prinaberel [Ligand Id: 6700] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL450940 (ERB-041, PF-00913086, Prinaberel)
  • Estrogen receptor-α/Estrogen receptor alpha in Human [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372]
  • Estrogen receptor-α/Estrogen receptor alpha in Mouse [ChEMBL: CHEMBL3065] [GtoPdb: 620] [UniProtKB: P19785]
  • Estrogen receptor-α/Estrogen receptor alpha in Rat [ChEMBL: CHEMBL2724] [GtoPdb: 620] [UniProtKB: P06211]
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  • Estrogen receptor-β/Estrogen receptor beta in Human [ChEMBL: CHEMBL242] [GtoPdb: 621] [UniProtKB: Q92731]
  • Estrogen receptor-β/Estrogen receptor beta in Mouse [ChEMBL: CHEMBL2995] [GtoPdb: 621] [UniProtKB: O08537]
  • Estrogen receptor-β/Estrogen receptor beta in Rat [ChEMBL: CHEMBL3021] [GtoPdb: 621] [UniProtKB: Q62986]
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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 Inhibitory concentration against human ER alpha expressed in Escherichia coli was determined using [3H]17-beta-estradiol as radio ligand B 5.92 pIC50 1216 nM IC50 J Med Chem (2004) 47: 5021-5040 [PMID:15456246]
GtoPdb - - 5.92 pIC50 1216 nM IC50 J Immunol (2008) 180: 630-6 [PMID:18097065]
Estrogen receptor-α/Estrogen receptor alpha in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3065] [GtoPdb: 620] [UniProtKB: P19785]
GtoPdb - - 6.12 pIC50 750 nM IC50 J Immunol (2008) 180: 630-6 [PMID:18097065]
ChEMBL Inhibition of [3H]17-beta-estradiol binding to mouse ER alpha expressed in Escherichia coli B 6.13 pIC50 746 nM IC50 J Med Chem (2004) 47: 5021-5040 [PMID:15456246]
Estrogen receptor-α/Estrogen receptor alpha in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2724] [GtoPdb: 620] [UniProtKB: P06211]
ChEMBL Inhibition of [3H]17-beta-estradiol binding to rat ER alpha expressed in Escherichia coli B 6.21 pIC50 618 nM IC50 J Med Chem (2004) 47: 5021-5040 [PMID:15456246]
GtoPdb - - 6.21 pIC50 620 nM IC50 J Immunol (2008) 180: 630-6 [PMID:18097065]
Estrogen receptor-β/Estrogen receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL242] [GtoPdb: 621] [UniProtKB: Q92731]
GtoPdb - - 8.3 pIC50 5 nM IC50 J Med Chem (2004) 47: 5021-40 [PMID:15456246];
J Immunol (2008) 180: 630-6 [PMID:18097065]
ChEMBL Inhibitory concentration against human ER beta expressed in Escherichia coli was determined using [3H]17-beta-estradiol as radio ligand B 8.3 pIC50 5 nM IC50 J Med Chem (2004) 47: 5021-5040 [PMID:15456246]
ChEMBL Binding affinity to ERbeta B 8.3 pIC50 5 nM IC50 Eur J Med Chem (2008) 43: 43-52 [PMID:17459530]
Estrogen receptor-β/Estrogen receptor beta in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2995] [GtoPdb: 621] [UniProtKB: O08537]
GtoPdb - - 8.43 pIC50 3.7 nM IC50 J Immunol (2008) 180: 630-6 [PMID:18097065]
ChEMBL Inhibition of [3H]17-beta-estradiol binding to mouse ER beta expressed in Escherichia coli B 8.43 pIC50 3.7 nM IC50 J Med Chem (2004) 47: 5021-5040 [PMID:15456246]
Estrogen receptor-β/Estrogen receptor beta in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3021] [GtoPdb: 621] [UniProtKB: Q62986]
ChEMBL Inhibition of [3H]17-beta-estradiol binding to rat ER beta expressed in Escherichia coli B 8.5 pIC50 3.14 nM IC50 J Med Chem (2004) 47: 5021-5040 [PMID:15456246]
GtoPdb - - 8.51 pIC50 3.1 nM IC50 J Immunol (2008) 180: 630-6 [PMID:18097065]

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]