ChEMBL ligand: CHEMBL59030 (GW3965)
Liver X receptor-α/LXR-alpha in Human [ChEMBL: CHEMBL2808] [GtoPdb: 602] [UniProtKB: Q13133] There should be some charts here, you may need to enable JavaScript!
Liver X receptor-β/LXR-beta in Human [ChEMBL: CHEMBL4093] [GtoPdb: 601] [UniProtKB: P55055] 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!
Retinoid X receptor-α/Liver X receptor-β/Retinoic acid receptor RXR-alpha/oxysterols receptor LXR-beta in Human [ChEMBL: CHEMBL3430878] [GtoPdb: 610, 601] [UniProtKB: P19793, P55055] 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
Liver X receptor-α/LXR-alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2808] [GtoPdb: 602] [UniProtKB: Q13133]
ChEMBL	Binding affinity to full-length human LXRalpha by surface plasmon resonance assay	B	5.16	pKd	6970	nM	Kd	J Med Chem (2021) 64: 9943-9959 [PMID:34251816]
ChEMBL	Displacement of [N-methyl-3H]GW0438 from human biotinylated LXRalpha ligand binding domain	B	6.63	pIC50	235	nM	IC50	J Med Chem (2008) 51: 5758-5765 [PMID:18800767]
ChEMBL	Displacement of [3H]T-0901317 from human LXR alpha receptor	B	7	pIC50	100	nM	IC50	J Med Chem (2006) 49: 6151-6154 [PMID:17034119]
ChEMBL	Displacement of [3H]TO901317 from human recombinant LXRalpha expressed in Escherichia coli by flashplate method	B	7	pIC50	100	nM	IC50	J Med Chem (2008) 51: 7161-7168 [PMID:18973288]
ChEMBL	Antagonist activity at LXRalpha ligand binding domain assessed as inhibition of T1317-induced transcriptional activity in african green monkey CV1 cells co-transfected with Gal4-SRC1 by luciferase reporter assay	B	7	pIC50	100	nM	IC50	J Med Chem (2010) 53: 3412-3416 [PMID:20345102]
ChEMBL	Agonist activity at LXRalpha (unknown origin)	B	5.89	pEC50	1300	nM	EC50	Bioorg Med Chem Lett (2015) 25: 2668-2674 [PMID:25998501]
ChEMBL	Agonist activity at Gal4-tagged LXRalpha (unknown origin) expressed in CHOK1 cells after 24 hrs by luciferase reporter gene assay	B	5.89	pEC50	1300	nM	EC50	Bioorg Med Chem Lett (2015) 25: 1274-1278 [PMID:25677664]
ChEMBL	Agonist activity at human LXRalpha by Gal4 assay	B	5.95	pEC50	1128	nM	EC50	J Med Chem (2016) 59: 3264-3271 [PMID:26990539]
ChEMBL	Agonist activity at LXRalpha ligand binding domain-mediated transcriptional activity in african green monkey CV1 cells co-transfected with Gal4-SRC1 by luciferase reporter assay	B	6.1	pEC50	794.33	nM	EC50	J Med Chem (2010) 53: 3412-3416 [PMID:20345102]
ChEMBL	Agonist activity at human recombinant LXRalpha ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay	B	6.18	pEC50	660	nM	EC50	J Med Chem (2008) 51: 7161-7168 [PMID:18973288]
ChEMBL	Agonist activity at LXRalpha LBD by HTRF cofactor peptide recruitment assay	F	6.44	pEC50	367	nM	EC50	Bioorg Med Chem Lett (2007) 17: 3473-3479 [PMID:17416521]
ChEMBL	Agonist activity at human LXRalpha receptor after 1 hr by HTRF cofactor recruitment assay	F	6.44	pEC50	367	nM	EC50	Bioorg Med Chem Lett (2007) 17: 4442-4446 [PMID:17587573]
ChEMBL	Agonist activity at human LXRalpha expressed in human SH-SY5Y cells co-transfected with Gal4-LBD after 24 hrs by luciferase reporter gene assay	F	6.51	pEC50	310	nM	EC50	Bioorg Med Chem Lett (2009) 19: 2009-2012 [PMID:19264481]
ChEMBL	Agonist activity at LXRalpha ligand binding domain by FRET based SRC1 recruitment assay	B	6.55	pEC50	280	nM	EC50	Bioorg Med Chem Lett (2009) 19: 2009-2012 [PMID:19264481]
ChEMBL	Agonist activity at human LXRalpha assessed as association of SRC1 to LXRalpha ligand binding domain by FRET based cell-free ligand sensing assay	B	6.7	pEC50	200	nM	EC50	Bioorg Med Chem Lett (2009) 19: 5617-5621 [PMID:19717304]
GtoPdb	-	-	6.7	pEC50	-	-	-	J Med Chem (2002) 45: 1963-6 [PMID:11985463]
