ChEMBL ligand: CHEMBL1358 (Faslodex, Fulvestrant, ICI 182,780, ICI-182780, NSC-759879, ZD9238, ZD-9238)
Bacterial beta-lactamase TEM in Bacteria [ChEMBL: CHEMBL2364670] [UniProtKB: P62593] There should be some charts here, you may need to enable JavaScript!
Farnesoid X receptor/Bile acid receptor FXR in Human [ChEMBL: CHEMBL2047] [GtoPdb: 603] [UniProtKB: Q96RI1] There should be some charts here, you may need to enable JavaScript!
epoxide hydrolase 2/Epoxide hydratase in Human [ChEMBL: CHEMBL2409] [GtoPdb: 2970] [UniProtKB: P34913] There should be some charts here, you may need to enable JavaScript!
Estrogen receptor-α/Estrogen receptor alpha in Human [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372] Estrogen receptor-α/Estrogen receptor alpha in Rat [ChEMBL: CHEMBL2724] [GtoPdb: 620] [UniProtKB: P06211] There should be some charts here, you may need to enable JavaScript!
Estrogen receptor-β/Estrogen receptor beta in Human [ChEMBL: CHEMBL242] [GtoPdb: 621] [UniProtKB: Q92731] There should be some charts here, you may need to enable JavaScript!
Estrogen-related receptor-α/Estrogen-related receptor alpha in Human [ChEMBL: CHEMBL3429] [GtoPdb: 622] [UniProtKB: P11474] There should be some charts here, you may need to enable JavaScript!
sirtuin 5/NAD-dependent protein deacylase sirtuin-5, mitochondrial in Human [ChEMBL: CHEMBL2163183] [GtoPdb: 2711] [UniProtKB: Q9NXA8] There should be some charts here, you may need to enable JavaScript!
Pregnane X receptor in Human [ChEMBL: CHEMBL3401] [GtoPdb: 606] [UniProtKB: O75469] There should be some charts here, you may need to enable JavaScript!
Progesterone receptor in Human [ChEMBL: CHEMBL208] [GtoPdb: 627] [UniProtKB: P06401] There should be some charts here, you may need to enable JavaScript!
GPER in Human [GtoPdb: 221] [UniProtKB: Q99527] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
Bacterial beta-lactamase TEM in Bacteria (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2364670] [UniProtKB: P62593]
ChEMBL	Inhibition of bacterial wild type Beta-lactamase TEM-1 pre-incubated for 5 mins before addition of chromogenic beta-lactamase substrate CENTA by spectrophotometry	B	4.25	pIC50	55900	nM	IC50	J Med Chem (2019) 62: 9593-9599 [PMID:31589047]
Farnesoid X receptor/Bile acid receptor FXR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2047] [GtoPdb: 603] [UniProtKB: Q96RI1]
ChEMBL	Antagonist activity at human GTS-tagged FXR after 20 mins by TR-FRET assay	B	6.1	pIC50	790	nM	IC50	Bioorg Med Chem (2013) 21: 4266-4278 [PMID:23688559]
epoxide hydrolase 2/Epoxide hydratase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2409] [GtoPdb: 2970] [UniProtKB: P34913]
ChEMBL	Competitive inhibition of human recombinant soluble epoxide hydrolase using [3H]-tDPPO as substrate	B	7.59	pKi	26	nM	Ki	Bioorg Med Chem Lett (2013) 23: 3818-3821 [PMID:23684894]
ChEMBL	Inhibition of human recombinant soluble epoxide hydrolase using (cyano(6-methoxy-naphthelen-2-yl)methyl trans-[(3-phenyl-oxiran-2-yl)methyl] carbonate) as substrate preincubated for 5 mins prior to substrate addition by fluorescence assay	B	8.22	pIC50	6	nM	IC50	Bioorg Med Chem Lett (2013) 23: 3818-3821 [PMID:23684894]
Estrogen receptor-α/Estrogen receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372]
