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KCNN1

gene
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Also known as KCa2.1hSK1

Summary

KCNN1 (potassium calcium-activated channel subfamily N member 1, HGNC:6290) is a protein-coding gene on chromosome 19p13.11, encoding Small conductance calcium-activated potassium channel protein 1 (Q92952). Small conductance calcium-activated potassium channel that mediates the voltage-independent transmembrane transfer of potassium across the cell membrane through a constitutive interaction with calmodulin which binds the intracellular calcium allowing its opening.

Action potentials in vertebrate neurons are followed by an afterhyperpolarization (AHP) that may persist for several seconds and may have profound consequences for the firing pattern of the neuron. Each component of the AHP is kinetically distinct and is mediated by different calcium-activated potassium channels. The protein encoded by this gene is activated before membrane hyperpolarization and is thought to regulate neuronal excitability by contributing to the slow component of synaptic AHP. The encoded protein is an integral membrane protein that forms a voltage-independent calcium-activated channel with three other calmodulin-binding subunits. This gene is a member of the KCNN family of potassium channel genes.

Source: NCBI Gene 3780 — RefSeq curated summary.

At a glance

  • GWAS associations: 2
  • Clinical variants (ClinVar): 82 total
  • Druggable target: yes
  • MANE Select transcript: NM_001386974

Identifiers

Gene identifiers

FieldValue
HGNC IDHGNC:6290
Approved symbolKCNN1
Namepotassium calcium-activated channel subfamily N member 1
Location19p13.11
Locus typegene with protein product
StatusApproved
AliasesKCa2.1, hSK1
Ensembl geneENSG00000105642
Ensembl biotypeprotein_coding
OMIM602982
Entrez3780

Gene structure

Transcript identifiers

Ensembl transcripts: 17 — 14 protein_coding, 2 nonsense_mediated_decay, 1 protein_coding_CDS_not_defined

ENST00000222249, ENST00000594192, ENST00000609922, ENST00000615435, ENST00000682421, ENST00000682726, ENST00000682733, ENST00000683588, ENST00000683930, ENST00000684725, ENST00000684775, ENST00000925809, ENST00000925810, ENST00000925811, ENST00000925812, ENST00000925813, ENST00000925814

RefSeq mRNA: 5 — MANE Select: NM_001386974 NM_001386974, NM_001386975, NM_001386976, NM_001386977, NM_002248

CCDS: CCDS67611, CCDS92562, CCDS92563

Canonical transcript exons

ENST00000684775 — 10 exons

ExonStartEnd
ENSE000034932131798841517988525
ENSE000035603981797380817974290
ENSE000035811561798971617989843
ENSE000036043411799349017993559
ENSE000036177011798531217985453
ENSE000036348041798170917982127
ENSE000036618951797509217975187
ENSE000037112171799305417993062
ENSE000037211651799815218000085
ENSE000039161081796710717967317

Expression profiles

Bgee: expression breadth ubiquitous, 147 present calls, max score 93.73.

FANTOM5 (CAGE): breadth broad, TPM avg 1.7213 / max 63.6792, expressed in 373 samples.

FANTOM5 promoters (4 alternative TSS)

Promoter IDTPM avgSamples expressed
1745701.0373262
1745690.3780157
1745680.2604120
1745670.045615

