Target Poor or Non Binder(s) Information
Target General Information | Top | ||||
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Target ID | T04831 | Target Info | |||
Target Name | Tyrosine-protein kinase EIF2AK2 (p68) | ||||
Synonyms |
p68 kinase; Proteinkinase RNA-activated; Interferon-inducible RNA-dependent protein kinase p68; Interferon-induced, double-stranded RNA-activated protein kinase p68
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Target Type | Patented-recorded Target | ||||
Gene Name | EIF2AK2 | ||||
Biochemical Class | Kinase | ||||
UniProt ID |
Poor Binders of This Target (in total, 15 binders) | Download | Top | |||
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Compound Name |
3-Methyl-2-[[4-(2-methyl-1H-indol-3-yl)pyrimidin-2-yl]amino]butan-1-ol
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1802617; BDBM50347900
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Activity |
IC50 = 50000 nM
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[1] | |||
Compound Name |
N-(4-Chlorophenyl)-4-(5-methoxy-2-methyl-1H-indol-3-yl)pyrimidin-2-amine
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1802780; BDBM50347878
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Activity |
IC50 = 50000 nM
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[1] | |||
Compound Name |
N-[2-(1H-Indol-3-yl)ethyl]-4-(5-pyridin-4-yl-1H-pyrazol-4-yl)pyrimidin-2-amine
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1802781; BDBM50347877
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Activity |
IC50 = 51000 nM
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[1] | |||
Compound Name |
4-(5-Methoxy-2-methyl-1H-indol-3-yl)-N-(4-methoxyphenyl)pyrimidin-2-amine
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1802775; BDBM50347881
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Activity |
IC50 = 55000 nM
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[1] | |||
Compound Name |
4-[4-(2-Methyl-1H-indol-3-yl)pyrimidin-2-yl]morpholine
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1802619; BDBM50347898
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Activity |
IC50 = 90000 nM
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[1] | |||
Compound Name |
4-(2-Phenyl-1H-indol-3-yl)-N-(pyridin-3-ylmethyl)pyrimidin-2-amine
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1802784; BDBM50347874
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Activity |
IC50 ~ 100000 nM
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[1] | |||
Compound Name |
4-(5-Methoxy-1H-indol-3-yl)-N-(2-morpholin-4-ylethyl)pyrimidin-2-amine
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1802786; BDBM50347872
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Activity |
IC50 ~ 100000 nM
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[1] | |||
Compound Name |
2-Methyl-3-[2-(4-pyridin-2-ylpiperazin-1-yl)pyrimidin-4-yl]-1H-indole
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1802625; BDBM50347894
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Activity |
IC50 ~ 100000 nM
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[1] | |||
Compound Name |
N-Cyclopentyl-4-(2-phenyl-1H-indol-3-yl)pyrimidin-2-amine
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1802776; BDBM50347882
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Activity |
IC50 ~ 100000 nM
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[1] | |||
Compound Name |
3-[2-[4-(4-Fluorophenyl)piperazin-1-yl]pyrimidin-4-yl]-2-methyl-1H-indole
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1802620; BDBM50347899
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Activity |
IC50 ~ 100000 nM
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[1] | |||
Compound Name |
3-[2-[4-(4-Fluorophenyl)piperazin-1-yl]pyrimidin-4-yl]-1H-indole
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1802785; BDBM50347873
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Activity |
IC50 ~ 100000 nM
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[1] | |||
Compound Name |
5-Chloro-2-methyl-3-(2-pyrrolidin-1-ylpyrimidin-4-yl)-1H-indole
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1802777; BDBM50347880
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Activity |
IC50 ~ 100000 nM
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[1] | |||
Compound Name |
5-Chloro-3-[2-[4-(4-fluorophenyl)piperazin-1-yl]pyrimidin-4-yl]-2-methyl-1H-indole
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1802626; BDBM50347892
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Activity |
IC50 ~ 100000 nM
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[1] | |||
Compound Name |
2-Methyl-3-(2-pyrrolidin-1-ylpyrimidin-4-yl)-1H-indole
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1802624; BDBM50347895
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Activity |
IC50 ~ 100000 nM
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[1] | |||
Compound Name |
Methyl 3-[2-[2-(dimethylamino)ethylsulfanyl]pyrimidin-4-yl]-1H-indole-6-carboxylate
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1802627; BDBM50347893
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Activity |
IC50 ~ 100000 nM
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[1] | |||
Click to Show/Hide the Information of All Poor Binders |
Non Binders of This Target (in total, 1 non binders) | Download | Top | |||
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Compound Name |
N-[5-(6,7-Dimethoxyquinolin-4-yl)oxypyridin-2-yl]-1-methyl-3-oxo-2,5-diphenylpyrazole-4-carboxamide
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Investigative | Compound Info | ||
Synonyms |
CHEMBL3407848; BDBM50072073
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Activity |
IC50 = 480000 nM
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[2] |
References | Top | ||||
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REF 1 | Identification of new inhibitors of protein kinase R guided by statistical modeling. Bioorg Med Chem Lett. 2011 Jul 1;21(13):4108-14. | ||||
REF 2 | Discovery of 1H-pyrazol-3(2H)-ones as potent and selective inhibitors of protein kinase R-like endoplasmic reticulum kinase (PERK). J Med Chem. 2015 Feb 12;58(3):1426-41. |
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