2hk5
From Proteopedia
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|SITE= | |SITE= | ||
|LIGAND= <scene name='pdbligand=1BM:3-{[2-(1H-BENZIMIDAZOL-1-YL)-6-{[2-(DIETHYLAMINO)ETHYL]AMINO}PYRIMIDIN-4-YL]AMINO}-4-METHYLPHENOL'>1BM</scene> | |LIGAND= <scene name='pdbligand=1BM:3-{[2-(1H-BENZIMIDAZOL-1-YL)-6-{[2-(DIETHYLAMINO)ETHYL]AMINO}PYRIMIDIN-4-YL]AMINO}-4-METHYLPHENOL'>1BM</scene> | ||
| - | |ACTIVITY= [http://en.wikipedia.org/wiki/Non-specific_protein-tyrosine_kinase Non-specific protein-tyrosine kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.10.2 2.7.10.2] | + | |ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Non-specific_protein-tyrosine_kinase Non-specific protein-tyrosine kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.10.2 2.7.10.2] </span> |
|GENE= HCK ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]) | |GENE= HCK ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]) | ||
| + | |DOMAIN= | ||
| + | |RELATEDENTRY= | ||
| + | |RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2hk5 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2hk5 OCA], [http://www.ebi.ac.uk/pdbsum/2hk5 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2hk5 RCSB]</span> | ||
}} | }} | ||
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[[Category: Sabat, M P.]] | [[Category: Sabat, M P.]] | ||
[[Category: Walter, R L.]] | [[Category: Walter, R L.]] | ||
| - | [[Category: 1BM]] | ||
[[Category: hck]] | [[Category: hck]] | ||
[[Category: kinase domain]] | [[Category: kinase domain]] | ||
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[[Category: transferase]] | [[Category: transferase]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 03:31:29 2008'' |
Revision as of 00:31, 31 March 2008
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| , resolution 2.0Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | |||||||
| Gene: | HCK (Homo sapiens) | ||||||
| Activity: | Non-specific protein-tyrosine kinase, with EC number 2.7.10.2 | ||||||
| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
Hck Kinase in Complex with Lck targetted Inhibitor PG-1009247
Overview
This communication details the synthesis, biological activity, and binding mode of a novel class of 2-benzimidazole substituted pyrimidines. The most potent analogs disclosed showed low nanomolar activity for the inhibition of Lck kinase and a representative analog was co-crystallized with Hck (a structurally related member of the Src family kinases).
About this Structure
2HK5 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
Reference
The development of 2-benzimidazole substituted pyrimidine based inhibitors of lymphocyte specific kinase (Lck)., Sabat M, VanRens JC, Laufersweiler MJ, Brugel TA, Maier J, Golebiowski A, De B, Easwaran V, Hsieh LC, Walter RL, Mekel MJ, Evdokimov A, Janusz MJ, Bioorg Med Chem Lett. 2006 Dec 1;16(23):5973-7. Epub 2006 Sep 25. PMID:16997556
Page seeded by OCA on Mon Mar 31 03:31:29 2008
