ChEMBL ligand: CHEMBL318457
Bile acid receptor in Mouse [ChEMBL: CHEMBL5343] [UniProtKB: Q60641] 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!
Vitamin D receptor in Human [ChEMBL: CHEMBL1977] [GtoPdb: 605] [UniProtKB: P11473] 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
Bile acid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5343] [UniProtKB: Q60641]
ChEMBL	Agonist activity at mouse chimeric FXR assessed as receptor transactivation by luciferase transcriptional reporter gene assay	F	5.7	pEC50	2000	nM	EC50	Bioorg Med Chem Lett (2009) 19: 2595-2598 [PMID:19328688]
Farnesoid X receptor/Bile acid receptor FXR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2047] [GtoPdb: 603] [UniProtKB: Q96RI1]
ChEMBL	Antagonist activity at FXR in human HepG2 cells incubated for 24 hrs by dual luciferase reporter assay	B	5.59	pIC50	2600	nM	IC50	J Med Chem (2016) 59: 6553-6579 [PMID:26878262]
ChEMBL	Displacement of radioligand from human FXR by scintillation proximity assay	B	6.95	pIC50	112	nM	IC50	Bioorg Med Chem Lett (2011) 21: 1134-1140 [PMID:21269824]
ChEMBL	Displacement of radioligand from human FXR by scintillation proximity assay	B	7.19	pIC50	64	nM	IC50	Bioorg Med Chem Lett (2009) 19: 2595-2598 [PMID:19328688]
ChEMBL	Antagonist activity at human GST-tagged FXR after 20 mins by TR-FRET assay	B	7.7	pIC50	19.8	nM	IC50	Bioorg Med Chem (2014) 22: 2919-2938 [PMID:24775917]
ChEMBL	Agonist activity at FXR (unknown origin) by coactivator recruitment assay	B	4.82	pEC50	15000	nM	EC50	J Med Chem (2014) 57: 8035-8055 [PMID:25255039]
ChEMBL	Agonist activity at Gal4-fused human FXR by luciferase reporter gene transactivation assay	F	6.04	pEC50	910	nM	EC50	Bioorg Med Chem Lett (2011) 21: 1134-1140 [PMID:21269824]
ChEMBL	Agonist activity at FXR (unknown origin) by reporter gene assay	B	6.05	pEC50	900	nM	EC50	J Med Chem (2014) 57: 8035-8055 [PMID:25255039]
ChEMBL	Agonist activity at chimeric FXR assessed as receptor transactivation by luciferase transcriptional reporter gene assay	F	6.05	pEC50	900	nM	EC50	Bioorg Med Chem Lett (2009) 19: 2595-2598 [PMID:19328688]
ChEMBL	Agonist activity at FXR (unknown origin) by reporter gene assay	B	6.05	pEC50	900	nM	EC50	Bioorg Med Chem (2014) 22: 2447-2460 [PMID:24685112]
ChEMBL	Binding affinity to human GTS-tagged FXR LBD using fluorescein-tagged SRC2-2 after 30 mins by TR-FRET assay	B	6.12	pEC50	753	nM	EC50	Bioorg Med Chem (2013) 21: 4266-4278 [PMID:23688559]
ChEMBL	Agonist activity at human farnesoid-X-receptor expressed in HEK293T cells co-expressing human RXRalpha assessed as receptor activation after 20 hrs by dual luciferase reporter assay	B	6.21	pEC50	610	nM	EC50	Medchemcomm (2015) 6: 1393-1403
ChEMBL	Agonist activity at FXR in HEK293T cells assessed as transcriptional activity by measuring fluorescence intensity by luciferase reporter assay	B	6.26	pEC50	550	nM	EC50	Bioorg Med Chem Lett (2022) 76: 128993-128993 [PMID:36130662]
ChEMBL	Agonist activity at human full length FXR expressed in HeLa cells cotransfected with pSG5-human RXR after 24 hrs by Dual-Glo luciferase reporter gene assay	B	6.29	pEC50	510	nM	EC50	Bioorg Med Chem (2015) 23: 3490-3498 [PMID:25934227]
ChEMBL	Agonist activity at human FXR transfected in CHO-K1 cells coexpressed with beta-galactosidase incubated for 3 to 16 hrs by PathHunter chemiluminescence based assay	B	6.4	pEC50	400	nM	EC50	J Med Chem (2022) 65: 9974-10000 [PMID:35797110]
