Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T87166 | Target Info | |||
| Target Name | Glucokinase (GCK) | ||||
| Synonyms |
Hexokinase type IV; Hexokinase D; HK4; HK IV
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| Target Type | Clinical trial Target | ||||
| Gene Name | GCK | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 25 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
1,1,1,3,3,3-Hexafluoro-2-{4-[4-(Thiophen-2-Ylsulfonyl)piperazin-1-Yl]phenyl}propan-2-Ol
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3113992; SCHEMBL17882; BDBM50447286; Q27452948; 1,1,1,3,3,3-hexafluoro-2-(4-(4-(2-thiophenylsulfonyl)-1-piperazinyl)phenyl)-2-propanol; 1,1,1,3,3,3-hexafluoro-2-[4-(4-thiophen-2-ylsulfonylpiperazin-1-yl)phenyl]propan-2-ol; 2-[4-[4-(2-Thienylsulfonyl)piperazino]phenyl]-1,1,1,3,3,3-hexafluoro-2-propanol
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| Activity |
EC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
N-[1-[2-(Diethylamino)ethyl]pyrazol-3-yl]-3-(3-methylpyridin-2-yl)-5-(4-methylsulfonylphenoxy)benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3235162; BDBM50008314
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| Activity |
EC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
1-[3-(2-Ethylpyridin-3-yl)oxy-5-pyridin-2-ylsulfanylpyridin-2-yl]-3-propan-2-ylurea
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3338062; BDBM50025831
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| Activity |
EC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
3-(3-Methylpyridin-2-yl)-5-(4-methylsulfonylphenoxy)-N-[4-(piperazin-1-ylmethyl)-1,3-thiazol-2-yl]benzamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3235154; BDBM50008302
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| Activity |
EC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
(2r)-1,1,1-Trifluoro-2-{4-[(2s)-2-{[(3s)-3-Methylmorpholin-4-Yl]methyl}-4-(Thiophen-2-Ylsulfonyl)piperazin-1-Yl]phenyl}propan-2-Ol
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|
Investigative | Compound Info | ||
| Synonyms |
AMG-1694; CHEMBL3113979; SCHEMBL17527; BDBM50447292; HY-12614; CS-0012081; Q27452590
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| Activity |
EC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
N-[1-(Ethoxymethyl)pyrazol-3-yl]-3-(3-methylpyridin-2-yl)-5-(4-methylsulfonylphenoxy)benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3235161; BDBM50008313
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| Activity |
EC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
N-[4-(Diethylaminomethyl)-1,3-thiazol-2-yl]-3-(3-methylpyridin-2-yl)-5-(4-methylsulfonylphenoxy)benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3235149; BDBM50008284
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| Activity |
EC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
(2S)-2-(2,4-Dioxo-1H-quinazolin-3-yl)-4-methyl-N-(1,3-thiazol-2-yl)pentanamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2346903; SCHEMBL2514564; BDBM50431779; (S)-2-(2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)-4-methyl-N-(thiazol-2-yl)pentanamide
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| Activity |
EC50 = 50000 nM
|
[4] | |||
| Compound Name |
3-(3-Methylpyridin-2-yl)-5-(4-methylsulfonylphenoxy)-N-[4-(propylaminomethyl)-1,3-thiazol-2-yl]benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3235159; BDBM50008311
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| Activity |
EC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
N-[3-(2-Ethylpyridin-3-yl)oxy-5-pyridin-2-ylsulfanylpyridin-2-yl]acetamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3338057; BDBM50025833
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|
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| Activity |
EC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
Ethyl N-[3-(2-ethylpyridin-3-yl)oxy-5-pyridin-2-ylsulfanylpyridin-2-yl]carbamate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3338058; BDBM50025832
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| Activity |
EC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
N,N-Dimethyl-5-[[2-methyl-6-(pyrimidin-2-ylcarbamoyl)-1-benzofuran-4-yl]oxy]pyrazine-2-carboxamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3218501
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|
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| Activity |
EC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
N-(5-Chloro-1,3-thiazol-2-yl)-2-(6-cyclopropylsulfonylindazol-1-yl)-3-(oxan-4-yl)propanamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4072997; SCHEMBL4303892; BDBM50242783
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| Activity |
EC50 ~ 100000 nM
|
[6] | |||
| Compound Name |
2-[1-(2-Chlorophenyl)pyrazolo[3,4-d]pyrimidin-4-yl]sulfanyl-N-pyrimidin-2-ylacetamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2206778; BDBM50402962
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|
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| Activity |
EC50 ~ 100000 nM
|
[7] | |||
| Compound Name |
2-(4-Tert-butylsulfonylpyrazol-1-yl)-N-(5-fluoro-1,3-thiazol-2-yl)-3-(oxan-4-yl)propanamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4090191; SCHEMBL2668531; BDBM50242784
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|
