Page last updated: 2024-08-05 15:49:58

EC 2.7.12.1 (dual-specificity kinase) inhibitor

An EC 2.7.12.* [dual-specificity kinases (those acting on Ser/Thr and Tyr residues)] inhibitor that inhibits the action of dual-specificity kinase (EC 2.7.12.1).

ChEBI ID: 195525

Members (2)

MemberDefinitionClass
((5z)5-(1,3-benzodioxol-5-yl)methylene-2-phenylamino-3,5-dihydro-4h-imidazol-4-one)A member of the class of benzodioxoles that is 1,3-benzodioxole substituted by a (2-anilino-5-oxo-1,5-dihydro-4H-imidazol-4-ylidene)methyl group at position 5. It is an inhibitor of DYRK1A, DYRK2, CLK1, and CLK3 (IC50s = 0.04, 0.035, 0.015, and 4.5 muM, respectively).leucettine L41
INDYA member of the class of benzothiazoles that is 2,3-dihydro-1,3-benzothiazole substituted by 2-oxopropylidene, ethyl, and hydroxy groups at positions 2, 3 and 5, respectively. It is an ATP-competitive inhibitor of Dyrk1A and Dyrk1B (IC50 of 0.24 muM and 0.23 muM, respectively).INDY

Research

Studies (13)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's11 (84.62)24.3611
2020's2 (15.38)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (7.14%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other13 (92.86%)84.16%

Protein Targets (40)

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
[Tau protein] kinase Sus scrofa (pig)IC502.935044
Cannabinoid receptor 1Homo sapiens (human)IC500.314011
Casein kinase II subunit alphaHomo sapiens (human)IC500.415022
Casein kinase II subunit alpha 3Homo sapiens (human)IC500.510011
Casein kinase II subunit alpha'Homo sapiens (human)IC500.415022
Casein kinase II subunit betaHomo sapiens (human)IC500.415022
Cyclin-A1Homo sapiens (human)IC5030.000011
Cyclin-A2Homo sapiens (human)IC5020.000022
Cyclin-dependent kinase 2Homo sapiens (human)IC5020.000022
Cyclin-dependent kinase 5 activator 1Homo sapiens (human)IC5013.470033
Cyclin-dependent kinase 7Homo sapiens (human)IC5010.000011
Cyclin-dependent kinase 9Homo sapiens (human)IC5014.000022
Cyclin-dependent-like kinase 5 Homo sapiens (human)IC5013.470033
Cyclin-HHomo sapiens (human)IC5010.000011
Cyclin-T1Homo sapiens (human)IC5014.000022
Cytochrome P450 3A4Homo sapiens (human)IC500.071011
Dual specificity protein kinase CLK1Homo sapiens (human)IC500.071011
Dual specificity protein kinase CLK1Mus musculus (house mouse)IC500.036044
Dual specificity protein kinase CLK2Mus musculus (house mouse)IC500.390033
Dual specificity protein kinase CLK3Mus musculus (house mouse)IC506.050044
Dual specificity protein kinase CLK4Mus musculus (house mouse)IC500.039333
Dual specificity tyrosine-phosphorylation-regulated kinase 1AHomo sapiens (human)IC500.104799
Dual specificity tyrosine-phosphorylation-regulated kinase 1ARattus norvegicus (Norway rat)IC500.030033
Dual specificity tyrosine-phosphorylation-regulated kinase 1BHomo sapiens (human)IC500.055044
Dual specificity tyrosine-phosphorylation-regulated kinase 2Homo sapiens (human)IC500.085544
Dual specificity tyrosine-phosphorylation-regulated kinase 3Homo sapiens (human)IC500.416733
Dual specificity tyrosine-phosphorylation-regulated kinase 4Homo sapiens (human)IC500.520011
Glycogen synthase kinase-3 alphaHomo sapiens (human)IC500.210011
Glycogen synthase kinase-3 betaHomo sapiens (human)IC500.380011
Glycogen synthase kinase-3 beta Sus scrofa (pig)IC502.935044
Kappa-type opioid receptorCavia porcellus (domestic guinea pig)IC505.035522
Mitogen-activated protein kinase 1Rattus norvegicus (Norway rat)IC5030.000011
Serine/threonine-protein kinase pim-1Homo sapiens (human)IC502.060033

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Dual specificity protein kinase CLK1Homo sapiens (human)Kd0.075011
Dual specificity protein kinase CLK2Homo sapiens (human)Kd0.360011
Dual specificity protein kinase CLK3Homo sapiens (human)Kd1.100011
Dual specificity protein kinase CLK4Homo sapiens (human)Kd0.070011
Dual specificity tyrosine-phosphorylation-regulated kinase 1AHomo sapiens (human)Kd0.007811
Dual specificity tyrosine-phosphorylation-regulated kinase 1BHomo sapiens (human)Kd0.140011
Dual specificity tyrosine-phosphorylation-regulated kinase 2Homo sapiens (human)Kd0.450011
Glycogen synthase kinase-3 alphaHomo sapiens (human)Kd0.550011
Homeodomain-interacting protein kinase 1Homo sapiens (human)Kd0.320011
Homeodomain-interacting protein kinase 3Homo sapiens (human)Kd0.230011
Interleukin-1 receptor-associated kinase 1Homo sapiens (human)Kd0.930011
Serine/threonine-protein kinase TAO1Homo sapiens (human)Kd1.700011

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Cannabinoid receptor 1Homo sapiens (human)Kb2.200011