Top tissues by expression

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

TissueAnatomy IDExpression scoreQuality
right frontal lobeUBERON:000281093.73gold quality
cingulate cortexUBERON:000302793.53gold quality
anterior cingulate cortexUBERON:000983593.43gold quality
prefrontal cortexUBERON:000045192.37gold quality
amygdalaUBERON:000187691.99gold quality
CA1 field of hippocampusUBERON:000388191.31gold quality
dorsolateral prefrontal cortexUBERON:000983490.77gold quality
Brodmann (1909) area 9UBERON:001354090.45gold quality
neocortexUBERON:000195090.13gold quality
frontal cortexUBERON:000187090.00gold quality
Ammon’s hornUBERON:000195489.95gold quality
cerebral cortexUBERON:000095689.20gold quality
type B pancreatic cellCL:000016987.82gold quality
telencephalonUBERON:000189387.52gold quality
olfactory bulbUBERON:000226487.34gold quality
ganglionic eminenceUBERON:000402386.99gold quality
temporal lobeUBERON:000187186.93gold quality
putamenUBERON:000187486.83gold quality
caudate nucleusUBERON:000187386.55gold quality
Brodmann (1909) area 10UBERON:001354186.55gold quality
nucleus accumbensUBERON:000188285.52gold quality
superior frontal gyrusUBERON:000266184.45gold quality
postcentral gyrusUBERON:000258184.25gold quality
Brodmann (1909) area 46UBERON:000648383.99gold quality
forebrainUBERON:000189083.71gold quality
primary visual cortexUBERON:000243683.13gold quality
cortical plateUBERON:000534382.85gold quality
entorhinal cortexUBERON:000272882.26gold quality
brainUBERON:000095581.83gold quality
orbitofrontal cortexUBERON:000416781.56silver quality

Single-cell (SCXA)

Detected in 1 experiment(s), a significant marker in 1.

ExperimentMarker?Max mean expression
E-ANND-3yes2.57

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

25 targeting KCNN1, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNAMax scoreAvg scoremiRNA target_count
HSA-MIR-188-3P100.0068.761240
HSA-MIR-449299.8768.253611
HSA-MIR-489-3P99.8066.46839
HSA-MIR-6763-5P99.7664.681767
HSA-MIR-6512-3P99.6566.071468
HSA-MIR-6720-5P99.6566.221459
HSA-MIR-317599.6566.302031
HSA-MIR-76299.5866.611994
HSA-MIR-449899.4767.422360
HSA-MIR-7158-5P99.2567.95796
HSA-MIR-6815-3P99.1368.981530
HSA-MIR-548AS-3P99.1269.122294
HSA-MIR-66199.0965.942062
HSA-MIR-5001-5P99.0566.761972
HSA-MIR-392698.9569.261438
HSA-MIR-429798.7766.952013
HSA-MIR-548S98.5067.171213
HSA-MIR-6864-5P98.3866.591079
HSA-MIR-317998.2265.901445
HSA-MIR-126398.1369.18459
HSA-MIR-5581-5P97.9166.50965
HSA-MIR-445697.5064.881678
HSA-MIR-606997.4565.88357
HSA-MIR-64597.2866.30486
HSA-MIR-390796.7665.04662

Literature-anchored findings (GeneRIF, showing 9)

  • IK1-like immunoreactivity is observed in enteric neurons of human colon, with a significant decrease of IK1-positive cells in inflamed colon from patients with Crohn’s disease and ulcerative colitis. (PMID:12598727)
  • Decreased expression of small-conductance Ca2+-activated K+ channels SK1 and SK2 in human chronic atrial fibrillation. (PMID:22154908)
  • Differentiated dopaminergic neurons expressed low levels of SK2 channels and high levels of SK1 and SK3 channels. (PMID:24434522)
  • SK current is increased via the enhanced activation of CaMKII in patients with atrial fibrillation. (PMID:29737974)
  • Data demonstrate that IKCa and SK1 subunits prefer to form heteromeric channels when coexpressed in a heterologous system that will alter their responsiveness to pharmacological tools typically used to define their expression pattern. (PMID:31048549)
  • Targeting Kca3.1 Channels in Cancer. (PMID:34043300)
  • Differential regulation of KCa 2.1 (KCNN1) K(+) channel expression by histone deacetylases in atrial fibrillation with concomitant heart failure. (PMID:34111326)
  • KCNN1 promotes proliferation and metastasis of breast cancer via ERLIN2-mediated stabilization and K63-dependent ubiquitination of Cyclin B1. (PMID:37831636)
  • A single coiled-coil domain mutation in hIKCa channel subunits disrupts preferential formation of heteromeric hSK1:hIKCa channels. (PMID:38018635)

