Structure of PDB 5fp3 Chain A

Receptor sequence
>5fp3A (length=435) Species: 9606 (Homo sapiens) [Search protein sequence]
PREKLNPPTPSIYLESKRDAFSPVLLQFCTDPRNPITVIRGLAGSLRLNL
GLFSTKTLVEASGEHTVEVRTQVQQPSDENWDLTGTRQIWPCESSRSHTT
IAKYAQYQASSFQESLPKNHHIIKFGTNIDLSDAKRWKPQLQELLKLPAF
MRVTSTGNMLSHVGHTILGMNTVQLYMKVPGSRTPGHQENNNFCSVNINI
GPGDCEWFAVHEHYWETISAFCDRHGVDYLTGSWWPILDDLYASNIPVYR
FVQRPGDLVWINAGTVHWVQATGWCNNIAWNVGPLTAYQYQLALERYEWN
EVKNVKSIVPMIHVSWNVARTVKISDPDLFKMIKFCLLQSMKHCQVQRES
LVRAGKKIAYQGRVKDEPAYYCNECDVEVFNILFVTSENGSRNTYLVHCE
GCARRRSAGLQGVVVLEQYRTEELAQAYDAFTLAP
3D structure
PDB5fp3 Cell Penetrant Inhibitors of the Kdm4 and Kdm5 Families of Histone Lysine Demethylases. 1. 3-Amino-4-Pyridine Carboxylate Derivatives.
ChainA
Resolution2.05 Å
3D
structure
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Enzymatic activity
Enzyme Commision number 1.14.11.68: [histone H3]-trimethyl-L-lysine(27) demethylase.
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 YC8 A R1246 F1328 T1330 Y1379 K1381 T1387 P1388 H1390 N1400 W1410 H1470 R70 F125 T127 Y176 K178 T184 P185 H187 N197 W207 H267 MOAD: ic50=1.259uM
BindingDB: IC50=1259nM
BS02 ZN A C1575 C1578 C1602 C1605 C372 C375 C399 C402
BS03 CO A H1390 E1392 H1470 H187 E189 H267
External links
PDB RCSB:5fp3, PDBe:5fp3, PDBj:5fp3
PDBsum5fp3
PubMed26771107
UniProtO15054|KDM6B_HUMAN Lysine-specific demethylase 6B (Gene Name=KDM6B)

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