Page last updated: 2024-08-05 15:17:49

K-ATP channel agonist

A compound which acts as an agonist at the ATP-sensitive K+ channel.

ChEBI ID: 64338

Members (2)

MemberDefinitionClass
diazoxideA benzothiadiazine that is the S,S-dioxide of 2H-1,2,4-benzothiadiazine which is substituted at position 3 by a methyl group and at position 7 by chlorine. A peripheral vasodilator, it increases the concentration of glucose in the plasma and inhibits the secretion of insulin by the beta- cells of the pancreas. It is used orally in the management of intractable hypoglycaemia and intravenously in the management of hypertensive emergencies.diazoxide
rottlerinA chromenol that is 2,2-dimethyl-2H-chromene substituted by hydroxy groups at positions 5 and 7, a 3-acetyl-2,4,6-trihydroxy-5-methylbenzyl group at position 6 and a (1E)-3-oxo-1-phenylprop-1-en-3-yl group at position 8. A potassium channel opener, it is isolated from Mallotus philippensis.rottlerin

Research

Studies (3,317)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19901,211 (36.51)18.7374
1990's427 (12.87)18.2507
2000's948 (28.58)29.6817
2010's609 (18.36)24.3611
2020's122 (3.68)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials87 (2.50%)5.53%
Reviews201 (5.78%)6.00%
Case Studies287 (8.25%)4.05%
Observational5 (0.14%)0.25%
Other2,899 (83.33%)84.16%

Protein Targets (102)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency20.855916
ATAD5 protein, partialHomo sapiens (human)Potency15.458022
Ataxin-2Homo sapiens (human)Potency25.118911
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency33.807811
atrial natriuretic peptide receptor 2 precursorHomo sapiens (human)Potency26.121611
Bloom syndrome protein isoform 1Homo sapiens (human)Potency31.622822
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency32.464812
Chain A, ATP-DEPENDENT DNA HELICASE Q1Homo sapiens (human)Potency32.765225
Chain A, Beta-lactamaseEscherichia coli K-12Potency17.782811
Chain A, CruzipainTrypanosoma cruziPotency21.712322
Chain A, Ferritin light chainEquus caballus (horse)Potency19.136024
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency28.183811
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency23.176913
chromobox protein homolog 1Homo sapiens (human)Potency12.589311
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency7.943311
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency19.952622
D(1A) dopamine receptorHomo sapiens (human)Potency1.299511
DNA polymerase betaHomo sapiens (human)Potency22.387211
DNA polymerase eta isoform 1Homo sapiens (human)Potency25.118911
DNA polymerase III, partialBacillus subtilisPotency18.887611
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency44.964712
DNA polymerase kappa isoform 1Homo sapiens (human)Potency34.411712
estrogen nuclear receptor alphaHomo sapiens (human)Potency6.001211
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency8.378133
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency9.462815
flap endonuclease 1Homo sapiens (human)Potency53.056212
Fumarate hydrataseHomo sapiens (human)Potency19.952611
GABA theta subunitRattus norvegicus (Norway rat)Potency19.952611
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency19.952611
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency19.952611
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency19.952611
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency19.952611
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency19.952611
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency19.952611
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency19.952611
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency19.952611
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency19.952611
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency19.952611
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency19.952611
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency19.952611
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency19.952611
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency19.952611
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency19.952611
gemininHomo sapiens (human)Potency3.130833
GLS proteinHomo sapiens (human)Potency9.149812
GTP-binding nuclear protein Ran isoform 1Homo sapiens (human)Potency6.513111
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency19.924514
IDH1Homo sapiens (human)Potency15.848911
importin subunit beta-1 isoform 1Homo sapiens (human)Potency6.513111
lamin isoform A-delta10Homo sapiens (human)Potency4.935925
M-phase phosphoprotein 8Homo sapiens (human)Potency31.778012
Microtubule-associated protein tauHomo sapiens (human)Potency16.723826
neuropeptide S receptor isoform AHomo sapiens (human)Potency1.000011
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency12.589311
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency12.589311
peptidyl-prolyl cis-trans isomerase NIMA-interacting 1Homo sapiens (human)Potency37.933011
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency4.053311
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency47.754811
polyproteinZika virusPotency19.952611
regulator of G-protein signaling 4Homo sapiens (human)Potency16.602013
serine-protein kinase ATM isoform aHomo sapiens (human)Potency16.397423
snurportin-1Homo sapiens (human)Potency6.513111
survival motor neuron protein isoform dHomo sapiens (human)Potency10.994514
TDP1 proteinHomo sapiens (human)Potency20.5161210
thioredoxin reductaseRattus norvegicus (Norway rat)Potency15.102724
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency6.309611
thyroid stimulating hormone receptorHomo sapiens (human)Potency20.483924
USP1 protein, partialHomo sapiens (human)Potency59.168923
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency25.664814

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC501.200011
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50133.000011
ATP-binding cassette sub-family C member 8Homo sapiens (human)IC50470.500044
ATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)IC50470.500044
B2 bradykinin receptorCavia porcellus (domestic guinea pig)IC501.200011
Beta-lactamaseEnterobacter cloacaeIC50119.000022
Beta-lactamaseEscherichia coli K-12IC5025.000044
Bile salt export pumpHomo sapiens (human)IC50422.666733
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50133.000011
Chymotrypsinogen ABos taurus (cattle)IC50119.000022
Chymotrypsinogen BHomo sapiens (human)IC5025.000011
Coagulation factor VIIHomo sapiens (human)IC50740.000011
Eukaryotic elongation factor 2 kinaseHomo sapiens (human)IC505.300011
M-phase inducer phosphatase 1Homo sapiens (human)IC5020.000011
Malate dehydrogenaseThermus thermophilusIC500.700011
MAP kinase-activated protein kinase 2Homo sapiens (human)IC505.400011
MAP kinase-activated protein kinase 5Homo sapiens (human)IC501.900022
Multidrug resistance-associated protein 4Homo sapiens (human)IC50133.000011
Protein kinase C alpha typeHomo sapiens (human)IC5020.000011
Protein kinase C delta typeHomo sapiens (human)IC503.000022
Protein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)IC5020.000011
Receptor protein-tyrosine kinase Homo sapiens (human)IC5020.000011
Receptor-type tyrosine-protein phosphatase etaHomo sapiens (human)IC5020.000011
RuvB-like 1Homo sapiens (human)IC5010.000011
Tissue factorHomo sapiens (human)IC50740.000011
Tyrosine-protein kinase JAK3Homo sapiens (human)IC5020.000011
Ubiquitin carboxyl-terminal hydrolase 1Homo sapiens (human)IC508.000011
WD repeat-containing protein 48Homo sapiens (human)IC508.000011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
ATP-binding cassette sub-family C member 8Homo sapiens (human)EC5023.016766
ATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)EC5023.016766
Nicotinamide phosphoribosyltransferaseHomo sapiens (human)Kd230.000011

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Glutamate receptor 1Rattus norvegicus (Norway rat)EC2x448.000011
Glutamate receptor 1Rattus norvegicus (Norway rat)EC5X1,000.000012
Glutamate receptor 2Rattus norvegicus (Norway rat)EC2x448.000011
Glutamate receptor 2Rattus norvegicus (Norway rat)EC5X1,000.000012
Glutamate receptor 3Rattus norvegicus (Norway rat)EC2x448.000011
Glutamate receptor 3Rattus norvegicus (Norway rat)EC5X1,000.000012
Glutamate receptor 4Rattus norvegicus (Norway rat)EC2x448.000011
Glutamate receptor 4Rattus norvegicus (Norway rat)EC5X1,000.000012