000175 | Cleft palate |
| HP:0000252 | Microcephaly |
| HP:0000340 | Sloping forehead |
| HP:0000463 | Anteverted nares |
| HP:0000486 | Strabismus |
| HP:0000622 | Blurred vision |
| HP:0000651 | Diplopia |
| HP:0000729 | Autistic behavior |
| HP:0000750 | Delayed speech and language development |
| HP:0000752 | Hyperactivity |
| HP:0000776 | Congenital diaphragmatic hernia |
| HP:0000826 | Precocious puberty |
| HP:0000975 | Hyperhidrosis |
| HP:0001155 | Abnormality of the hand |
| HP:0001188 | Hand clenching |
| HP:0001249 | Intellectual disability |
| HP:0001250 | Seizure |
| HP:0001251 | Ataxia |
| HP:0001254 | Lethargy |
| HP:0001257 | Spasticity |
| HP:0001260 | Dysarthria |
| HP:0001263 | Global developmental delay |
| HP:0001266 | Choreoathetosis |
| HP:0001270 | Motor delay |
| HP:0001272 | Cerebellar atrophy |
| HP:0001276 | Hypertonia |
GWAS associations
0 associations (top):
MeSH disease descriptors (5)
| Descriptor | Name | Tree numbers |
|---|---|---|
| D018270 | Carcinoma, Ductal, Breast | C04.557.470.200.025.232.500; C04.557.470.615.132.500; C04.588.180.390; C17.800.090.500.390 |
| D004827 | Epilepsy | C10.228.140.490 |
| C567389 | Atrial Fibrillation, Familial, 7 (supp.) | |
| C563719 | Generalized Epilepsy and Paroxysmal Dyskinesia (supp.) | |
| C531684 | Hereditary spinal ataxia (supp.) |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (3): CHEMBL2309 (SINGLE PROTEIN), CHEMBL2362996 (PROTEIN FAMILY), CHEMBL3988636 (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: 287,199 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).
| Molecule | Name | Phase | Patents |
|---|---|---|---|
| CHEMBL193 | NIFEDIPINE | 4 | 74,353 |
| CHEMBL284348 | DALFAMPRIDINE | 4 | 25,690 |
| CHEMBL294199 | CAPSAICIN | 4 | 52,939 |
| CHEMBL1499 | CORTISONE | 3 | 79,011 |
| CHEMBL9324 | TETRYLAMMONIUM | 2 | 55,206 |
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 (15 total), top 15:
| Ligand | Action | Affinity | Parameter |
|---|---|---|---|
| ShK Toxin | Channel blocker | 10.8 | pIC50 |
| hongotoxin-1 | Channel blocker | 10.5 | pIC50 |
| α-dendrotoxin | Channel blocker | 9.0 | pEC50 |
| dendrotoxin-k | Pore blocker | 8.6 | pIC50 |
| margatoxin | Inhibition | 8.4 | pIC50 |
| dendrotoxin-I | Channel blocker | 7.7 | pIC50 |
| kaliotoxin | Channel blocker | 7.4 | pIC50 |
| mast cell degranulating peptide | Channel blocker | 6.3 | pIC50 |
| resiniferatoxin | Channel blocker | 5.1 | pIC50 |
| HelaTx1 | Pore blocker | 5.0 | pEC50 |
| capsaicin | Channel blocker | 4.5 | pIC50 |
| nifedipine | Channel blocker | 4.0 | pIC50 |
| diltiazem | Channel blocker | 3.8 | pIC50 |
| flecainide | Channel blocker | 3.7 | pKd |
| tetraethylammonium | Inhibition | 3.5 | pKd |
Binding affinities (BindingDB)
1 measured of 3 human assays (3 total across all organisms); most potent 1 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value |
|---|---|---|
| SR 147778 | KI | 1000 nM |
ChEMBL bioactivities
72 potent at pChembl≥5 of 91 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 10.99 | IC50 | 0.0102 | nM | CHEMBL3609249 |
| 10.96 | IC50 | 0.011 | nM | CHEMBL3608998 |
| 10.96 | IC50 | 0.011 | nM | CHEMBL3609244 |
| 10.96 | IC50 | 0.011 | nM | CHEMBL3609086 |
| 10.85 | IC50 | 0.014 | nM | CHEMBL3609028 |
| 10.85 | IC50 | 0.014 | nM | CHEMBL3609093 |
| 10.82 | IC50 | 0.015 | nM | CHEMBL3609089 |
| 10.81 | IC50 | 0.0154 | nM | CHEMBL3609046 |
| 10.80 | IC50 | 0.0157 | nM | CHEMBL3609247 |
| 10.76 | IC50 | 0.0172 | nM | CHEMBL3608317 |
| 10.74 | IC50 | 0.0182 | nM | CHEMBL3609226 |
| 10.74 | IC50 | 0.0181 | nM | CHEMBL3609023 |
| 10.71 | IC50 | 0.0195 | nM | CHEMBL3609044 |
| 10.70 | IC50 | 0.02 | nM | CHEMBL3609029 |
| 10.70 | IC50 | 0.02 | nM | CHEMBL3609093 |
| 10.59 | IC50 | 0.0256 | nM | CHEMBL3609268 |
| 10.58 | IC50 | 0.0262 | nM | CHEMBL3609253 |
| 10.56 | IC50 | 0.0274 | nM | CHEMBL3609246 |
| 10.55 | IC50 | 0.028 | nM | CHEMBL3609242 |
| 10.55 | IC50 | 0.028 | nM | CHEMBL3609030 |
| 10.54 | IC50 | 0.029 | nM | CHEMBL3609273 |
| 10.49 | IC50 | 0.032 | nM | CHEMBL3609269 |
| 10.49 | IC50 | 0.0324 | nM | CHEMBL3609051 |
| 10.47 | IC50 | 0.0335 | nM | CHEMBL3609079 |
| 10.40 | IC50 | 0.04 | nM | CHEMBL3609264 |
| 10.40 | IC50 | 0.04 | nM | CHEMBL3609076 |
| 10.38 | IC50 | 0.042 | nM | CHEMBL3609277 |
| 10.34 | IC50 | 0.046 | nM | CHEMBL3609040 |
| 10.31 | IC50 | 0.0489 | nM | CHEMBL3609248 |
| 10.29 | IC50 | 0.051 | nM | CHEMBL3609275 |
| 10.28 | IC50 | 0.0527 | nM | CHEMBL3609072 |
| 10.26 | IC50 | 0.055 | nM | CHEMBL3609047 |
| 10.15 | IC50 | 0.07 | nM | CHEMBL3609056 |
| 10.12 | IC50 | 0.075 | nM | CHEMBL3609080 |
| 10.06 | IC50 | 0.087 | nM | CHEMBL3609093 |
| 9.82 | Ki | 0.15 | nM | CHEMBL5722941 |
| 9.76 | IC50 | 0.174 | nM | CHEMBL3609082 |
| 9.74 | IC50 | 0.18 | nM | CHEMBL5722941 |
| 9.67 | IC50 | 0.214 | nM | CHEMBL3609095 |
| 9.57 | IC50 | 0.266 | nM | CHEMBL3609081 |
| 9.52 | IC50 | 0.305 | nM | CHEMBL3609243 |
| 9.51 | IC50 | 0.308 | nM | CHEMBL3608999 |
| 9.35 | IC50 | 0.446 | nM | CHEMBL3609234 |
| 9.34 | IC50 | 0.458 | nM | CHEMBL3609064 |
| 9.31 | IC50 | 0.49 | nM | CHEMBL3609025 |
| 9.23 | IC50 | 0.59 | nM | CHEMBL3609059 |
| 9.22 | IC50 | 0.6 | nM | CHEMBL3609087 |
| 9.13 | IC50 | 0.74 | nM | CHEMBL3609085 |
| 9.12 | IC50 | 0.76 | nM | CHEMBL3609228 |
| 9.07 | IC50 | 0.847 | nM | CHEMBL3609094 |
PubChem BioAssay actives
141 with measured affinity, of 289 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.
