Application | Comment | Organism |
---|---|---|
drug development | DNA polymerases are promising drug targets for the treatment of cancer | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(2E)-2-(3-nitro-4-[[6-(trifluoromethyl)pyridin-3-yl]sulfanyl]benzylidene)-5-thioxo-1,3-thiazolidin-4-one | - |
Homo sapiens | |
(2E)-2-(4-chloro-3-ethylbenzylidene)-5-thioxo-1,3-thiazolidin-4-one | - |
Homo sapiens | |
(2E)-2-(pentafluorobenzylidene)-5-thioxodihydrothiophen-3(2H)-one | - |
Homo sapiens | |
(2E)-2-[4-(2-hydroxyethyl)-3-nitrobenzylidene]-5-thioxo-1,3-thiazolidin-4-one | - |
Homo sapiens | |
(5Z)-5-(4-chloro-3-nitrobenzylidene)-2-thioxo-1,3-thiazolidin-4-one | - |
Homo sapiens | |
(5Z)-5-[3-bromo-4-[(4-fluorobenzyl)oxy]benzylidene]-1,3-thiazolidine-2,4-dione | - |
Homo sapiens | |
(5Z)-5-[3-bromo-4-[(4-fluorophenyl)sulfanyl]benzylidene]-2-thioxo-1,3-thiazolidin-4-one | - |
Homo sapiens | |
(5Z)-5-[3-nitro-4-(pyridin-3-ylsulfanyl)benzylidene]-2-thioxo-1,3-thiazolidin-4-one | - |
Homo sapiens | |
(5Z)-5-[4-(4-methylphenoxy)-3-nitrobenzylidene]-2-thioxo-1,3-thiazolidin-4-one | - |
Homo sapiens | |
(5Z)-5-[4-(cyclohexylsulfanyl)-3-nitrobenzylidene]-2-thioxo-1,3-thiazolidin-4-one | - |
Homo sapiens | |
(5Z)-5-[4-[(4-bromophenyl)sulfanyl]-3-nitrobenzylidene]-2-thioxo-1,3-thiazolidin-4-one | - |
Homo sapiens | |
(5Z)-5-[4-[(4-chlorophenyl)sulfanyl]-3-nitrobenzylidene]-2-thioxo-1,3-thiazolidin-4-one | - |
Homo sapiens | |
(5Z)-5-[4-[(4-fluorobenzyl)oxy]-3-nitrobenzylidene]-2-thioxo-1,3-thiazolidin-4-one | - |
Homo sapiens | |
(5Z)-5-[4-[(4-fluorobenzyl)oxy]benzylidene]-2-thioxo-1,3-thiazolidin-4-one | - |
Homo sapiens | |
(5Z)-5-[4-[(4-methylphenyl)sulfanyl]-3-nitrobenzylidene]-3-(prop-2-en-1-yl)-2-thioxo-1,3-thiazolidin-4-one | - |
Homo sapiens | |
2-methoxy-4-[(Z)-(4-oxo-2-thioxo-1,3-thiazolidin-5-ylidene)methyl]phenyl 2,4-dichlorobenzoate | - |
Homo sapiens | |
2-methoxy-4-[(Z)-(4-oxo-2-thioxo-1,3-thiazolidin-5-ylidene)methyl]phenyl 3-bromobenzoate | - |
Homo sapiens | |
4-chlorophenyl 2,4-dinitrophenyl sulfide | - |
Homo sapiens | |
4-[(4-methylphenyl)sulfanyl]-3-nitrobenzaldehyde | - |
Homo sapiens | |
4-[(Z)-(2,4-dioxo-1,3-thiazolidin-5-ylidene)methyl]-2-methoxyphenyl 3-bromobenzoate | - |
Homo sapiens | |
4-[(Z)-(4-oxo-2-thioxo-1,3-thiazolidin-5-ylidene)methyl]phenyl 2-chlorobenzoate | - |
Homo sapiens | |
5-(5-nitro-2-[[6-(trifluoromethyl)pyridin-3-yl]sulfanyl]benzylidene)-2-thioxo-1,3-thiazolidin-4-one | - |
Homo sapiens | |
5-[2-(cyclohexylsulfanyl)-5-nitrobenzylidene]-2-thioxo-1,3-thiazolidin-4-one | - |
Homo sapiens | |
5-[2-[(4-chlorophenyl)sulfanyl]-5-nitrobenzylidene]-2-thioxo-1,3-thiazolidin-4-one | - |
Homo sapiens | |
5-[2-[(4-methylphenyl)sulfanyl]-5-nitrobenzylidene]-2-thioxo-1,3-thiazolidin-4-one | - |
Homo sapiens | |
epigallocatechin gallate | - |
Homo sapiens | |
rhodanines | most potent inhibitors for DNA Pol lambda, they are up to 10times less active against the highly similar DNA polymerase beta, structure-activity relationships, overview. 5-Arylidene-2,4-thiazolidinediones are class I rhodanines, rhodanine class II has members of carbohydrazides, and class III contains a common 2,4-pentadione substructure element | Homo sapiens | |
[3-[(Z)-(4-oxo-2-thioxo-1,3-thiazolidin-5-ylidene)methyl]phenoxy]acetic acid | - |
Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
deoxynucleoside triphosphate + DNAn | Homo sapiens | - |
diphosphate + DNAn+1 | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
deoxynucleoside triphosphate + DNAn | - |
