Page last updated: 2024-11-04

tolazamide

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

Tolazamide: A sulphonylurea hypoglycemic agent with actions and uses similar to those of CHLORPROPAMIDE. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

tolazamide : An N-sulfonylurea that is 1-tosylurea in which a hydrogen attached to the nitrogen at position 3 is replaced by an azepan-1-yl group. A hypoglycemic agent, it is used for the treatment of type 2 diabetes mellitus. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID5503
CHEMBL ID817
CHEBI ID9613
SCHEMBL ID34417
MeSH IDM0021626

Synonyms (227)

Synonym
CBIOL_001918
unii-9lt1bro48q
tolazamide [usan:usp:inn:ban:jan]
9lt1bro48q ,
5-20-04-00062 (beilstein handbook reference)
tolazamida
tolazamidum
MLS001076161
AB00052247-15
BRD-K32164935-001-06-8
KBIO1_000212
DIVK1C_000212
n-[(azepan-1-ylamino)carbonyl]-4-methylbenzenesulfonamide
EU-0101195
urea, 1-(hexahydroazepin-1-yl)-3-p-tolylsulfonyl-
1156-19-0
nsc-70762
4-(p-tolylsulfonyl)-1,1-hexamethylenesemicarbazide
tolinase
wln: t7ntj amvmswr d1
nsc70762
u-17835
benzenesulfonamide, n-[[(hexahydro-1h-azepin-1-yl)amino]carbonyl]-4-methyl-
norglycin
1-(hexahydro-1h-azepin-1-yl)-3-(p-tolylsulfonyl)urea
n-(p-toluenesulfonyl)-n'-hexamethyleniminourea
1-(hexahydro-1-azepinyl)-3-p-tolylsulfonylurea
tolanase
nci-c03327
u 17835
urea, 1-(hexahydro-1h-azepin-1-yl)-3-(p-tolylsulfonyl)-
tolazamide
SPECTRUM_001269
BSPBIO_000627
BCBCMAP01_000061
BSPBIO_001505
IDI1_000212
PRESTWICK_865
BIO1_000204
NCGC00016009-01
BIO2_000705
lopac-t-2408
NCGC00016009-02
BIO2_000225
BIO1_001182
BIO1_000693
cas-1156-19-0
SPECTRUM5_001204
benzenesulfonamide, {n-[[(hexahydro-1h-azepin-1-yl)amino]carbonyl]-4-methyl-}
1-(((((4-methylphenyl)sulfonyl)amino)carbonyl)amino)azepane
1-(azepan-1-yl)-3-(p-tolylsulfonyl)urea
PRESTWICK3_000554
LOPAC0_001195
OPREA1_061180
BPBIO1_000691
AB00052247
benzenesulfonamide, n-(((hexahydro-1h-azepin-1-yl)amino)carbonyl)-4-methyl-
einecs 214-588-3
tolazolamide
ai3-50826
n-(((hexahydro-1h-azepin-1-yl)amino)carbonyl)-4-methylbenzenesulfonamide
benzenesulfonamide, n-(((hexahydro-1h-azepin-1-yl)-amino)carbonyl)-4-methyl-
hsdb 3192
n-(((hexahydro-1h-azepin-1-yl)-amino)carbonyl)-4-methylbenzenesulfonamide
nsc 70762
brn 1323565
tolazamidum [inn-latin]
tolazamida [inn-spanish]
ccris 591
diabewas
DB00839
D00379
tolinase (tn)
tolazamide (jan/usp/inn)
IDI1_033975
NCGC00023701-07
NCGC00023701-04
NCGC00023701-05
NCGC00023701-08
NCGC00023701-09
MLS000028534 ,
smr000058290
KBIOGR_000225
KBIO2_005361
KBIO3_000450
KBIO2_004317
KBIO3_000449
KBIOSS_001749
KBIO2_006885
KBIO2_001749
KBIO2_002793
KBIOSS_000225
KBIO2_000225
KBIOGR_000939
KBIO3_002525
SPBIO_001317
PRESTWICK1_000554
PRESTWICK0_000554
SPBIO_002548
NCIOPEN2_008361
SPECTRUM4_000240
SPECTRUM2_001449
SPECTRUM3_001473
NINDS_000212
SR-01000003105-4
SPECTRUM1501201
BSPBIO_003025
PRESTWICK2_000554
3-azepan-1-yl-1-(4-methylphenyl)sulfonyl-urea
NCGC00023701-03
NCGC00016009-03
NCGC00023701-06
NCGC00023701-10
NCGC00016009-06
HMS1989L07
T 2408 ,
HMS2092L09
HMS2089L10
NCGC00016009-14
chebi:9613 ,
CHEMBL817
HMS1791L07
HMS1361L07
HMS500K14
HMS1569P09
HMS1921P19
1-(azepan-1-yl)-3-(4-methylphenyl)sulfonylurea
NCGC00016009-10
HMS3259O18
HMS2096P09
HMS3263P11
NCGC00259058-01
NCGC00254501-01
tox21_300416
tox21_201507
pharmakon1600-01501201
nsc758149
nsc-758149
dtxcid401358
dtxsid3021358 ,
tox21_110281
HMS2232L21
CCG-39178
NCGC00016009-17
NCGC00016009-07
NCGC00016009-12
NCGC00016009-04
NCGC00016009-15
NCGC00016009-09
NCGC00016009-11
NCGC00016009-13
NCGC00016009-05
NCGC00016009-08
NCGC00016009-16
1-(azepan-1-yl)-3-(4-methylbenzenesulfonyl)urea
FT-0675268
n-{[(hexahydro-1h-azepin-1-yl)-amino]carbonyl}-4-methylbenzenesulfonamide
n-(azepan-1-ylcarbamoyl)-4-methylbenzenesulfonamide
LP01195
AKOS015913823
HMS3369L04
gtpl6847
tolazamide [who-dd]
tolazamide [vandf]
tolazamide [mart.]
tolazamide [inn]
tolazamide [usp monograph]
tolazamide [orange book]
tolazamide [mi]
tolbutamide impurity c [ep impurity]
tolazamide [hsdb]
tolazamide [usp-rs]
tolazamide [jan]
tolazamide [usan]
NC00590
SCHEMBL34417
tox21_110281_1
NCGC00016009-19
NCGC00261880-01
tox21_501195
OUDSBRTVNLOZBN-UHFFFAOYSA-N
1-[(([(4-methylphenyl)sulfonyl]amino)carbonyl)amino]azepane #
benzenesulfonamide, n-[[(hexahydro-1-azepinyl)amino]carbonyl]-4-methyl-
n-[[(hexahydro-1h-azepin-1-yl)amino]carbonyl]-4-methylbenzenesulfonamide
ronase
W-109110
1-(hexahydro-1h-azepin-1-yl)-3-(p-toluenesulfonyl)urea
HY-B0920
HMS3402L07
AB00052247_16
OPERA_ID_1740
AB00052247_17
KS-1438
1-(azepan-1-yl)-3-[(4-methylbenzene)sulfonyl]urea
SR-01000003105-2
sr-01000003105
tolazamide, united states pharmacopeia (usp) reference standard
SR-01000003105-5
SR-01000003105-8
SBI-0051162.P003
HMS3713P09
SW196991-3
F2173-1137
1-[({[(4-methylphenyl)sulfonyl]amino}carbonyl)amino]azepane
BCP23550
Q7814101
BRD-K32164935-001-28-2
BRD-K32164935-001-17-5
SDCCGSBI-0051162.P004
NCGC00016009-24
1-[(azepan-1-ylamino)carbonyl]-4-methylbenzenesulfonamide
1-(4-methylphenylsulfonyl)-3-(hexahydro-1h-azepin-1-yl)urea
A921617
C71499
3-(azepan-1-yl)-1-(4-methylphenyl)sulfonyl-urea
Z1575267190
tolazamidum (inn-latin)
tolazamida (inn-spanish)
tolbutamide impurity c (ep impurity)
tolazamide (mart.)
nci-co3327
tolazamide (usan:usp:inn:ban:jan)
tolazamide (usp monograph)
benzenesulfonamide, n,((hexahydro-1h-azepin-1-yl)amino)carbonyl)-4-methyl-
tolazamide (usp-rs)
tolazamid
a10bb05