ChEMBL	Agonist activity at human FXR transfected in HEK293 cells assessed as transcriptional activity by luciferase reporter gene assay	B	6.43	pEC50	373	nM	EC50	J Med Chem (2015) 58: 9768-9772 [PMID:26568144]
ChEMBL	Binding affinity to human GTS-tagged FXR LBD using fluorescein-tagged SRC2-2 after 20 mins by TR-FRET assay	B	6.43	pEC50	373	nM	EC50	Bioorg Med Chem (2013) 21: 4266-4278 [PMID:23688559]
ChEMBL	Binding affinity to human GTS-tagged FXR LBD using fluorescein-tagged SRC2-2 after 15 mins by TR-FRET assay	B	6.5	pEC50	317	nM	EC50	Bioorg Med Chem (2013) 21: 4266-4278 [PMID:23688559]
ChEMBL	Agonist activity at human FXR expressed in HEK293T cells co-transfected with BSEP plasmid assessed as receptor transactivation after 24 hrs by BSEP-luciferase reporter gene assay	B	6.59	pEC50	260	nM	EC50	Eur J Med Chem (2021) 209: 112910-112910 [PMID:33049605]
ChEMBL	Agonist activity at human FXR expressed in HEK293T cells by luciferase reporter assay	B	6.64	pEC50	231.5	nM	EC50	Eur J Med Chem (2022) 230: 114089-114089 [PMID:34998040]
ChEMBL	Agonist activity at recombinant His-tagged human FXR ligand binding domain assessed as SRC-1 coactivator recruitment after 4 hrs by luminescence analysis	B	6.66	pEC50	220	nM	EC50	J Med Chem (2015) 58: 9768-9772 [PMID:26568144]
ChEMBL	Agonist activity at human FXR expressed in HEK293T cells assessed as BSEP promoter driven cellular transcriptional activity after 24 hrs by luciferase reporter gene assay	B	7.02	pEC50	95	nM	EC50	J Med Chem (2017) 60: 9960-9973 [PMID:29148806]
ChEMBL	Agonist activity at FXR (unknown origin) by cell based assay	B	7.05	pEC50	90	nM	EC50	J Med Chem (2020) 63: 5031-5073 [PMID:31930920]
ChEMBL	Activation of human FXR LBD expressed in HEK293T cells assessed as induction of receptor activation incubated for 12 to 14 hrs by luciferase reporter gene assay	B	7.05	pEC50	90	nM	EC50	J Med Chem (2020) 63: 8369-8379 [PMID:32687365]
ChEMBL	Activation of human farnesoid X receptor	B	7.15	pEC50	70	nM	EC50	J Med Chem (2005) 48: 5383-5403 [PMID:16107136]
ChEMBL	Agonist activity at human recombinant FXR expressed in HEK293 cells coexpressing CMX-GAL4N by luciferase reporter gene assay	F	7.15	pEC50	70	nM	EC50	Bioorg Med Chem Lett (2012) 22: 3962-3966 [PMID:22583617]
ChEMBL	Agonist activity FXR (unknown origin)	B	7.15	pEC50	70	nM	EC50	J Med Chem (2019) 62: 2112-2126 [PMID:30702885]
ChEMBL	Agonistic activity at FXR in HEK293 cells by GAL4 transactivation activity	F	7.15	pEC50	70	nM	EC50	Bioorg Med Chem (2007) 15: 2587-2600 [PMID:17292610]
ChEMBL	Agonist activity at human FXR LBD iexpressed in monkey CV-1 cells assessed as transactivation of luciferase reporter gene expression	F	7.19	pEC50	65	nM	EC50	Bioorg Med Chem Lett (2011) 21: 1206-1213 [PMID:21256005]
ChEMBL	Agonist activity at human FXR LBD transfected in african green monkey CV1 cells after overnight incubation by luciferase reporter gene assay	F	7.19	pEC50	65	nM	EC50	Bioorg Med Chem Lett (2011) 21: 6154-6160 [PMID:21890356]
ChEMBL	Agonist activity at FXR-LBD (unknown origin) assessed by ligand binding ability incubated for 3 hrs in absence of light measured by TR-FRET Coactivator assay	B	7.19	pEC50	65	nM	EC50	Eur J Med Chem (2021) 211: 113106-113106 [PMID:33360559]
