camizestrant [Ligand Id: 12716] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4650365 (AZ-14066724, AZ14066724, Azd9833, AZD-9833, AZD9833, Camizestrant)
  • Estrogen receptor-α/Estrogen receptor alpha in Human [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372]
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  • H3 receptor/Histamine H3 receptor in Human [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
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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 Agonist activity at ERalpha in human MCF7 cells assessed as increase in progesterone receptor expression level by western blot analysis B 6.5 pIC50 >316.23 nM IC50 J Med Chem (2020) 63: 14530-14559 [PMID:32910656]
ChEMBL Induction of ERalpha degradation in human MCF7 cells assessed as decrease in ERalpha expression in presence of tamoxifen by Western blot analysis B 8.2 pIC50 6.31 nM IC50 J Med Chem (2020) 63: 14530-14559 [PMID:32910656]
ChEMBL Displacement of fluormone ES2 green reagent from human GST-tagged ERalpha LBD (282 to 595 residues) expressed in baculovirus infected insect cells incubated for 1 hrs by TR-FRET Lanthascreen assay B 8.6 pIC50 2.51 nM IC50 J Med Chem (2020) 63: 14530-14559 [PMID:32910656]
ChEMBL Displacement of fluorescent labelled fluormone ES2 from human recombinant GST tagged ER alpha LBD ( 282 to 595 residues) expressed in baculovirus infected insect cells incubate for 20 mins measured after 1 hr by TR-FRET Lanthascreen assay B 8.6 pIC50 2.51 nM IC50 ACS Med Chem Lett (2020) 11: 2519-2525 [PMID:33335676]
ChEMBL Induction of ERalpha degradation in human MCF7 cells incubated for 18 to 22 hrs by immuno-fluorescence assay B 9.8 pIC50 0.16 nM IC50 ACS Med Chem Lett (2020) 11: 2519-2525 [PMID:33335676]
ChEMBL Induction of ERalpha degradation in human MCF7 cells assessed as decrease in ERalpha expression by Western blot analysis B 9.8 pIC50 0.16 nM IC50 J Med Chem (2020) 63: 14530-14559 [PMID:32910656]
ChEMBL Induction of ERalpha degradation in human MCF7 cells assessed as decrease in ER-alpha level incubated for 18 to 24 hrs by Alexa fluor 488/Hoechst staining based immunofluorescence imaging analysis B 9.8 pIC50 0.16 nM IC50 J Med Chem (2020) 63: 14530-14559 [PMID:32910656]
GtoPdb - - 9.8 pIC50 0.16 nM IC50 J Med Chem (2020) 63: 14530-14559 [PMID:32910656]
ChEMBL Induction of ERalpha degradation in human MCF7 cells assessed as decrease in ERalpha expression in presence of cycloheximide by Western blot analysis B 9.9 pIC50 0.13 nM IC50 J Med Chem (2020) 63: 14530-14559 [PMID:32910656]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG by plate-based planar patch clamp technique B 4.66 pIC50 22000 nM IC50 J Med Chem (2020) 63: 14530-14559 [PMID:32910656]
H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
ChEMBL Antagonist activity at human histamine H3 receptor expressed in CHO-K1 cells after 10 mins by HTRF assay B 6.48 pIC50 330 nM IC50 J Med Chem (2020) 63: 14530-14559 [PMID:32910656]

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]