ChEMBL	Effective concentration in LXR alpha-Gal4 receptor gene assay	B	6.72	pEC50	190	nM	EC50	J Med Chem (2002) 45: 1963-1966 [PMID:11985463]
ChEMBL	Agonist activity at LXRalpha by FRET assay	F	6.76	pEC50	175	nM	EC50	Bioorg Med Chem Lett (2009) 19: 1097-1100 [PMID:19167885]
ChEMBL	Ligand-dependent recruitment of steroid receptor co-activator 1 (SRC1) to Liver X receptor-alpha	B	6.9	pEC50	125	nM	EC50	J Med Chem (2002) 45: 1963-1966 [PMID:11985463]
ChEMBL	Agonist activity at GAL-linked human LXRalpha expressed in THP1 cells assessed as stimulation of coactivator recruitment by FRET assay	F	7.01	pEC50	97	nM	EC50	J Med Chem (2007) 50: 4255-4259 [PMID:17665897]
ChEMBL	Effective concentration for Steroid receptor coactivator-1 (SRC1) recruitment to human LXRalpha (Liver X receptor)	B	7.1	pEC50	80	nM	EC50	J Med Chem (2005) 48: 5419-5422 [PMID:16107141]
ChEMBL	Activity at human LXRalpha by Gal4 transactivation assay	B	7.18	pEC50	66	nM	EC50	J Med Chem (2007) 50: 4255-4259 [PMID:17665897]
ChEMBL	Binding affinity to human LXRalpha	B	7.66	pEC50	22	nM	EC50	J Med Chem (2016) 59: 3264-3271 [PMID:26990539]
Liver X receptor-β/LXR-beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4093] [GtoPdb: 601] [UniProtKB: P55055]
ChEMBL	Binding affinity to recombinant human LXRbeta-LBD expressed in Escherichia coli BL21 (DE3) assessed as inhibitory constant incubated for 30 mins by fluorescence polarization binding assay	B	8.66	pKi	2.2	nM	Ki	Eur J Med Chem (2019) 178: 458-467 [PMID:31202993]
ChEMBL	Displacement of hyodeoxycholicacid-based fluorescent tracer from recombinant human LXRbeta LBD (215 to 461 residues) expressed in Escherichia coli BL21 (DE3) preincubated for 10 mins under shaking condition and measured after 30 mins by fluorescence polarization assay	B	8.66	pKi	2.2	nM	Ki	Eur J Med Chem (2020) 194: 112240-112240 [PMID:32248003]
ChEMBL	Antagonist activity at LXRbeta ligand binding domain assessed as inhibition of T1317-induced transcriptional activity in african green monkey CV1 cells co-transfected with Gal4-SRC1 by luciferase reporter assay	B	7.4	pIC50	39.81	nM	IC50	J Med Chem (2010) 53: 3412-3416 [PMID:20345102]
ChEMBL	Displacement of [N-methyl-3H]GW0438 from human biotinylated LXRbeta ligand binding domain	B	7.52	pIC50	30	nM	IC50	J Med Chem (2008) 51: 5758-5765 [PMID:18800767]
ChEMBL	Displacement of [3H]T-0901317 from human LXR beta receptor	B	7.92	pIC50	12	nM	IC50	J Med Chem (2006) 49: 6151-6154 [PMID:17034119]
ChEMBL	Displacement of [3H]TO901317 from human recombinant LXRbeta expressed in Escherichia coli by flashplate method	B	7.92	pIC50	12	nM	IC50	J Med Chem (2008) 51: 7161-7168 [PMID:18973288]
ChEMBL	Displacement of [N-methyl-3H]T1317 from human biotinylated LXRbeta LBD after 3 hrs by LEAD seeker binding assay	B	8.1	pIC50	7.94	nM	IC50	J Med Chem (2010) 53: 3412-3416 [PMID:20345102]
ChEMBL	Agonist activity at LXRbeta ligand binding domain-mediated transcriptional activity in african green monkey CV1 cells co-transfected with Gal4-SRC1 by luciferase reporter assay	B	6.3	pEC50	501.19	nM	EC50	J Med Chem (2010) 53: 3412-3416 [PMID:20345102]
ChEMBL	Agonist activity at Gal4-tagged LXRbeta (unknown origin) expressed in CHOK1 cells after 24 hrs by luciferase reporter gene assay	B	6.38	pEC50	420	nM	EC50	Bioorg Med Chem Lett (2015) 25: 1274-1278 [PMID:25677664]
ChEMBL	Agonist activity at human LXR beta receptor expressed in CHO cells by reporter assay	F	6.39	pEC50	410	nM	EC50	J Med Chem (2006) 49: 6151-6154 [PMID:17034119]
ChEMBL	Agonist activity at LXRbeta (unknown origin)	B	6.4	pEC50	400	nM	EC50	Bioorg Med Chem Lett (2015) 25: 2668-2674 [PMID:25998501]
