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ChEMBL ligand: CHEMBL318457 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 | 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 FXR (unknown origin) by reporter gene assay | B | 6.05 | pEC50 | 900 | nM | EC50 | Bioorg Med Chem (2014) 22: 2447-2460 [PMID:24685112] |
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 | 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 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 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 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 | 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 FXR (unknown origin) | B | 7.15 | pEC50 | 70 | nM | EC50 | J Med Chem (2019) 62: 2112-2126 [PMID:30702885] |
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 | 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 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 | 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 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 (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 | 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 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 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 | 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 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 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 | 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 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 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 | 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 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 (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 | 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 | F | 7.82 | pEC50 | 15 | nM | EC50 | Bioorg Med Chem Lett (2012) 22: 6848-6853 [PMID:23040732] |
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 33:
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]