Cross-species orthologs

9 orthologs

OrganismSymbolGene ID
danio_reriokcnn1bENSDARG00000023546
danio_reriokcnn1aENSDARG00000091306
mus_musculusKcnn1ENSMUSG00000002908
rattus_norvegicusKcnn1ENSRNOG00000029264
drosophila_melanogasterSKFBGN0029761
caenorhabditis_elegansWBGENE00007176
caenorhabditis_elegansWBGENE00008265
caenorhabditis_eleganskcnl-2WBGENE00008570
caenorhabditis_elegansWBGENE00015387

Paralogs (3): KCNN2 (ENSG00000080709), KCNN4 (ENSG00000104783), KCNN3 (ENSG00000143603)

Protein

Protein identifiers

Small conductance calcium-activated potassium channel protein 1 — Q92952 (reviewed: Q92952)

Alternative names: KCa2.1

All UniProt accessions (7): A0A087X2E7, A0A804HIF9, A0A804HIJ6, A0A804HIW7, A0A804HK94, Q92952, V9GYV2

UniProt curated annotations — full annotation on UniProt →

Function. Small conductance calcium-activated potassium channel that mediates the voltage-independent transmembrane transfer of potassium across the cell membrane through a constitutive interaction with calmodulin which binds the intracellular calcium allowing its opening. The current is characterized by a voltage-independent activation, an intracellular calcium concentration increase-dependent activation and a single-channel conductance of about 3 picosiemens. Also presents an inwardly rectifying current, thus reducing its already small outward conductance of potassium ions, which is particularly the case when the membrane potential displays positive values, above + 20 mV. Activation is followed by membrane hyperpolarization. Thought to regulate neuronal excitability by contributing to the slow component of synaptic afterhyperpolarization.

Subunit / interactions. Homodimer. Heteromultimer with KCNN2 and KCNN3. The complex is composed of 4 channel subunits each of which binds to a calmodulin subunit which regulates the channel activity through calcium-binding. Interacts with calmodulin.

Subcellular location. Membrane. Cytoplasm. Myofibril. Sarcomere. Z line.

Activity regulation. Inhibited by bee venom neurotoxin apamin. Inhibited by d-tubocurarine and tetraethylammonium (TEA).

Domain organisation. The coiled-coil domaim mediates heteromeic assembly.

Similarity. Belongs to the potassium channel KCNN family. KCa2.1/KCNN1 subfamily.

Isoforms (2)

UniProt IDNamesCanonical?
Q92952-11yes
Q92952-22

RefSeq proteins (5): NP_001373903, NP_001373904, NP_001373905, NP_001373906, NP_002239 (=MANE)

Domains & families (InterPro)

IDNameType
IPR004178CaM-bd_domDomain
IPR013099K_chnl_domDomain
IPR015449K_chnl_Ca-activ_SKFamily
IPR036122CaM-bd_dom_sfHomologous_superfamily

Pfam: PF02888, PF03530, PF07885

Catalyzed reactions (Rhea), 1 shown:

  • K(+)(in) = K(+)(out) (RHEA:29463)

UniProt features (21 total): transmembrane region 6, mutagenesis site 6, region of interest 3, compositionally biased region 2, chain 1, splice variant 1, sequence conflict 1, intramembrane region 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-Q92952-F178.560.45

Functional residue map

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

Mutagenesis-validated functional residues (6):

PositionPhenotype
216significantly increased inhibition by apamin (ic(50)=167 pm). no effect on inhibition by d-tubocurarine and tetraethylam
310loss of inhibition by apamin. no effect on inhibition by d-tubocurarine. increased inhibition by apamin; when associated
312increased inhibition by apamin or d-tubocurarine (ic(50)=62.6 um). additive increase in inhibition by apamin or d-tubocu
332–334impairs small conductance calcium-activated potassium channel activity of kcnn2.
337increased inhibition by tetraethylammonium (tea).
339increased inhibition by apamin or d-tubocurarine (ic(50)=11.1 um). additive increase in inhibition by apamin or d-tubocu

Function

Pathways and Gene Ontology

Reactome pathways

3 pathways

IDPathway
R-HSA-1296052Ca2+ activated K+ channels
R-HSA-112316Neuronal System
R-HSA-1296071Potassium Channels

