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Literature summary for 3.6.5.5 extracted from

  • Odell, L.R.; Abdel-Hamid, M.K.; Hill, T.A.; Chau, N.; Young, K.A.; Deane, F.M.; Sakoff, J.A.; Andersson, S.; Daniel, J.A.; Robinson, P.J.; McCluskey, A.
    Pyrimidine-based inhibitors of dynamin I GTPase activity competitive inhibition at the pleckstrin homology domain (2017), J. Med. Chem., 60, 349-361 .
    View publication on PubMed
Search for more literature for 3.6.5.5

Inhibitors

Inhibitors Comment Organism Structure
(2-chloro-6-methylpyrimidin-4-yl)butylamine
-
 Homo sapiens
(2-chloro-6-methylpyrimidin-4-yl)cyclohexylamine
-
 Homo sapiens
(2-chloro-6-methylpyrimidin-4-yl)cyclopropylmethylpropylamine
-
 Homo sapiens
(2-chloro-6-methylpyrimidin-4-yl)decylamine
-
 Homo sapiens
(2-chloro-6-methylpyrimidin-4-yl)dimethylamine
-
 Homo sapiens
(2-chloro-6-methylpyrimidin-4-yl)ethylamine
-
 Homo sapiens
(2-chloro-6-methylpyrimidin-4-yl)hexylamine
-
 Homo sapiens
(2-chloro-6-methylpyrimidin-4-yl)octylamine
-
 Homo sapiens
(2-chloro-6-methylpyrimidin-4-yl)propylamine
-
 Homo sapiens
(2-chloro-6-methylpyrimidin-4-yl)tetradecylamine
-
 Homo sapiens
(4-chloro-6-methylpyrimidin-2-yl)(1-cyclopropylmethylpropyl)amine
-
 Homo sapiens
(4-chloro-6-methylpyrimidin-2-yl)-dimethylamine
-
 Homo sapiens
(4-chloro-6-methylpyrimidin-2-yl)butylamine
-
 Homo sapiens
(4-chloro-6-methylpyrimidin-2-yl)cyclohexylamine
-
 Homo sapiens
(4-chloro-6-methylpyrimidin-2-yl)decylamine
-
 Homo sapiens
(4-chloro-6-methylpyrimidin-2-yl)hexylamine
-
 Homo sapiens
(4-chloro-6-methylpyrimidin-2-yl)octylamine
-
 Homo sapiens
(4-chloro-6-methylpyrimidin-2-yl)propylamine
-
 Homo sapiens
(4-chloro-6-methylpyrimidin-2-yl)tetradecylamine
-
 Homo sapiens
2-(2-dimethylaminoethyl)-4-N-(didecylamino)-6-methylpyrimidine
-
 Homo sapiens
2-chloro-4-(2-dimethylaminopropylamine)-6-methylpyrimidine
-
 Homo sapiens
2-chloro-5-methyl-4-(4-methylpiperazin-1-yl)pyrimidine
-
 Homo sapiens
2-chloro-N-(4-methoxybenzyl)-6-methylpyrimidin-4-amine
-
 Homo sapiens
4-(2-dimethylaminoethyl)-2-N-(didecylamino)-6-methylpyrimidine
-
 Homo sapiens
4-chloro-6-methyl-2-(4-methylpiperazin-1-yl)pyrimidine
-
 Homo sapiens
4-chloro-N-(4-methoxybenzyl)-6-methylpyrimidin-2-amine
-
 Homo sapiens
additional information computational approach of binding site identification, docking, and interaction energy calculations to design a library of aminopyrimidine analogues targeting site-2 of the pleckstrin homology (PH) domain. Synthesis and evaluation of pyrimidine-based inhibitors of dynamin I GTPase activity, competitive inhibition at the pleckstrin homology domain, overview. The optimized analogues show low micromolar inhibition against both dynamin I and CME and off-target effects at the cholecystokinin, dopamine D2, histamine H1 and H2, melanocortin, melatonin, muscarinic M1 and M3, neurokinin, opioid KOP and serotonin receptors. No inhibition by (4-chloro-6-methylpyrimidin-2-yl)ethylamine at 0.3 mM Homo sapiens
N'-(2-chloro-6-methylpyrimidin-4-yl)ethane-1,2-diamine
-
 Homo sapiens
N'-(4-Chloro-6-methylpyrimidin-2-yl)-ethane-1,2-diamine
-
 Homo sapiens
N-benzyl-2-chloro-6-methylpyrimidin-4-amine
-
 Homo sapiens
N-benzyl-4-chloro-6-methylpyrimidin-2-amine
-
 Homo sapiens
N-decyl-N'-(2-dimethylaminoethyl)-pyrimidine-4,6-diamine
-
 Homo sapiens
N-dodecyl-N'-(2-dimethylaminoethyl)pyrimidine-4,6-diamine
-
 Homo sapiens
N1-(4-chloro-6-methylpyrimidin-2-yl)-N3,N3-dimethylpropane-1,3-diamine
-
 Homo sapiens
N2-(2-dimethylaminoethyl)-6-methyl-N4-octadecylpyrimidine-2,4-diamine
