Page last updated: 2024-08-05 15:14:25

EC 3.6.3.49 (channel-conductance-controlling ATPase) inhibitor

A EC 3.6.3.* (acid anhydride hydrolase catalysing transmembrane movement of substances) inhibitor that interferes with the action of channel-conductance-controlling ATPase (EC 3.6.3.49, also known as cystic fibrosis conductance regulator, CFCR).

ChEBI ID: 131770

Members (2)

MemberDefinitionClass
bumetanideA member of the class of benzoic acids that is 4-phenoxybenzoic acid in which the hydrogens ortho to the phenoxy group are substituted by butylamino and sulfamoyl groups. Bumetanide is a diuretic, and is used for treatment of oedema associated with congestive heart failure, hepatic and renal disease.bumetanide
glyburideAn N-sulfonylurea that is acetohexamide in which the acetyl group is replaced by a 2-(5-chloro-2-methoxybenzamido)ethyl group.glyburide

Research

Studies (8,129)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19901,462 (17.98)18.7374
1990's2,608 (32.08)18.2507
2000's2,187 (26.90)29.6817
2010's1,538 (18.92)24.3611
2020's334 (4.11)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials770 (8.97%)5.53%
Reviews316 (3.68%)6.00%
Case Studies314 (3.66%)4.05%
Observational4 (0.05%)0.25%
Other7,183 (83.65%)84.16%

Protein Targets (130)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency21.585514
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency23.266216
AR proteinHomo sapiens (human)Potency35.837045
ATAD5 protein, partialHomo sapiens (human)Potency6.510411
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency0.463212
Bloom syndrome protein isoform 1Homo sapiens (human)Potency59.976324
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency23.519014
Chain A, Ferritin light chainEquus caballus (horse)Potency39.810711
Chain A, HADH2 proteinHomo sapiens (human)Potency28.100324
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency1.526613
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency19.072812
Chain B, HADH2 proteinHomo sapiens (human)Potency28.100324
chromobox protein homolog 1Homo sapiens (human)Potency94.562612
cytochrome P450 2C19 precursorHomo sapiens (human)Potency10.000011
cytochrome P450 2C9 precursorHomo sapiens (human)Potency4.150213
cytochrome P450 2C9, partialHomo sapiens (human)Potency8.423013
cytochrome P450 2D6Homo sapiens (human)Potency26.835813
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency10.000011
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency5.700827
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency4.605813
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency5.448312
Disintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)Potency6.309611
estrogen nuclear receptor alphaHomo sapiens (human)Potency18.262635
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency58.914633
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency39.933614
GVesicular stomatitis virusPotency8.423013
GABA theta subunitRattus norvegicus (Norway rat)Potency5.485814
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency5.485814
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency5.485814
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency5.485814
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency5.485814
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency5.485814
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency5.485814
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency5.485814
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency5.485814
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency5.485814
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency5.485814
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency5.485814
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency5.485814
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency5.485814
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency5.485814
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency5.485814
gemininHomo sapiens (human)Potency0.145811
GLI family zinc finger 3Homo sapiens (human)Potency1.247412
GLS proteinHomo sapiens (human)Potency0.631012
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency13.610834
Guanine nucleotide-binding protein GHomo sapiens (human)Potency8.912511
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa)Homo sapiens (human)Potency35.481311
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency4.150219
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency23.445112
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency8.423013
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency2.3036210
IDH1Homo sapiens (human)Potency12.995311
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency8.423016
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency31.622811
Interferon betaHomo sapiens (human)Potency8.423013
lamin isoform A-delta10Homo sapiens (human)Potency8.585413
LuciferasePhotinus pyralis (common eastern firefly)Potency9.003812
Microtubule-associated protein tauHomo sapiens (human)Potency39.810711
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency22.387211
muscleblind-like protein 1 isoform 1Homo sapiens (human)Potency100.000011
neuropeptide S receptor isoform AHomo sapiens (human)Potency3.162311
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency17.782811
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency43.867934
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency6.159022
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency31.622811
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency29.849323
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency112.202011
ParkinHomo sapiens (human)Potency9.200011
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency0.002311
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency84.921411
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency20.448534
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency13.718733
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency35.481311
pregnane X nuclear receptorHomo sapiens (human)Potency29.779022
progesterone receptorHomo sapiens (human)Potency34.376211
RAR-related orphan receptor gammaMus musculus (house mouse)Potency30.256223
regulator of G-protein signaling 4Homo sapiens (human)Potency2.119211
retinoid X nuclear receptor alphaHomo sapiens (human)Potency33.270422
SMAD family member 2Homo sapiens (human)Potency24.657124
SMAD family member 3Homo sapiens (human)Potency24.657124
TDP1 proteinHomo sapiens (human)Potency29.855411
thioredoxin reductaseRattus norvegicus (Norway rat)Potency24.697834
thyroid stimulating hormone receptorHomo sapiens (human)Potency4.248423
ubiquitin carboxyl-terminal hydrolase 2 isoform aHomo sapiens (human)Potency6.309611
USP1 protein, partialHomo sapiens (human)Potency70.794611

