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)
| Member | Definition | Class |
|---|---|---|
| ((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 |
| INDY | A 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)
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 11 (84.62) | 24.3611 |
| 2020's | 2 (15.38) | 2.80 |
Study Types
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 1 (7.14%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 13 (92.86%) | 84.16% |
Protein Targets (40)
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| [Tau protein] kinase | Sus scrofa (pig) | IC50 | 2.9350 | 4 | 4 |
| Cannabinoid receptor 1 | Homo sapiens (human) | IC50 | 0.3140 | 1 | 1 |
| Casein kinase II subunit alpha | Homo sapiens (human) | IC50 | 0.4150 | 2 | 2 |
| Casein kinase II subunit alpha 3 | Homo sapiens (human) | IC50 | 0.5100 | 1 | 1 |
| Casein kinase II subunit alpha' | Homo sapiens (human) | IC50 | 0.4150 | 2 | 2 |
| Casein kinase II subunit beta | Homo sapiens (human) | IC50 | 0.4150 | 2 | 2 |
| Cyclin-A1 | Homo sapiens (human) | IC50 | 30.0000 | 1 | 1 |
| Cyclin-A2 | Homo sapiens (human) | IC50 | 20.0000 | 2 | 2 |
| Cyclin-dependent kinase 2 | Homo sapiens (human) | IC50 | 20.0000 | 2 | 2 |
| Cyclin-dependent kinase 5 activator 1 | Homo sapiens (human) | IC50 | 13.4700 | 3 | 3 |
| Cyclin-dependent kinase 7 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| Cyclin-dependent kinase 9 | Homo sapiens (human) | IC50 | 14.0000 | 2 | 2 |
| Cyclin-dependent-like kinase 5 | Homo sapiens (human) | IC50 | 13.4700 | 3 | 3 |
| Cyclin-H | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| Cyclin-T1 | Homo sapiens (human) | IC50 | 14.0000 | 2 | 2 |
| Cytochrome P450 3A4 | Homo sapiens (human) | IC50 | 0.0710 | 1 | 1 |
| Dual specificity protein kinase CLK1 | Homo sapiens (human) | IC50 | 0.0710 | 1 | 1 |
| Dual specificity protein kinase CLK1 | Mus musculus (house mouse) | IC50 | 0.0360 | 4 | 4 |
| Dual specificity protein kinase CLK2 | Mus musculus (house mouse) | IC50 | 0.3900 | 3 | 3 |
| Dual specificity protein kinase CLK3 | Mus musculus (house mouse) | IC50 | 6.0500 | 4 | 4 |
| Dual specificity protein kinase CLK4 | Mus musculus (house mouse) | IC50 | 0.0393 | 3 | 3 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Homo sapiens (human) | IC50 | 0.1047 | 9 | 9 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Rattus norvegicus (Norway rat) | IC50 | 0.0300 | 3 | 3 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 1B | Homo sapiens (human) | IC50 | 0.0550 | 4 | 4 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 2 | Homo sapiens (human) | IC50 | 0.0855 | 4 | 4 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 3 | Homo sapiens (human) | IC50 | 0.4167 | 3 | 3 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 4 | Homo sapiens (human) | IC50 | 0.5200 | 1 | 1 |
| Glycogen synthase kinase-3 alpha | Homo sapiens (human) | IC50 | 0.2100 | 1 | 1 |
| Glycogen synthase kinase-3 beta | Homo sapiens (human) | IC50 | 0.3800 | 1 | 1 |
| Glycogen synthase kinase-3 beta | Sus scrofa (pig) | IC50 | 2.9350 | 4 | 4 |
| Kappa-type opioid receptor | Cavia porcellus (domestic guinea pig) | IC50 | 5.0355 | 2 | 2 |
| Mitogen-activated protein kinase 1 | Rattus norvegicus (Norway rat) | IC50 | 30.0000 | 1 | 1 |
| Serine/threonine-protein kinase pim-1 | Homo sapiens (human) | IC50 | 2.0600 | 3 | 3 |
Activation Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Dual specificity protein kinase CLK1 | Homo sapiens (human) | Kd | 0.0750 | 1 | 1 |
| Dual specificity protein kinase CLK2 | Homo sapiens (human) | Kd | 0.3600 | 1 | 1 |
| Dual specificity protein kinase CLK3 | Homo sapiens (human) | Kd | 1.1000 | 1 | 1 |
| Dual specificity protein kinase CLK4 | Homo sapiens (human) | Kd | 0.0700 | 1 | 1 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Homo sapiens (human) | Kd | 0.0078 | 1 | 1 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 1B | Homo sapiens (human) | Kd | 0.1400 | 1 | 1 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 2 | Homo sapiens (human) | Kd | 0.4500 | 1 | 1 |
| Glycogen synthase kinase-3 alpha | Homo sapiens (human) | Kd | 0.5500 | 1 | 1 |
| Homeodomain-interacting protein kinase 1 | Homo sapiens (human) | Kd | 0.3200 | 1 | 1 |
| Homeodomain-interacting protein kinase 3 | Homo sapiens (human) | Kd | 0.2300 | 1 | 1 |
| Interleukin-1 receptor-associated kinase 1 | Homo sapiens (human) | Kd | 0.9300 | 1 | 1 |
| Serine/threonine-protein kinase TAO1 | Homo sapiens (human) | Kd | 1.7000 | 1 | 1 |
Other Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Cannabinoid receptor 1 | Homo sapiens (human) | Kb | 2.2000 | 1 | 1 |