ChEMBL	Agonist activity at human LXRbeta by Gal4 assay	B	6.41	pEC50	390	nM	EC50	J Med Chem (2016) 59: 3264-3271 [PMID:26990539]
ChEMBL	Agonist activity at human recombinant LXRbeta ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay	B	6.51	pEC50	310	nM	EC50	J Med Chem (2008) 51: 7161-7168 [PMID:18973288]
ChEMBL	Agonist activity at recombinant human LXRbeta-LBD expressed in Escherichia coli BL21 (DE3) assessed as peptide D22 recruitment fluorescence polarization binding assay	B	6.54	pEC50	289	nM	EC50	Eur J Med Chem (2019) 178: 458-467 [PMID:31202993]
ChEMBL	Agonist activity at human LXRbeta expressed in human SH-SY5Y cells co-transfected with Gal4-LBD after 24 hrs by luciferase reporter gene assay	F	6.89	pEC50	130	nM	EC50	Bioorg Med Chem Lett (2009) 19: 2009-2012 [PMID:19264481]
ChEMBL	Agonist activity at LXRbeta ligand binding domain by FRET based SRC1 recruitment assay	B	7.11	pEC50	78	nM	EC50	Bioorg Med Chem Lett (2009) 19: 2009-2012 [PMID:19264481]
ChEMBL	Agonist activity at human LXRbeta assessed as association of SRC1 to LXRbeta ligand binding domain by FRET based cell-free ligand sensing assay	B	7.4	pEC50	40	nM	EC50	Bioorg Med Chem Lett (2009) 19: 5617-5621 [PMID:19717304]
ChEMBL	Agonist activity at LXRbeta LBD by HTRF cofactor peptide recruitment assay	F	7.46	pEC50	35	nM	EC50	Bioorg Med Chem Lett (2007) 17: 3473-3479 [PMID:17416521]
ChEMBL	Agonist activity at human LXRbeta receptor after 1 hr by HTRF cofactor recruitment assay	F	7.46	pEC50	35	nM	EC50	Bioorg Med Chem Lett (2007) 17: 4442-4446 [PMID:17587573]
GtoPdb	-	-	7.52	pEC50	-	-	-	J Med Chem (2002) 45: 1963-6 [PMID:11985463]
ChEMBL	Agonist activity at GAL-linked human LXRbeta expressed in THP1 cells assessed as stimulation of co-activator recruitment by FRET assay	F	7.57	pEC50	27	nM	EC50	J Med Chem (2007) 50: 4255-4259 [PMID:17665897]
ChEMBL	Agonist activity at LXRbeta by FRET assay	F	7.6	pEC50	25	nM	EC50	Bioorg Med Chem Lett (2009) 19: 1097-1100 [PMID:19167885]
ChEMBL	Effective concentration for Steroid receptor coactivator-1 (SRC1) recruitment to human LXRbeta (Liver X receptor)	B	7.7	pEC50	20	nM	EC50	J Med Chem (2005) 48: 5419-5422 [PMID:16107141]
ChEMBL	Agonist activity at human LXRbeta receptor transfected in COS7 cells after 16 hrs by reporter transactivation assay	F	7.82	pEC50	15	nM	EC50	Bioorg Med Chem Lett (2007) 17: 4442-4446 [PMID:17587573]
ChEMBL	Activation of LXRbeta co-transfected in COS7 cells with RXRalpha by reporter transactivation assay	F	7.82	pEC50	15	nM	EC50	Bioorg Med Chem Lett (2007) 17: 3473-3479 [PMID:17416521]
ChEMBL	Binding to human LXRbeta	B	8.3	pEC50	5	nM	EC50	J Med Chem (2016) 59: 3264-3271 [PMID:26990539]
ChEMBL	Activity at human LXRbeta by Gal4 transactivation assay	B	8.4	pEC50	4	nM	EC50	J Med Chem (2007) 50: 4255-4259 [PMID:17665897]
Pregnane X receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3401] [GtoPdb: 606] [UniProtKB: O75469]
ChEMBL	Binding affinity to PXR by scintillation proximity binding assay	B	5.7	pKi	2000	nM	Ki	Bioorg Med Chem Lett (2009) 19: 5617-5621 [PMID:19717304]
Retinoid X receptor-α/Liver X receptor-β/Retinoic acid receptor RXR-alpha/oxysterols receptor LXR-beta in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3430878] [GtoPdb: 610, 601] [UniProtKB: P19793, P55055]
GtoPdb	-	-	7.52	pEC50	-	-	-	J Med Chem (2002) 45: 1963-6 [PMID:11985463]
ChEMBL	Agonist activity at human RXRalpha/LXRbeta expressed in HEK293 cells measured after 20 hrs by dual luciferase reporter gene assay	B	9.64	pEC50	0.23	nM	EC50	Eur J Med Chem (2020) 194: 112240-112240 [PMID:32248003]

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]