Cloned (Comment) | Organism |
---|---|
expression in Escherichia coli as C-terminal His-tagged protein | Homo sapiens |
Protein Variants | Comment | Organism |
---|---|---|
A133D | substantially reduced sensitivity to ispinesib and other quinazoline Eg5 inhibitors | Homo sapiens |
A356T | substantially reduced sensitivity to ispinesib and other quinazoline Eg5 inhibitors | Homo sapiens |
D130V | substantially reduced sensitivity to ispinesib and other quinazoline Eg5 inhibitors | Homo sapiens |
I299F | substantially reduced sensitivity to ispinesib and other quinazoline Eg5 inhibitors | Homo sapiens |
additional information | mutant KHC-L5, loop L5 replaced by that of kinesin heavy chain. Substantially reduced sensitivity to ispinesib and other quinazoline Eg5 inhibitors | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
6-[4-(trifluoromethyl)phenyl]-3,4-dihydroquinolin-2(1H)-one | - |
Homo sapiens | |
docetaxel | - |
Homo sapiens | |
SB-731489 | - |
Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
isoform Eg5 | - |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.0000017 | - |
6-[4-(trifluoromethyl)phenyl]-3,4-dihydroquinolin-2(1H)-one | wild-type, pH 6.8 | Homo sapiens | |
0.000066 | - |
6-[4-(trifluoromethyl)phenyl]-3,4-dihydroquinolin-2(1H)-one | mutant I299F, pH 6.8 | Homo sapiens | |
0.000109 | - |
6-[4-(trifluoromethyl)phenyl]-3,4-dihydroquinolin-2(1H)-one | mutant A356T, pH 6.8 | Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.00000023 | - |
mutant D130V, pH 6.8 | Homo sapiens | docetaxel | |
0.0000003 | - |
wild-type, pH 6.8 | Homo sapiens | docetaxel | |
0.00000045 | - |
mutant D130V, pH 6.8 | Homo sapiens | 6-[4-(trifluoromethyl)phenyl]-3,4-dihydroquinolin-2(1H)-one | |
0.00000046 | - |
wild-type, pH 6.8 | Homo sapiens | SB-731489 | |
0.000036 | - |
wild-type, pH 6.8 | Homo sapiens | 6-[4-(trifluoromethyl)phenyl]-3,4-dihydroquinolin-2(1H)-one | |
0.000903 | - |
mutant D130V, pH 6.8 | Homo sapiens | SB-731489 |