MSigDB gene sets: 115 (showing top): GOBP_POTASSIUM_ION_TRANSPORT, MODULE_274, REACTOME_POTASSIUM_CHANNELS, MODULE_64, TGACCTY_ERR1_Q2, MEF2_02, FOXO1_01, GOBP_MONOATOMIC_CATION_TRANSPORT, GOBP_CELL_CELL_SIGNALING, MODULE_379, GOBP_SYNAPTIC_SIGNALING, BYSTRYKH_HEMATOPOIESIS_STEM_CELL_AND_BRAIN_QTL_TRANS, GOCC_NEURON_PROJECTION, MODULE_242, MEF2_Q6_01

GO Biological Process (6): potassium ion transport (GO:0006813), chemical synaptic transmission (GO:0007268), potassium ion transmembrane transport (GO:0071805), monoatomic ion transport (GO:0006811), monoatomic ion transmembrane transport (GO:0034220), monoatomic cation transmembrane transport (GO:0098655)

GO Molecular Function (5): inward rectifier potassium channel activity (GO:0005242), calmodulin binding (GO:0005516), calcium-activated potassium channel activity (GO:0015269), small conductance calcium-activated potassium channel activity (GO:0016286), potassium channel activity (GO:0005267)

GO Cellular Component (8): plasma membrane (GO:0005886), voltage-gated potassium channel complex (GO:0008076), Z disc (GO:0030018), neuron projection (GO:0043005), neuronal cell body (GO:0043025), synapse (GO:0045202), cytoplasm (GO:0005737), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-2 pathways:

CategoryPathways
Potassium Channels1
Neuronal System1

GO top-level categories

Rollup of top GO terms by namespace:

CategoryTerms
cellular anatomical structure3
metal ion transport1
anterograde trans-synaptic signaling1
potassium ion transport1
monoatomic cation transmembrane transport1
transport1
monoatomic ion transport1
transmembrane transport1
monoatomic cation transport1
monoatomic ion transmembrane transport1
voltage-gated potassium channel activity1
ligand-gated monoatomic cation channel activity1
protein binding1
calcium-activated cation channel activity1
potassium channel activity1
calcium-activated potassium channel activity1
monoatomic cation channel activity1
potassium ion transmembrane transporter activity1
membrane1
cell periphery1
potassium channel complex1
plasma membrane protein complex1
I band1
plasma membrane bounded cell projection1
somatodendritic compartment1
cell body1
cell junction1
intracellular anatomical structure1

Protein interactions and networks

STRING

958 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
KCNN1KCNMA1Q12791809
KCNN1CSN3P07498718
KCNN1KCNQ1P51787641
KCNN1KCNU1A8MYU2603
KCNN1KCNT1Q5JUK3546
KCNN1KCNT2Q6UVM3532
KCNN1KCNJ5P48544524
KCNN1KCND3Q9UK17499
KCNN1KCNJ3P48549490
KCNN1CALML4Q96GE6488
KCNN1KCNH2Q12809486
KCNN1KCNA3P22001481
KCNN1CALM1P02593480
KCNN1CALML3P27482478
KCNN1CALML5Q9NZT1478

IntAct

8 interactions, top by confidence:

ABTypeScore
KCNN1psi-mi:“MI:0915”(physical association)0.560
GRB2KCNN1psi-mi:“MI:0915”(physical association)0.400
KCNN1RPS18psi-mi:“MI:0915”(physical association)0.400
KCNN1FXR1psi-mi:“MI:0915”(physical association)0.370
DSCAMKCNN1psi-mi:“MI:0915”(physical association)0.000

BioGRID (11): CALM2 (Two-hybrid), CALM3 (Two-hybrid), CALM1 (Two-hybrid), KCNN1 (Proximity Label-MS), KCNN1 (Two-hybrid), KCNN1 (Two-hybrid), ERLIN2 (Affinity Capture-MS), KCNN1 (Affinity Capture-Western), ERLIN2 (Affinity Capture-Western), KCNN1 (Affinity Capture-MS), KCNN1 (Affinity Capture-RNA)

