4-hydroxytamoxifen [Ligand Id: 2817] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL10041 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| lysine demethylase 1A/Lysine-specific histone demethylase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6136] [GtoPdb: 2669] [UniProtKB: O60341] | ||||||||
| ChEMBL | Inhibition of LSD1 (unknown origin) incubated for 90 mins by fluorescence based assay | B | 4.3 | pIC50 | >50000 | nM | IC50 | Eur J Med Chem (2020) 195: 112281-112281 [PMID:32283297] |
| Estrogen receptor-α in Human [GtoPdb: 620] [UniProtKB: P03372] | ||||||||
| GtoPdb | - | - | 9.85 | pKi | - | - | - | Endocrinology (1997) 138: 863-70 [PMID:9048584] |
| GtoPdb | - | - | 9.85 | pKi | - | - | - | Endocrinology (1997) 138: 863-70 [PMID:9048584] |
| GtoPdb | - | - | 8.7 | pIC50 | 2 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 821-4 [PMID:16307879] |
| Estrogen receptor-β in Human [GtoPdb: 621] [UniProtKB: Q92731] | ||||||||
| GtoPdb | - | - | 10.6 | pKi | - | - | - | Endocrinology (1997) 138: 863-70 [PMID:9048584] |
| Estrogen-related receptor-γ in Human [GtoPdb: 624] [UniProtKB: P62508] | ||||||||
| GtoPdb | - | - | 7.46 | pKd | 35 | nM | Kd | Proc Natl Acad Sci USA (2001) 98: 8880-4 [PMID:11447273] |
| GtoPdb | - | - | 7.89 | pIC50 | 13 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 821-4 [PMID:16307879] |
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]