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" An understanding of structure-activity relationships (SARs) of chemicals can make a significant contribution to the identification of potential toxic effects early in the drug development process and aid in avoiding such problems."( Developing structure-activity relationships for the prediction of hepatotoxicity.
Fisk, L; Greene, N; Naven, RT; Note, RR; Patel, ML; Pelletier, DJ, 2010
)
0.36

Pharmacokinetics

ExcerptReferenceRelevance
"The described pharmacokinetic analysis involved two separate studies on nine dogs randomly assigned to three groups of three dogs each."( Pharmacokinetic interactions of tolazamide and oxyphenbutazone in dogs.
Abidi, SE; Cleary, RW; Harland, EC; Jones, AB; Kibbe, AH, 1982
)
0.55

Bioavailability

ExcerptReferenceRelevance
" Glyburide and glipizide are well absorbed after oral administration."( Glyburide and glipizide, second-generation oral sulfonylurea hypoglycemic agents.
Prendergast, BD,
)
0.13
"The relative bioavailability of tolazamide was determined, in healthy male volunteers, from four different tablet formulations manufactured by direct compaction or granulation processes and the results were compared with in vitro disintegration and dissolution values."( Bioavailability of tolazamide from tablets: comparison of in vitro and in vivo results.
Albert, KS; Craig, WA; Gillespie, WR; Patel, RB; Patel, UR; Welling, PG, 1982
)
0.88
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

A method is described for the determination of N-nitrosohexamethyleneimine, a potential carcinogen, in tolazamide bulk drug and pharmaceutical dosage forms. In 13 subjects in whom adequate metabolic control was achieved with combination therapy, metabolic control worsened.

ExcerptRelevanceReference
" Insulin (8 h) increased the quantity of glucose transporters, with a maximal twofold increase at 10(-7) M and a dose-response curve similar to that for insulin stimulation of glucose uptake."( Coordinate regulation of glucose transporter function, number, and gene expression by insulin and sulfonylureas in L6 rat skeletal muscle cells.
Flier, JS; Moller, D; Nayak, RC; Smith, RJ; Wang, PH, 1989
)
0.28
"A method is described for the determination of N-nitrosohexamethyleneimine, a potential carcinogen, in tolazamide bulk drug and pharmaceutical dosage forms."( Monitoring a potential carcinogen in pharmaceutical formulations at the low part per billion level. High-performance liquid chromatographic determination of N-nitrosohexamethyleneimine in tolazamide.
Severin, G, 1987
)
0.68
" In 13 subjects in whom adequate metabolic control was achieved with combination therapy, metabolic control worsened on withdrawal of tolazamide while continuing insulin in the same dosage and adequate metabolic control promptly returned on reinstitution of combination therapy with insulin and tolazamide."( Adjuvant therapy with tolazamide and insulin improves metabolic control in type I diabetes mellitus.
Kabadi, UM,
)
0.65
"The chemistry, pharmacology, pharmacokinetics, clinical efficacy, adverse effects, and dosage of glyburide and glipizide, two second-generation oral sulfonylurea hypoglycemic agents, are reviewed."( Glyburide and glipizide, second-generation oral sulfonylurea hypoglycemic agents.
Prendergast, BD,
)
0.13
" In the first study, the effect of varying the dosage of tolazamide was examined."( Pharmacokinetic interactions of tolazamide and oxyphenbutazone in dogs.
Abidi, SE; Cleary, RW; Harland, EC; Jones, AB; Kibbe, AH, 1982
)
0.79
" A short 12-week study was conducted which incorporated a cross-over design and the results were examined by variance analysis after dosage was individualized to the patient's requirements."( CLINICAL STUDIES OF TOLAZAMIDE AND TOLBUTAMIDE: COMPARATIVE EFFECTIVENESS OF CONTROL OF DIABETES MELLITUS.
ANDERSON, DO; RENNIE, CS, 1963
)
0.56
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
hypoglycemic agentA drug which lowers the blood glucose level.
potassium channel blockerAn agent that inhibits cell membrane glycoproteins that are selectively permeable to potassium ions.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (1)

ClassDescription
N-sulfonylureaA urea in which one of the hydrogens attached to a nitrogen of the urea group is replaced by a sulfonyl group. The N-sulfonylurea moiety is a key group in various herbicides, as well as in a number of antidiabetic drugs used in the management of type 2 diabetis mellitus.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (62)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency3.54610.003245.467312,589.2998AID2517
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency17.74070.140911.194039.8107AID2451
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency56.23410.631035.7641100.0000AID504339
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency31.09890.177814.390939.8107AID2147
endonuclease IVEscherichia coliPotency0.11220.707912.432431.6228AID1708
thioredoxin reductaseRattus norvegicus (Norway rat)Potency47.77550.100020.879379.4328AID588453
phosphopantetheinyl transferaseBacillus subtilisPotency34.89370.141337.9142100.0000AID1490
USP1 protein, partialHomo sapiens (human)Potency39.81070.031637.5844354.8130AID504865
NFKB1 protein, partialHomo sapiens (human)Potency17.78280.02827.055915.8489AID895; AID928
GLS proteinHomo sapiens (human)Potency10.61010.35487.935539.8107AID624146; AID624170
GLI family zinc finger 3Homo sapiens (human)Potency3.43760.000714.592883.7951AID1259392
Microtubule-associated protein tauHomo sapiens (human)Potency19.95260.180013.557439.8107AID1460
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency20.04620.011212.4002100.0000AID1030
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency21.13170.000657.913322,387.1992AID1259377
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency9.77170.01237.983543.2770AID1645841
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency7.94330.28189.721235.4813AID2326
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency5.35380.000214.376460.0339AID720691
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency61.13060.003041.611522,387.1992AID1159552; AID1159555
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency5.30800.001530.607315,848.9004AID1224821
estrogen nuclear receptor alphaHomo sapiens (human)Potency26.56700.000229.305416,493.5996AID743069; AID743075; AID743078; AID743079
GVesicular stomatitis virusPotency10.68400.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency9.77170.00108.379861.1304AID1645840
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency79.43280.707936.904389.1251AID504333
arylsulfatase AHomo sapiens (human)Potency2.68551.069113.955137.9330AID720538
alpha-galactosidaseHomo sapiens (human)Potency5.62344.466818.391635.4813AID2107
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency15.65390.035520.977089.1251AID504332
lysosomal alpha-glucosidase preproproteinHomo sapiens (human)Potency14.12540.036619.637650.1187AID2100
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency12.58930.316212.443531.6228AID902
polyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)Potency7.07951.000012.232631.6228AID1452
chromobox protein homolog 1Homo sapiens (human)Potency28.18380.006026.168889.1251AID488953
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency27.30600.000323.4451159.6830AID743066
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency24.33650.000627.21521,122.0200AID720636
gemininHomo sapiens (human)Potency0.28380.004611.374133.4983AID624296; AID624297
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency39.81070.031610.279239.8107AID884; AID885
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency14.12540.251215.843239.8107AID504327
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency0.01120.00106.000935.4813AID943
chaperonin GroELMethanococcus maripaludis S2Potency100.000031.622831.622831.6228AID488978
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency39.81071.000012.224831.6228AID885
Interferon betaHomo sapiens (human)Potency10.68400.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency10.68400.01238.964839.8107AID1645842
Cellular tumor antigen p53Homo sapiens (human)Potency68.58960.002319.595674.0614AID651631
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency39.81071.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency39.81071.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency39.81071.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency39.81071.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency39.81071.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency39.81071.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency39.81071.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency39.81071.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency39.81071.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency39.81071.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency39.81071.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency39.81071.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency39.81071.000012.224831.6228AID885
GABA theta subunitRattus norvegicus (Norway rat)Potency39.81071.000012.224831.6228AID885
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency10.68400.01238.964839.8107AID1645842
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency39.81071.000012.224831.6228AID885
cytochrome P450 2C9, partialHomo sapiens (human)Potency10.68400.01238.964839.8107AID1645842
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency8.49210.060110.745337.9330AID485368
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Bile salt export pumpHomo sapiens (human)IC50 (µMol)285.70000.11007.190310.0000AID1449628
Polyunsaturated fatty acid lipoxygenase ALOX15Oryctolagus cuniculus (rabbit)IC50 (µMol)5.10600.11003.26419.0330AID625146
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (195)