ESM2 similar proteins: A0AV02, A2A6C4, E9PY61, G3HQ82, O95382, P04920, P23347, P35523, P35524, P40682, P70606, Q07175, Q148L1, Q498W5, Q49LS1, Q49LS3, Q5GH66, Q5PQL3, Q5RD44, Q5T1A1, Q5VW38, Q5ZJY9, Q60943, Q640M6, Q64347, Q6P6V6, Q6UX68, Q76MJ5, Q78IQ7, Q7TNJ2, Q7Z465, Q8BGI5, Q8BSD4, Q8CIP5, Q8CJI3, Q8IUH8, Q8VI23, Q8WTR4, Q91V24, Q91WD0

Diamond homologs: O15554, O89109, P58390, P58391, P58392, P70604, P70605, P70606, Q02006, Q7KVW5, Q92952, Q9EQR3, Q9H2S1, Q9QYW1, Q9UGI6, O43525, O88944, P58126, Q11122, Q8K3F6, P17971

SIGNOR signaling

4 interactions.

AEffectBMechanism
Riluzole“up-regulates activity”KCNN1“chemical activation”
Anthra[2,1-d]thiazol-2-ylamine“up-regulates activity”KCNN1“chemical activation”
Naphtho[1,2-d]thiazol-2-amine“up-regulates activity”KCNN1“chemical activation”
EGFR“up-regulates activity”KCNN1phosphorylation

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

ClassificationCount (floor)
Pathogenic0
Likely pathogenic0
Uncertain significance71
Likely benign2
Benign2

Top pathogenic / likely-pathogenic (0)

SpliceAI

1857 predictions. Top by Δscore:

VariantEffectΔscore
19:17974289:AGGT:Adonor_loss1.0000
19:17974290:GGTA:Gdonor_loss1.0000
19:17981703:CCACA:Cacceptor_loss1.0000
19:17981704:CACAG:Cacceptor_loss1.0000
19:17981705:ACAG:Aacceptor_loss1.0000
19:17981706:C:Gacceptor_gain1.0000
19:17981706:CA:Cacceptor_loss1.0000
19:17981707:A:ACacceptor_loss1.0000
19:17985296:ACTCT:Aacceptor_gain1.0000
19:17985300:T:Aacceptor_gain1.0000
19:17985301:G:Aacceptor_gain1.0000
19:17985309:CA:Cacceptor_loss1.0000
19:17985310:A:ACacceptor_loss1.0000
19:17985311:GGT:Gacceptor_gain1.0000
19:17988409:A:AGacceptor_gain1.0000
19:17988410:C:Gacceptor_gain1.0000
19:17988411:A:AGacceptor_gain1.0000
19:17988411:ACAG:Aacceptor_gain1.0000
19:17988412:C:Gacceptor_gain1.0000
19:17988412:CAGGG:Cacceptor_gain1.0000
19:17988413:A:AGacceptor_gain1.0000
19:17988413:AG:Aacceptor_gain1.0000
19:17988413:AGGGA:Aacceptor_gain1.0000
19:17988414:G:GGacceptor_gain1.0000
19:17988414:GG:Gacceptor_gain1.0000
19:17988414:GGGA:Gacceptor_gain1.0000
19:17988414:GGGAG:Gacceptor_gain1.0000
19:17988522:GCGG:Gdonor_gain1.0000
19:17989707:T:TAacceptor_gain1.0000
19:17989713:CAGGT:Cacceptor_loss1.0000

AlphaMissense

0 scored. Top likely-pathogenic:

dbSNP variants (sampled 300 via entrez): RS1000006098 (19:17958447 C>T), RS1000174189 (19:17998645 G>A,C), RS1000205292 (19:17961334 T>C), RS1000243075 (19:17950747 G>A,T), RS1000248418 (19:17973408 G>A), RS1000254326 (19:17967374 C>T), RS1000261288 (19:17987564 A>C,G), RS1000300999 (19:17957364 G>C), RS1000348671 (19:17967138 G>A), RS1000496018 (19:17968082 A>C,G), RS1000502347 (19:17974733 G>A), RS1000547723 (19:17985076 C>T), RS1000559553 (19:17997356 C>A,G), RS1000581477 (19:17954873 A>G), RS1000631107 (19:17998469 C>G)

