General Information of the Protein
Protein ID
PT01821
Protein Name
Calcium-activated potassium channel subunit alpha-1
Secondarily
Protein Name
BK channel
BKCA alpha
Calcium-activated potassium channel
subfamily M subunit alpha-1
K(VCA)alpha
KCa1.1
Maxi K channel
Slo-alpha
Slo1
Slowpoke homolog
Gene Name
KCNMA1
Secondarily
Gene Name
KCNMA
SLO
Sequence
MANGGGGGGGSSGGGGGGGGSSLRMSSNIHANHLSLDASSSSSSSSSSSSSSSSSSSSSSVHEPKMDALIIPVTMEVPCDSRGQRMWWAFLASSMVTFFGGLFIILLWRTLKYLWTVCCHCGGKTKEAQKINNGSSQADGTLKPVDEKEEAVAAEVGWMTSVKDWAGVMISAQTLTGRVLVVLVFALSIGALVIYFIDSSNPIESCQNFYKDFTLQIDMAFNVFFLLYFGLRFIAANDKLWFWLEVNSVVDFFTVPPVFVSVYLNRSWLGLRFLRALRLIQFSEILQFLNILKTSNSIKLVNLLSIFISTWLTAAGFIHLVENSGDPWENFQNNQALTYWECVYLLMVTMSTVGYGDVYAKTTLGRLFMVFFILGGLAMFASYVPEIIELIGNRKKYGGSYSAVSGRKHIVVCGHITLESVSNFLKDFLHKDRDDVNVEIVFLHNISPNLELEALFKRHFTQVEFYQGSVLNPHDLARVKIESADACLILANKYCADPDAEDASNIMRVISIKNYHPKIRIITQMLQYHNKAHLLNIPSWNWKEGDDAICLAELKLGFIAQSCLAQGLSTMLANLFSMRSFIKIEEDTWQKYYLEGVSNEMYTEYLSSAFVGLSFPTVCELCFVKLKLLMIAIEYKSANRESRILINPGNHLKIQEGTLGFFIASDAKEVKRAFFYCKACHDDITDPKRIKKCGCKRPKMSIYKRMRRACCFDCGRSERDCSCMSGRVRGNVDTLERAFPLSSVSVNDCSTSFRAFEDEQPSTLSPKKKQRNGGMRNSPNTSPKLMRHDPLLIPGNDQIDNMDSNVKKYDSTGMFHWCAPKEIEKVILTRSEAAMTVLSGHVVVCIFGDVSSALIGLRNLVMPLRASNFHYHELKHIVFVGSIEYLKREWETLHNFPKVSILPGTPLSRADLRAVNINLCDMCVILSANQNNIDDTSLQDKECILASLNIKSMQFDDSIGVLQANSQGFTPPGMDRSSPDNSPVHGMLRQPSITTGVNIPIITELVNDTNVQFLDQDDDDDPDTELYLTQPFACGTAFAVSVLDSLMSATYFNDNILTLIRTLVTGGATPELEALIAEENALRGGYSTPQTLANRDRCRVAQLALLDGPFADLGDGGCYGDLFCKALKTYNMLCFGIYRLRDAHLSTPSQCTKRYVITNPPYEFELVPTDLIFCLMQFDHNAGQSRASLSHSSHSSQSSSKKSSSVHSIPSTANRQNRPKSRESRDKQKYVQEERL
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Organism
Homo sapiens, Human
Protein Classification
Ion channel
>
Voltage-gated ion channel
>
Potassium channels
>
Calcium-activated potassium channel
Function
Potassium channel activated by both membrane depolarization or increase in cytosolic Ca(2+) that mediates export of K(+) (PubMed:29330545, PubMed:31152168). It is also activated by the concentration of cytosolic Mg(2+). Its activation dampens the excitatory events that elevate the cytosolic Ca(2+) concentration and/or depolarize the cell membrane. It therefore contributes to repolarization of the membrane potential. Plays a key role in controlling excitability in a number of systems, such as regulation of the contraction of smooth muscle, the tuning of hair cells in the cochlea, regulation of transmitter release, and innate immunity. In smooth muscles, its activation by high level of Ca(2+), caused by ryanodine receptors in the sarcoplasmic reticulum, regulates the membrane potential. In cochlea cells, its number and kinetic properties partly determine the characteristic frequency of each hair cell and thereby helps to establish a tonotopic map. Kinetics of KCNMA1 channels are determined by alternative splicing, phosphorylation status and its combination with modulating beta subunits. Highly sensitive to both iberiotoxin (IbTx) and charybdotoxin (CTX).