ChEMBL	Selective estrogen receptor down-regulator activity at FLAG-tagged ERalpha (unknown origin) expressed in HEK293 cells assessed as induction of ERalpha degradation by measuring dissociation constant for degradation by luciferase reporter gene assay relative to untreated control	B	8.33	pKd	4.69	nM	Kd	Bioorg Med Chem (2019) 27: 1952-1961 [PMID:30940565]
GtoPdb	-	-	8.98	pKi	1.04	nM	Ki	J Med Chem (2003) 46: 1408-18 [PMID:12672240]
ChEMBL	In vitro displacement of 0.5 nM [3H]17-beta-estradiol from human Estrogen receptor alpha	B	8.98	pKi	1.04	nM	Ki	J Med Chem (2003) 46: 1408-1418 [PMID:12672240]
ChEMBL	Displacement of fluorescent estradiol from full-length ERalpha (unknown origin) measured after 2 hrs by fluorescence polarization assay	B	7.05	pIC50	88.5	nM	IC50	Eur J Med Chem (2021) 226: 113870-113870 [PMID:34610548]
ChEMBL	Displacement of [3H]-E2 from estrogen receptor-alpha (unknown origin) by scintillation counting analysis	B	7.62	pIC50	24	nM	IC50	J Med Chem (2015) 58: 4888-4904 [PMID:25879485]
ChEMBL	Downregulation of ER-alpha expression in human T47D cells measured after 5 days by Western blot analysis	B	8.03	pIC50	9.3	nM	IC50	J Med Chem (2016) 59: 8134-8140 [PMID:27529700]
ChEMBL	Downregulation of ER-alpha expression in human tamoxifen-resistant T47D cells over-expressing PKC-alpha measured after 5 days by Western blot analysis	B	8.07	pIC50	8.5	nM	IC50	J Med Chem (2016) 59: 8134-8140 [PMID:27529700]
ChEMBL	Displacement of [3H]17-beta-estradiol from human Estrogen receptor alpha	B	8.22	pIC50	6	nM	IC50	Bioorg Med Chem Lett (2000) 10: 147-151 [PMID:10673099]
ChEMBL	Antagonist activity at ERalpha in human MCF7 cells assessed as inhibition of estradiol-driven cell growth measured after 7 days by SYTOX green-based assay	B	8.3	pIC50	5.01	nM	IC50	J Med Chem (2019) 62: 1593-1608 [PMID:30640465]
ChEMBL	Binding affinity to human ERalpha	B	8.31	pIC50	4.9	nM	IC50	J Med Chem (2007) 50: 4471-4481 [PMID:17696335]
ChEMBL	Antagonist activity at estrogen receptor alpha ligand binding domain expressed in african green monkey COS7 cells co-transfected with Gal4-LBD by luciferase reporter gene assay	B	8.4	pIC50	4	nM	IC50	J Nat Prod (2009) 72: 1944-1948 [PMID:19863083]
ChEMBL	Induction of selective estrogen receptor alpha degradation in human MCF7 cells harboring TK-ERE-Luc assessed as reduction in estradiol-induced GREB1 mRNA expression after 24 hrs by TaqMan assay	B	8.42	pIC50	3.8	nM	IC50	J Med Chem (2018) 61: 2837-2864 [PMID:29562737]
ChEMBL	Antagonist activity at ERalpha in human MCF7 cells assessed as inhibition of estrogen-induced transcription preincubated overnight followed by estrogen addition measured after 24 hrs by dual luciferase reporter gene assay	B	8.47	pIC50	3.4	nM	IC50	J Med Chem (2017) 60: 2790-2818 [PMID:28296398]
ChEMBL	Induction of selective estrogen receptor alpha degradation in human MCF7 cells harboring TK-ERE-Luc assessed as reduction in estradiol-induced transcriptional activity after 24 hrs by luciferase reporter gene assay	B	8.47	pIC50	3.4	nM	IC50	J Med Chem (2018) 61: 2837-2864 [PMID:29562737]
ChEMBL	Displacement of fluoromone ligand from recombinant ER-alpha (unknown origin) by LanthaScreen TR-FRET assay	B	8.52	pIC50	3	nM	IC50	J Med Chem (2016) 59: 8134-8140 [PMID:27529700]
ChEMBL	Displacement of fluorescent-labeled E2 from LBD of ERalpha (unknown origin) by TR-FRET assay	B	8.55	pIC50	2.85	nM	IC50	J Med Chem (2021) 64: 5766-5786 [PMID:33904307]
ChEMBL	Displacement of fluorescent-labelled E2 from recombinant human GST-tagged ERalpha by LanthaScreen TR-FRET assay	B	8.55	pIC50	2.85	nM	IC50	Eur J Med Chem (2020) 192: 112191-112191 [PMID:32169784]