Disease associations

OMIM: gene MIM:602982 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

2 associations (top):

StudyTraitp-value
GCST007100_12Asthma exacerbations in inhaled corticosteroid treatment4.000000e-06
GCST90002396_27Mean reticulocyte volume2.000000e-15

EFO canonical traits (2, from GWAS)

EFO IDTrait name
EFO:0007614asthma exacerbation measurement
EFO:0010701mean reticulocyte volume

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL2369 (SINGLE PROTEIN), CHEMBL4524132 (PROTEIN FAMILY)

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

PharmGKB variants

1 variants.

VariantGenesLevelScore#Clin annotsDrugs
rs2278992KCNN10.000

GtoPdb / IUPHAR curated pharmacology

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

Target class: vgic — Calcium- and sodium-activated potassium channels (KCa, KNa)

Most potent curated ligand interactions (19 total), top 19:

LigandActionAffinityParameter
UCL1684Inhibitor9.1pIC50
UCL1848Antagonist9.0pIC50
apaminInhibitor8.39pIC50
CM-TPMFAgonist7.62pEC50
B-TPMFAntagonist7.51pEC50
tamapinAntagonist7.4pIC50
leiurotoxin IAntagonist7.1pIC50
Ca2+Agonist6.52pEC50
dequaliniumAntagonist6.4pIC50
NS8593Channel blocker6.4pIC50
SKA-20Agonist6.37pEC50
AP30663Channel blocker5.96pIC50
SKA-31Agonist5.54pEC50
Lei-Dab7Antagonist5.22pIC50
GW542573XAgonist5.09pEC50
bicucullineAntagonist4.8pIC50
riluzoleAgonist4.68pEC50
tubocurarineAntagonist4.6pIC50
tetraethylammoniumChannel blocker2.7pIC50

ChEMBL bioactivities

11 potent at pChembl≥5 of 11 total, top 11 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChemblTypeValueUnitMolecule
10.85IC500.014nMAPAMIN
9.00IC501nMCHEMBL612120
8.52IC503nMCHEMBL45193
8.40IC504nMCHEMBL476339
7.37IC5043nMCHEMBL489770
7.27Kd54nMCHEMBL511710
6.52IC50300nMCHEMBL472452
6.22EC50600nMCHEMBL499968
5.92IC501190nMCHEMBL452406
5.42IC503800nMCHEMBL257156
5.30EC505000nMCHEMBL444449

PubChem BioAssay actives

11 with measured affinity, of 26 total; 10 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