Processvia Protein(s)Taxonomy
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cellular response to starvationAlbuminHomo sapiens (human)
negative regulation of mitochondrial depolarizationAlbuminHomo sapiens (human)
cellular response to calcium ion starvationAlbuminHomo sapiens (human)
cellular oxidant detoxificationAlbuminHomo sapiens (human)
transportAlbuminHomo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycle G2/M phase transitionCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
ER overload responseCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
mitophagyCellular tumor antigen p53Homo sapiens (human)
in utero embryonic developmentCellular tumor antigen p53Homo sapiens (human)
somitogenesisCellular tumor antigen p53Homo sapiens (human)
release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
hematopoietic progenitor cell differentiationCellular tumor antigen p53Homo sapiens (human)
T cell proliferation involved in immune responseCellular tumor antigen p53Homo sapiens (human)
B cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
T cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
response to ischemiaCellular tumor antigen p53Homo sapiens (human)
nucleotide-excision repairCellular tumor antigen p53Homo sapiens (human)
double-strand break repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
protein import into nucleusCellular tumor antigen p53Homo sapiens (human)
autophagyCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrestCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in transcription of p21 class mediatorCellular tumor antigen p53Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
Ras protein signal transductionCellular tumor antigen p53Homo sapiens (human)
gastrulationCellular tumor antigen p53Homo sapiens (human)
neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
protein localizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA replicationCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
determination of adult lifespanCellular tumor antigen p53Homo sapiens (human)
mRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
rRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
response to salt stressCellular tumor antigen p53Homo sapiens (human)
response to inorganic substanceCellular tumor antigen p53Homo sapiens (human)
response to X-rayCellular tumor antigen p53Homo sapiens (human)
response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
positive regulation of gene expressionCellular tumor antigen p53Homo sapiens (human)
cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
viral processCellular tumor antigen p53Homo sapiens (human)
glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
cerebellum developmentCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell growthCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
mitotic G1 DNA damage checkpoint signalingCellular tumor antigen p53Homo sapiens (human)
negative regulation of telomere maintenance via telomeraseCellular tumor antigen p53Homo sapiens (human)
T cell differentiation in thymusCellular tumor antigen p53Homo sapiens (human)
tumor necrosis factor-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
regulation of tissue remodelingCellular tumor antigen p53Homo sapiens (human)
cellular response to UVCellular tumor antigen p53Homo sapiens (human)
multicellular organism growthCellular tumor antigen p53Homo sapiens (human)
positive regulation of mitochondrial membrane permeabilityCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
entrainment of circadian clock by photoperiodCellular tumor antigen p53Homo sapiens (human)
mitochondrial DNA repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
transcription initiation-coupled chromatin remodelingCellular tumor antigen p53Homo sapiens (human)
negative regulation of proteolysisCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of RNA polymerase II transcription preinitiation complex assemblyCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
response to antibioticCellular tumor antigen p53Homo sapiens (human)
fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
circadian behaviorCellular tumor antigen p53Homo sapiens (human)
bone marrow developmentCellular tumor antigen p53Homo sapiens (human)
embryonic organ developmentCellular tumor antigen p53Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationCellular tumor antigen p53Homo sapiens (human)
protein stabilizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of helicase activityCellular tumor antigen p53Homo sapiens (human)
protein tetramerizationCellular tumor antigen p53Homo sapiens (human)
chromosome organizationCellular tumor antigen p53Homo sapiens (human)
neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
hematopoietic stem cell differentiationCellular tumor antigen p53Homo sapiens (human)
negative regulation of glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
type II interferon-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
cardiac septum morphogenesisCellular tumor antigen p53Homo sapiens (human)
positive regulation of programmed necrotic cell deathCellular tumor antigen p53Homo sapiens (human)
protein-containing complex assemblyCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stressCellular tumor antigen p53Homo sapiens (human)
thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
necroptotic processCellular tumor antigen p53Homo sapiens (human)
cellular response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
cellular response to xenobiotic stimulusCellular tumor antigen p53Homo sapiens (human)
cellular response to ionizing radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to UV-CCellular tumor antigen p53Homo sapiens (human)
stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
cellular response to actinomycin DCellular tumor antigen p53Homo sapiens (human)
positive regulation of release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
cellular senescenceCellular tumor antigen p53Homo sapiens (human)
replicative senescenceCellular tumor antigen p53Homo sapiens (human)
oxidative stress-induced premature senescenceCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
oligodendrocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of execution phase of apoptosisCellular tumor antigen p53Homo sapiens (human)
negative regulation of mitophagyCellular tumor antigen p53Homo sapiens (human)
regulation of mitochondrial membrane permeability involved in apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of G1 to G0 transitionCellular tumor antigen p53Homo sapiens (human)
negative regulation of miRNA processingCellular tumor antigen p53Homo sapiens (human)
negative regulation of glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
negative regulation of pentose-phosphate shuntCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
regulation of fibroblast apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
positive regulation of cellular senescenceCellular tumor antigen p53Homo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (63)