ChEMBL	Inhibition of ERalpha in human MCF7:WS8 cells assessed as increase in degradation of ERalpha incubated for 24 hrs by In-Cell Western assay	B	8.8	pIC50	1.58	nM	IC50	J Med Chem (2019) 62: 11301-11323 [PMID:31746603]
ChEMBL	Induction of ERalpha degradation in human MCF7 cells after 18 hrs by Western blot analysis	B	8.92	pIC50	1.2	nM	IC50	J Med Chem (2017) 60: 2790-2818 [PMID:28296398]
ChEMBL	Induction of selective estrogen receptor alpha degradation in human MCF7 cells after 18 to 24 hrs by in-cell Western analysis	B	8.92	pIC50	1.2	nM	IC50	J Med Chem (2018) 61: 2837-2864 [PMID:29562737]
ChEMBL	Induction of ERalpha degradation in human MCF7 cells after 18 to 24 hrs by Western blot analysis	B	9	pIC50	1	nM	IC50	J Med Chem (2017) 60: 2790-2818 [PMID:28296398]
ChEMBL	Induction of ERalpha degradation in human T47D cells	B	9.08	pIC50	0.84	nM	IC50	ACS Med Chem Lett (2020) 11: 1342-1347 [PMID:32551022]
ChEMBL	Binding affinity to ERalpha receptor (unknown origin)	B	9.09	pIC50	0.81	nM	IC50	J Med Chem (2015) 58: 8128-8140 [PMID:26407012]
ChEMBL	Antagonist activity at FLAG-tagged ERalpha (unknown origin) expressed in HEK293 cells assessed as reduction in E2-induced ER-alpha-mediated transcriptional activity by luciferase reporter gene assay	B	9.11	pIC50	0.78	nM	IC50	Bioorg Med Chem (2019) 27: 1952-1961 [PMID:30940565]
ChEMBL	Antagonist effect on transcriptional activation in MCF-7 cells expressing estrogen receptor alpha	F	9.33	pIC50	0.47	nM	IC50	Bioorg Med Chem Lett (2000) 10: 147-151 [PMID:10673099]
ChEMBL	Induction of ERalpha degradation in human MCF7 cells after 4 hrs by FITC/Hoechst staining based immunofluorescence imaging analysis	B	9.49	pIC50	0.32	nM	IC50	ACS Med Chem Lett (2020) 11: 1342-1347 [PMID:32551022]
ChEMBL	Downregulation of human ERalpha in human MCF-7 cells after 24 hrs by in-cell Western immunoassay method	B	9.52	pIC50	0.3	nM	IC50	J Med Chem (2017) 60: 6321-6336 [PMID:28657320]
ChEMBL	Antagonist activity at estrogen receptor in human T47D cells incubated for 18 hrs by ultra high sensitivity luminescence reporter gene assay	B	9.6	pIC50	0.25	nM	IC50	J Med Chem (2021) 64: 11841-11856 [PMID:34251202]
ChEMBL	Antagonist activity at ERalpha receptor in human MCF7 cells	B	10.2	pIC50	0.06	nM	IC50	J Med Chem (2015) 58: 8128-8140 [PMID:26407012]
ChEMBL	Induction of ERalpha degradation in human MCF7 cells assessed as inhibition of insulin-mediated cell proliferation after 6 days by Hoechst 33258 dye-based assay	B	10.22	pIC50	0.06	nM	IC50	J Med Chem (2017) 60: 2790-2818 [PMID:28296398]
ChEMBL	Selective estrogen receptor down-regulator activity at FLAG-tagged ERalpha (unknown origin) expressed in HEK293 cells assessed as induction of ERalpha degradation by luciferase reporter gene assay	B	8.85	pEC50	1.4	nM	EC50	Bioorg Med Chem (2019) 27: 1952-1961 [PMID:30940565]
ChEMBL	Induction of estrogen receptor-alpha degradation in human MCF7 cells after 4 hrs by in-cell western assay	B	9.4	pEC50	0.4	nM	EC50	J Med Chem (2015) 58: 4888-4904 [PMID:25879485]
ChEMBL	Induction of ERalpha degradation in human MCF7 cells in phenol red free RPMI medium containing 5% charcoal-stripped FBS incubated for 4 hrs by IRDye 800CW/DRAQ5 dye based in-cell Western assay	B	9.4	pEC50	0.4	nM	EC50	Bioorg Med Chem Lett (2019) 29: 367-372 [PMID:30587451]
Estrogen receptor-α/Estrogen receptor alpha in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2724] [GtoPdb: 620] [UniProtKB: P06211]