ChEMBL	Increase in human FXR-mediated transient transcription of luciferase reporter gene transfected in african green monkey CV1 cells	B	7.19	pEC50	65	nM	EC50	Bioorg Med Chem Lett (2009) 19: 4733-4739 [PMID:19586769]
ChEMBL	Agonist activity at FXR (unknown origin) transfected into african green monkey CV1 cells assessed as ligand-mediated transcription by luciferase reporter/ transient transfection assay	B	7.19	pEC50	65	nM	EC50	Bioorg Med Chem Lett (2015) 25: 280-284 [PMID:25499883]
ChEMBL	Agonist activity at human FXR transfected in african green monkey CV1 cells by luciferase reporter gene transient transfection assay	F	7.19	pEC50	65	nM	EC50	Bioorg Med Chem Lett (2009) 19: 2969-2973 [PMID:19410460]
ChEMBL	Agonist activity at FXR expressed in african green monkey CV1 cells by luciferase reporter transient transfection assay	F	7.19	pEC50	65	nM	EC50	Bioorg Med Chem Lett (2008) 18: 4339-4343 [PMID:18621523]
ChEMBL	Agonist activity at human amino-terminal polyhistidine-tagged FXR alpha LBD (amino acids 237 to 472) assessed as cofactor peptide SRC-1 interaction with receptor ligand binding domain after 2 hrs by FRET assay	B	7.23	pEC50	59	nM	EC50	Bioorg Med Chem Lett (2011) 21: 6154-6160 [PMID:21890356]
ChEMBL	Agonist activity at human FXR assessed as SRC1 peptide interaction with receptor ligand binding domain by FRET assay	B	7.23	pEC50	59	nM	EC50	Bioorg Med Chem Lett (2009) 19: 2969-2973 [PMID:19410460]
ChEMBL	Agonist activity at human FXR LBD assessed as SRC1 peptide recruitment by FRET assay	F	7.23	pEC50	59	nM	EC50	Bioorg Med Chem Lett (2011) 21: 1206-1213 [PMID:21256005]
ChEMBL	Agonist activity at FXR (unknown origin) assessed as ligand-mediated interaction of the SRC1 peptide with protein LBD by FRET assay	B	7.23	pEC50	59	nM	EC50	Bioorg Med Chem Lett (2015) 25: 280-284 [PMID:25499883]
ChEMBL	Induction of SRC1 coactivator peptide binding to ligand binding domain of human FXR by FRET assay	B	7.23	pEC50	59	nM	EC50	Bioorg Med Chem Lett (2009) 19: 4733-4739 [PMID:19586769]
ChEMBL	Agonist activity at FXR assessed as receptor-SRC-1 peptide interaction by FRET assay	F	7.23	pEC50	59	nM	EC50	Bioorg Med Chem Lett (2008) 18: 4339-4343 [PMID:18621523]
ChEMBL	Agonist activity at human FXR assessed as recruitment of SRC1 peptide by TR-FRET assay	B	7.35	pEC50	45	nM	EC50	Bioorg Med Chem (2013) 21: 4266-4278 [PMID:23688559]
ChEMBL	Agonist activity at FXR (unknown origin)	B	7.43	pEC50	37	nM	EC50	Eur J Med Chem (2020) 197: 112311-112311 [PMID:32339855]
ChEMBL	Effective concentration against Farnesoid X receptor (FXR)	B	7.43	pEC50	37	nM	EC50	J Med Chem (2002) 45: 3569-3572 [PMID:12166927]
ChEMBL	Agonist activity at C-terminal Gal4-tagged human FXR (187 to 472 residues) expressed in HEK-293 cells co-expressing pFRluc by mammalian one hybrid assay	B	7.46	pEC50	35	nM	EC50	Bioorg Med Chem Lett (2016) 26: 3746-3753 [PMID:27268696]
ChEMBL	Agonist activity at human GST-fused FXR LBD expressed in HEK293 cells coexpressing GAL4-DNA bindig domain and pFRluc by mammalian one-hybrid assay	F	7.46	pEC50	35	nM	EC50	Bioorg Med Chem Lett (2010) 20: 4911-4917 [PMID:20638278]
ChEMBL	Agonist activity at human full length FXR transfected in HEK293 cells coexpressing pTRexDest/pGL2promotor assessed as luciferase activity by direct reporter cellular assay	F	7.52	pEC50	30	nM	EC50	Bioorg Med Chem Lett (2010) 20: 4911-4917 [PMID:20638278]
