LG190178 [Ligand Id: 2787] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL197589 (LG-190178) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Androgen receptor/Androgen Receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275] | ||||||||
| ChEMBL | Antagonist activity at human androgen receptor expressed in HEK293 cells assessed as inhibition of transcriptional activity by luciferase and beta-galactosidase reporter gene assay | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem (2013) 21: 1643-1651 [PMID:23462715] |
| Androgen receptor/Androgen Receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3056] [GtoPdb: 628] [UniProtKB: P19091] | ||||||||
| ChEMBL | Androgen antagonistic activity as inhibitory concentration against testosterone-induced SC-3 cell proliferation | F | 7.72 | pIC50 | 19 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 4327-4331 [PMID:16019211] |
| Vitamin D receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1977] [GtoPdb: 605] [UniProtKB: P11473] | ||||||||
| GtoPdb | - | - | 6.82 | pKi | - | - | - | Chem Biol (1999) 6: 265-75 [PMID:10322128] |
| ChEMBL | Agonist activity at VDR (unknown origin) by reporter gene assay | B | 7.4 | pEC50 | 40 | nM | EC50 | Bioorg Med Chem (2013) 21: 1643-1651 [PMID:23462715] |
| Vitamin D receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5601] [UniProtKB: P48281] | ||||||||
| ChEMBL | Activation of VDR in mouse ASZ001 cells assessed as change in Cyp24A1 mRNA expression after 48 hrs by q-PCR analysis | B | 8.11 | pEC50 | 7.7 | nM | EC50 | Eur J Med Chem (2019) 162: 495-506 [PMID:30471551] |
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]