| Compound | Assay | Type | Value | Unit |
|---|---|---|---|---|
| (1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,45R,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-10,51,75-tris(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-93-(3-amino-3-oxopropyl)-60,96-dibenzyl-19,28-bis[(2S)-butan-2-yl]-4,54,69-tris(3-carbamimidamidopropyl)-25-(carboxymethyl)-2a,22,39,48-tetrakis[(1R)-1-hydroxyethyl]-7,63,81-tris(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-84-(1H-imidazol-5-ylmethyl)-99-methyl-66-(2-methylpropyl)-78-(2-methylsulfanylethyl)-87-(naphthalen-1-ylmethyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectane-36-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,45R,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-10,51,75,87-tetrakis(4-aminobutyl)-93-(3-amino-3-oxopropyl)-31-[[(2S)-2-[[(2S)-2-aminopropanoyl]amino]-3-hydroxypropanoyl]amino]-60,96-dibenzyl-19,28-bis[(2S)-butan-2-yl]-4,54,69-tris(3-carbamimidamidopropyl)-25-(carboxymethyl)-2a,22,39,48-tetrakis[(1R)-1-hydroxyethyl]-7,63,81-tris(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-84-(1H-imidazol-5-ylmethyl)-99-methyl-66-(2-methylpropyl)-78-(2-methylsulfanylethyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectane-36-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,45R,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-10,51,75,87-tetrakis(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-93-(3-amino-3-oxopropyl)-60,96-dibenzyl-19,28-bis[(2S)-butan-2-yl]-4,54,69-tris(3-carbamimidamidopropyl)-25-(carboxymethyl)-2a,22,39,48-tetrakis[(1R)-1-hydroxyethyl]-7,63,81-tris(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-84-(1H-imidazol-5-ylmethyl)-99-methyl-66-(2-methylpropyl)-78-(2-methylsulfanylethyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectane-36-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,45R,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-10,51,75,87-tetrakis(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-93-(3-amino-3-oxopropyl)-60,96-dibenzyl-19-[(2S)-butan-2-yl]-4,54,69-tris(3-carbamimidamidopropyl)-25-(carboxymethyl)-2a,22,39,48-tetrakis[(1R)-1-hydroxyethyl]-7,63,81-tris(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-84-(1H-imidazol-5-ylmethyl)-28,99-dimethyl-66-(2-methylpropyl)-78-(2-methylsulfanylethyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectane-36-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,45R,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-10,51,75,87-tetrakis(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-93-(3-amino-3-oxopropyl)-60,96-dibenzyl-19,28-bis[(2S)-butan-2-yl]-4,54,69-tris(3-carbamimidamidopropyl)-25-(carboxymethyl)-2a,39,48-tris[(1R)-1-hydroxyethyl]-7,63,81-tris(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-84-(1H-imidazol-5-ylmethyl)-22,99-dimethyl-66-(2-methylpropyl)-78-(2-methylsulfanylethyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectane-36-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,45R,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-10,51,75,87-tetrakis(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-93-(3-amino-3-oxopropyl)-60,96-dibenzyl-28-[(2S)-butan-2-yl]-4,54,69-tris(3-carbamimidamidopropyl)-25-(carboxymethyl)-2a,22,39,48-tetrakis[(1R)-1-hydroxyethyl]-7,63,81-tris(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-84-(1H-imidazol-5-ylmethyl)-19,99-dimethyl-66-(2-methylpropyl)-78-(2-methylsulfanylethyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectane-36-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,4S,7S,10S,13R,19S,22R,27R,30S,33S,36S,39S,42S,45S,48S,51S,54R,57S,60S,63S,66S,69R,72S,75S,78S,81S,84S,87S,90S,93S,96S,99S)-7,45,72,84-tetrakis(4-aminobutyl)-27-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-66-(3-amino-3-oxopropyl)-63,99-dibenzyl-30,39-bis[(2S)-butan-2-yl]-4,51,90-tris(3-carbamimidamidopropyl)-33-(carboxymethyl)-10,19,36,57-tetrakis[(1R)-1-hydroxyethyl]-48,78,96-tris(hydroxymethyl)-87-[(4-hydroxyphenyl)methyl]-75-(1H-imidazol-5-ylmethyl)-42,60-dimethyl-93-(2-methylpropyl)-81-(2-methylsulfanylethyl)-a,2,5,8,11,14,17,20,28,31,34,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontaoxo-3a,4a,7a,8a,24,25-hexathia-1a,3,6,9,12,15,18,21,29,32,35,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontazatricyclo[52.47.4.413,69]nonahectane-22-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,45R,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-51,75,87-tris(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-93-(3-amino-3-oxopropyl)-60,96-dibenzyl-19,28-bis[(2S)-butan-2-yl]-4,54,69-tris(3-carbamimidamidopropyl)-25-(carboxymethyl)-2a,22,39,48-tetrakis[(1R)-1-hydroxyethyl]-7,63,81-tris(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-84-(1H-imidazol-5-ylmethyl)-10,99-dimethyl-66-(2-methylpropyl)-78-(2-methylsulfanylethyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectane-36-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,45R,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-10,51,75,87-tetrakis(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-93-(3-amino-3-oxopropyl)-60,96-dibenzyl-19,28-bis[(2S)-butan-2-yl]-4,54,69-tris(3-carbamimidamidopropyl)-99-(2-carboxyethyl)-2a,22,39,48-tetrakis[(1R)-1-hydroxyethyl]-7,63,81-tris(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-84-(1H-imidazol-5-ylmethyl)-66-(2-methylpropyl)-78-(2-methylsulfanylethyl)-25-(naphthalen-1-ylmethyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectane-36-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,45R,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-10,51,75,87-tetrakis(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-93-(3-amino-3-oxopropyl)-60,96-dibenzyl-19,28-bis[(2S)-butan-2-yl]-4,54,69-tris(3-carbamimidamidopropyl)-84-(2-carboxyethyl)-25-(carboxymethyl)-2a,22,39,48-tetrakis[(1R)-1-hydroxyethyl]-7,63,81-tris(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-99-methyl-66-(2-methylpropyl)-78-(2-methylsulfanylethyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectane-36-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,45R,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-10,51,75,87-tetrakis(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-93-(3-amino-3-oxopropyl)-60,96-dibenzyl-19,28-bis[(2S)-butan-2-yl]-4,54-bis(3-carbamimidamidopropyl)-69-(2-carboxyethyl)-25-(carboxymethyl)-2a,22,39,48-tetrakis[(1R)-1-hydroxyethyl]-7,63,81-tris(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-84-(1H-imidazol-5-ylmethyl)-99-methyl-66-(2-methylpropyl)-78-(2-methylsulfanylethyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectane-36-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,45R,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-10,51,75,87-tetrakis(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-93-(3-amino-3-oxopropyl)-60,96-dibenzyl-19,28-bis[(2S)-butan-2-yl]-4,54,69-tris(3-carbamimidamidopropyl)-66-(2-carboxyethyl)-25-(carboxymethyl)-2a,22,39,48-tetrakis[(1R)-1-hydroxyethyl]-7,63,81-tris(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-84-(1H-imidazol-5-ylmethyl)-99-methyl-78-(2-methylsulfanylethyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectane-36-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,45R,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-10,51,75,87-tetrakis(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-93-(3-amino-3-oxopropyl)-60,96-dibenzyl-19,28-bis[(2S)-butan-2-yl]-4,54,69-tris(3-carbamimidamidopropyl)-63-(2-carboxyethyl)-25-(carboxymethyl)-2a,22,39,48-tetrakis[(1R)-1-hydroxyethyl]-7,81-bis(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-84-(1H-imidazol-5-ylmethyl)-99-methyl-66-(2-methylpropyl)-78-(2-methylsulfanylethyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectane-36-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,45R,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-10,51,75,87-tetrakis(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-93-(3-amino-3-oxopropyl)-60,96-dibenzyl-19,28-bis[(2S)-butan-2-yl]-4,69-bis(3-carbamimidamidopropyl)-54-(2-carboxyethyl)-25-(carboxymethyl)-2a,22,39,48-tetrakis[(1R)-1-hydroxyethyl]-7,63,81-tris(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-84-(1H-imidazol-5-ylmethyl)-99-methyl-66-(2-methylpropyl)-78-(2-methylsulfanylethyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectane-36-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,45R,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-10,75,87-tris(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-93-(3-amino-3-oxopropyl)-60,96-dibenzyl-19,28-bis[(2S)-butan-2-yl]-4,54,69-tris(3-carbamimidamidopropyl)-51-(2-carboxyethyl)-25-(carboxymethyl)-2a,22,39,48-tetrakis[(1R)-1-hydroxyethyl]-7,63,81-tris(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-84-(1H-imidazol-5-ylmethyl)-99-methyl-66-(2-methylpropyl)-78-(2-methylsulfanylethyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectane-36-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,45R,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-10,51,75,87-tetrakis(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-93-(3-amino-3-oxopropyl)-60,96-dibenzyl-19,28-bis[(2S)-butan-2-yl]-4,54,69-tris(3-carbamimidamidopropyl)-48-(2-carboxyethyl)-25-(carboxymethyl)-2a,22,39-tris[(1R)-1-hydroxyethyl]-7,63,81-tris(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-84-(1H-imidazol-5-ylmethyl)-99-methyl-66-(2-methylpropyl)-78-(2-methylsulfanylethyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectane-36-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,42S,45R,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-10,51,75,87-tetrakis(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-93-(3-amino-3-oxopropyl)-60,96-dibenzyl-19,28-bis[(2S)-butan-2-yl]-4,54,69-tris(3-carbamimidamidopropyl)-42-(2-carboxyethyl)-25-(carboxymethyl)-2a,22,39,48-tetrakis[(1R)-1-hydroxyethyl]-7,63,81-tris(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-84-(1H-imidazol-5-ylmethyl)-99-methyl-66-(2-methylpropyl)-78-(2-methylsulfanylethyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectane-36-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,45R,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-10,51,75,87-tetrakis(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-93-(3-amino-3-oxopropyl)-60,96-dibenzyl-19,28-bis[(2S)-butan-2-yl]-4,54,69-tris(3-carbamimidamidopropyl)-39-(2-carboxyethyl)-25-(carboxymethyl)-2a,22,48-tris[(1R)-1-hydroxyethyl]-7,63,81-tris(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-84-(1H-imidazol-5-ylmethyl)-99-methyl-66-(2-methylpropyl)-78-(2-methylsulfanylethyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectane-36-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,45R,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-10,51,75,87-tetrakis(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