Structure of PDB 5fqp Chain A

Receptor sequence

>5fqpA (length=242) Species: 9606 (Homo sapiens) [Search protein sequence]

ALSLTADQMVSALLDAEPPILYSEYDPTRPFSEASMMGLLTNLADRELVH
MINWAKRVPGFVDLTLHDQVHLLESAWLEILMIGLVWRSMEHPGKLLFAP
NLLLDRNQGKSVEGMVEIFDMLLATSSRFRMMNLQGEEFVCLKSIILLNS
GVYTFLSSTLKSLEEKDHIHRVLDKITDTLIHLMAKAGLTLQQQHQRLAQ
LLLILSHIRHMSNKGMEHLYSMKCKNVVPSYDLLLEMLDAHR

3D structure

PDB

5fqp Tetrahydroisoquinoline Phenols: Selective Estrogen Receptor Downregulator Antagonists with Oral Bioavailability in Rat.

Chain

Resolution

1.88 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	GQD	A	L346 T347 A350 E353 F404 L525 V533 V534	L40 T41 A44 E47 F98 L219 V227 V228	MOAD: ic50=19nM PDBbind-CN: -logKd/Ki=7.72,IC50=19nM BindingDB: IC50=1.3nM

External links

PDB	RCSB:5fqp, PDBe:5fqp, PDBj:5fqp
PDBsum	5fqp
PubMed	26819673
UniProt	P03372\|ESR1_HUMAN Estrogen receptor (Gene Name=ESR1)

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