flutamide [Ligand Id: 6943] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL806 (Chimax, Drogenil, Eulexin, Flutamide, NSC-215876, SCH 13521, SCH-13521) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| 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 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]
