General Information of the Protein
Protein ID
PT02933
Protein Name
Potassium voltage-gated channel subfamily A member 1
Secondarily
Protein Name
Voltage-gated K(+) channel HuKI
Voltage-gated potassium channel HBK1
Voltage-gated potassium channel subunit Kv1.1
Gene Name
KCNA1
Sequence
MTVMSGENVDEASAAPGHPQDGSYPRQADHDDHECCERVVINISGLRFETQLKTLAQFPNTLLGNPKKRMRYFDPLRNEYFFDRNRPSFDAILYYYQSGGRLRRPVNVPLDMFSEEIKFYELGEEAMEKFREDEGFIKEEERPLPEKEYQRQVWLLFEYPESSGPARVIAIVSVMVILISIVIFCLETLPELKDDKDFTGTVHRIDNTTVIYNSNIFTDPFFIVETLCIIWFSFELVVRFFACPSKTDFFKNIMNFIDIVAIIPYFITLGTEIAEQEGNQKGEQATSLAILRVIRLVRVFRIFKLSRHSKGLQILGQTLKASMRELGLLIFFLFIGVILFSSAVYFAEAEEAESHFSSIPDAFWWAVVSMTTVGYGDMYPVTIGGKIVGSLCAIAGVLTIALPVPVIVSNFNYFYHRETEGEEQAQLLHVSSPNLASDSDLSRRSSSTMSKSEYMEIEEDMNNSIAHYRQVNIRTANCTTANQNCVNKSKLLTDV
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Organism
Homo sapiens, Human
Protein Classification
Ion channel
>
Voltage-gated ion channel
>
Potassium channels
>
Voltage-gated potassium channel
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 (PubMed:8845167, PubMed:19903818). Contributes to the regulation of the membrane potential and nerve signaling, and prevents neuronal hyperexcitability (PubMed:17156368). 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 (PubMed:19912772). 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 (PubMed:12077175, PubMed:17156368). 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 (PubMed:12077175, PubMed:17156368). 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 (PubMed:19912772, PubMed:19968958, PubMed:19307729, PubMed:19903818). In contrast, a heterotetrameric channel formed by KCNA1 and KCNA4 shows rapid inactivation (PubMed:17156368). 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 (By similarity). May function as down-stream effector for G protein-coupled receptors and inhibit GABAergic inputs to basolateral amygdala neurons (By similarity). May contribute to the regulation of neurotransmitter release, such as gamma-aminobutyric acid (GABA) release (By similarity). 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 (By similarity). Required for normal neuromuscular responses (PubMed:11026449, PubMed:17136396). 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 (By similarity). Required for normal responses to auditory stimuli and precise location of sound sources, but not for sound perception (By similarity). The use of toxins that block specific channels suggest that it contributes to the regulation of the axonal release of the neurotransmitter dopamine (By similarity). Required for normal postnatal brain development and normal proliferation of neuronal precursor cells in the brain (By similarity). 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 (PubMed:23903368, PubMed:19307729).
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Uniprot ID
Primary ID:
Q09470

Secondarily ID:
A6NM83
Q3MIQ9
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Ensembl ID
ENSG00000111262
HGNC ID
HGNC:6218
Subcellular Location
Cell membrane
Membrane
Cell projection
Axon
Cytoplasmic vesicle
Perikaryon
Endoplasmic reticulum
Cell projection
Dendrite
Cell junction
Synapse
Presynaptic cell membrane
Presynapse
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000011 , CHO
Compound ID Compound Name Compound Formula
CP0153862
4-(4-phenoxybutoxy)-7H-furo[3,2-g]chromen-7-one
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C21H18O5
 1
1
IC50 = 250 nM
   TI
   LI
   LO
   TS
CP0271660
(R)-1-(Methylsulfonylamino)-3-[2-(4-methoxyphenyl)ethyl]-4-(4-methoxy-phenyl)-2-imidazolidinone
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C20H25N3O5S
 1
1
IC50 = 2660 nM
   TI
   LI
   LO
   TS
CP0383207
N-[(E)-3-(2-amino-1H-imidazol-5-yl)prop-2-enyl]-4-bromo-5-methyl-1H-pyrrole-2-carboxamide
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C12H14BrN5O
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0383208
N-[(E)-3-(2-amino-1H-imidazol-5-yl)prop-2-enyl]-4-bromo-1H-pyrrole-2-carboxamide
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C11H12BrN5O
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0383210
N-[(E)-3-(2-amino-1H-imidazol-5-yl)prop-2-enyl]-4-chloro-5-methyl-1H-pyrrole-2-carboxamide
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C12H14ClN5O
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0383921
N-[(E)-3-(2-amino-1H-imidazol-5-yl)prop-2-enyl]-1H-indole-2-carboxamide
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C15H15N5O
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0383922
N-[(E)-3-(2-amino-1H-imidazol-5-yl)prop-2-enyl]-5-fluoro-1H-indole-2-carboxamide
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C15H14FN5O
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0402452
N-[(E)-3-(2-amino-1H-imidazol-5-yl)prop-2-enyl]-5-chloro-1H-indole-2-carboxamide
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C15H14ClN5O
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0410962
Clathrodin
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C11H13N5O
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0410963
N-[(E)-3-(2-amino-1H-imidazol-5-yl)prop-2-enyl]-3,4-dibromo-5-methyl-1H-pyrrole-2-carboxamide
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C12H13Br2N5O
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0412411
N-[(E)-3-(2-amino-1H-imidazol-5-yl)prop-2-enyl]-4,5-dichloro-1H-pyrrole-2-carboxamide
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C11H11Cl2N5O
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0655034
Oroidin
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C11H11Br2N5O
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0153862
4-(4-phenoxybutoxy)-7H-furo[3,2-g]chromen-7-one
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C21H18O5
 1
1 EC50 = 65 nM
Clinical Information about the Protein
Target 1 ( Voltage-gated potassium channel Kv1.1 (KCNA1) )
Target Type Literature-reported Target