methyl-piperidino-pyrazole [Ligand Id: 3459] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL520107
  • Estrogen receptor-α/Estrogen receptor alpha in Human [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372]
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  • Estrogen receptor-β/Estrogen receptor beta in Human [ChEMBL: CHEMBL242] [GtoPdb: 621] [UniProtKB: Q92731]
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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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]