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC50100.000011
ATP synthase subunit beta, mitochondrialBos taurus (cattle)IC50100.000011
ATP synthase subunit delta, mitochondrialBos taurus (cattle)IC50100.000011
ATP synthase subunit epsilon, mitochondrialBos taurus (cattle)IC50100.000011
ATP synthase subunit gamma, mitochondrialBos taurus (cattle)IC50100.000011
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC5083.000012
ATP-binding cassette sub-family C member 8Homo sapiens (human)IC500.004311
ATP-binding cassette sub-family C member 9Homo sapiens (human)IC500.220011
ATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)IC500.112222
Beta-lactamaseEscherichia coli K-12IC50300.000011
Bile salt export pumpHomo sapiens (human)IC50112.2000811
Bile salt export pumpRattus norvegicus (Norway rat)IC509.033333
Bile salt export pumpHomo sapiens (human)Ki27.500011
Bile salt export pumpRattus norvegicus (Norway rat)Ki6.100011
Broad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)IC50150.000022
Carbonic anhydrase 1Homo sapiens (human)Ki18.3242112
Carbonic anhydrase 12Homo sapiens (human)Ki18.3242112
Carbonic anhydrase 13Mus musculus (house mouse)Ki18.3242112
Carbonic anhydrase 14Homo sapiens (human)Ki18.3242112
Carbonic anhydrase 2Homo sapiens (human)Ki18.3242112
Carbonic anhydrase 3Homo sapiens (human)Ki18.3242112
Carbonic anhydrase 4Homo sapiens (human)Ki18.3242112
Carbonic anhydrase 5A, mitochondrialHomo sapiens (human)Ki18.3242112
Carbonic anhydrase 5B, mitochondrialHomo sapiens (human)Ki18.3242112
Carbonic anhydrase 6Homo sapiens (human)Ki18.3242112
Carbonic anhydrase 7Homo sapiens (human)Ki18.3242112
Carbonic anhydrase 9Homo sapiens (human)Ki18.3242112
CDGSH iron-sulfur domain-containing protein 1Homo sapiens (human)IC5039.100011
CDGSH iron-sulfur domain-containing protein 1Homo sapiens (human)Ki1.671011
Cholesteryl ester transfer proteinOryctolagus cuniculus (rabbit)IC50238.600011
Chymotrypsinogen ABos taurus (cattle)IC50360.000011
Cystic fibrosis transmembrane conductance regulatorHomo sapiens (human)IC5015.000011
Cytochrome P450 2C9 Homo sapiens (human)IC501.602011
Malate dehydrogenase, cytoplasmicHomo sapiens (human)IC50400.000011
Multidrug resistance-associated protein 4Homo sapiens (human)IC5071.750012
NACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)IC5012.000011
NACHT, LRR and PYD domains-containing protein 3 Mus musculus (house mouse)IC5010.000011
Peroxisome proliferator-activated receptor gammaHomo sapiens (human)Ki0.660011
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC5074.065544
Solute carrier family 12 member 2Homo sapiens (human)IC500.800011
Solute carrier family 15 member 1Rattus norvegicus (Norway rat)Ki25.000011
Solute carrier family 15 member 2Rattus norvegicus (Norway rat)Ki7.800011
Solute carrier family 22 member 6Rattus norvegicus (Norway rat)Ki3.550022
Solute carrier family 22 member 7Rattus norvegicus (Norway rat)Ki12.300011
Solute carrier organic anion transporter family member 1B1Homo sapiens (human)IC508.200033

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Potassium channel subfamily K member 2Homo sapiens (human)EC5064.000011

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Carbonic anhydrase 1Homo sapiens (human)Kinact4.930011
Carbonic anhydrase 12Homo sapiens (human)Kinact0.021111
Carbonic anhydrase 13Mus musculus (house mouse)Kinact2.570011
Carbonic anhydrase 14Homo sapiens (human)Kinact0.250011
Carbonic anhydrase 2Homo sapiens (human)Kinact6.980011
Carbonic anhydrase 4Homo sapiens (human)Kinact0.303011
Carbonic anhydrase 5A, mitochondrialHomo sapiens (human)Kinact0.700011
Carbonic anhydrase 5B, mitochondrialHomo sapiens (human)Kinact0.159011
Carbonic anhydrase 6Homo sapiens (human)Kinact3.890011
Carbonic anhydrase 7Homo sapiens (human)Kinact0.062011
Carbonic anhydrase 9Homo sapiens (human)Kinact0.025811
Solute carrier organic anion transporter family member 2B1 Homo sapiens (human)Km6.260011