Processvia Protein(s)Taxonomy
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
oxygen bindingAlbuminHomo sapiens (human)
DNA bindingAlbuminHomo sapiens (human)
fatty acid bindingAlbuminHomo sapiens (human)
copper ion bindingAlbuminHomo sapiens (human)
protein bindingAlbuminHomo sapiens (human)
toxic substance bindingAlbuminHomo sapiens (human)
antioxidant activityAlbuminHomo sapiens (human)
pyridoxal phosphate bindingAlbuminHomo sapiens (human)
identical protein bindingAlbuminHomo sapiens (human)
protein-folding chaperone bindingAlbuminHomo sapiens (human)
exogenous protein bindingAlbuminHomo sapiens (human)
enterobactin bindingAlbuminHomo sapiens (human)
transcription cis-regulatory region bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
core promoter sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
TFIID-class transcription factor complex bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
protease bindingCellular tumor antigen p53Homo sapiens (human)
p53 bindingCellular tumor antigen p53Homo sapiens (human)
DNA bindingCellular tumor antigen p53Homo sapiens (human)
chromatin bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activityCellular tumor antigen p53Homo sapiens (human)
mRNA 3'-UTR bindingCellular tumor antigen p53Homo sapiens (human)
copper ion bindingCellular tumor antigen p53Homo sapiens (human)
protein bindingCellular tumor antigen p53Homo sapiens (human)
zinc ion bindingCellular tumor antigen p53Homo sapiens (human)
enzyme bindingCellular tumor antigen p53Homo sapiens (human)
receptor tyrosine kinase bindingCellular tumor antigen p53Homo sapiens (human)
ubiquitin protein ligase bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase regulator activityCellular tumor antigen p53Homo sapiens (human)
ATP-dependent DNA/DNA annealing activityCellular tumor antigen p53Homo sapiens (human)
identical protein bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase bindingCellular tumor antigen p53Homo sapiens (human)
protein heterodimerization activityCellular tumor antigen p53Homo sapiens (human)
protein-folding chaperone bindingCellular tumor antigen p53Homo sapiens (human)
protein phosphatase 2A bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingCellular tumor antigen p53Homo sapiens (human)
14-3-3 protein bindingCellular tumor antigen p53Homo sapiens (human)
MDM2/MDM4 family protein bindingCellular tumor antigen p53Homo sapiens (human)
disordered domain specific bindingCellular tumor antigen p53Homo sapiens (human)
general transcription initiation factor bindingCellular tumor antigen p53Homo sapiens (human)
molecular function activator activityCellular tumor antigen p53Homo sapiens (human)
promoter-specific chromatin bindingCellular tumor antigen p53Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (45)

Processvia Protein(s)Taxonomy
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular regionAlbuminHomo sapiens (human)
extracellular spaceAlbuminHomo sapiens (human)
nucleusAlbuminHomo sapiens (human)
endoplasmic reticulumAlbuminHomo sapiens (human)
endoplasmic reticulum lumenAlbuminHomo sapiens (human)
Golgi apparatusAlbuminHomo sapiens (human)
platelet alpha granule lumenAlbuminHomo sapiens (human)
extracellular exosomeAlbuminHomo sapiens (human)
blood microparticleAlbuminHomo sapiens (human)
protein-containing complexAlbuminHomo sapiens (human)
cytoplasmAlbuminHomo sapiens (human)
nuclear bodyCellular tumor antigen p53Homo sapiens (human)
nucleusCellular tumor antigen p53Homo sapiens (human)
nucleoplasmCellular tumor antigen p53Homo sapiens (human)
replication forkCellular tumor antigen p53Homo sapiens (human)
nucleolusCellular tumor antigen p53Homo sapiens (human)
cytoplasmCellular tumor antigen p53Homo sapiens (human)
mitochondrionCellular tumor antigen p53Homo sapiens (human)
mitochondrial matrixCellular tumor antigen p53Homo sapiens (human)
endoplasmic reticulumCellular tumor antigen p53Homo sapiens (human)
centrosomeCellular tumor antigen p53Homo sapiens (human)
cytosolCellular tumor antigen p53Homo sapiens (human)
nuclear matrixCellular tumor antigen p53Homo sapiens (human)
PML bodyCellular tumor antigen p53Homo sapiens (human)
transcription repressor complexCellular tumor antigen p53Homo sapiens (human)
site of double-strand breakCellular tumor antigen p53Homo sapiens (human)
germ cell nucleusCellular tumor antigen p53Homo sapiens (human)
chromatinCellular tumor antigen p53Homo sapiens (human)
transcription regulator complexCellular tumor antigen p53Homo sapiens (human)
protein-containing complexCellular tumor antigen p53Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (155)

