Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T92803 | Target Info | |||
| Target Name | Dual-specificity tyrosine-phosphorylation regulated kinase 1A (DYRK1A) | ||||
| Synonyms |
hMNB; Protein kinase minibrain homolog; MNBH; MNB; HP86; Dual specificity tyrosine-phosphorylation-regulated kinase 1A; Dual specificity YAK1-related kinase; DYRK
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|
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| Target Type | Patented-recorded Target | ||||
| Gene Name | DYRK1A | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 30 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
1-(3,4-Dichlorophenyl)-4-(3,5-dihydroxybenzylidene)pyrazolidine-3,5-dione
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL470411; BDBM50278683
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
1-(3,4-Dichlorophenyl)-4-(2,4-dimethoxybenzylidene)pyrazolidine-3,5-dione
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL469570; BDBM50278681
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
4-(2,3-Dichlorobenzylidene)-1-(4-methoxyphenyl)pyrazolidine-3,5-dione
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL496675; BDBM50278831
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
(4E)-4-Benzylidene-1-(3,4-dichlorophenyl)pyrazolidine-3,5-dione
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL469775; ZINC194520; BDBM50278597; AKOS001607853; 4-benzylidene-1-(3,4-dichlorophenyl)pyrazolidine-3,5-dione
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
4-(3-Hydroxy-4-methoxybenzylidene)-1-(4-methoxyphenyl)pyrazolidine-3,5-dione
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL485532; BDBM50278085
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
4-(2,6-Dichlorobenzylidene)-1-(3,4-dichlorophenyl)pyrazolidine-3,5-dione
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL509892; BDBM50278685
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
1-(3,4-Dichlorophenyl)-4-(2-methoxybenzylidene)pyrazolidine-3,5-dione
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL472499; BDBM50278602
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
1-(3,4-Dichlorophenyl)-4-(3-methoxybenzylidene)pyrazolidine-3,5-dione
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL511841; BDBM50278601
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|
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
1-(3,4-Dichlorophenyl)-4-(3-hydroxy-4-methoxybenzylidene)pyrazolidine-3,5-dione
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL469347; BDBM50278638
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|
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
1-(3,4-Dichlorophenyl)-4-(4-hydroxy-3,5-dimethoxybenzylidene)pyrazolidine-3,5-dione
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL470632; BDBM50278754
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|
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
1-(3,4-Dichlorophenyl)-4-(4-methoxybenzylidene)pyrazolidine-3,5-dione
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL469777; ZINC1084629; BDBM50278600; (4E)-1-(3,4-dichlorophenyl)-4-(4-methoxybenzylidene)pyrazolidine-3,5-dione
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
1-(3,4-Dichlorophenyl)-4-(2-fluorobenzylidene)pyrazolidine-3,5-dione
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL513188; BDBM50278637
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|
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
1-(3,4-Dichlorophenyl)-4-(2-nitrobenzylidene)pyrazolidine-3,5-dione
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL513717; BDBM50278635
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|
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
4-(4-(3-Hydroxy-4-methoxybenzylidene)-3,5-dioxopyrazolidin-1-yl)benzonitrile
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL498719; BDBM50278827
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|
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
1-(3,4-Dichlorophenyl)-4-(3,4-dimethoxybenzylidene)pyrazolidine-3,5-dione
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL469348; ZINC5676063; BDBM50278639; CCG-12362; AKOS003234220; AKOS024354922; BIM-0025367.P001; ST50981929; SR-01000214297; SR-01000214297-1
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|
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
4-(2-Methoxybenzylidene)-1-(4-methoxyphenyl)pyrazolidine-3,5-dione
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL496665; BDBM50278828
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|
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
4-(3,5-Dihydroxybenzylidene)-1-(4-methoxyphenyl)pyrazolidine-3,5-dione
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL484334; BDBM50278084
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|
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
4-(2-Fluorobenzylidene)-1-(4-methoxyphenyl)pyrazolidine-3,5-dione
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL523580; BDBM50278830
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|
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
4-(4-Hydroxy-3,5-dimethoxybenzylidene)-1-(4-methoxyphenyl)pyrazolidine-3,5-dione
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL519700; BDBM50278087
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|
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
1-(4-Fluorophenyl)-4-(2-methoxybenzylidene)pyrazolidine-3,5-dione
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL470817; ZINC90183; BDBM50278144; AKOS024289092; MCULE-7393254870
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|
