flutamide [Ligand Id: 6943] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL806 (Flutamide, NSC-215876, Chimax, SCH-13521, Drogenil, Eulexin)
  • Androgen receptor/Androgen Receptor in Human [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275]
  • Androgen receptor/Androgen Receptor in Rat [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207]
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  • Serotonin 4 (5-HT4) receptor in Guinea pig [ChEMBL: CHEMBL5017] [UniProtKB: O70528]
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  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
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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 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]