Crystallization (Comment) | Organism |
---|---|
in complex with inhibitors 6-(2,6-dibromophenyl)pyrido[2,3-d]pyrimidine-2,7-diamine and 6-(2,6-methoxyphenyl)pyrido[2,3-d]pyrimidine-2,7-diamine | Escherichia coli |
Protein Variants | Comment | Organism |
---|---|---|
H438P | decrease in sensitivity to inhibitors 6-(2,6-dibromophenyl)pyrido[2,3-d]pyrimidine-2,7-diamine and 6-(2,6-methoxyphenyl)pyrido[2,3-d]pyrimidine-2,7-diamine | Escherichia coli |
I437T | decrease in sensitivity to inhibitors 6-(2,6-dibromophenyl)pyrido[2,3-d]pyrimidine-2,7-diamine and 6-(2,6-methoxyphenyl)pyrido[2,3-d]pyrimidine-2,7-diamine | Escherichia coli |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
6-(2,6-dibromophenyl)pyrido[2,3-d]pyrimidine-2,7-diamine | targets the ATP-binding site of biotin carboxylase. Biophysics of binding, crystallization data. Effective in vivo and in vitro, selective for bacterial biotin carboxylase. Pharmacological studies in rat and mouse | Escherichia coli | |
6-(2,6-dimethoxyphenyl)pyrido[2,3-d]pyrimidine-2,7-diamine | targets the ATP-binding site of biotin carboxylase. Biophysics of binding, crystallization data. Effective in vivo and in vitro, selective for bacterial biotin carboxylase. Pharmacological studies in rat and mouse | Escherichia coli |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Escherichia coli | P24182 | - |
- |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.000005 | - |
or below, wild-type | Escherichia coli | 6-(2,6-dibromophenyl)pyrido[2,3-d]pyrimidine-2,7-diamine | |
0.000028 | - |
wild-type | Escherichia coli | 6-(2,6-dimethoxyphenyl)pyrido[2,3-d]pyrimidine-2,7-diamine | |
0.00016 | - |
mutant H438P | Escherichia coli | 6-(2,6-dibromophenyl)pyrido[2,3-d]pyrimidine-2,7-diamine | |
0.00056 | - |
mutant I437T | Escherichia coli | 6-(2,6-dibromophenyl)pyrido[2,3-d]pyrimidine-2,7-diamine | |
0.0012 | - |
wild-type | Escherichia coli | 6-(2,6-dimethoxyphenyl)pyrido[2,3-d]pyrimidine-2,7-diamine | |
0.0073 | - |
wild-type | Escherichia coli | 6-(2,6-dimethoxyphenyl)pyrido[2,3-d]pyrimidine-2,7-diamine |