ChEMBL	Binding affinity for human Farnesoid X receptor in FRET assay	B	7.52	pEC50	30	nM	EC50	J Med Chem (2004) 47: 4559-4569 [PMID:15317466]
ChEMBL	Agonist activity at FXR-LBD (unknown origin) assessed as induction of coactivator SRC-1 peptide recruitment measured by TR-FRET assay	B	7.57	pEC50	26.73	nM	EC50	Eur J Med Chem (2022) 230: 114089-114089 [PMID:34998040]
ChEMBL	Agonist activity at human FXR expressed in HEK293 cells by luciferase reporter gene assay	B	7.59	pEC50	26	nM	EC50	Bioorg Med Chem Lett (2014) 24: 5265-5267 [PMID:25305688]
ChEMBL	Agonist activity at human FXR expressed in human Huh-7 cells co-transfected with FXRE-Luc reporter plasmid assessed as receptor transactivation incubated for 16 hrs by luciferase reporter gene assay	B	7.65	pEC50	22.3	nM	EC50	Bioorg Med Chem (2021) 43: 116280-116280 [PMID:34256254]
ChEMBL	Transactivation of human FXR (unknown origin) expressed in HepG2 cells co-expressing pSG5RXR/pGL4.70 after 24 hrs post transfection by luciferase reporter gene assay	B	7.7	pEC50	20	nM	EC50	ACS Med Chem Lett (2019) 10: 407-412 [PMID:30996771]
ChEMBL	Agonist activity at GST-tagged FXR LBD (187 to 472 residues) (unknown origin) assessed as FXR interaction with b-CPSSHSSLTERHKILHRLLQEGSPS-COOH by FRET assay	B	7.7	pEC50	20	nM	EC50	Bioorg Med Chem Lett (2016) 26: 3746-3753 [PMID:27268696]
ChEMBL	Agonist activity at human GST-fused FXR LBD assessed as cofactor peptide interaction with receptor ligand binding domain by FRET assay	B	7.7	pEC50	20	nM	EC50	Bioorg Med Chem Lett (2010) 20: 4911-4917 [PMID:20638278]
ChEMBL	Agonist activity at recombinant human GST-tagged FXR ligand binding domain (193 to 472 residues) expressed in baculovirus infected insect cells assessed as induction of interaction with biotin labelled SRC-1 after 1 hr by HTRF assay	B	7.72	pEC50	19	nM	EC50	J Med Chem (2017) 60: 9960-9973 [PMID:29148806]
GtoPdb	-	-	7.8	pEC50	-	-	-	J Med Chem (2000) 43: 2971-4 [PMID:10956205]
ChEMBL	Agonist activity at FXR	F	7.82	pEC50	15	nM	EC50	Bioorg Med Chem Lett (2012) 22: 6848-6853 [PMID:23040732]
ChEMBL	Ligand dependent recruitment of SRC1(676-700) peptide to human Farnesoid X-activated receptor by fluorescence resonance energy transfer assay	B	7.82	pEC50	15	nM	EC50	J Med Chem (2000) 43: 2971-2974 [PMID:10956205]
ChEMBL	Agonist activity at FXR (unknown origin) by coactivator recruitment assay	B	7.82	pEC50	15	nM	EC50	Bioorg Med Chem (2014) 22: 2447-2460 [PMID:24685112]
ChEMBL	Agonist activity at FXR (unknown origin)	B	7.82	pEC50	15	nM	EC50	J Med Chem (2020) 63: 5031-5073 [PMID:31930920]
ChEMBL	Agonist activity at human FXR expressed in human HuH7 cells by luciferase reporter gene assay	B	7.88	pEC50	13.2	nM	EC50	Bioorg Med Chem (2020) 28: 115512-115512 [PMID:32616182]
ChEMBL	Agonist activity at human FXR expressed in HEK293 cells measured after 18 hrs by steady-glo luciferase reporter gene assay	B	7.92	pEC50	12	nM	EC50	J Med Chem (2020) 63: 12748-12772 [PMID:32991173]
Vitamin D receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1977] [GtoPdb: 605] [UniProtKB: P11473]
ChEMBL	Antagonist activity at human VDR transfected in HEK293T cells measured after 24 hrs by luciferase reporter gene assay	B	5	pIC50	>10000	nM	IC50	Bioorg Med Chem (2020) 28: 115512-115512 [PMID:32616182]

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]