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Literature summary for 1.17.4.4 extracted from
- Human VKORC1 mutations cause variable degrees of 4-hydroxycoumarin resistance and affect putative warfarin binding interfaces (2013), Blood, 122, 2743-2750 .
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| A26P | the IC50 ratio of wild-type to mutant enzyme is 49.6 | Homo sapiens |
| A26T | the IC50 ratio of wild-type to mutant enzyme is 3.0 | Homo sapiens |
| D36G | the IC50 ratio of wild-type to mutant enzyme is 3.2 | Homo sapiens |
| D36Y | the IC50 ratio of wild-type to mutant enzyme is 3.8 | Homo sapiens |
| G71A | the IC50 ratio of wild-type to mutant enzyme is 5.1 | Homo sapiens |
| H28Q | the IC50 ratio of wild-type to mutant enzyme is 2.9 | Homo sapiens |
| I123N | the IC50 ratio of wild-type to mutant enzyme is 8.5 | Homo sapiens |
| L128R | the IC50 ratio of wild-type to mutant enzyme is 49.7 | Homo sapiens |
| L27V | the IC50 ratio of wild-type to mutant enzyme is 2.5 | Homo sapiens |
| N77S | the IC50 ratio of wild-type to mutant enzyme is 5.3 | Homo sapiens |
| N77Y | the IC50 ratio of wild-type to mutant enzyme is 3.9 | Homo sapiens |
| R58G | the IC50 ratio of wild-type to mutant enzyme is 3.4 | Homo sapiens |
| S52L | the IC50 ratio of wild-type to mutant enzyme is 7.4 | Homo sapiens |
| S53W | the IC50 ratio of wild-type to mutant enzyme is 5.7 | Homo sapiens |
| S56F | the IC50 ratio of wild-type to mutant enzyme is 6.8 | Homo sapiens |
| V29L | the IC50 ratio of wild-type to mutant enzyme is 5.5 | Homo sapiens |
| V45A | the IC50 ratio of wild-type to mutant enzyme is 6.2 | Homo sapiens |
| V54L | the IC50 ratio of wild-type to mutant enzyme is 4.5 | Homo sapiens |
| V66G | the IC50 ratio of wild-type to mutant enzyme is 2.8 | Homo sapiens |
| V66M | the IC50 ratio of wild-type to mutant enzyme is 5.4 | Homo sapiens |
| W59C | the IC50 ratio of wild-type to mutant enzyme is 7.6 | Homo sapiens |
| W59L | the IC50 ratio of wild-type to mutant enzyme is 75.2 | Homo sapiens |
| W59R | the IC50 ratio of wild-type to mutant enzyme is 17.5 | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| warfarin | - |
Homo sapiens |  |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | Q9BQB6 | - |
- |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| VKORC1 | - |
Homo sapiens |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.0000247 | - |
wild-type enzyme, pH and temperature not specified in the publication | Homo sapiens | warfarin | |
| 0.000062 | - |
mutant enzyme L27V, pH and temperature not specified in the publication | Homo sapiens | warfarin | |
| 0.000069 | - |
mutant enzyme V66G, pH and temperature not specified in the publication | Homo sapiens | warfarin | |
| 0.000072 | - |
mutant enzyme H28Q, pH and temperature not specified in the publication | Homo sapiens | warfarin | |
| 0.000074 | - |
mutant enzyme A26T, pH and temperature not specified in the publication | Homo sapiens | warfarin | |
| 0.000078 | - |
mutant enzyme D36G, pH and temperature not specified in the publication | Homo sapiens | warfarin | |
| 0.000085 | - |
mutant enzyme R58G, pH and temperature not specified in the publication | Homo sapiens | warfarin | |
| 0.000093 | - |
mutant enzyme D36Y, pH and temperature not specified in the publication | Homo sapiens | warfarin | |
| 0.000096 | - |
mutant enzyme N77Y, pH and temperature not specified in the publication | Homo sapiens | warfarin | |
| 0.000112 | - |
mutant enzyme V54L, pH and temperature not specified in the publication | Homo sapiens | warfarin | |
| 0.000127 | - |
mutant enzyme G71A, pH and temperature not specified in the publication | Homo sapiens | warfarin | |
| 0.000131 | - |
mutant enzyme N77S, pH and temperature not specified in the publication | Homo sapiens | warfarin | |
| 0.000134 | - |
mutant enzyme V66M, pH and temperature not specified in the publication | Homo sapiens | warfarin | |
| 0.000136 | - |
mutant enzyme V29L, pH and temperature not specified in the publication | Homo sapiens | warfarin | |
| 0.00014 | - |
mutant enzyme S53W, pH and temperature not specified in the publication | Homo sapiens | warfarin | |
| 0.000152 | - |
mutant enzyme V45A, pH and temperature not specified in the publication | Homo sapiens | warfarin | |
| 0.000167 | - |
mutant enzyme S56F, pH and temperature not specified in the publication | Homo sapiens | warfarin | |
| 0.000182 | - |
mutant enzyme S52L, pH and temperature not specified in the publication | Homo sapiens | warfarin | |
| 0.000188 | - |
mutant enzyme W59C, pH and temperature not specified in the publication | Homo sapiens | warfarin | |
| 0.000209 | - |
mutant enzyme I123N, pH and temperature not specified in the publication | Homo sapiens | warfarin | |
| 0.000433 | - |
mutant enzyme W59R, pH and temperature not specified in the publication | Homo sapiens | warfarin | |
| 0.001224 | - |
mutant enzyme A26P, pH and temperature not specified in the publication | Homo sapiens | warfarin | |
| 0.001226 | - |
mutant enzyme L128R, pH and temperature not specified in the publication | Homo sapiens | warfarin | |
| 0.001858 | - |
mutant enzyme W59L, pH and temperature not specified in the publication | Homo sapiens | warfarin | |
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