Structure of PDB 6dl2 Chain A

Receptor sequence

>6dl2A (length=128) Species: 9606 (Homo sapiens) [Search protein sequence]

SNANPPPPETSNPNKPKRQTNQLQYLLRVVLKTLWKHQFAWPFQQPVDAV
KLNLPDYYKIIKTPMDMGTIKKRLENNYYWNAQECIQDFNTMFTNCYIYN
KPGDDIVLMAEALEKLFLQKINELPTEE

3D structure

PDB

6dl2 Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression.

Chain

Resolution

1.47 Å

3D
structure

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Enzymatic activity

Enzyme Commision number

Interaction with ligand

Site #	Ligand	Ligand chain	Binding residues on receptor (original residue number in PDB)	Binding residues on receptor (residue number reindexed from 1)	Binding affinity
BS01	GUJ	A	W81 P82 V87 L92 N140 I146 M149	W41 P42 V47 L52 N100 I106 M109	MOAD: Ki=33nM PDBbind-CN: -logKd/Ki=7.48,Ki=33nM BindingDB: IC50=100nM,Ki=33nM

External links

PDB	RCSB:6dl2, PDBe:6dl2, PDBj:6dl2
PDBsum	6dl2
PubMed	30019901
UniProt	O60885\|BRD4_HUMAN Bromodomain-containing protein 4 (Gene Name=BRD4)

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