ChEMBL ligand: CHEMBL1358 (Faslodex, Fulvestrant, ICI 182,780, ICI-182780, NSC-759879, ZD-9238, ZD9238)
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]
ChEMBL	Binding affinity to ERalpha (unknown origin) assessed as inhibition constant incubated for 2 hrs by fluorescence polarization assay	B	7.4	pKi	40	nM	Ki	J Med Chem (2023) 66: 6631-6651 [PMID:37161783]
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	Antagonist activity at ER-alpha (unknown origin) by ER-alpha coactivator assay	B	7.89	pIC50	13	nM	IC50	Bioorg Med Chem (2024) 101: 117645-117645 [PMID:38401456]
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	Binding affinity to human ERalpha Y537S mutant ligand binding domain	B	8.42	pIC50	3.8	nM	IC50	J Med Chem (2023) 66: 8339-8381 [PMID:37377342]
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	Binding affinity to human ERalpha D538G mutant ligand binding domain	B	8.48	pIC50	3.3	nM	IC50	J Med Chem (2023) 66: 8339-8381 [PMID:37377342]
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-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	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	Binding affinity to human wild type ERalpha ligand binding domain	B	8.8	pIC50	1.6	nM	IC50	J Med Chem (2023) 66: 8339-8381 [PMID:37377342]
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 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 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 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	Antagonist activity at ERalpha expressed in HEK293/Gal4 cells incubated for 24 hrs in presence of estradiol by luciferase reporter gene assay	B	9	pIC50	1	nM	IC50	J Med Chem (2022) 65: 5724-5750 [PMID:35357160]
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	Inhibition of ERalpha (246 to 595 residues) in doxycycline-induced human HEK293 cells incubated overnight by luciferase based assay	B	9.3	pIC50	0.5	nM	IC50	J Med Chem (2023) 66: 8339-8381 [PMID:37377342]
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	Antagonist activity against ERalpha in estradiol stimulated HEK293T cells measuring luciferase activity after 24 hrs by luciferase reporter assay	B	9.38	pEC50	0.42	nM	EC50	Eur J Med Chem (2023) 253: 115328-115328 [PMID:37037140]
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]
ChEMBL	Induction of ERalpha degradation in human MCF7 cells	B	9.7	pEC50	0.2	nM	EC50	J Med Chem (2023) 66: 8339-8381 [PMID:37377342]
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	Binding affinity to ERbeta (unknown origin) assessed as inhibition constant incubated for 2 hrs by fluorescence polarization assay	B	6.72	pKi	190	nM	Ki	J Med Chem (2023) 66: 6631-6651 [PMID:37161783]
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-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	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	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]
ChEMBL	Inhibition of ERbeta (261 to 500 residues) in doxycycline-induced human HEK293 cells incubated overnight by luciferase based assay	B	9.05	pIC50	0.9	nM	IC50	J Med Chem (2023) 66: 8339-8381 [PMID:37377342]
ChEMBL	Antagonist activity at ERbeta expressed in HEK293/Gal4 cells incubated for 24 hrs in presence of di-arylpropionitrile by luciferase reporter gene assay	B	9.52	pIC50	0.3	nM	IC50	J Med Chem (2022) 65: 5724-5750 [PMID:35357160]
ChEMBL	Antagonist activity against ERbeta in estradiol stimulated HEK293T cells measuring luciferase activity after 24 hrs by luciferase reporter assay	B	9.18	pEC50	0.67	nM	EC50	Eur J Med Chem (2023) 253: 115328-115328 [PMID:37037140]
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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]