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
4-(3,5-Dimethoxybenzylidene)-1-(4-methoxyphenyl)pyrazolidine-3,5-dione
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL484166; BDBM50278083
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|
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
CID 67284258
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3609656; SCHEMBL2122461; BDBM50114678; 1-(2,6-dioxo-1,3,4,10b-tetrahydropyrido[2,1-a]isoindol-10-yl)-3-pyrazin-2-ylurea
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|
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| Activity |
IC50 = 50000 nM
|
[2] | |||
| Compound Name |
4-(3-Methoxybenzylidene)-1-(4-methoxyphenyl)pyrazolidine-3,5-dione
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL496666; BDBM50278829
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|
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
2-(3-Methoxyphenyl)-N-[(4-methylphenyl)methyl]pyrimidin-4-amine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2392379; KUC104517N; BDBM50435495; CMC-46-280-C3; NCGC00188812-01
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|
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| Activity |
IC50 = 65400 nM
|
[3] | |||
| Compound Name |
1-(6-Oxospiro[1,3,4,10b-tetrahydropyrido[2,1-a]isoindole-2,2'-1,3-dioxolane]-10-yl)-3-pyridin-2-ylurea
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3609564; SCHEMBL1723818; BDBM50114575
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|
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| Activity |
IC50 = 80000 nM
|
[2] | |||
| Compound Name |
2-[2-[[4-[(3-Carboxy-5,6-dihydro-4H-cyclopenta[b]thiophen-2-yl)amino]-2-methyl-4-oxobutan-2-yl]amino]-2-oxoethyl]-5,6-dihydro-4H-cyclopenta[b]thiophene-3-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1933801; BDBM50361147
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|
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| Activity |
IC50 = 88130 nM
|
[4] | |||
| Compound Name |
1-(6-Oxospiro[1,3,4,10b-tetrahydropyrido[2,1-a]isoindole-2,2'-1,3-dioxolane]-10-yl)-3-pyrazin-2-ylurea
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3609569; SCHEMBL1724419; BDBM50114580
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|
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| Activity |
IC50 = 93000 nM
|
[2] | |||
| Compound Name |
Butyrolactone I 3-sulfate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL460464; BDBM50242741
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|
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| Activity |
IC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
(4Z)-2-Anilino-4-benzylidene-1H-imidazol-5-one
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3092860; BDBM50443641
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|
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| Activity |
IC50 ~ 100000 nM
|
[6] | |||
| Compound Name |
Chembl4276946
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|
Investigative | Compound Info | ||
| Synonyms |
GTPL9965; compound 3a [Pipionne et al, 2018]; 1-[5-amino-4-(3,4-dichlorophenyl)-3-methyl-1H-pyrazol-1-yl]ethan-1-one
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|
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| Activity |
IC50 ~ 100000 nM
|
[7] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 2 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Chembl4291088
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|
Investigative | Compound Info | ||
| Synonyms |
BDBM50466854
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|
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| Activity |
IC50 = 420000 nM
|
[8] | |||
| Compound Name |
N-(4-Methoxybenzyl)benzofuro[2,3-b]pyridin-4-amine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1290072; BDBM50331612
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|
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| Activity |
Ki > 1000000 nM
|
[9] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | QSAR analysis of pyrazolidine-3,5-diones derivatives as Dyrk1A inhibitors. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2324-8. | ||||
| REF 2 | Advances in tetrahydropyrido[1,2-a]isoindolone (valmerins) series: Potent glycogen synthase kinase 3 and cyclin dependent kinase 5 inhibitors. Eur J Med Chem. 2015 Aug 28;101:274-87. | ||||
| REF 3 | Small-molecule pyrimidine inhibitors of the cdc2-like (Clk) and dual specificity tyrosine phosphorylation-regulated (Dyrk) kinases: development of chemical probe ML315. Bioorg Med Chem Lett. 2013 Jun15;23(12):3654-61. | ||||
| REF 4 | Discovery of potent small molecule inhibitors of DYRK1A by structure-based virtual screening and bioassay. Bioorg Med Chem Lett. 2012 Jan 1;22(1):168-71. | ||||
| REF 5 | Butyrolactone I derivatives from Aspergillus terreus carrying an unusual sulfate moiety. J Nat Prod. 2008 Apr;71(4):689-92. | ||||
| REF 6 | Chemical synthesis and biological validation of immobilized protein kinase inhibitory Leucettines. Eur J Med Chem. 2013 Apr;62:728-37. | ||||
| REF 7 | N-Acetyl-3-aminopyrazoles block the non-canonical NF-kB cascade by selectively inhibiting NIK. Medchemcomm. 2018 Apr 12;9(6):963-968. | ||||
| REF 8 | Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase 1A (DYRK1A) Inhibitors as Potential Therapeutics. J Med Chem. 2018 Nov 21;61(22):9791-9810. | ||||
| REF 9 | Discovery and selectivity-profiling of 4-benzylamino 1-aza-9-oxafluorene derivatives as lead structures for IGF-1R inhibitors. Bioorg Med Chem Lett. 2010 Dec 1;20(23):6915-9. | ||||
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