XCT790 [Ligand Id: 2832] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL189753 (XCT790) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Estrogen-related receptor-α/Estrogen-related receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3429] [GtoPdb: 622] [UniProtKB: P11474] | ||||||||
| ChEMBL | Inhibition of estrogen-related receptor alpha Gal4 activity | B | 6.43 | pIC50 | 370 | nM | IC50 | J Med Chem (2004) 47: 5593-5596 [PMID:15509154] |
| ChEMBL | Antagonist activity at ERRalpha LBD expressed in HEK293 cells assessed as Gal4-SRC2 interaction by two hybrid luciferase reporter gene assay | F | 6.43 | pIC50 | 370 | nM | IC50 | J Med Chem (2011) 54: 788-808 [PMID:21218783] |
| ChEMBL | Inverse agonist activity at GAL4-fused ERRalpha (unknown origin) transfected in african green monkey CV1 cells after 24 hrs by luciferase reporter gene assay | B | 6.43 | pIC50 | 370 | nM | IC50 | J Med Chem (2013) 56: 4631-4640 [PMID:23656512] |
| ChEMBL | Inverse agonist activity at CMX-gal4-fused ERRgamma (unknown origin) transfected in (African Green monkey CV1 cells incubated for 20 hrs by luciferase reporter gene assay | B | 6.43 | pIC50 | 370 | nM | IC50 | ACS Med Chem Lett (2019) 10: 767-772 [PMID:31097997] |
| GtoPdb | - | - | 6.5 | pIC50 | - | - | IC50 | Proc Natl Acad Sci USA (2004) 101: 8912-7 [PMID:15184675] |
| ChEMBL | Inverse agonist activity at GAL4-DNA binding domain-fused human ERRalpha ligand binding domain expressed in HEK293 cells assessed as inhibition of transcriptional activity after 48 hrs by luciferase reporter gene assay | B | 6.57 | pIC50 | 270 | nM | IC50 | Eur J Med Chem (2017) 136: 457-467 [PMID:28525844] |
| ChEMBL | Binding affinity to GST-tagged ERRalpha-LBD (unknown origin) using fluorescein-conjugated coactivator PGC-1alpha incubated for 1 hr by TR-FRET assay | B | 7.21 | pIC50 | 61.33 | nM | IC50 | ACS Med Chem Lett (2019) 10: 767-772 [PMID:31097997] |
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]