-93-(3-amino-3-oxopropyl)-60,96-dibenzyl-19,28-bis[(2S)-butan-2-yl]-4,54,69-tris(3-carbamimidamidopropyl)-25-(carboxymethyl)-2a,22,39,48-tetrakis[(1R)-1-hydroxyethyl]-7,63,81-tris(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-84-(1H-imidazol-5-ylmethyl)-99-methyl-66-(2-methylpropyl)-78-(2-methylsulfanylethyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectane-36-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,45R,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-10,51,75,87-tetrakis(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-93-(3-amino-3-oxopropyl)-60,96-dibenzyl-19-[(2S)-butan-2-yl]-4,28,54,69-tetrakis(3-carbamimidamidopropyl)-25-(carboxymethyl)-2a,22,39,48-tetrakis[(1R)-1-hydroxyethyl]-7,63,81-tris(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-84-(1H-imidazol-5-ylmethyl)-99-methyl-66-(2-methylpropyl)-78-(2-methylsulfanylethyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectane-36-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,45R,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-10,51,75,87-tetrakis(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-93-(3-amino-3-oxopropyl)-60,96-dibenzyl-19,28-bis[(2S)-butan-2-yl]-4,22,54,69-tetrakis(3-carbamimidamidopropyl)-25-(carboxymethyl)-2a,48-bis[(1R)-1-hydroxyethyl]-7,63,81-tris(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-84-(1H-imidazol-5-ylmethyl)-99-methyl-66-(2-methylpropyl)-78-(2-methylsulfanylethyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-39-propan-2-yl-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectane-36-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,45R,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-10,51,75,87-tetrakis(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-93-(3-amino-3-oxopropyl)-60,96-dibenzyl-28-[(2S)-butan-2-yl]-4,19,54,69-tetrakis(3-carbamimidamidopropyl)-25-(carboxymethyl)-2a,22,39,48-tetrakis[(1R)-1-hydroxyethyl]-7,63,81-tris(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-84-(1H-imidazol-5-ylmethyl)-99-methyl-66-(2-methylpropyl)-78-(2-methylsulfanylethyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectane-36-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,4S,7S,10S,13R,19S,22R,27R,30S,33S,36S,39S,42S,45S,48S,51S,54R,57S,60S,63S,66S,69R,72S,75S,78S,81S,84S,87S,90S,93S,96S,99S)-7,45,72,84-tetrakis(4-aminobutyl)-27-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-66-(3-amino-3-oxopropyl)-63,99-dibenzyl-30,39-bis[(2S)-butan-2-yl]-4,42,51,90-tetrakis(3-carbamimidamidopropyl)-33-(carboxymethyl)-10,19,36,57-tetrakis[(1R)-1-hydroxyethyl]-48,78,96-tris(hydroxymethyl)-87-[(4-hydroxyphenyl)methyl]-75-(1H-imidazol-5-ylmethyl)-60-methyl-93-(2-methylpropyl)-81-(2-methylsulfanylethyl)-a,2,5,8,11,14,17,20,28,31,34,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontaoxo-3a,4a,7a,8a,24,25-hexathia-1a,3,6,9,12,15,18,21,29,32,35,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontazatricyclo[52.47.4.413,69]nonahectane-22-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,45R,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-51,75,87-tris(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-93-(3-amino-3-oxopropyl)-60,96-dibenzyl-19,28-bis[(2S)-butan-2-yl]-4,10,54,69-tetrakis(3-carbamimidamidopropyl)-25-(carboxymethyl)-2a,22,39,48-tetrakis[(1R)-1-hydroxyethyl]-7,63,81-tris(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-84-(1H-imidazol-5-ylmethyl)-99-methyl-66-(2-methylpropyl)-78-(2-methylsulfanylethyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectane-36-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,45R,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-10,51,75,87-tetrakis(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-93-(3-amino-3-oxopropyl)-60,96-dibenzyl-19,28-bis[(2S)-butan-2-yl]-4,7,54,69-tetrakis(3-carbamimidamidopropyl)-25-(carboxymethyl)-2a,22,39,48-tetrakis[(1R)-1-hydroxyethyl]-63,81-bis(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-84-(1H-imidazol-5-ylmethyl)-99-methyl-66-(2-methylpropyl)-78-(2-methylsulfanylethyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectane-36-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,45R,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-10,51,75,87-tetrakis(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-93-(3-amino-3-oxopropyl)-60,96-dibenzyl-19,28-bis[(2S)-butan-2-yl]-2a,4,54,69-tetrakis(3-carbamimidamidopropyl)-25-(carboxymethyl)-22,39,48-tris[(1R)-1-hydroxyethyl]-7,63,81-tris(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-84-(1H-imidazol-5-ylmethyl)-99-methyl-66-(2-methylpropyl)-78-(2-methylsulfanylethyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectane-36-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,45R,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-10,51,75,87-tetrakis(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-93-(3-amino-3-oxopropyl)-60,96-dibenzyl-19,28-bis[(2S)-butan-2-yl]-4,54,69,99-tetrakis(3-carbamimidamidopropyl)-2a,22,39,48-tetrakis[(1R)-1-hydroxyethyl]-7,63,81-tris(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-84-(1H-imidazol-5-ylmethyl)-66-(2-methylpropyl)-78-(2-methylsulfanylethyl)-25-(naphthalen-1-ylmethyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectane-36-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,45R,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-10,51,75,87-tetrakis(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