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Uniprot ID
Primary ID:
Q12791

Secondarily ID:
F8WA96
Q12886
Q12917
Q12921
Q12960
Q13150
Q5JQ23
Q5SQR9
Q96LG8
Q9UBB0
Q9UCX0
Q9UQK6
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Ensembl ID
ENSG00000156113
HGNC ID
HGNC:6284
Subcellular Location
Cell membrane
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: CL000006 , HEK293
Compound ID Compound Name Compound Formula
CP0393271
2-Azepan-1-yl-1H-pyrrolo[3,2-b]pyridine-3-carbonitrile
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C14H16N4
 1
1
EC50 = 3340 nM
   TI
   LI
   LO
   TS
CP0404746
2-Morpholin-4-yl-1H-pyrrolo[3,2-b]pyridine-3-carbonitrile
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C12H12N4O
 1
1
EC50 = 3860 nM
   TI
   LI
   LO
   TS
CP0430223
2-(3-Aza-bicyclo[3.2.2]non-3-yl)-1H-pyrrolo[3,2-b]pyridine-3-carbonitrile
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C16H18N4
 1
1
EC50 = 4430 nM
   TI
   LI
   LO
   TS
CP0404591
2-((S)-3-Hydroxy-piperidin-1-yl)-1H-pyrrolo[3,2-b]pyridine-3-carbonitrile
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C13H14N4O
 1
1
EC50 = 5070 nM
   TI
   LI
   LO
   TS
CP0393270
2-Dimethylamino-1H-pyrrolo[3,2-b]pyridine-3-carbonitrile
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C10H10N4
 1
1
EC50 = 5130 nM
   TI
   LI
   LO
   TS
CP0538288
2-Imidazol-1-yl-1H-pyrrolo[3,2-b]pyridine-3-carbonitrile
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C11H7N5
 1
1
EC50 = 5860 nM
   TI
   LI
   LO
   TS
CP0495748
2-[(2-Dimethylamino-ethyl)-methyl-amino]-1H-pyrrolo[3,2-b]pyridine-3-carbonitrile
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C13H17N5
 1
1
EC50 = 6750 nM
   TI
   LI
   LO
   TS
CP0431153
2-Diethylamino-1H-pyrrolo[3,2-b]pyridine-3-carbonitrile
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C12H14N4
 1
1
EC50 = 6940 nM
   TI
   LI
   LO
   TS
CP0480727
2-Pyrrolidin-1-yl-1H-pyrrolo[3,2-b]pyridine-3-carbonitrile
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C12H12N4
 1
1
EC50 = 8120 nM
   TI
   LI
   LO
   TS
CP0874517
2-Hydroxy-1H-pyrrolo[3,2-b]pyridine-3-carbonitrile
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C8H5N3O
 1
1
EC50 = 13400 nM
   TI
   LI
   LO
   TS
CP0430204
2-(4-Hydroxy-piperidin-1-yl)-1H-pyrrolo[3,2-b]pyridine-3-carbonitrile
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C13H14N4O
 1
1
EC50 = 15100 nM
   TI
   LI
   LO
   TS
CP0462342
1-(3-Cyano-1H-pyrrolo[3,2-b]pyridin-2-yl)-piperidine-4-carboxylic acid methyl ester
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C15H16N4O2
 1
1
EC50 = 17000 nM
   TI
   LI
   LO
   TS
CP0547360
N-(5-chloro-2-methoxyphenyl)-2-[(2R)-2-methyl-4-(4-methylpiperidin-1-yl)sulfonylpiperazin-1-yl]acetamide
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C20H31ClN4O4S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0569389
N-[2-methoxy-5-(trifluoromethyl)phenyl]-2-[4-(4-methylpiperidin-1-yl)sulfonylpiperazin-1-yl]acetamide
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C20H29F3N4O4S
 1
1
IC50 > 10000 nM
   TI
   LI
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Clinical Information about the Protein
Target 1 ( Calcium-activated potassium channel KCa1.1 (KCNMA1) )
Target Type Clinical trial Target