Assay IDTitleYearJournalArticle
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID5985271-Octanol-sodium citrate buffer distribution coefficient, log D of the compound at pH 5.5 by shake-flask method2011Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
Lipophilicity of acidic compounds: impact of ion pair partitioning on drug design.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID91481Binding constant against human serum albumin (HSA)2001Journal of medicinal chemistry, Dec-06, Volume: 44, Issue:25
Cheminformatic models to predict binding affinities to human serum albumin.
AID188370Evaluated in glucose-primed, fasted rat for the percentage reduction in blood glucose level after 2 hr as compared to control groups at a dose of 500 mg of free base / kg body weight administered orally1982Journal of medicinal chemistry, Apr, Volume: 25, Issue:4
Chemistry and hypoglycemic activity of N-[[(Dialkylamino)alkoxy]phenyl]benzamidines.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID77194Evaluated in normal, fasted guinea pig for the percentage reduction in blood glucose level after 5 hr as compared to pretreatment blood glucose values at a dose of 160 mg of free base / kg body weight administered orally1982Journal of medicinal chemistry, Apr, Volume: 25, Issue:4
Chemistry and hypoglycemic activity of N-[[(Dialkylamino)alkoxy]phenyl]benzamidines.
AID188895Percent reduction in blood glucose after perorally administration of compound at 10 mg/kg in in adrenalectomized rat(p= 0.05)1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Chemistry and hypoglycemic activity of benzimidoylpyrazoles.
AID409954Inhibition of mouse brain MAOA2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID77200Percent reduction in blood glucose after perorally administration of compound at 125 mg/kg in in normal fasted guinea pig1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Chemistry and hypoglycemic activity of benzimidoylpyrazoles.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID188904Percent reduction in blood glucose after perorally administration of compound at 250 mg/kg in glucose-primed rat1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Chemistry and hypoglycemic activity of benzimidoylpyrazoles.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID134722Lethal dose required to produce 50% lethality in male and female carworth farms CF-1 strain mice weighing 16-25 g administered orally1982Journal of medicinal chemistry, Apr, Volume: 25, Issue:4
Chemistry and hypoglycemic activity of N-[[(Dialkylamino)alkoxy]phenyl]benzamidines.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID588210Human drug-induced liver injury (DILI) modelling dataset from Ekins et al2010Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 38, Issue:12
A predictive ligand-based Bayesian model for human drug-induced liver injury.
AID188901Percent reduction in blood glucose after perorally administration of compound at 25 mg/kg in glucose-primed rat1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Chemistry and hypoglycemic activity of benzimidoylpyrazoles.
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID239780Percentage plasma protein binding towards human serum albumin2005Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7
Predicting human serum albumin affinity of interleukin-8 (CXCL8) inhibitors by 3D-QSPR approach.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID188894Percent reduction in blood glucose after perorally administration of compound at 10 mg/kg in glucose-primed rat1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Chemistry and hypoglycemic activity of benzimidoylpyrazoles.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID409956Inhibition of mouse brain MAOB2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID188240Evaluated in glucose-primed, fasted rat for the percentage reduction in blood glucose level after 2 hr as compared to control groups at a dose of 10 mg of free base / kg body weight administered orally1982Journal of medicinal chemistry, Apr, Volume: 25, Issue:4
Chemistry and hypoglycemic activity of N-[[(Dialkylamino)alkoxy]phenyl]benzamidines.
AID599064Plasma protein binding in human2011Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
Lipophilicity of acidic compounds: impact of ion pair partitioning on drug design.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID188897Percent reduction in blood glucose after perorally administration of compound at 100 mg/kg in in alloxanized rat1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Chemistry and hypoglycemic activity of benzimidoylpyrazoles.
AID126664Evaluated in normal, fasted monkey for the percentage reduction in blood glucose level after 5 hr as compared to pretreatment blood glucose values at a dose of 20 mg of free base / kg body weight administered orally1982Journal of medicinal chemistry, Apr, Volume: 25, Issue:4
Chemistry and hypoglycemic activity of N-[[(Dialkylamino)alkoxy]phenyl]benzamidines.
AID134721Lethal dose required to produce 50% lethality in male and female carworth farms CF-1 strain mice weighing 16-25 g administered intraperitoneally1982Journal of medicinal chemistry, Apr, Volume: 25, Issue:4
Chemistry and hypoglycemic activity of N-[[(Dialkylamino)alkoxy]phenyl]benzamidines.
AID188237Evaluated in glucose primed, adrenalectomized rat for the percentage reduction in blood glucose level after 2 hr as compared to pretreatment blood glucose values at a dose of 20 mg of free base / kg body weight administered orally1982Journal of medicinal chemistry, Apr, Volume: 25, Issue:4
Chemistry and hypoglycemic activity of N-[[(Dialkylamino)alkoxy]phenyl]benzamidines.
AID134583Lethal dose after intraperitoneal administration in mouse1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Chemistry and hypoglycemic activity of benzimidoylpyrazoles.
AID77079Evaluated in normal, fasted guinea pig for the percentage reduction in blood glucose level after 5 hr as compared to pretreatment blood glucose values at a dose of 125 mg of free base / kg body weight administered orally1982Journal of medicinal chemistry, Apr, Volume: 25, Issue:4
Chemistry and hypoglycemic activity of N-[[(Dialkylamino)alkoxy]phenyl]benzamidines.
AID588209Literature-mined public compounds from Greene et al multi-species hepatotoxicity modelling dataset2010Chemical research in toxicology, Jul-19, Volume: 23, Issue:7
Developing structure-activity relationships for the prediction of hepatotoxicity.
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID77078Evaluated in normal, fasted guinea pig for the percentage reduction in blood glucose level after 5 hr as compared to pretreatment blood glucose values at a dose of 100 mg of free base / kg body weight administered orally1982Journal of medicinal chemistry, Apr, Volume: 25, Issue:4
Chemistry and hypoglycemic activity of N-[[(Dialkylamino)alkoxy]phenyl]benzamidines.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID134584Lethal dose after peroral administration in mouse1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Chemistry and hypoglycemic activity of benzimidoylpyrazoles.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID77201Percent reduction in blood glucose after perorally administration of compound at 150 mg/kg in in normal fasted guinea pig1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Chemistry and hypoglycemic activity of benzimidoylpyrazoles.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID188236Evaluated in glucose primed, adrenalectomized rat for the percentage reduction in blood glucose level after 2 hr as compared to pretreatment blood glucose values at a dose of 10 mg of free base / kg body weight administered orally1982Journal of medicinal chemistry, Apr, Volume: 25, Issue:4
Chemistry and hypoglycemic activity of N-[[(Dialkylamino)alkoxy]phenyl]benzamidines.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID5985261-Octanol-water distribution coefficient, log D of the compound at pH 7.4 by shake-flask method2011Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
Lipophilicity of acidic compounds: impact of ion pair partitioning on drug design.
AID188242Evaluated in glucose-primed, fasted rat for the percentage reduction in blood glucose level after 2 h as compared to control groups at a dose of 25 mg of free base / kg body weight administered orally1982Journal of medicinal chemistry, Apr, Volume: 25, Issue:4
Chemistry and hypoglycemic activity of N-[[(Dialkylamino)alkoxy]phenyl]benzamidines.
AID521220Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID126665Evaluated in normal, fasted monkey for the percentage reduction in blood glucose level after 5 hr as compared to pretreatment blood glucose values at a dose of 40 mg of free base / kg body weight administered orally1982Journal of medicinal chemistry, Apr, Volume: 25, Issue:4
Chemistry and hypoglycemic activity of N-[[(Dialkylamino)alkoxy]phenyl]benzamidines.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID188900Percent reduction in blood glucose after perorally administration of compound at 20 mg/kg in in adrenalectomized rat1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Chemistry and hypoglycemic activity of benzimidoylpyrazoles.
AID77202Percent reduction in blood glucose after perorally administration of compound at 160 mg/kg in in normal fasted guinea pig1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Chemistry and hypoglycemic activity of benzimidoylpyrazoles.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID77080Evaluated in normal, fasted guinea pig for the percentage reduction in blood glucose level after 5 hr as compared to pretreatment blood glucose values at a dose of 150 mg of free base / kg body weight administered orally1982Journal of medicinal chemistry, Apr, Volume: 25, Issue:4
Chemistry and hypoglycemic activity of N-[[(Dialkylamino)alkoxy]phenyl]benzamidines.
AID189024Percent reduction in blood glucose after perorally administration of compound at 500 mg/kg in glucose-primed rat1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Chemistry and hypoglycemic activity of benzimidoylpyrazoles.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID513647Induction of autophagy in rat stable inducible PC12 cells expressing A53T alpha-synuclein assessed as A53T alpha-synuclein clearance at 10 uM after 24 hrs by densitometric analysis2008Nature chemical biology, May, Volume: 4, Issue:5
Novel targets for Huntington's disease in an mTOR-independent autophagy pathway.
AID188368Evaluated in glucose-primed, fasted rat for the percentage reduction in blood glucose level after 2 hr as compared to control groups at a dose of 250 mg of free base / kg body weight administered orally1982Journal of medicinal chemistry, Apr, Volume: 25, Issue:4
Chemistry and hypoglycemic activity of N-[[(Dialkylamino)alkoxy]phenyl]benzamidines.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID188903Percent reduction in blood glucose after perorally administration of compound at 25 mg/kg in non-glucose-primed rat1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Chemistry and hypoglycemic activity of benzimidoylpyrazoles.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID188231Evaluated in alloxanized, diabetic rat for the percentage reduction in blood glucose level as compared to pretreatment blood glucose values at a dose of 100 mg of free base / kg body weight administered orally1982Journal of medicinal chemistry, Apr, Volume: 25, Issue:4
Chemistry and hypoglycemic activity of N-[[(Dialkylamino)alkoxy]phenyl]benzamidines.
AID77198Percent reduction in blood glucose after perorally administration of compound at 100 mg/kg in in normal fasted guinea pig1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Chemistry and hypoglycemic activity of benzimidoylpyrazoles.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID243230Binding affinity towards human serum albumin2005Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7
Predicting human serum albumin affinity of interleukin-8 (CXCL8) inhibitors by 3D-QSPR approach.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (190)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990137 (72.11)18.7374
1990's11 (5.79)18.2507
2000's8 (4.21)29.6817
2010's26 (13.68)24.3611
2020's8 (4.21)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 42.02

