Binding Site Information of Target
Target General Information | Top | ||||
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Target ID | T84791 | Target Info | |||
Target Name | JUN activation domain binding protein (COPS5) | ||||
Synonyms | Signalosome subunit 5; SGN5; Jun activation domain-binding protein 1; JAB1; CSN5; COP9 signalosome complex subunit 5 | ||||
Target Type | Literature-reported Target | ||||
Gene Name | COPS5 | ||||
Biochemical Class | Peptidase | ||||
UniProt ID |
Drug Binding Sites of Target | Top | |||||
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Ligand Name: 2'-Chloro-6-[(5s,6s)-6-Hydroxy-6,7,8,9-Tetrahydro-5h-Imidazo[1,5-A]azepin-5-Yl][1,1'-Biphenyl]-3-Carbonitrile | Ligand Info | |||||
Structure Description | CRYSTAL STRUCTURE OF CSN5(2-257) IN COMPLEX WITH CNS5i-1b | PDB:5JOH | ||||
Method | X-ray diffraction | Resolution | 1.99 Å | Mutation | No | [1] |
PDB Sequence |
SGSGMAQKTW
13 ELANNMQEAQ23 SIDEIYKYDK33 KQQQEILAAK43 PWTKDHHYFK53 YCKISALALL 63 KMVMHARSGG73 NLEVMGLMLG83 KVDGETMIIM93 DSFALPVNAQ110 AAAYEYMAAY 120 IENAKQVGRL130 ENAIGWYHSH140 PGYGCWLSGI150 DVSTQMLNQQ160 FQEPFVAVVI 170 DPTRKVNLGA185 FRTYPKGYKP195 PDEGPSEYQT205 IPLNKIEDFG215 VHCKQYYALE 225 VSYFKSSLDR235 K
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Ligand Name: 1-[(3~{r})-3-(1~{h}-Benzimidazol-2-Yl)morpholin-4-Yl]-3-[2-(4-Methyl-2-Phenyl-Phenyl)-1~{h}-Pyrrolo[2,3-B]pyridin-3-Yl]propan-1-One | Ligand Info | |||||
Structure Description | COPS5(2-257) IN COMPLEX WITH A AZAINDOLE (COMPOUND 4) | PDB:5M5Q | ||||
Method | X-ray diffraction | Resolution | 2.20 Å | Mutation | No | [2] |
PDB Sequence |
SGSGMAQKTW
13 ELANNMQEAQ23 SIDEIYKYDK33 KQQQEILAAK43 PWTKDHHYFK53 YCKISALALL 63 KMVMHARSGG73 NLEVMGLMLG83 KVDGETMIIM93 DSFALPAQAA112 AYEYMAAYIE 122 NAKQVGRLEN132 AIGWYHSHPG142 YGCWLSGIDV152 STQMLNQQFQ162 EPFVAVVIDP 172 TRKVNLGAFR187 TYPKGYKPPD197 EGPSEYQTIP207 LNKIEDFGVH217 CKQYYALEVS 227 YFKSSLDRK
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Ligand Name: 3-(difluoromethyl)-N-(6-((5s,6s)-6-hydroxy-6,7,8,9-tetrahydro-5h-imidazo[1,5-a]azepin-5-yl)-[1,1'-biphenyl]-3-yl)-1-isopropyl-1h-pyrazole-5-carboxamide | Ligand Info | |||||
Structure Description | CRYSTAL STRUCTURE OF CSN5(2-257) IN COMPLEX WITH CNS5i-3 | PDB:5JOG | ||||
Method | X-ray diffraction | Resolution | 2.46 Å | Mutation | No | [1] |
PDB Sequence |
SGSGMAQKTW
13 ELANNMQEAQ23 SIDEIYKYDK33 KQQQEILAAK43 PWTKDHHYFK53 YCKISALALL 63 KMVMHARSGG73 NLEVMGLMLG83 KVDGETMIIM93 DSFALPVNAQ110 AAAYEYMAAY 120 IENAKQVGRL130 ENAIGWYHSH140 PGYGCWLSGI150 DVSTQMLNQQ160 FQEPFVAVVI 170 DPTRKVNLGA185 FRTYPKGYKP195 PDEGPSEYQT205 IPLNKIEDFG215 VHCKQYYALE 225 VSYFKSSLDR235 K
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Click to Show 3D Structure of This Binding Site
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References | Top | ||||
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REF 1 | Targeted inhibition of the COP9 signalosome for treatment of cancer. Nat Commun. 2016 Oct 24;7:13166. | ||||
REF 2 | Azaindoles as Zinc-Binding Small-Molecule Inhibitors of the JAMM Protease CSN5. Angew Chem Int Ed Engl. 2017 Jan 24;56(5):1294-1297. |
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