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| Activity |
EC50 ~ 100000 nM
|
[6] | |||
| Compound Name |
4-Methyl-2-(4-methylsulfonylpiperazin-1-yl)-N-(1,3-thiazol-2-yl)pentanamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2346908; BDBM50431775
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|
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| Activity |
EC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
2-[1-(2-Chlorophenyl)pyrazolo[3,4-d]pyrimidin-4-yl]sulfanyl-N-phenylacetamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2206776; ZINC1346483; BDBM50402964; AKOS000794419; MCULE-3731658650
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| Activity |
EC50 ~ 100000 nM
|
[7] | |||
| Compound Name |
2-[4-(3-Chlorophenyl)sulfonylpyrazol-1-yl]-N-(5-fluoro-1,3-thiazol-2-yl)-3-(oxan-4-yl)propanamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4069128; BDBM50242785
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|
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| Activity |
EC50 ~ 100000 nM
|
[6] | |||
| Compound Name |
(2S)-2-(2,4-Dioxo-1H-quinazolin-3-yl)-3-phenyl-N-(1,3-thiazol-2-yl)propanamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2346906; BDBM50431778
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|
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| Activity |
EC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
2-(1,3-Dihydroisoindol-2-yl)-4-methyl-N-(1,3-thiazol-2-yl)pentanamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2346907; BDBM50431774
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|
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| Activity |
EC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
N-(4-Methylthiazol-2-yl)-2-((1-phenyl-1H-pyrazolo[3,4-d]pyrimidin-4-yl)thio)acetamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2206775; Oprea1_451640; ZINC929264; BDBM50402950; AKOS001109901; MCULE-8445764804; SR-01000018339; SR-01000018339-1; F1874-0077
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| Activity |
EC50 ~ 100000 nM
|
[7] | |||
| Compound Name |
(2S)-2-[1-(3-Chloropyridin-2-yl)pyrazolo[3,4-d]pyrimidin-4-yl]oxy-N-(5-cyanopyridin-2-yl)-3-[(2S)-1-hydroxypropan-2-yl]oxypropanamide
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|
Investigative | Compound Info | ||
| Synonyms |
SCHEMBL838901; CHEMBL3221511
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|
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| Activity |
EC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
6-[3-(4-Methylsulfonylphenoxy)-5-propan-2-yloxyphenyl]-1H-pyrimidin-2-one
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2408134; BDBM50437903
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|
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| Activity |
EC50 ~ 100000 nM
|
[9] | |||
| Compound Name |
2-[1-(2-Chlorophenyl)pyrazolo[3,4-d]pyrimidin-4-yl]sulfanyl-N-(4-methyl-1,3-thiazol-2-yl)-2-phenylacetamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2206783; BDBM50402957
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|
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| Activity |
EC50 ~ 100000 nM
|
[7] | |||
| Compound Name |
N-[1-Benzofuran-2-yl(phenyl)methyl]-3,4-dihydro-2H-1,5-benzodioxepine-7-sulfonamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3746823; SCHEMBL12988812; BDBM50500197
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|
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| Activity |
EC50 ~ 100000 nM
|
[10] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 1. Discovery of a novel tool compound for in vivo proof-of-concept. J Med Chem. 2014 Jan 23;57(2):309-24. | ||||
| REF 2 | Discovery of 3-(4-methanesulfonylphenoxy)-N-[1-(2-methoxy-ethoxymethyl)-1H-pyrazol-3-yl]-5-(3-methylpyridin-2-yl)-benzamide as a novel glucokinase activator (GKA) for the treatment of type 2 diabetes mellitus. Bioorg Med Chem. 2014 Apr 1;22(7):2280-93. | ||||
| REF 3 | Discovery of 2-pyridylureas as glucokinase activators. J Med Chem. 2014 Oct 9;57(19):8180-6. | ||||
| REF 4 | Design, synthesis and SAR of novel glucokinase activators. Bioorg Med Chem Lett. 2013 Apr 1;23(7):2166-71. | ||||
| REF 5 | Designing glucokinase activators with reduced hypoglycemia risk: discovery of N,N-dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl)benzofuran-4-yloxy)pyrimidine-2-carboxamide as a clinical candidate for the treatment of type 2 diabetes mellitus. Medchemcomm. 2011;2:828-39. | ||||
| REF 6 | Discovery of potent and orally active 1,4-disubstituted indazoles as novel allosteric glucokinase activators. Bioorg Med Chem Lett. 2017 Jun 15;27(12):2678-2682. | ||||
| REF 7 | The discovery of a novel series of glucokinase activators based on a pyrazolopyrimidine scaffold. Bioorg Med Chem Lett. 2012 Dec 15;22(24):7302-5. | ||||
| REF 8 | Optimising pharmacokinetics of glucokinase activators with matched triplicate design sets - the discovery of AZD3651 and AZD9485. Medchemcomm. 2013;4:663-8. | ||||
| REF 9 | Pyrimidone-based series of glucokinase activators with alternative donor-acceptor motif. Bioorg Med Chem Lett. 2013 Aug 15;23(16):4571-8. | ||||
| REF 10 | Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N-S (nN-sigma*S-X) Interaction for Conformational Constraint. J Med Chem. 2015 Dec 24;58(24):9663-79. | ||||
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