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 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]