PDB 5ls6

PDB Links
Overview

PDB Information

PDB	5LS6
Method	X-RAY DIFFRACTION
Host Organism	Escherichia coli K-12
Gene Source	Homo sapiens
Primary Citation	Identification of (R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide (CPI-1205), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, Suitable for Phase I Clinical Trials for B-Cell Lymphomas. Vaswani, R.G., Gehling, V.S., Dakin, L.A., Cook, A.S., Nasveschuk, C.G., Duplessis, M., Iyer, P., Balasubramanian, S., Zhao, F., Good, A.C., Campbell, R., Lee, C., Cantone, N., Cummings, R.T., Normant, E., Bellon, S.F., Albrecht, B.K., Harmange, J.C., Trojer, P., Audia, J.E., Zhang, Y., Justin, N., Chen, S., Wilson, J.R., Gamblin, S.J. J. Med. Chem.
Header	Transferase/Inhibitor
Released	2016-08-22
Resolution	3.470
CATH Insert Date	07 May, 2017

PDB Images (25)

5ls6

PDB 5ls6

5ls6A

PDB Chain 5ls6A

5ls6B

PDB Chain 5ls6B

5ls6C

PDB Chain 5ls6C

5ls6D

PDB Chain 5ls6D

5ls6E

PDB Chain 5ls6E

5ls6F

PDB Chain 5ls6F

5ls6G

PDB Chain 5ls6G

5ls6H

PDB Chain 5ls6H

5ls6I

PDB Chain 5ls6I

5ls6J

PDB Chain 5ls6J

5ls6K

PDB Chain 5ls6K

5ls6L

PDB Chain 5ls6L

5ls6Q

PDB Chain 5ls6Q

5ls6R

PDB Chain 5ls6R

5ls6S

PDB Chain 5ls6S

5ls6T

PDB Chain 5ls6T

5ls6B00

CATH Domain 5ls6B00

5ls6C01

CATH Domain 5ls6C01

5ls6E00

CATH Domain 5ls6E00

5ls6F01

CATH Domain 5ls6F01

5ls6H00

CATH Domain 5ls6H00

5ls6I01

CATH Domain 5ls6I01

5ls6K00

CATH Domain 5ls6K00

5ls6L01

CATH Domain 5ls6L01

PDB Prints

PDB Chains (16)

Chain ID	Date inserted into CATH	CATH Status
A	08 May, 2017	Holding pen
B	08 May, 2017	Chopped
C	08 May, 2017	Chopped
D	08 May, 2017	Holding pen
E	08 May, 2017	Chopped
F	08 May, 2017	Chopped
G	08 May, 2017	Holding pen
H	08 May, 2017	Chopped
I	08 May, 2017	Chopped
J	08 May, 2017	Holding pen
K	08 May, 2017	Chopped
L	08 May, 2017	Chopped
Q	08 May, 2017	Rejected
R	08 May, 2017	Rejected
S	08 May, 2017	Rejected
T	08 May, 2017	Rejected

CATH Domains (8)

Domain ID	Date inserted into CATH	Superfamily	CATH Status
5ls6B00	14 Dec, 2017	2.130.10.10	Assigned
5ls6C01	11 Jan, 2018		Holding pen
5ls6E00	14 Dec, 2017	2.130.10.10	Assigned
5ls6F01	11 Jan, 2018		Holding pen
5ls6H00	14 Dec, 2017	2.130.10.10	Assigned
5ls6I01	11 Jan, 2018		Holding pen
5ls6K00	14 Dec, 2017	2.130.10.10	Assigned
5ls6L01	11 Jan, 2018		Holding pen

UniProtKB Entries (12)

Accession	Gene ID	Taxon	Description
Q92833	JARD2_HUMAN	Homo sapiens	Protein Jumonji
Q92833	JARD2_HUMAN	Homo sapiens	Protein Jumonji
Q15910	EZH2_HUMAN	Homo sapiens	Histone-lysine N-methyltransferase EZH2
Q92833	JARD2_HUMAN	Homo sapiens	Protein Jumonji
Q92833	JARD2_HUMAN	Homo sapiens	Protein Jumonji
O75530	EED_HUMAN	Homo sapiens	Polycomb protein EED
Q15910	EZH2_HUMAN	Homo sapiens	Histone-lysine N-methyltransferase EZH2
Q15910	EZH2_HUMAN	Homo sapiens	Histone-lysine N-methyltransferase EZH2
O75530	EED_HUMAN	Homo sapiens	Polycomb protein EED
O75530	EED_HUMAN	Homo sapiens	Polycomb protein EED
O75530	EED_HUMAN	Homo sapiens	Polycomb protein EED
Q15910	EZH2_HUMAN	Homo sapiens	Histone-lysine N-methyltransferase EZH2