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index42.02 (24.57)
Research Supply Index5.43 (2.92)
Research Growth Index4.57 (4.65)
Search Engine Demand Index65.76 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (42.02)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials17 (8.10%)5.53%
Reviews11 (5.24%)6.00%
Case Studies18 (8.57%)4.05%
Observational0 (0.00%)0.25%
Other164 (78.10%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (4)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Incretin-based Drugs and the Risk of Heart Failure: A Multi-center Network Observational Study [NCT02456428]1,499,650 participants (Actual)Observational2014-03-31Completed
A Multi-center, Double-blind, Placebo-controlled, Randomized Study to Compare the Effect of a Subcutaneous Canakinumab Administration to Placebo in Patients With Impaired Glucose Tolerance or Patients With Type 2 Diabetes Treated With Differing Baseline D [NCT01068860]Phase 2246 participants (Actual)Interventional2010-02-28Completed
The Use of Incretin-based Drugs and the Risk of Acute Pancreatitis in Patients With Type 2 Diabetes [NCT02476760]1,417,914 participants (Actual)Observational2014-03-31Completed
The Use of Incretin-based Drugs and the Risk of Pancreatic Cancer in Patients With Type 2 Diabetes [NCT02475499]886,172 participants (Actual)Observational2014-03-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT01068860 (16) [back to overview]Mean Change in Absolute Glucose Level at 2 Hours, From Baseline to 4 Weeks
NCT01068860 (16) [back to overview]Mean Change in C-peptide Area Under the Curve (AUC), 0-4 Hours, From Baseline to 4 Weeks
NCT01068860 (16) [back to overview]Mean Change in Fasting Plasma Glucose, From Baseline to 4 Weeks
NCT01068860 (16) [back to overview]Mean Change in Fasting Plasma Insulin, From Baseline to 4 Weeks
NCT01068860 (16) [back to overview]Mean Change in Fructosamine, From Baseline to 4 Weeks
NCT01068860 (16) [back to overview]Mean Change in Insulin Area Under the Curve (AUC) 0-4 Hours, From Baseline to 4 Weeks
NCT01068860 (16) [back to overview]Mean Change in Meal Stimulated Insulin Secretion Rate (ISR) Relative to Glucose 0-2 Hours, From Baseline to 4 Weeks.
NCT01068860 (16) [back to overview]Mean Change in Meal Stimulated Insulin Secretion Rate (ISR) Relative to Glucose 0-4 Hours, From Baseline to 4 Weeks.
NCT01068860 (16) [back to overview]Mean Change in Meal Stimulated Insulin Secretion Rate (ISR) Relative to Glucose 2-4 Hours, From Baseline to 4 Weeks
NCT01068860 (16) [back to overview]Mean Change in Peak Plasma C-peptide Level, From Baseline to 4 Weeks
NCT01068860 (16) [back to overview]Mean Change in Peak Plasma Glucose, From Baseline to 4 Weeks
NCT01068860 (16) [back to overview]Mean Change in Peak Plasma Insulin, From Baseline to 4 Weeks
NCT01068860 (16) [back to overview]Mean Change in Post-prandial Glucose Area Under the Curve (AUC)0-4 Hours, From Baseline to 4 Weeks
NCT01068860 (16) [back to overview]Mean Change in Quantitative Insulin Sensitivity Check Index (QUICKI) Score, From Baseline to 4 Weeks
NCT01068860 (16) [back to overview]Mean Change in Fasting Glucose Disposition Index(GDI)1 and Index 2, From Baseline to 4 Weeks
NCT01068860 (16) [back to overview]Number of Participants Reporting Death, Serious Adverse Events (SAEs) and Adverse Events (AEs) Above 5% Frequency, From Baseline to 4 Weeks

Mean Change in Absolute Glucose Level at 2 Hours, From Baseline to 4 Weeks

"Change in glucose level measured after 2 hours of fasting. Blood sample was drawn at 0 minutes and at 240 minutes.~A mixed model with treatment fitted as fixed effect, and population and the interaction of population and treatment fitted as random effects were used for the comparison of Canakinumab versus placebo within each T2DM population. The mixed model did not include participants from the IGT population." (NCT01068860)
Timeframe: Baseline, 4 weeks

Interventionmmol/L (Least Squares Mean)
Canakinumab 150 mg + Metformin-0.53
Placebo + Metformin0.13
Canakinumab 150 mg + Metformin + Sulfonylurea-0.60
Placebo + Metformin + Sulfonylurea0.18
Canakinumab 150 mg Canakinumab 150 mg + Met + Sulfonyl + Thia-1.08
Placebo + Met + Sulfonyl + Thiaz-0.56
Canakinumab 150 mg + Insulin-0.56
Placebo + Insulin-0.16
Canakinumab 150 mg in Participants With IGT-0.26
Placebo in Participants With IGT-0.25

[back to top]

Mean Change in C-peptide Area Under the Curve (AUC), 0-4 Hours, From Baseline to 4 Weeks

Blood samples were drawn after a test meal at 0, 15, 30, 45, 60, 90, 120, 180 and 240 min. Insulin levels over 4 hrs were shown as Area Under the Curve,(AUC). AUC was calculated as: x=1 AUC ΣAx n Where Ax = AUC for the 240 min.interval, and X = 1 for the 1st interval. A mixed model with treatment fitted as fixed effect, and population and the interaction of population and treatment fitted as random effects were used for the comparison of Canakinumab vs placebo within each T2DM group. The mixed model didn't include the IGT group. (NCT01068860)
Timeframe: Baseline, 4 weeks

Interventionnmol*hour/L (Least Squares Mean)
Canakinumab 150 mg + Metformin-0.18
Placebo + Metformin-0.18
Canakinumab 150 mg + Metformin + Sulfonylurea-0.21
Placebo + Metformin + Sulfonylurea0.12
Canakinumab 150 mg Canakinumab 150 mg + Met + Sulfonyl + Thia-0.61
Placebo + Met + Sulfonyl + Thiaz0.02
Canakinumab 150 mg + Insulin0.16
Placebo + Insulin-0.29
Canakinumab 150 mg in Participants With IGT-0.43
Placebo in Participants With IGT-0.40

[back to top]

Mean Change in Fasting Plasma Glucose, From Baseline to 4 Weeks

"Change in Fasting Glucose Level measured from plasma taken at Baseline and after 4 weeks of treatment.~A mixed model with treatment fitted as fixed effect, and population and the interaction of population and treatment fitted as random effects were used for the comparison of Canakinumab versus placebo within each T2DM population. The mixed model did not include participants from the IGT population" (NCT01068860)
Timeframe: Baseline, 4 weeks

Interventionmmol/L (Least Squares Mean)
Canakinumab 150 mg + Metformin-0.32
Placebo + Metformin0.33
Canakinumab 150 mg + Metformin + Sulfonylurea-0.20
Placebo + Metformin + Sulfonylurea-0.23
Canakinumab 150 mg Canakinumab 150 mg + Met + Sulfonyl + Thia-0.33
Placebo + Met + Sulfonyl + Thiaz-0.36
Canakinumab 150 mg + Insulin-0.26
Placebo + Insulin-0.80
Canakinumab 150 mg in Participants With IGT-0.06
Placebo in Participants With IGT0.10

[back to top]

Mean Change in Fasting Plasma Insulin, From Baseline to 4 Weeks

"Change in Fasting Insulin level taken from plasma, measured at Baseline and after 4 weeks of treatment.~A mixed model with treatment fitted as fixed effect, and population and the interaction of population and treatment fitted as random effects were used for the comparison of Canakinumab versus placebo within each T2DM population. The mixed model did not include participants from the IGT population" (NCT01068860)
Timeframe: Baseline, 4 weeks

Interventionpmol/L (Least Squares Mean)
Canakinumab 150 mg + Metformin-3.58
Placebo + Metformin10.73
Canakinumab 150 mg + Metformin + Sulfonylurea-16.07
Placebo + Metformin + Sulfonylurea-9.40
Canakinumab 150 mg Canakinumab 150 mg + Met + Sulfonyl + Thia-0.77
Placebo + Met + Sulfonyl + Thiaz2.31
Canakinumab 150 mg + Insulin21.27
Placebo + Insulin25.67
Canakinumab 150 mg in Participants With IGT-.021
Placebo in Participants With IGT-3.43

