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ChEMBL ligand: CHEMBL196585 (SJ000143975) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Androgen receptor/Androgen Receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207] | ||||||||
ChEMBL | Inhibitory concentration against recombinant rat androgen receptor expressed in Escherichia coli using [3H]methyltrienolone (R 1881) | B | 5.04 | pIC50 | 9120.11 | nM | IC50 | J Med Chem (2005) 48: 5666-5674 [PMID:16134935] |
Estrogen receptor-α/Estrogen receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372] | ||||||||
ChEMBL | Displacement of [3H]17-beta estradiol from GST-fused human recombinant ERalpha ligand binding domain expressed in Escherichia coli BL21alpha cells incubated for 1 hr by liquid scintillation counting method | B | 7.36 | pIC50 | 43.4 | nM | IC50 | Bioorg Med Chem (2020) 28: 115274-115274 [PMID:31879182] |
ChEMBL | Agonist activity at ERalpha (unknown origin) expressed in human HeLa cells assessed as transcriptional activation measured after 24 hrs by luciferase reporter gene assay | B | 7.51 | pEC50 | 30.7 | nM | EC50 | Bioorg Med Chem (2020) 28: 115274-115274 [PMID:31879182] |
Estrogen receptor-β/Estrogen receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL242] [GtoPdb: 621] [UniProtKB: Q92731] | ||||||||
ChEMBL | Antagonist activity at ERbeta (unknown origin) expressed in human HeLa cells assessed as inhibition of E2-induced transcriptional activity measured after 24 hrs by luciferase reporter gene assay based Schild plot analysis | B | 7.95 | pKd | 11.22 | nM | Kd | Bioorg Med Chem (2020) 28: 115274-115274 [PMID:31879182] |
GtoPdb | - | - | 7.64 | pKi | - | - | - | Br J Pharmacol (1999) 126: 810-8 [PMID:10188995] |
ChEMBL | Antagonist activity at ERbeta (unknown origin) expressed in human HeLa cells assessed as inhibition of E2-induced transcriptional activity measured after 24 hrs by luciferase reporter gene assay based Schild plot analysis | B | 7.07 | pIC50 | 85.4 | nM | IC50 | Bioorg Med Chem (2020) 28: 115274-115274 [PMID:31879182] |
ChEMBL | Displacement of [3H]17-beta estradiol from GST-fused human recombinant ERbeta ligand binding domain expressed in Escherichia coli BL21alpha cells incubated for 1 hr by liquid scintillation counting method | B | 7.81 | pIC50 | 15.4 | nM | IC50 | Bioorg Med Chem (2020) 28: 115274-115274 [PMID:31879182] |
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
ChEMBL | ST_JUDE: Plasmodium falciparum 3D7 EC50 (uM) as measured by SYBR green dye | F | 5.4 | pEC50 | 3953.4 | nM | EC50 | Nature (2010) 465: 311-315 [PMID:20485428] |
ChEMBL | ST_JUDE: Plasmodium falciparum K1 EC50 (uM) as measured by SYBR green dye | F | 5.44 | pEC50 | 3596.9 | nM | EC50 | Nature (2010) 465: 311-315 [PMID:20485428] |
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]