-93-(3-amino-3-oxopropyl)-60-benzyl-19,28-bis[(2S)-butan-2-yl]-4,54,69,96-tetrakis(3-carbamimidamidopropyl)-25-(carboxymethyl)-2a,22,39,48-tetrakis[(1R)-1-hydroxyethyl]-7,63,81-tris(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-84,99-dimethyl-66-(2-methylpropyl)-78-(2-methylsulfanylethyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectane-36-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,45R,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-10,51,75-tris(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-93-(3-amino-3-oxopropyl)-60,96-dibenzyl-19,28-bis[(2S)-butan-2-yl]-4,54,69,87-tetrakis(3-carbamimidamidopropyl)-25-(carboxymethyl)-2a,22,39,48-tetrakis[(1R)-1-hydroxyethyl]-7,63,81-tris(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-84-(1H-imidazol-5-ylmethyl)-99-methyl-66-(2-methylpropyl)-78-(2-methylsulfanylethyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectane-36-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,45R,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-10,51,75,87-tetrakis(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-93-(3-amino-3-oxopropyl)-60,96-dibenzyl-19,28-bis[(2S)-butan-2-yl]-4,54,69,84-tetrakis(3-carbamimidamidopropyl)-25-(carboxymethyl)-2a,22,39,48-tetrakis[(1R)-1-hydroxyethyl]-7,63,81-tris(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-99-methyl-66-(2-methylpropyl)-78-(2-methylsulfanylethyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectane-36-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,45R,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-10,51,75,87-tetrakis(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-93-(3-amino-3-oxopropyl)-60,96-dibenzyl-19,28-bis[(2S)-butan-2-yl]-4,54,69,78-tetrakis(3-carbamimidamidopropyl)-25-(carboxymethyl)-2a,22,39,48-tetrakis[(1R)-1-hydroxyethyl]-7,63,81-tris(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-84-(1H-imidazol-5-ylmethyl)-99-methyl-66-(2-methylpropyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectane-36-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,45R,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-31-[[(2S)-6-amino-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]hexanoyl]amino]-10,51,75,87-tetrakis(4-aminobutyl)-93-(3-amino-3-oxopropyl)-60,96-dibenzyl-19,28-bis[(2S)-butan-2-yl]-4,54,69-tris(3-carbamimidamidopropyl)-25-(carboxymethyl)-2a,22,39,48-tetrakis[(1R)-1-hydroxyethyl]-7,63,81-tris(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-84-(1H-imidazol-5-ylmethyl)-99-methyl-66-(2-methylpropyl)-78-(2-methylsulfanylethyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectane-36-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,45R,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-10,51,75,87-tetrakis(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-93-(3-amino-3-oxopropyl)-60,96-dibenzyl-19,28-bis[(2S)-butan-2-yl]-4,54,66,69-tetrakis(3-carbamimidamidopropyl)-25-(carboxymethyl)-2a,22,39,48-tetrakis[(1R)-1-hydroxyethyl]-7,63,81-tris(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-84-(1H-imidazol-5-ylmethyl)-99-methyl-78-(2-methylsulfanylethyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectane-36-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,45R,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-10,75,87-tris(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-93-(3-amino-3-oxopropyl)-60,96-dibenzyl-19,28-bis[(2S)-butan-2-yl]-4,51,54,69-tetrakis(3-carbamimidamidopropyl)-25-(carboxymethyl)-2a,22,39,48-tetrakis[(1R)-1-hydroxyethyl]-7,63,81-tris(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-84-(1H-imidazol-5-ylmethyl)-99-methyl-66-(2-methylpropyl)-78-(2-methylsulfanylethyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectane-36-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,42S,45R,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-10,51,75,87-tetrakis(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-93-(3-amino-3-oxopropyl)-60,96-dibenzyl-19,28-bis[(2S)-butan-2-yl]-4,42,54,69-tetrakis(3-carbamimidamidopropyl)-25-(carboxymethyl)-2a,22,39,48-tetrakis[(1R)-1-hydroxyethyl]-7,63,81-tris(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-84-(1H-imidazol-5-ylmethyl)-99-methyl-66-(2-methylpropyl)-78-(2-methylsulfanylethyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectane-36-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,45R,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-10,51,75,87-tetrakis(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-93-(3-amino-3-oxopropyl)-60,96-dibenzyl-19,28-bis[(2S)-butan-2-yl]-4,39,54,69-tetrakis(3-carbamimidamidopropyl)-25-(carboxymethyl)-2a,22,48-tris[(1R)-1-hydroxyethyl]-7,63,81-tris(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-84-(1H-imidazol-5-ylmethyl)-99-methyl-66-(2-methylpropyl)-78-(2-methylsulfanylethyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectane-36-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,45R,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-10,51,75,87-tetrakis(4-aminobutyl)-93-(3-amino-3-oxopropyl)-60,96-dibenzyl-19,28-bis[(2S)-butan-2-yl]-4,54,69-tris(3-carbamimidamidopropyl)-25-(carboxymethyl)-31-[[(2S)-2-[[(2S)-2,6-diaminohexanoyl]amino]-3-hydroxypropanoyl]amino]-2a,22,39,48-tetrakis[(1R)-1-hydroxyethyl]-7,63,81-tris(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-84-(1H-imidazol-5-ylmethyl)-99-methyl-66-(2-methylpropyl)-78-(2-methylsulfanylethyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectane-36-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,45R,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-10,28,51,75,87-pentakis(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-93-(3-amino-3-oxopropyl)-60,96-dibenzyl-19-[(2S)-butan-2-yl]-4,54,69-tris(3-carbamimidamidopropyl)-25-(carboxymethyl)-2a,22,39,48-tetrakis[(1R)-1-hydroxyethyl]-7,63,81-tris(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-84-(1H-imidazol-5-ylmethyl)-99-methyl-66-(2-methylpropyl)-78-(2-methylsulfanylethyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectane-36-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,45R,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-10,22,51,75,87-pentakis(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-93-(3-amino-3-oxopropyl)-60,96-dibenzyl-19,28-bis[(2S)-butan-2-yl]-4,54,69-tris(3-carbamimidamidopropyl)-25-(carboxymethyl)-2a,48-bis[(1R)-1-hydroxyethyl]-7,63,81-tris(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-84-(1H-imidazol-5-ylmethyl)-99-methyl-66-(2-methylpropyl)-78-(2-methylsulfanylethyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-39-propan-2-yl-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectane-36-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,4S,7S,10S,13R,19S,22R,27R,30S,33S,36S,39S,42S,45S,48S,51S,54R,57S,60S,63S,66S,69R,72S,75S,78S,81S,84S,87S,90S,93S,96S,99S)-7,42,45,72,84-pentakis(4-aminobutyl)-27-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-66-(3-amino-3-oxopropyl)-63,99-dibenzyl-30,39-bis[(2S)-butan-2-yl]-4,51,90-tris(3-carbamimidamidopropyl)-33-(carboxymethyl)-10,19,36,57-tetrakis[(1R)-1-hydroxyethyl]-48,78,96-tris(hydroxymethyl)-87-[(4-hydroxyphenyl)methyl]-75-(1H-imidazol-5-ylmethyl)-60-methyl-93-(2-methylpropyl)-81-(2-methylsulfanylethyl)-a,2,5,8,11,14,17,20,28,31,34,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontaoxo-3a,4a,7a,8a,24,25-hexathia-1a,3,6,9,12,15,18,21,29,32,35,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontazatricyclo[52.47.4.413,69]nonahectane-22-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,45R,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-7,10,51,75,87-pentakis(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-93-(3-amino-3-oxopropyl)-60,96-dibenzyl-19,28-bis[(2S)-butan-2-yl]-4,54,69-tris(3-carbamimidamidopropyl)-25-(carboxymethyl)-2a,22,39,48-tetrakis[(1R)-1-hydroxyethyl]-63,81-bis(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-84-(1H-imidazol-5-ylmethyl)-99-methyl-66-(2-methylpropyl)-78-(2-methylsulfanylethyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectane-36-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,45R,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-4,10,51,75,87-pentakis(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-93-(3-amino-3-oxopropyl)-60,96-dibenzyl-19,28-bis[(2S)-butan-2-yl]-54,69-bis(3-carbamimidamidopropyl)-25-(carboxymethyl)-2a,22,39,48-tetrakis[(1R)-1-hydroxyethyl]-7,63,81-tris(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-84-(1H-imidazol-5-ylmethyl)-99-methyl-66-(2-methylpropyl)-78-(2-methylsulfanylethyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectane-36-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,45R,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-2a,10,51,75,87-pentakis(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-93-(3-amino-3-oxopropyl)-60,96-dibenzyl-19,28-bis[(2S)-butan-2-yl]-4,54,69-tris(3-carbamimidamidopropyl)-25-(carboxymethyl)-22,39,48-tris[(1R)-1-hydroxyethyl]-7,63,81-tris(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-84-(1H-imidazol-5-ylmethyl)-99-methyl-66-(2-methylpropyl)-78-(2-methylsulfanylethyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectane-36-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,45R,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-10,51,75,87,99-pentakis(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-93-(3-amino-3-oxopropyl)-60,96-dibenzyl-19,28-bis[(2S)-butan-2-yl]-4,54,69-tris(3-carbamimidamidopropyl)-2a,22,39,48-tetrakis[(1R)-1-hydroxyethyl]-7,63,81-tris(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-84-(1H-imidazol-5-ylmethyl)-66-(2-methylpropyl)-78-(2-methylsulfanylethyl)-25-(naphthalen-1-ylmethyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectane-36-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,45R,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-10,51,75,84,87-pentakis(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-93-(3-amino-3-oxopropyl)-60,96-dibenzyl-19,28-bis[(2S)-butan-2-yl]-4,54,69-tris(3-carbamimidamidopropyl)-25-(carboxymethyl)-2a,22,39,48-tetrakis[(1R)-1-hydroxyethyl]-7,63,81-tris(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-99-methyl-66-(2-methylpropyl)-78-(2-methylsulfanylethyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectane-36-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,45R,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-10,51,75,81,87-pentakis(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-93-(3-amino-3-oxopropyl)-60,96-dibenzyl-19,28-bis[(2S)-butan-2-yl]-4,54,69-tris(3-carbamimidamidopropyl)-25-(carboxymethyl)-2a,22,39,48-tetrakis[(1R)-1-hydroxyethyl]-7,63-bis(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-84-(1H-imidazol-5-ylmethyl)-99-methyl-66-(2-methylpropyl)-78-(2-methylsulfanylethyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectane-36-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,45R,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-10,51,75,78,87-pentakis(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-93-(3-amino-3-oxopropyl)-60,96-dibenzyl-19,28-bis[(2S)-butan-2-yl]-4,54,69-tris(3-carbamimidamidopropyl)-25-(carboxymethyl)-2a,22,39,48-tetrakis[(1R)-1-hydroxyethyl]-7,63,81-tris(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-84-(1H-imidazol-5-ylmethyl)-99-methyl-66-(2-methylpropyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectane-36-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,45R,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-10,51,69,75,87-pentakis(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-93-(3-amino-3-oxopropyl)-60,96-dibenzyl-19,28-bis[(2S)-butan-2-yl]-4,54-bis(3-carbamimidamidopropyl)-25-(carboxymethyl)-2a,22,39,48-tetrakis[(1R)-1-hydroxyethyl]-7,63,81-tris(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-84-(1H-imidazol-5-ylmethyl)-99-methyl-66-(2-methylpropyl)-78-(2-methylsulfanylethyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectane-36-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,45R,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-10,51,66,75,87-pentakis(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-93-(3-amino-3-oxopropyl)-60,96-dibenzyl-19,28-bis[(2S)-butan-2-yl]-4,54,69-tris(3-carbamimidamidopropyl)-25-(carboxymethyl)-2a,22,39,48-tetrakis[(1R)-1-hydroxyethyl]-7,63,81-tris(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-84-(1H-imidazol-5-ylmethyl)-99-methyl-78-(2-methylsulfanylethyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectane-36-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
| (1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,45R,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-10,51,63,75,87-pentakis(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-93-(3-amino-3-oxopropyl)-60,96-dibenzyl-19,28-bis[(2S)-butan-2-yl]-4,54,69-tris(3-carbamimidamidopropyl)-25-(carboxymethyl)-2a,22,39,48-tetrakis[(1R)-1-hydroxyethyl]-7,81-bis(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-84-(1H-imidazol-5-ylmethyl)-99-methyl-66-(2-methylpropyl)-78-(2-methylsulfanylethyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectane-36-carboxylic acid | 1243416: Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay | ic50 | <0.0001 | uM |
CTD chemical–gene interactions
24 total (human), top 24 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Valproic Acid | increases expression, affects cotreatment, decreases expression, affects expression | 6 |
| entinostat | decreases expression, affects cotreatment | 2 |
| Benzo(a)pyrene | increases expression, increases methylation | 2 |
| Cyclosporine | decreases expression, increases expression | 2 |
| bisphenol F | affects cotreatment, increases methylation | 1 |
| methylmercuric chloride | decreases expression | 1 |
| trichostatin A | decreases expression | 1 |
| arsenite | increases methylation | 1 |
| CGP 52608 | increases reaction, affects binding | 1 |
| 4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide | affects cotreatment, decreases expression | 1 |
| dorsomorphin | affects cotreatment, decreases expression | 1 |
| Resveratrol | affects cotreatment, decreases expression | 1 |
| Fulvestrant | affects cotreatment, increases methylation | 1 |
| Diazinon | increases methylation | 1 |
| Diethylhexyl Phthalate | decreases expression | 1 |
| Drugs, Chinese Herbal | increases expression | 1 |
| Naphthoquinones | increases expression | 1 |
| Nickel | decreases expression | 1 |
| Plant Extracts | decreases expression, affects cotreatment | 1 |
| Scorpion Venoms | affects binding, decreases reaction | 1 |
| Triclosan | decreases expression | 1 |
| Cadmium Chloride | increases expression | 1 |
| Okadaic Acid | increases expression | 1 |
| Tetraethylammonium | affects binding, decreases reaction | 1 |
ChEMBL screening assays
59 unique, capped per target: 52 binding, 6 functional, 1 toxicity
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1039576 | Binding | Inhibition of Kv1.1 expressed in CHO cells by patch-clamp technique | Selective Kv1.5 blockers: development of (R)-1-(methylsulfonylamino)-3-[2-(4-methoxyphenyl)ethyl]-4-(4-methoxyphenyl)-2-imidazolidinone (KVI-020/WYE-160020) as a potential treatment for atrial arrhythmia. — J Med Chem |
| CHEMBL703981 | Functional | K+ channel blocking activity as blockade at 25 uM in Xenopus laevis Ranvier nodes | Alkoxypsoralens, novel nonpeptide blockers of Shaker-type K+ channels: synthesis and photoreactivity. — J Med Chem |
| 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 |
Cellosaurus cell lines
6 cell lines: 4 induced pluripotent stem cell, 2 spontaneously immortalized cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_C0XX | B’SYS CHO Kv1.1 | Spontaneously immortalized cell line | Female |
| CVCL_D1JU | PrecisION hKv1.1-CHO | Spontaneously immortalized cell line | Female |
| CVCL_E7L7 | KOLF2.1J KCNA1 R239S SNV/SNV | Induced pluripotent stem cell | Male |
| CVCL_E7L8 | KOLF2.1J KCNA1 R239S SNV/WT | Induced pluripotent stem cell | Male |
| CVCL_E7LA | KOLF2.1J KCNA1 R417X SNV/SNV | Induced pluripotent stem cell | Male |
| CVCL_E7LB | KOLF2.1J KCNA1 R417X SNV/WT | Induced pluripotent stem cell | Male |
Clinical trials (associated diseases)
322 trials via MONDO — disease-level, not drug-specific.