Homo sapiens | diphosphate + DNAn+1 | - |
? |
Synonyms | Comment | Organism |
---|---|---|
DNA Pol lambda | - |
Homo sapiens |
DNA polymerase lambda | - |
Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0038 | - |
pH and temperature not specified in the publication | Homo sapiens | epigallocatechin gallate | |
0.0059 | - |
pH and temperature not specified in the publication, inhibition of DNA Pol lambda | Homo sapiens | (5Z)-5-[4-[(4-fluorobenzyl)oxy]benzylidene]-2-thioxo-1,3-thiazolidin-4-one | |
0.0081 | - |
pH and temperature not specified in the publication, inhibition of DNA Pol lambda | Homo sapiens | 5-[2-[(4-chlorophenyl)sulfanyl]-5-nitrobenzylidene]-2-thioxo-1,3-thiazolidin-4-one | |
0.0083 | - |
pH and temperature not specified in the publication, inhibition of DNA Pol lambda | Homo sapiens | (5Z)-5-[3-bromo-4-[(4-fluorophenyl)sulfanyl]benzylidene]-2-thioxo-1,3-thiazolidin-4-one | |
0.0093 | - |
pH and temperature not specified in the publication, inhibition of DNA Pol lambda | Homo sapiens | (5Z)-5-[4-(4-methylphenoxy)-3-nitrobenzylidene]-2-thioxo-1,3-thiazolidin-4-one | |
0.01 | - |
pH and temperature not specified in the publication, inhibition of DNA Pol lambda | Homo sapiens | 5-[2-[(4-methylphenyl)sulfanyl]-5-nitrobenzylidene]-2-thioxo-1,3-thiazolidin-4-one | |
0.011 | - |
pH and temperature not specified in the publication, inhibition of DNA Pol lambda | Homo sapiens | (2E)-2-(3-nitro-4-[[6-(trifluoromethyl)pyridin-3-yl]sulfanyl]benzylidene)-5-thioxo-1,3-thiazolidin-4-one | |
0.0124 | - |
pH and temperature not specified in the publication, inhibition of DNA Pol lambda | Homo sapiens | 4-[(Z)-(4-oxo-2-thioxo-1,3-thiazolidin-5-ylidene)methyl]phenyl 2-chlorobenzoate | |
0.0429 | - |
pH and temperature not specified in the publication, inhibition of DNA Pol beta | Homo sapiens | 5-[2-[(4-chlorophenyl)sulfanyl]-5-nitrobenzylidene]-2-thioxo-1,3-thiazolidin-4-one | |
0.0455 | - |
pH and temperature not specified in the publication, inhibition of DNA Pol beta | Homo sapiens | 5-[2-[(4-methylphenyl)sulfanyl]-5-nitrobenzylidene]-2-thioxo-1,3-thiazolidin-4-one | |
0.0644 | - |
pH and temperature not specified in the publication, inhibition of DNA Pol beta | Homo sapiens | (5Z)-5-[4-[(4-fluorobenzyl)oxy]benzylidene]-2-thioxo-1,3-thiazolidin-4-one | |
0.08 | - |
pH and temperature not specified in the publication, inhibition of DNA Pol beta | Homo sapiens | (5Z)-5-[3-bromo-4-[(4-fluorophenyl)sulfanyl]benzylidene]-2-thioxo-1,3-thiazolidin-4-one | |
0.0888 | - |
pH and temperature not specified in the publication, inhibition of DNA Pol beta | Homo sapiens | 4-[(Z)-(4-oxo-2-thioxo-1,3-thiazolidin-5-ylidene)methyl]phenyl 2-chlorobenzoate | |
0.1 | - |
above, pH and temperature not specified in the publication, inhibition of DNA Pol beta | Homo sapiens | (2E)-2-(3-nitro-4-[[6-(trifluoromethyl)pyridin-3-yl]sulfanyl]benzylidene)-5-thioxo-1,3-thiazolidin-4-one | |
0.1 | - |
above, pH and temperature not specified in the publication, inhibition of DNA Pol beta | Homo sapiens | (5Z)-5-[4-(4-methylphenoxy)-3-nitrobenzylidene]-2-thioxo-1,3-thiazolidin-4-one |
General Information | Comment | Organism |
---|---|---|
evolution | human DNA polymerase lambda is a member of the DNA polymerase X family | Homo sapiens |
metabolism | high levels of DNA polymerases of the X family might cause genomic instability | Homo sapiens |
physiological function | DNA Pol lambda has a backup role for DNA Pol beta in base-excision repair | Homo sapiens |