methyl-piperidino-pyrazole [Ligand Id: 3459] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL520107 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Estrogen receptor-α/Estrogen receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372] | ||||||||
| ChEMBL | Inhibition of ERalpha in human MCF7 cells | B | 8.57 | pKi | 2.7 | nM | Ki | Eur J Med Chem (2019) 177: 116-143 [PMID:31129450] |
| GtoPdb | - | - | 8.57 | pKi | 2.7 | nM | Ki | Endocrinology (2002) 143: 941-7 [PMID:11861516] |
| ChEMBL | Antagonist activity at human ERalpha receptor expressed in HEC1 cells assessed as transcriptional activation after 24 hrs by luciferase reporter gene assay | F | 7.1 | pIC50 | 80 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 108-110 [PMID:19014882] |
| Estrogen receptor-β/Estrogen receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL242] [GtoPdb: 621] [UniProtKB: Q92731] | ||||||||
| ChEMBL | Inhibition of ERbeta in human MCF7 cells | B | 5.74 | pKi | 1800 | nM | Ki | Eur J Med Chem (2019) 177: 116-143 [PMID:31129450] |
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]