ChEMBL	Displacement of [3H]estradiol from rat uterine cytosolic estrogen receptor	B	8.23	pIC50	5.89	nM	IC50	Bioorg Med Chem (2012) 20: 2353-2361 [PMID:22377671]
Estrogen receptor-β/Estrogen receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL242] [GtoPdb: 621] [UniProtKB: Q92731]
ChEMBL	In vitro displacement of 0.5 nM [3H]17-beta-estradiol from human Estrogen receptor beta	B	8.86	pKi	1.39	nM	Ki	J Med Chem (2003) 46: 1408-1418 [PMID:12672240]
GtoPdb	-	-	8.86	pKi	1.39	nM	Ki	J Med Chem (2003) 46: 1408-18 [PMID:12672240]
ChEMBL	Binding affinity to human ERbeta	B	7.36	pIC50	44.1	nM	IC50	J Med Chem (2007) 50: 4471-4481 [PMID:17696335]
ChEMBL	Displacement of [3H]-E2 from estrogen receptor-beta (unknown origin) by scintillation counting analysis	B	7.68	pIC50	21	nM	IC50	J Med Chem (2015) 58: 4888-4904 [PMID:25879485]
ChEMBL	Displacement of fluorescent-labeled E2 from LBD of ERbeta (unknown origin) by TR-FRET assay	B	7.99	pIC50	10.2	nM	IC50	J Med Chem (2021) 64: 5766-5786 [PMID:33904307]
ChEMBL	Displacement of fluorescent-labelled E2 from recombinant human GST-tagged ERbeta by LanthaScreen TR-FRET assay	B	7.99	pIC50	10.2	nM	IC50	Eur J Med Chem (2020) 192: 112191-112191 [PMID:32169784]
ChEMBL	Inhibition of human estrogen receptor 2 using tritiated estradiol incubated for 3 hr	B	8.08	pIC50	8.4	nM	IC50	Bioorg Med Chem Lett (2005) 15: 3912-3916 [PMID:15993065]
ChEMBL	Displacement of [3H]17-beta-estradiol from human Estrogen receptor beta	B	8.15	pIC50	7	nM	IC50	Bioorg Med Chem Lett (2000) 10: 147-151 [PMID:10673099]
ChEMBL	Antagonist activity at estrogen receptor beta ligand binding domain expressed in african green monkey COS7 cells co-transfected with Gal4-LBD by luciferase reporter gene assay	B	8.42	pIC50	3.8	nM	IC50	J Nat Prod (2009) 72: 1944-1948 [PMID:19863083]
Estrogen-related receptor-α/Estrogen-related receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3429] [GtoPdb: 622] [UniProtKB: P11474]
ChEMBL	Antagonist activity at ERalpha receptor in human MCF7 cells assessed as inhibition of cell growth after 6 days by crystal violet staining method	B	8.7	pIC50	2	nM	IC50	J Med Chem (2013) 56: 2779-2790 [PMID:23448346]
sirtuin 5/NAD-dependent protein deacylase sirtuin-5, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2163183] [GtoPdb: 2711] [UniProtKB: Q9NXA8]
ChEMBL	Inhibition of SIRT5 (unknown origin)	B	5.59	pIC50	2600	nM	IC50	Eur J Med Chem (2020) 206: 112676-112676 [PMID:32858418]
Pregnane X receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3401] [GtoPdb: 606] [UniProtKB: O75469]
ChEMBL	Agonist activity at PXR (unknown origin) expressed in human HepG2 cells assessed as induction of CYP3A4 transactivation after 16 hrs by luciferase reporter gene assay	B	5.71	pEC50	1950	nM	EC50	Bioorg Med Chem (2013) 21: 4266-4278 [PMID:23688559]
Progesterone receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL208] [GtoPdb: 627] [UniProtKB: P06401]
ChEMBL	Agonist activity at progesterone receptor in human MCF7 cells	B	4	pIC50	>100000	nM	IC50	J Med Chem (2015) 58: 8128-8140 [PMID:26407012]
ChEMBL	Antagonist activity at progesterone receptor in human MCF cells assessed as estradiol-induced receptor response	B	9.68	pIC50	0.21	nM	IC50	J Med Chem (2015) 58: 8128-8140 [PMID:26407012]
GPER in Human [GtoPdb: 221] [UniProtKB: Q99527]
GtoPdb	-	-	7	pKi	-	-	-	Endocrinology (2005) 146: 624-32 [PMID:15539556]

ChEMBL data shown on this page come from version 32:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]