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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 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]