| Trial | Phase | Status | Title |
|---|---|---|---|
| NCT00004637 | PHASE4 | COMPLETED | Double-Blind, Placebo-Controlled Trial of Vitamin E as Add-on Therapy for Children With Epilepsy |
| NCT00043914 | PHASE4 | COMPLETED | Measurement Of Serum Levels Of Two Antiepileptic Drugs During Conversion In Patients With Epilepsy |
| NCT00132223 | PHASE4 | UNKNOWN | Effects on the Diagnostic Accuracy of Magnetic Imaging Angiographies of the Supra-Aortic Vessels by Three Different Magnetic Resonance Contrast Agents in Patients |
| NCT00133081 | PHASE4 | UNKNOWN | Study to Improve the Treatment of Epilepsy (SITE) |
| NCT00137709 | PHASE4 | UNKNOWN | Hormone Profiles in Adults With Newly Diagnosed Epilepsy |
| NCT00154076 | PHASE4 | COMPLETED | A Multicenter Comparative Trial of Zonisamide and Topiramate as Initial Monotherapy in Untreated Epilepsies |
| NCT00165828 | PHASE4 | TERMINATED | Efficacy and Safety of an add-on Treatment With Zonisamide in Adults With Focal Epileptic Seizures With or Without Secondary Generalization |
| NCT00181116 | PHASE4 | COMPLETED | Levetiracetam for Benign Rolandic Epilepsy |
| NCT00207935 | PHASE4 | COMPLETED | Use of Sustained Release Antiepileptic Medication (Depakote® ER) for Pediatric Epilepsy in a Mental Retardation/Developmental Disorder Population |
| NCT00215592 | PHASE4 | COMPLETED | Open Label, Zonegran (Zonisamide) In Partial Onset Seizures |
| NCT00266604 | PHASE4 | COMPLETED | A Study to Evaluate the Dosing, Effectiveness and Safety of Topiramate for the Treatment of Epilepsy |
| NCT00288639 | PHASE4 | COMPLETED | Lyrica (Pregabalin) Administered as an Add-on Therapy for Partial Seizures (LEADER). |
| NCT00312676 | PHASE4 | UNKNOWN | Compare Tolerability of an Overnight Switch to Gradual Switch Between Two Different Forms of Depakote |
| NCT00323947 | PHASE4 | COMPLETED | Methylphenidate for Treating Attention Deficit Hyperactivity Disorder in Children With Both ADHD and Epilepsy |
| NCT00385411 | PHASE4 | COMPLETED | Study of Valproate in Young Patients Suffering From Epilepsy |
| NCT00522418 | PHASE4 | TERMINATED | Study Comparing Best Medical Practice With or Without VNS Therapy in Pharmacoresistant Partial Epilepsy Patients |
| NCT00537940 | PHASE4 | COMPLETED | Comparative Study Of Pregabalin And Gabapentin As Adjunctive Therapy In Subjects With Partial Seizures |
| NCT00552526 | PHASE4 | UNKNOWN | Ketogenic Diet vs.Antiepileptic Drug Treatment in Drug Resistant Epilepsy |
| NCT00564915 | PHASE4 | COMPLETED | RCT of the Efficacy of the Ketogenic Diet in the Treatment of Epilepsy |
| NCT00571155 | PHASE4 | COMPLETED | Trial of Levetiracetam in Patients With Primary Brain Tumors and Symptomatic Seizures Who Undergo Surgery |
| NCT00572195 | PHASE4 | COMPLETED | RNS® System LTT Study |
| NCT00610532 | PHASE4 | TERMINATED | Evaluating the Transporter Protein Inhibitor Probenecid In Patients With Epilepsy |
| NCT00630357 | PHASE4 | COMPLETED | Trial to Evaluate the Safety and Efficacy of Keppra After Conversion to Mono-therapy in Subjects With Partial Epilepsy |
| NCT00630630 | PHASE4 | COMPLETED | Study on Safety and Efficacy of Levetiracetam in the Adjunctive Treatment of Female Subjects With C1 Catamenial Epilepsy |
| NCT00630968 | PHASE4 | COMPLETED | S.K.A.T.E.: Safety of Keppra as Adjunctive Therapy in Epilepsy |
| NCT00631150 | PHASE4 | COMPLETED | A Phase IV-Pharmacovigilance Study of Keppra Greece - S.K.A.T.E.: Safety of Keppra as Adjunctive Therapy in Epilepsy |
| NCT00659958 | PHASE4 | COMPLETED | ZAGAL Study: Evaluating Effectiveness and Tolerability of Zonisamide as Adjunctive Therapy in Patients With Partial Onset Seizures Treated With Two Antiepileptic Drugs |
| NCT00713622 | PHASE4 | COMPLETED | Comparing The Effect On Cognition Of Adjunctive Therapy With Zonisamide Versus Sodium Valproate |
| NCT00807989 | PHASE4 | COMPLETED | The Efficacy and Safety of Low Dose Combination of LTG and VPA Compared to CBZ Monotherapy |
| NCT00832884 | PHASE4 | COMPLETED | The Safety of Intravenous Lacosamide |
| NCT00869622 | PHASE4 | COMPLETED | Antiepileptic Drugs and Osteoporotic Prevention Trial |
| NCT00896987 | PHASE4 | COMPLETED | Lamotrigine Cognitive Function Study in Adult Untreated Epilepsies |
| NCT00952081 | PHASE4 | COMPLETED | A Pilot Study to Evaluate Efficacy and Safety of Clevidipine in Neurosurgical Patients |
| NCT01118455 | PHASE4 | TERMINATED | Trial to Assess Vagus Nerve Stimulation Therapy vs. Anti-Epileptic Drug (AED) Treatment in Children With Refractory Seizures |
| NCT01127165 | PHASE4 | COMPLETED | Low and High Dose Zonisamide in Children as Monotherapy |
| NCT01127256 | PHASE4 | COMPLETED | Comparative Study of Zonisamide and Carbamazepine as an Initial Monotherapy: Efficacy and Safety Evaluation |
| NCT01140867 | PHASE4 | COMPLETED | Open-label, Multi-center Trial of Zonisamide as Adjunctive Therapy in Patients With Uncontrolled Partial Epilepsy |
| NCT01175954 | PHASE4 | COMPLETED | Cognitive and Behavioral Effects of Lacosamide |
| NCT01229735 | PHASE4 | COMPLETED | Levetiracetam Versus Topiramate as Adjunctive Therapy to Evaluate Efficacy and Safety in Subjects With Refractory Partial Onset Seizures |
| NCT01244724 | PHASE4 | TERMINATED | Lexapro for Major Depression in Patients With Epilepsy |
Related Atlas pages
- Associated diseases: episodic ataxia type 1, genetic developmental and epileptic encephalopathy, isolated autosomal dominant hypomagnesemia, Glaudemans type, episodic kinesigenic dyskinesia 1, epilepsy
- Targeted by drugs: Capsaicin, Diltiazem, Flecainide, Nifedipine, Potassium, Resiniferatoxin
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): atrial fibrillation, familial, 7, epilepsy, episodic ataxia type 1, episodic kinesigenic dyskinesia, generalized epilepsy-paroxysmal dyskinesia syndrome, genetic developmental and epileptic encephalopathy, hereditary ataxia, isolated autosomal dominant hypomagnesemia, Glaudemans type