-
 Homo sapiens
N2-(2-dimethylaminoethyl)-6-methyl-N4-propylpyrimidine-2,4-diamine
-
 Homo sapiens
N2-(2-dimethylaminoethyl)-6-methyl-N4-tetradecylpyrimidine-2,4-diamine
-
 Homo sapiens
N2-(2-dimethylaminoethyl)-N4-decyl-6-methylpyrimidine-2,4-diamine
-
 Homo sapiens
N2-(2-dimethylaminoethyl)-N4-hexyl-6-methylpyrimidine-2,4-diamine
-
 Homo sapiens
N2-(2-dimethylaminoethyl)-N4-octyl-6-methylpyrimidine-2,4-diamine
-
 Homo sapiens
N2-benzyl-N4-(2-dimethylaminoethyl)-6-methylpyrimidine-2,4-diamine
-
 Homo sapiens
N2-butyl-N4-(2-dimethylaminoethyl)-6-methylpyrimidine-2,4-diamine
-
 Homo sapiens
N2-cyclohexyl-N4-(2-dimethylaminoethyl)-6-methylpyrimidine-2,4-diamine
-
 Homo sapiens
N2-cyclopropylmethyl-N4-(2-dimethylamin-ethyl)-6-methyl-N2-propylpyrimidine-2,4-diamine
-
 Homo sapiens
N2-decyl-N4-(2-dimethylaminoethyl)pyrimidine-2,4-diamine
-
 Homo sapiens
N2-dodecyl-N4-(2-dimethylaminoethyl)-pyrimidine-2,4-diamine
-
 Homo sapiens
N2-sec-butyl-N4-(2-dimethylaminoethyl)-6-methylpyrimidine-2,4-diamine
-
 Homo sapiens
N4-(2-dimethylaminoethyl)-6-methyl-N2-octadecylpyrimidine-2,4-diamine
-
 Homo sapiens
N4-(2-dimethylaminoethyl)-6-methyl-N2-propylpyrimidine-2,4-diamine
-
 Homo sapiens
N4-(2-dimethylaminoethyl)-6-methyl-N2-tetradecylpyrimidine-2,4-diamine
-
 Homo sapiens
N4-(2-dimethylaminoethyl)-N2-decyl-6-methylpyrimidine-2,4-diamine
-
 Homo sapiens
N4-(2-dimethylaminoethyl)-N2-hexyl-6-methylpyrimidine-2,4-diamine
-
 Homo sapiens
N4-(2-dimethylaminoethyl)-N2-octyl-6-methylpyrimidine-2,4-diamine
-
 Homo sapiens
N4-Benzyl-N2-(2-dimethylaminoethyl)-6-methylpyrimidine-2,4-diamine
-
 Homo sapiens
N4-butyl-N2-(2-dimethylaminoethyl)-6-methylpyrimidine-2,4-diamine
-
 Homo sapiens
N4-cyclohexyl-N2-(2-dimethylaminoethyl)-6-methylpyrimidine-2,4-diamine
-
 Homo sapiens
N4-cyclopropylmethyl-N2-(2-dimethylamin-ethyl)-6-methyl-N2-propylpyrimidine-2,4-diamine
-
 Homo sapiens
N4-decyl-N2-(2-dimethylaminoethyl)pyrimidine-2,4-diamine
-
 Homo sapiens
N4-dodecyl-N2-(2-dimethylaminoethyl)pyrimidine-2,4-diamine
-
 Homo sapiens
N4-sec-butyl-N2-(2-dimethylaminoethyl)-6-methylpyrimidine-2,4-diamine
-
 Homo sapiens
sec-butyl-(2-chloro-6-methylpyrimidin-4-yl)amine
-
 Homo sapiens
sec-butyl-(4-chloro-6-methylpyrimidin-2-yl)amine
-
 Homo sapiens
[2-(2-chloro-6-methylpyrimidin-4-ylamino)ethyl]carbamic acid tert-butyl ester
-
 Homo sapiens
[2-(4-chloro-6-methylpyrimidin-2-ylamino)ethyl]carbamic acid tert-butyl ester
-
 Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ required Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
GTP + H2O Homo sapiens
-
 GDP + phosphate
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens Q05193
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
GTP + H2O
-
 Homo sapiens GDP + phosphate
-
 ?

Synonyms

Synonyms Comment Organism
Dnm1
-
 Homo sapiens
dynamin
-
 Homo sapiens
dynamin I
-
 Homo sapiens
dynI GTPase
-
 Homo sapiens
large GTPase
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
additional information
-
 IC50 values, overview Homo sapiens additional information
0.264
-
 pH and temperature not specified in the publication Homo sapiens 2-chloro-4-(2-dimethylaminopropylamine)-6-methylpyrimidine
0.327
-
 pH and temperature not specified in the publication Homo sapiens N1-(4-chloro-6-methylpyrimidin-2-yl)-N3,N3-dimethylpropane-1,3-diamine

General Information

General Information Comment Organism
physiological function the large GTPase dynamin mediates membrane fission during clathrin-mediated endocytosis (CME) Homo sapiens