[back to top]

Mean Change in Fructosamine, From Baseline to 4 Weeks

"Change in Fructosamine Level taken from plasma, measured at Baseline and after 4 weeks of treatment.~A mixed model with treatment fitted as fixed effect, and population and the interaction of population and treatment fitted as random effects were used for the comparison of Canakinumab versus placebo within each T2DM population. The mixed model did not include participants from the IGT population" (NCT01068860)
Timeframe: Baseline, 4 weeks

Interventionmmol/L (Least Squares Mean)
Canakinumab 150 mg + Metformin-5.30
Placebo + Metformin-0.75
Canakinumab 150 mg + Metformin + Sulfonylurea-3.45
Placebo + Metformin + Sulfonylurea-7.50
Canakinumab 150 mg Canakinumab 150 mg + Met + Sulfonyl + Thia-1.81
Placebo + Met + Sulfonyl + Thiaz-3.07
Canakinumab 150 mg + Insulin-3.00
Placebo + Insulin-19.73
Canakinumab 150 mg in Participants With IGT-6.36
Placebo in Participants With IGT1.39

[back to top]

Mean Change in Insulin Area Under the Curve (AUC) 0-4 Hours, From Baseline to 4 Weeks

Blood samples were drawn after a test meal at 0, 15, 30, 45, 60, 90, 120, 180 and 240 min. Insulin levels over 4 hrs were shown as Area Under the Curve,(AUC). AUC was calculated as: x=1 AUC ΣAx n Where Ax = AUC for the 240 min.interval, and X = 1 for the 1st interval. A mixed model with treatment fitted as fixed effect, and population and the interaction of population and treatment fitted as random effects were used for the comparison of Canakinumab vs placebo within each T2DM group. The mixed model didn't include the IGT group. (NCT01068860)
Timeframe: Baseline, 4 weeks

Interventionpmol*hour/L (Least Squares Mean)
Canakinumab 150 mg + Metformin-9.37
Placebo + Metformin1.21
Canakinumab 150 mg + Metformin + Sulfonylurea-73.25
Placebo + Metformin + Sulfonylurea-38.32
Canakinumab 150 mg Canakinumab 150 mg + Met + Sulfonyl + Thia-36.96
Placebo + Met + Sulfonyl + Thiaz8.46
Canakinumab 150 mg + Insulin163.87
Placebo + Insulin139.24
Canakinumab 150 mg in Participants With IGT44.27
Placebo in Participants With IGT-106.68

[back to top]

Mean Change in Meal Stimulated Insulin Secretion Rate (ISR) Relative to Glucose 0-2 Hours, From Baseline to 4 Weeks.

Change in Insulin Secretion Rate stimulated by Liquid mixed-meal challenge. Blood samples were taken prior to and after meal for glucose and insulin at sample times: -20, -10, -1 and 10, 20, 30, 60, 90, 120, 180, and 240 minutes relative to the start of the meal.A mixed model with treatment fitted as fixed effect, and population and the interaction of population and treatment fitted as random effects were used for the comparison of Canakinumab versus placebo within each T2DM population. The mixed model did not include patients from the IGT population (NCT01068860)
Timeframe: Baseline, 4 weeks

Interventionpmol/min/m^2/mmol/L (Least Squares Mean)
Canakinumab 150 mg + Metformin-0.06
Placebo + Metformin-0.23
Canakinumab 150 mg + Metformin + Sulfonylurea0.04
Placebo + Metformin + Sulfonylurea0.45
Canakinumab 150 mg Canakinumab 150 mg + Met + Sulfonyl + Thia-0.79
Placebo + Met + Sulfonyl + Thiaz1.16
Canakinumab 150 mg + Insulin1.23
Placebo + Insulin-0.49
Canakinumab 150 mg in Participants With IGT-1.50
Placebo in Participants With IGT-1.93

[back to top]

Mean Change in Meal Stimulated Insulin Secretion Rate (ISR) Relative to Glucose 0-4 Hours, From Baseline to 4 Weeks.

Change in Insulin Secretion Rate stimulated by Liquid mixed-meal challenge. Blood samples were taken prior to and after meal for glucose, insulin and C-peptide at sample times: -20, -10, -1 and 10, 20, 30, 60, 90, 120, 180, and 240 minutes relative to the start of the meal. A mixed model with treatment fitted as fixed effect, and population and the interaction of population and treatment fitted as random effects were used for the comparison of Canakinumab versus placebo within each T2DM population. The mixed model did not include participants from the IGT population. (NCT01068860)
Timeframe: Baseline, 4 weeks

Interventionpmol/min/m^2/mmol/L (Least Squares Mean)
Canakinumab 150 mg + Metformin0.44
Placebo + Metformin-0.99
Canakinumab 150 mg + Metformin + Sulfonylurea-0.32
Placebo + Metformin + Sulfonylurea1.22
Canakinumab 150 mg Canakinumab 150 mg + Met + Sulfonyl + Thia-0.63
Placebo + Met + Sulfonyl + Thiaz1.24
Canakinumab 150 mg + Insulin0.53
Placebo + Insulin-0.49
Canakinumab 150 mg in Participants With IGT-1.38
Placebo in Participants With IGT-1.35

[back to top]

Mean Change in Meal Stimulated Insulin Secretion Rate (ISR) Relative to Glucose 2-4 Hours, From Baseline to 4 Weeks

Change in Insulin Secretion Rate stimulated by Liquid mixed-meal challenge Blood samples were taken prior to and after meal for glucose and insulin at sample times: -20, -10, -1 and 10, 20, 30, 60, 90, 120, 180, and 240 minutes relative to the start of the meal. A mixed model with treatment fitted as fixed effect, and population and the interaction of population and treatment fitted as random effects were used for the comparison of Canakinumab versus placebo within each T2DM population. The mixed model did not include participants from the IGT population (NCT01068860)
Timeframe: Baseline, 4 weeks

Interventionpmol/min/m^2/mmol/L (Least Squares Mean)
Canakinumab 150 mg + Metformin0.21
Placebo + Metformin-2.15
Canakinumab 150 mg + Metformin + Sulfonylurea-2.98
Placebo + Metformin + Sulfonylurea2.02
Canakinumab 150 mg Canakinumab 150 mg + Met + Sulfonyl + Thia0.15
Placebo + Met + Sulfonyl + Thiaz1.19
Canakinumab 150 mg + Insulin-0.43
Placebo + Insulin-0.51
Canakinumab 150 mg in Participants With IGT-0.71
Placebo in Participants With IGT-1.00

[back to top]

Mean Change in Peak Plasma C-peptide Level, From Baseline to 4 Weeks

"Change in mean peak plasma C-peptide level measured from Baseline to 4 weeks of treatment.~A mixed model with treatment fitted as fixed effect, and population and the interaction of population and treatment fitted as random effects were used for the comparison of Canakinumab versus placebo within each T2DM population. The mixed model did not include participants from the IGT population." (NCT01068860)
Timeframe: Baseline, 4 weeks

Interventionnmol/L (Least Squares Mean)
Canakinumab 150 mg + Metformin-0.04
Placebo + Metformin-0.04
Canakinumab 150 mg + Metformin + Sulfonylurea-0.10
Placebo + Metformin + Sulfonylurea0.16
Canakinumab 150 mg Canakinumab 150 mg + Met + Sulfonyl + Thia-0.21
Placebo + Met + Sulfonyl + Thiaz0.05
Canakinumab 150 mg + Insulin0.07
Placebo + Insulin-0.14
Canakinumab 150 mg in Participants With IGT-0.18
Placebo in Participants With IGT-0.18

