The Ligandable Human Proteome

Estrogen receptor

Nuclear hormone receptor, ligand-binding domain

Index	Ligand Name	Structure	PDB code	Compound Potency nM
1	ezt	Crystal structure of the ER alpha ligand binding domain with the agonist ortho-trifluoromethylphenylvinyl estradiol	2p15	0.05
2	des	HUMAN ESTROGEN RECEPTOR ALPHA LIGAND-BINDING DOMAIN IN COMPLEX WITH DIETHYLSTILBESTROL AND A GLUCOCORTICOID RECEPTOR INTERACTING PROTEIN 1 NR BOX II PEPTIDE	3erd	0.126
3	est	ESTROGEN RECEPTOR ALPHA LIGAND-BINDING DOMAIN COMPLEXED TO ESTRADIOL	1a52	0.138
4	oht	HUMAN ESTROGEN RECEPTOR ALPHA LIGAND-BINDING DOMAIN IN COMPLEX WITH 4-HYDROXYTAMOXIFEN	3ert	0.249
5	wst	Benzopyrans as Selective Estrogen Receptor b Agonists (SERBAs). Part 2: Structure Activity Relationship Studies on the Benzopyran Scaffold.	2pog	0.29
6	llc	Estrogen receptor alpha ligand-binding domain in complex with a SERM	2r6y	0.32
7	aiu	HUMAN ESTROGEN RECEPTOR ALPHA LIGAND-BINDING DOMAIN IN COMPLEX WITH COMPOUND 16	1xp6	0.4
8	llb	Estrogen receptor alpha ligand-binding domain complexed to a SERM	2r6w	0.44
9	aih	HUMAN ESTROGEN RECEPTOR ALPHA LIGAND-BINDING DOMAIN IN COMPLEX WITH COMPOUND 15	1xp1	0.5
10	l4g	A SERM Designed for the Treatment of Uterine Leiomyoma with Unique Tissue Specificity for Uterus and Ovaries in Rats	2ayr	0.51
11	e4d	Human Estrogen Receptor Alpha Ligand-binding Domain in Complex with the Antagonist Ligand 4-D	1sj0	0.8
12	est	MUTANT ESTROGEN NUCLEAR RECEPTOR LIGAND BINDING DOMAIN COMPLEXED WITH ESTRADIOL	1qkt	0.92
13	iok	Human estrogen receptor alpha ligand-binding domain in complex with compound 1D	2iok	1
14	aij	HUMAN ESTROGEN RECEPTOR ALPHA LIGAND-BINDING DOMAIN IN COMPLEX WITH COMPOUND 18	1xp9	1.3
15	est	The Estrogen Receptor Alpha Ligand Binding Domain D538G Mutant in Complex with Estradiol and a glucocorticoid receptor-interacting protein 1 NR box II peptide	4pxm	1.3
16	ait	HUMAN ESTROGEN RECEPTOR ALPHA LIGAND-BINDING DOMAIN IN COMPLEX WITH COMPOUND 19	1xpc	1.7
17	i0g	Benzopyrans are Selective Estrogen Receptor beta Agonists (SERBAs) with Novel Activity in Models of Benign Prostatic Hyperplasia	2i0j	2.68
18	85z	Oxyphenylpropenoic acids as Oral Selective Estrogen Receptor Down- Regulators.	5ak2	3.9
19	ral	HUMAN ESTROGEN RECEPTOR LIGAND-BINDING DOMAIN IN COMPLEX WITH RALOXIFENE	1err	7.7
20	iog	Human estrogen receptor alpha ligand-binding domain in complex with compound 11F	2iog	8
21	dc8	Estrogen receptor alpha ligand-binding domain complxed to a benzopyran ligand	2q70	8.3
22	gen	CRYSTAL STRUCTURE OF ESTROGEN RECEPTOR ALPHA COMPLEXED WITH GENISTEIN	1x7r	9
23	jj3	Estrogen receptor alpha ligand-binding domain in complex with a benzopyran agonist	2qe4	11
24	77w	ESTROGEN RECEPTOR ALPHA LIGAND BINDING DOMAIN IN COMPLEX WITH (2E)-3-{4-[(1R)-2-(4-fluorophenyl)-6-hydroxy-1-methy l-1,2,3,4- tetrahydroisoquinolin-1-yl]phenyl}prop-2-enoic acid	5t92	16
25	782	ESTROGEN RECEPTOR ALPHA LIGAND BINDING DOMAIN IN COMPLEX WITH (2E)-3-(4-{(1R)-6-hydroxy-1-methyl-2-[4-(propan-2 -yl)phenyl]-1,2,3,4- tetrahydroisoquinolin-1-yl}phenyl)prop-2-enoic acid	5t97	17
26	pti	The Structure of Estrogen Receptor in Complex with a Selective and Potent Tetrahydroisochiolin Ligand.	1uom	19
27	gqd	Selective estrogen receptor downregulator antagonists: Tetrahydroisoquinoline phenols 1.	5fqp	19
28	qhg	Selective estrogen receptor downregulator antagonists: Tetrahydroisoquinoline phenols 2.	5fqr	26
29	j0w	Selective estrogen receptor downregulator antagonists: Tetrahydroisoquinoline phenols 3.	5fqs	44
30	aej	X-ray structure of ERalpha LBD bound to a tetrahydroisoquinoline SERM ligand at 2.05A resolution	1xqc	63
31	17m	Human estrogen receptor alpha ligand-binding domain in complex with 17methyl-17alpha-dihydroequilenin and a glucoc interacting protein 1 NR box II peptide	2b1z	79
32	7qn	Selective estrogen receptor downregulator antagonists: Tetrahydroisoquinoline phenols 4.	5fqt	160
33	27j	Crystal structure of hERa-LBD (Y537S) in complex with alpha-zearalanol	4mg8	330
34	27h	Crystal structure of hERa-LBD (Y537S) in complex with ferutinine	4mg7	440
35	27m	Crystal structure of hERa-LBD (Y537S) in complex with benzophenone-2	4mgc	480
36	est	CRYSTAL STRUCTURE OF A WILD TYPE HER ALPHA LBD AT 2.9 ANGSTROM RESOLUTION	1g50	530
37	459	Human Estrogen Receptor Alpha Ligand-Binding Domain In Complex With OBCP-2M and A Glucocorticoid Receptor Interacting Protein 1 NR Box II Peptide	2fai	570
38	vqi	Selective estrogen receptor downregulator antagonists: Tetrahydroisoquinoline phenols 5.	5fqv	610
39	gen	Crystal Structure of the Estrogen Receptor Alpha Ligand Binding Domain Mutant 537S Complexed with Genistein	2qa8	990
40	27g	Crystal structure of hERa-LBD (Y537S) in complex with benzylbutylphtalate	4mg6	2420