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Literature summary for 2.7.11.20 extracted from

  • Pan, Z.; Chen, Y.; Liu, J.; Jiang, Q.; Yang, S.; Guo, L.; He, G.
    Design, synthesis, and biological evaluation of polo-like kinase 1/eukaryotic elongation factor 2 kinase (PLK1/EEF2K) dual inhibitors for regulating breast cancer cells apoptosis and autophagy (2018), Eur. J. Med. Chem., 144, 517-528 .
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(4-[[4-(1H-benzimidazol-5-ylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]benzene-1,2-diyl)dicyanamide
-
Homo sapiens
1-[3-[(5,6,7-trimethyl-2-phenyl-7H-cyclopenta[d]pyrimidin-4-yl)amino]propyl]pyrrolidin-2-one
-
Homo sapiens
2-chloro-4-hydroxy-5-(3-phenoxyphenyl)-7,7a-dihydrothieno[2,3-b]pyridin-6(3aH)-one 21% inhibition at 0.05 mM Homo sapiens
3-([4-[(5-methoxy-2-methylphenyl)amino]pyrimidin-2-yl]amino)benzamide 36% inhibition at 0.05 mM Homo sapiens
3-[4-(pyridin-4-yl)-1,3-thiazol-2-yl]-3,4-dihydroquinazolin-2(1H)-one 48% inhibition at 0.05 mM Homo sapiens
4-(4-amino-2-methylphenyl)-N-methylpyridin-2-amine 75% inhibition at 0.05 mM Homo sapiens
A-484954
-
Homo sapiens
N,N'-bis(2-methylphenyl)quinazoline-2,4-diamine
-
Homo sapiens
N-(2,6-dimethylphenyl)-N'-[4-[2-(ethylamino)pyridin-4-yl]-3-methoxyphenyl]urea
-
Homo sapiens
N-(2,6-dimethylphenyl)-N'-[4-[2-(ethylamino)pyridin-4-yl]-3-methylphenyl]urea 8.7% inhibition at 0.02 mM Homo sapiens
N-(2-chlorophenyl)-N'-[4-[2-(ethylamino)pyridin-4-yl]-3-(trifluoromethyl)phenyl]urea 53.6% inhibition at 0.02 mM Homo sapiens
N-(2-chlorophenyl)-N'-[4-[2-(ethylamino)pyridin-4-yl]-3-methoxyphenyl]urea 6.4% inhibition at 0.02 mM Homo sapiens
N-(2-chlorophenyl)-N'-[4-[2-(ethylamino)pyridin-4-yl]-3-methylphenyl]urea 21.7% inhibition at 0.02 mM Homo sapiens
N-(2-hydroxyethyl)-1-(4-[(E)-[(7-hydroxy-6H-[1,3]thiazolo[5,4-e]indol-8-yl)methylidene]amino]phenyl)methanesulfonamide
-
Homo sapiens
N-(3-chlorophenyl)-N'-[4-[2-(ethylamino)pyridin-4-yl]-3-(trifluoromethyl)phenyl]urea 82.7% inhibition at 0.02 mM Homo sapiens
N-(3-chlorophenyl)-N'-[4-[2-(ethylamino)pyridin-4-yl]-3-fluorophenyl]urea 52.5% inhibition at 0.02 mM Homo sapiens
N-(3-chlorophenyl)-N'-[4-[2-(ethylamino)pyridin-4-yl]-3-methoxyphenyl]urea 30.6% inhibition at 0.02 mM Homo sapiens
N-(3-chlorophenyl)-N'-[4-[2-(ethylamino)pyridin-4-yl]-3-methylphenyl]urea 73.4% inhibition at 0.02 mM Homo sapiens
N-(3-chlorophenyl)-N'-[4-[2-(propylamino)pyridin-4-yl]-3-(trifluoromethyl)phenyl]urea 38.2% inhibition at 0.02 mM Homo sapiens
N-(3-chlorophenyl)-N'-[4-[2-[(cyclopropylmethyl)amino]pyridin-4-yl]-3-(trifluoromethyl)phenyl]urea 27.8% inhibition at 0.02 mM Homo sapiens
N-[3,5-bis(trifluoromethyl)phenyl]-N'-[4-[2-(ethylamino)pyridin-4-yl]-3-(trifluoromethyl)phenyl]urea 37.2% inhibition at 0.02 mM Homo sapiens
