Binding Site Information of Target
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T46000 | Target Info | |||
| Target Name | MEK kinase kinase 3 (MAP4K3) | ||||
| Synonyms | RAB8IPL1; Mitogen-activated protein kinase kinase kinase kinase 3; MEKKK 3; MAPK/ERK kinase kinase kinase 3; Germinal center kinase-related protein kinase; GLK | ||||
| Target Type | Literature-reported Target | ||||
| Gene Name | MAP4K3 | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| Ligand Name: Phosphonothreonine | Ligand Info | |||||
| Structure Description | GLK co-crystal structure with aminopyrrolopyrimidine inhibitor | PDB:5J5T | ||||
| Method | X-ray diffraction | Resolution | 2.85 Å | Mutation | Yes | [1] |
| PDB Sequence |
SQEDFELIQR
21 IGSGTYGDVY31 KARNVNTGEL41 AAIKVIKLEP51 GEDFAVVQQE61 IIMMKDCKHP 71 NIVAYFGSYL81 RRDKLWICME91 FCGGGSLQDI101 YHVTGPLSEL111 QIAYVSRETL 121 QGLYYLHSKG131 KMHRDIKGAN141 ILLDNGHVKL152 ADFGVSAQIT162 ATIAAFIGTP 175 YWMAPEVAAV185 ERKGGYNQLC195 DLWAVGITAI205 ELAELQPPMF215 DLHPMRALFL 225 MTKSNFQPPK235 LKDKMKWSNS245 FHHFVKMALT255 KNPKKRPTAE265 KLLQHPFVTQ 275 HLTRSLAIEL285 LDKVNNPSTY297 HDFDDDDPEP307 LVAVPHR
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| Ligand Name: 5-[2-(Piperidin-4-Yl)-1,3-Thiazol-5-Yl]-3-[(Pyridin-4-Yl)methoxy]pyridin-2-Amine | Ligand Info | |||||
| Structure Description | GLK co-crystal structure with aminopyrrolopyrimidine inhibitor | PDB:5J5T | ||||
| Method | X-ray diffraction | Resolution | 2.85 Å | Mutation | Yes | [1] |
| PDB Sequence |
SQEDFELIQR
21 IGSGTYGDVY31 KARNVNTGEL41 AAIKVIKLEP51 GEDFAVVQQE61 IIMMKDCKHP 71 NIVAYFGSYL81 RRDKLWICME91 FCGGGSLQDI101 YHVTGPLSEL111 QIAYVSRETL 121 QGLYYLHSKG131 KMHRDIKGAN141 ILLDNGHVKL152 ADFGVSAQIT162 ATIAAFIGTP 175 YWMAPEVAAV185 ERKGGYNQLC195 DLWAVGITAI205 ELAELQPPMF215 DLHPMRALFL 225 MTKSNFQPPK235 LKDKMKWSNS245 FHHFVKMALT255 KNPKKRPTAE265 KLLQHPFVTQ 275 HLTRSLAIEL285 LDKVNNPSTY297 HDFDDDDPEP307 LVAVPHR
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| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Germinal-center kinase-like kinase co-crystal structure reveals a swapped activation loop and C-terminal extension. Protein Sci. 2017 Feb;26(2):152-162. | ||||
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