Structure of PDB 4yax Chain A

Receptor sequence
>4yaxA (length=180) Species: 9606 (Homo sapiens) [Search protein sequence]
SPNEDWCAVCQNGGELLCCEKCPKVFHLSCHVPTLTNFPSGEWICTFCRD
LSKPEVEYDCDAPSKKKTEGLVKLTPIDKRKCERLLLFLYCHEMSLAFQD
PVPLTVPDYYKIIKNPMDLSTIKKRLQEDYSMYSKPEDFVADFRLIFQNC
AEFNEPDSEVANAGIKLENYFEELLKNLYP
3D structure
PDB4yax Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor.
ChainA
Resolution2.25 Å
3D
structure
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Enzymatic activity
Enzyme Commision number 2.3.2.27: RING-type E3 ubiquitin transferase.
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 4AE A L922 A923 V928 P929 V932 F979 N980 V986 L96 A97 V102 P103 V106 F153 N154 V160 MOAD: ic50=1.5uM
PDBbind-CN: -logKd/Ki=5.82,IC50=1.5uM
BindingDB: IC50=730nM
BS02 ZN A C841 C844 C870 C19 C22 C48
BS03 ZN A C829 C832 H849 C852 C7 C10 H27 C30
External links
PDB RCSB:4yax, PDBe:4yax, PDBj:4yax
PDBsum4yax
PubMed26061247
UniProtO15164|TIF1A_HUMAN Transcription intermediary factor 1-alpha (Gene Name=TRIM24)

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