N-[4-([4-(azetidin-1-yl)-6-[(3-methyl-1H-pyrazol-5-yl)amino]pyrimidin-2-yl]sulfanyl)phenyl]propanamide
-
Homo sapiens
N-[4-[2-(ethylamino)pyridin-4-yl]-3-(trifluoromethyl)phenyl]-N'-(4-methoxyphenyl)urea 51.3% inhibition at 0.02 mM Homo sapiens
N-[4-[2-(ethylamino)pyridin-4-yl]-3-(trifluoromethyl)phenyl]-N'-(4-methylphenyl)urea 37.9% inhibition at 0.02 mM Homo sapiens
N-[4-[2-(ethylamino)pyridin-4-yl]-3-(trifluoromethyl)phenyl]-N'-[4-(naphthalen-2-yl)phenyl]urea 44% inhibition at 0.02 mM Homo sapiens
N-[4-[2-(ethylamino)pyridin-4-yl]-3-(trifluoromethyl)phenyl]-N'-[4-(trifluoromethyl)phenyl]urea 76.3% inhibition at 0.02 mM Homo sapiens
N-[4-[2-(ethylamino)pyridin-4-yl]-3-fluorophenyl]-N'-(4-methoxyphenyl)urea 34.4% inhibition at 0.02 mM Homo sapiens
N-[4-[2-(ethylamino)pyridin-4-yl]-3-fluorophenyl]-N'-[4-(trifluoromethyl)phenyl]urea 41.2% inhibition at 0.02 mM Homo sapiens
N-[4-[2-(ethylamino)pyridin-4-yl]-3-methoxyphenyl]-N'-(4-methoxyphenyl)urea 9.0% inhibition at 0.02 mM Homo sapiens
N-[4-[2-(ethylamino)pyridin-4-yl]-3-methoxyphenyl]-N'-[4-(trifluoromethyl)phenyl]urea 34.6% inhibition at 0.02 mM Homo sapiens
N-[4-[2-(ethylamino)pyridin-4-yl]-3-methylphenyl]-N'-(4-methoxyphenyl)urea 33.4% inhibition at 0.02 mM Homo sapiens
N-[4-[2-(ethylamino)pyridin-4-yl]-3-methylphenyl]-N'-(4-methylphenyl)urea 35.4% inhibition at 0.02 mM Homo sapiens
N-[4-[2-(ethylamino)pyridin-4-yl]-3-methylphenyl]-N'-[4-(naphthalen-2-yl)phenyl]urea
-
Homo sapiens
N-[4-[2-(ethylamino)pyridin-4-yl]-3-methylphenyl]-N'-[4-(trifluoromethyl)phenyl]urea 55.3% inhibition at 0.02 mM Homo sapiens
N-[4-[2-(propylamino)pyridin-4-yl]-3-(trifluoromethyl)phenyl]-N'-[4-(trifluoromethyl)phenyl]urea 33.3% inhibition at 0.02 mM Homo sapiens
N-[4-[2-[(cyclopropylmethyl)amino]pyridin-4-yl]-3-(trifluoromethyl)phenyl]-N'-[4-(trifluoromethyl)phenyl]urea 15.1% inhibition at 0.02 mM Homo sapiens
N2,N2-dimethyl-6-[[(2-phenoxyethyl)amino]methyl]-N4-[(1S)-1-phenylethyl]-1,3,5-triazine-2,4-diamine
-
Homo sapiens
NH125 1-benzyl-3-cetyl-2-methylimidazolium iodide Homo sapiens
rottlerin
-
Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + [elongation factor 2] Homo sapiens the enzyme phosphorylates elongation factor 2 at Ser56 and Thr58 ADP + [elongation factor 2] phosphate
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens O00418
-
-

Source Tissue

Source Tissue Comment Organism Textmining
breast cancer cell
-
Homo sapiens
-
BT-483 cell
-
Homo sapiens
-
MCF-7 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + [elongation factor 2] the enzyme phosphorylates elongation factor 2 at Ser56 and Thr58 Homo sapiens ADP + [elongation factor 2] phosphate
-
?

Synonyms

Synonyms Comment Organism
calcium/calmodulin-dependent protein kinase-III
-
Homo sapiens
CaMK-III
-
Homo sapiens
eEF2K
-
Homo sapiens
eukaryotic elongation factor 2 kinase
-
Homo sapiens