[back to top]

Mean Change in Peak Plasma Glucose, From Baseline to 4 Weeks

"Change in peak plasma glucose level as measured from Baseline to 4 weeks of treatment.~A mixed model with treatment fitted as fixed effect, and population and the interaction of population and treatment fitted as random effects were used for the comparison of Canakinumab versus placebo within each T2DM population. The mixed model did not include participants from the IGT population." (NCT01068860)
Timeframe: Baseline, 4 weeks

Interventionmmol/L (Least Squares Mean)
Canakinumab 150 mg + Metformin-0.41
Placebo + Metformin0.21
Canakinumab 150 mg + Metformin + Sulfonylurea-0.43
Placebo + Metformin + Sulfonylurea-0.03
Canakinumab 150 mg Canakinumab 150 mg + Met + Sulfonyl + Thia-0.82
Placebo + Met + Sulfonyl + Thiaz-0.77
Canakinumab 150 mg + Insulin-0.15
Placebo + Insulin-0.60
Canakinumab 150 mg in Participants With IGT-0.34
Placebo in Participants With IGT-0.04

[back to top]

Mean Change in Peak Plasma Insulin, From Baseline to 4 Weeks

Change in mean peak plasma Insulin level as measured from Baseline to 4 weeks of treatment. A mixed model with treatment fitted as fixed effect, and population and the interaction of population and treatment fitted as random effects were used for the comparison of Canakinumab versus placebo within each T2DM population. The mixed model did not include participants from the IGT population. (NCT01068860)
Timeframe: Baseline, 4 weeks

Interventionpmol/L (Least Squares Mean)
Canakinumab 150 mg + Metformin8.09
Placebo + Metformin44.56
Canakinumab 150 mg + Metformin + Sulfonylurea-55.07
Placebo + Metformin + Sulfonylurea11.33
Canakinumab 150 mg Canakinumab 150 mg + Met + Sulfonyl + Thia5.13
Placebo + Met + Sulfonyl + Thiaz-5.15
Canakinumab 150 mg + Insulin91.74
Placebo + Insulin36.87
Canakinumab 150 mg in Participants With IGT56.21
Placebo in Participants With IGT-26.43

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Mean Change in Post-prandial Glucose Area Under the Curve (AUC)0-4 Hours, From Baseline to 4 Weeks

Blood samples were drawn after a test meal at 0, 15, 30, 45, 60, 90, 120, 180 and 240 min. Insulin levels over 4 hrs were shown as Area Under the Curve,(AUC). AUC was calculated as: x=1 AUC ΣAx n Where Ax = AUC for the 240 min.interval, and X = 1 for the 1st interval. A mixed model with treatment fitted as fixed effect, and population and the interaction of population and treatment fitted as random effects were used for the comparison of Canakinumab vs placebo within each T2DM group. The mixed model didn't include the IGT group. (NCT01068860)
Timeframe: Baseline, 4 weeks

Interventionmmol*hr/L (Least Squares Mean)
Canakinumab 150 mg + Metformin-0.59
Placebo + Metformin0.46
Canakinumab 150 mg + Metformin + Sulfonylurea-1.37
Placebo + Metformin + Sulfonylurea-1.24
Canakinumab 150 mg Canakinumab 150 mg + Met + Sulfonyl + Thia-3.58
Placebo + Met + Sulfonyl + Thiaz-2.88
Canakinumab 150 mg + Insulin-1.49
Placebo + Insulin-1.76
Canakinumab 150 mg in Participants With IGT-0.71
Placebo in Participants With IGT-0.10

[back to top]

Mean Change in Quantitative Insulin Sensitivity Check Index (QUICKI) Score, From Baseline to 4 Weeks

"The Quantitative Insulin Sensitivity Check Index (QUICKI) score, measures insulin sensitivity which is the inverse of insulin resistance. The score is calculated by the equation: 1 /(log(fasting insulin µU/mL) + log(fasting glucose mg/dL)). In normal subjects the mean score ± SE is 0.366 ± 0.029.~A mixed model with treatment fitted as fixed effect, and population and the interaction of population and treatment fitted as random effects were used for the comparison of Canakinumab versus placebo within each T2DM population. The mixed model did not include participants from the IGT population." (NCT01068860)
Timeframe: Baseline, 4 weeks

Interventionnumber (Least Squares Mean)
Canakinumab 150 mg + Metformin0.004
Placebo + Metformin-0.000
Canakinumab 150 mg + Metformin + Sulfonylurea0.002
Placebo + Metformin + Sulfonylurea0.009
Canakinumab 150 mg Canakinumab 150 mg + Met + Sulfonyl + Thia0.018
Placebo + Met + Sulfonyl + Thiaz-0.001
Canakinumab 150 mg + Insulin-0.003
Placebo + Insulin0.005
Canakinumab 150 mg in Participants With IGT-0.001
Placebo in Participants With IGT0.001

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Mean Change in Fasting Glucose Disposition Index(GDI)1 and Index 2, From Baseline to 4 Weeks

GDI 1 is the product of insulin sensitivity index (Si)during the 1st phase of insulin secretion and β-cell function as measured by the acute insulin response (AIR).GDI 2 is the product of (Si)during the 2nd phase of insulin secretion and β-cell function as measured by the acute insulin response (AIR). A mixed model with treatment fitted as fixed effect, and population and the interaction of population and treatment fitted as random effects were used for the comparison of Canakinumab versus placebo within each T2DM population. The mixed model did not include participants from the IGT group. (NCT01068860)
Timeframe: Baseline, 4 weeks

,,,,,,,,,
Interventionnumber (Least Squares Mean)
Index 1Index 2 (n= 32,15, 29,15, 30,13, 25, 15, 20, 26)
Canakinumab 150 mg + Insulin0.25-0.21
Canakinumab 150 mg + Metformin0.060.14
Canakinumab 150 mg + Metformin + Sulfonylurea0.06-0.94
Canakinumab 150 mg Canakinumab 150 mg + Met + Sulfonyl + Thia0.240.62
Canakinumab 150 mg in Participants With IGT-0.51-0.16
Placebo + Insulin-0.27-0.25
Placebo + Met + Sulfonyl + Thiaz0.330.49
Placebo + Metformin-0.29-0.81
Placebo + Metformin + Sulfonylurea0.370.81
Placebo in Participants With IGT-0.64-0.31

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Number of Participants Reporting Death, Serious Adverse Events (SAEs) and Adverse Events (AEs) Above 5% Frequency, From Baseline to 4 Weeks

An adverse event is any unwanted event, whether related to study drug or not occuring during the study period. A Serious Adverse Event (SAE) is an event resulting in death, requiring or prolonging hospitalization, a congenital anomaly or other important medical event. AEs and SAEs were recorded at each visit. (NCT01068860)
Timeframe: Baseline, 4 weeks

,,,,,,,,,
Interventionparticipants (Number)
Number of Participants with Serious Adverse EventsNumber of Participants with Non-serious AEs > 5%
Canakinumab 150 mg + Insulin06
Canakinumab 150 mg + Metformin00
Canakinumab 150 mg + Metformin + Sulfonylurea06
Canakinumab 150 mg Canakinumab 150 mg + Met + Sulfonyl + Thia04
Canakinumab 150 mg in Participants With IGT00
Placebo + Insulin03
Placebo + Met + Sulfonyl + Thiaz03
Placebo + Metformin04
Placebo + Metformin + Sulfonylurea03
Placebo in Participants With IGT00

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