flutamide [Ligand Id: 6943] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL806 (Chimax, Drogenil, Eulexin, Flutamide, NSC-215876, SCH 13521, SCH-13521) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Androgen receptor/Androgen Receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275] | ||||||||
| GtoPdb | - | - | 5.43 | pKi | 3700 | nM | Ki | Bioorg Med Chem (2008) 16: 6799-812 [PMID:18571420] |
| ChEMBL | Displacement of [3H]testosterone from wild type human androgen receptor | B | 5.43 | pKi | 3700 | nM | Ki | Bioorg Med Chem (2008) 16: 6799-6812 [PMID:18571420] |
| ChEMBL | Binding affinity against GST-hARLBD was measured in SC-3 cell by using [3H]testosterone as radioligand | B | 5.89 | pKi | 1300 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 2655-2658 [PMID:12873487] |
| ChEMBL | Antagonist activity at wild type human recombinant androgen receptor assessed as inhibition of testosterone-induced growth of mouse androgen dependent SC3 cells by WST-1 method | F | 5.38 | pIC50 | 4200 | nM | IC50 | Bioorg Med Chem (2008) 16: 6799-6812 [PMID:18571420] |
| ChEMBL | Antiandrogenic activity in human MDA-MB-453 cells expressing androgen receptor assessed as inhibition of DHT-induced androgen-dependent transcription by luciferase reporter gene assay | B | 5.7 | pIC50 | 2000 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 1218-1223 [PMID:19131248] |
| ChEMBL | Antagonist activity at AR in human MDA-kb2 cells co-transfected with MMTV-luc assessed as decrease in DHT-induced luciferase activity by reporter gene assay | F | 6 | pIC50 | 1000 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 2111-2114 [PMID:20226658] |
| ChEMBL | Antagonist activity at human androgen receptor expressed in mouse NIH3T3 cells assessed as inhibition of DHT-induced transcriptional activation after 24 hrs by androgen response element-mediated luciferase reporter gene assay | F | 6.24 | pIC50 | 580 | nM | IC50 | Bioorg Med Chem (2008) 16: 8022-8028 [PMID:18707892] |
| ChEMBL | Inhibition of 1.0 nM [3H]mibolerone binding to human androgen receptor of PC3/AR cell lysate | B | 6.81 | pIC50 | 154 | nM | IC50 | J Med Chem (2003) 46: 5258-5270 [PMID:14613328] |
| ChEMBL | Inhibition of [3H]mibolerone binding to human Androgen receptor of PC3/AR Cell Lysate | B | 6.81 | pIC50 | 154 | nM | IC50 | J Med Chem (2004) 47: 5690-5699 [PMID:15509168] |
| Androgen receptor/Androgen Receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207] | ||||||||
| ChEMBL | DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone) | B | 5.05 | pKi | 8927 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone) | B | 4.87 | pIC50 | 13390 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| ABCB11/Bile salt export pump in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073674] [GtoPdb: 778] [UniProtKB: O70127] | ||||||||
| ChEMBL | Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake | B | 4.1 | pIC50 | 78700 | nM | IC50 | Drug Metab Dispos (2012) 40: 130-138 [PMID:21965623] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay | F | 4.9 | pIC50 | 12589.25 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay | F | 4.9 | pIC50 | 12589.25 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay | F | 4.9 | pIC50 | 12589.25 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| Serotonin 4 (5-HT4) receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5017] [UniProtKB: O70528] | ||||||||
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808) | B | 5.65 | pKi | 2258 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808) | B | 4.87 | pIC50 | 13545 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406] | ||||||||
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) | B | 5.08 | pKi | 8271 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) | B | 4.75 | pIC50 | 17814 | nM | IC50 | DrugMatrix in vitro pharmacology data |
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]
