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Ligands
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JSW [(5~{S})-5-[3,5-bis(fluoranyl)phenyl]pyrazolidin-1-yl]-[1-(5-methyl-1,3,4-oxadiazol-2-yl)piperidin-4-yl]methanone
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Code : 6R5F   PDBj   RCSB PDB   PDBe
Header : TRANSFERASE
Title : Crystal structure of RIP1 kinase in complex with DHP77
Release Data : 2019-05-01
Compound :
mol_id molecule chains synonym
1 Receptor-interacting serine/threonine-protein kinase 1 A,B,C,D Cell death protein RIP,Receptor-interacting protein 1,RIP-1,Serine/threonine-protein kinase RIP
ec: 2.7.11.1
Source :
mol_id organism_scientific organism_common expression_system
1 Homo sapiens  (taxid:9606) Human Baculovirus expression vector pFastBac1-HM  (taxid:274590)
gene: RIPK1, RIP, RIP1
Authors : Thorpe, J.H., Campobasso, N., Harris, P.A.
Keywords : Inhibitor, Complex, TRANSFERASE
Exp. method : X-RAY DIFFRACTION ( 3.25 Å )
Citation :

Discovery and Lead-Optimization of 4,5-Dihydropyrazoles as Mono-Kinase Selective, Orally Bioavailable and Efficacious Inhibitors of Receptor Interacting Protein 1 (RIP1) Kinase.

Harris, P.A.,Faucher, N.,George, N.  et al.
(2019)  J.Med.Chem.  62 : 5096 - 5110

PubMed: 31013427
DOI: 10.1021/acs.jmedchem.9b00318

Chain : A, B, C, D
UniProt : Q13546 (RIPK1_HUMAN)
Reaction: EC: Evidence:
Physiological Direction:
ATP + L-seryl-[protein] = ADP + H(+) + O-phospho-L-seryl- [protein] 2.7.11.1 PubMed:23473668, PubMed:30988283, PubMed:31827280, PubMed:8612133
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ATP + L-threonyl-[protein] = ADP + H(+) + O-phospho-L- threonyl-[protein] 2.7.11.1 PubMed:23473668, PubMed:30988283, PubMed:31827280, PubMed:8612133
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