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 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]