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 | Comment | Organism | Structure |
---|---|---|---|
Mg2+ | required | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
GTP + H2O | Homo sapiens | - |
GDP + phosphate | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | Q05193 | - |
- |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
GTP + H2O | - |
Homo sapiens | GDP + phosphate | - |
? |
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 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 | Comment | Organism |
---|---|---|
physiological function | the large GTPase dynamin mediates membrane fission during clathrin-mediated endocytosis (CME) | Homo sapiens |