CompoundAssayTypeValueUnit
3-[(1R,4S,7S,13S,16S,19S,22S,25S,28R,31S,34S,37S,40R,47S,50R)-50-amino-40-[[(2S)-5-amino-1-[[(2S)-5-amino-1-[[(2S)-1-amino-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]carbamoyl]-4-(4-aminobutyl)-47-(2-amino-2-oxoethyl)-34,37-bis(3-carbamimidamidopropyl)-19-[(1R)-1-hydroxyethyl]-7,22,31-trimethyl-25-(2-methylpropyl)-2,5,8,14,17,20,23,26,29,32,35,38,46,49-tetradecaoxo-42,43,52,53-tetrathia-3,6,9,15,18,21,24,27,30,33,36,39,45,48-tetradecazatricyclo[26.16.10.09,13]tetrapentacontan-16-yl]propanoic acid346467: Displacement of radiolabeled apamin from calcium-activated SK channelic50<0.0001uM
15,21-diaza-1,7-diazoniapentacyclo[20.6.2.27,14.08,13.023,28]dotriaconta-1(29),7(32),8,10,12,14(31),22(30),23,25,27-decaene;bis(2,2,2-trifluoroacetate)200297: Inhibition of hSK1 calcium activated potassium channel (SKCa channel); Range is 1-2ic500.0010uM
17,24-diaza-1,9-diazoniaheptacyclo[23.6.2.29,16.219,22.13,7.010,15.026,31]octatriaconta-1(32),3(38),4,6,9(37),10,12,14,16(36),19,21,25(33),26,28,30,34-hexadecaene dibromide200296: Inhibition of hSK1 calcium activated potassium channel (SKCa channel)ic500.0030uM
N-(4-methyl-2-pyridinyl)-4-pyridin-2-yl-1,3-thiazol-2-amine387519: Inhibition of Kca2.1 channel expressed in HEK293 cells by thallium flux assayic500.0040uM
N,4-dipyridin-2-yl-1,3-thiazol-2-amine387519: Inhibition of Kca2.1 channel expressed in HEK293 cells by thallium flux assayic500.0430uM
N-(6,7-dichloro-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-benzimidazol-2-amine347104: Inhibition of human SK1 channel by inside-out patch clamp techniquekd0.0540uM
5-chloro-N-(thiophen-2-ylmethyl)pyrazolo[1,5-a]pyrimidin-7-amine349491: Inhibition of Kca2.1 channel expressed in HEK293 cells by thallium flux assayic500.3000uM
6,7-dichloro-3-nitroso-1H-indol-2-ol1974164: Positive modulation of SK1 in HEK293 cells in presence of Ca2+ by patch-clamp methodec500.6000uM
N-benzyl-5-chloropyrazolo[1,5-a]pyrimidin-7-amine349491: Inhibition of Kca2.1 channel expressed in HEK293 cells by thallium flux assayic501.1900uM
(1S)-1-[3-[(1S)-6,7-dimethoxy-2-methyl-3,4-dihydro-1H-isoquinolin-1-yl]propyl]-6,7-dimethoxy-2-methyl-3,4-dihydro-1H-isoquinoline;dihydrochloride332056: Inhibition of SK1 expressed in CHO FlipIn cells by whole cell patch-clamp assayic503.8000uM

CTD chemical–gene interactions

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

ChemicalActions (top 5)PubMed papers
sodium arseniteaffects methylation, decreases expression, increases expression3
Valproic Acidaffects expression, increases methylation2
propionaldehydeincreases expression1
bisphenol Aincreases methylation, affects cotreatment1
bicuculline methiodidedecreases activity1
butyraldehydeincreases expression1
aflatoxin B2increases methylation1
S-(1,2-dichlorovinyl)cysteineincreases expression, affects cotreatment, decreases expression, affects response to substance1
pentanalincreases expression1
leiurotoxin Idecreases activity1
6,10-diaza-3(1,3),8(1,4)dibenzena-1,5(1,4)diquinolinacyclodecaphanedecreases activity1
abrineincreases expression1
Resveratrolaffects cotreatment, decreases expression1
Fulvestrantaffects cotreatment, increases methylation1
Aldehydesincreases expression1
Apamindecreases activity1
Benzo(a)pyreneaffects methylation1
Carbamazepineaffects expression1
Dequaliniumdecreases activity1
Diethylhexyl Phthalatedecreases expression1
Lipopolysaccharidesaffects response to substance, increases expression, affects cotreatment, decreases expression1
Pesticidesdecreases methylation1
Phthalic Acidsincreases methylation1
Plant Extractsaffects cotreatment, decreases expression1
Silicon Dioxidedecreases expression1
Smokeincreases expression1
Tobacco Smoke Pollutionincreases expression1
Tretinoindecreases expression1
Tubocurarinedecreases activity1
Aflatoxin B1decreases methylation1

ChEMBL screening assays

25 unique, capped per target: 25 binding

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL1008912BindingInhibition of human SK1 channel by inside-out patch clamp techniqueSynthesis and structure-activity relationship studies of 2-(N-substituted)-aminobenzimidazoles as potent negative gating modulators ofsmall conductance Ca2+-activated K+ channels. — J Med Chem

Clinical trials (associated diseases)

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

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
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Sources 79

This page pulls from 79 datasets indexed by BioBTree:

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