budesonide [Ligand Id: 7434] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1370 (Pulmicort, Entocort Ec, Pulmicort Flexhaler, Entocort, Pulmicort Respules, Rhinocort Aqua 64, Rhinocort allergy, Budesonide, Cortiment, Entocort CR, MAP-0010, Pulmaxan, Rhinocort, Ortikos, R01AD05, Symbicort, Budenofalk, Uceris, DuoResp Spiromax, Preferid, MAP0010, Budeflam Aquanase, Rhinocort Aqua, Aircort, Pulmicort L.S., Budelin Novolizer, S-1320)
  • Androgen receptor/Androgen Receptor in Rat [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207]
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  • Estrogen receptor-α/Estrogen receptor alpha in Human [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372]
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  • Estrogen receptor-β/Estrogen receptor beta in Human [ChEMBL: CHEMBL242] [GtoPdb: 621] [UniProtKB: Q92731]
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  • MMP9/Matrix metalloproteinase 9 in Human [ChEMBL: CHEMBL321] [GtoPdb: 1633] [UniProtKB: P14780]
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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 Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207]
ChEMBL DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone) B 5.96 pKi 1090 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone) B 5.79 pIC50 1635 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Displacement of fluormone labelled AL green from rat recombinant His/GST-tagged androgen receptor LBD after 4 to 6 hrs by fluorescence polarization assay B 6.15 pIC50 710 nM IC50 J Med Chem (2017) 60: 8591-8605 [PMID:28937774]
Estrogen receptor-α/Estrogen receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372]
ChEMBL Displacement of fluormone labelled EL Red from human recombinant estrogen receptor alpha after 1 to 5 hrs by fluorescence polarization assay B 5 pIC50 >10000 nM IC50 J Med Chem (2017) 60: 8591-8605 [PMID:28937774]
Estrogen receptor-β/Estrogen receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL242] [GtoPdb: 621] [UniProtKB: Q92731]
ChEMBL Displacement of fluormone labelled EL Red from human recombinant estrogen receptor beta after 1 to 5 hrs by fluorescence polarization assay B 5 pIC50 >10000 nM IC50 J Med Chem (2017) 60: 8591-8605 [PMID:28937774]
Glucocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034] [GtoPdb: 625] [UniProtKB: P04150]
ChEMBL DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone) B 8.69 pKi 2.03 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Displacement of [3H]dexamethasone from human recombinant glucocorticoid receptor expressed in insect cells after 24 hrs by scintillation proximity assay B 8.89 pKi 1.3 nM Ki J Med Chem (2018) 61: 4757-4773 [PMID:29741897]
ChEMBL DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone) B 8.35 pIC50 4.47 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Displacement of fluormone labelled GS Red from human recombinant glucocorticoid receptor after 2 hrs by fluorescence polarization assay B 8.42 pIC50 3.8 nM IC50 J Med Chem (2017) 60: 8591-8605 [PMID:28937774]
ChEMBL Transrepression of glucocorticoid receptor in human PBMC assessed as inhibition of LPS induced TNF alpha release preincubated for 45 mins followed by LPS addition measured after 18 hrs by ELISA B 8.8 pIC50 1.57 nM IC50 J Med Chem (2017) 60: 8591-8605 [PMID:28937774]
ChEMBL Transrepression of glucocorticoid receptor in PMA-stimulated human ChaGoK1 cells expressing TRE-LacZ construct assessed as inhibition of AP-1 mediated TRE-LacZ activity after 24 hrs by beta-galactosidase reporter gene assay B 9.3 pIC50 0.5 nM IC50 J Med Chem (2017) 60: 8591-8605 [PMID:28937774]
GtoPdb - - 7.42 pEC50 38 nM EC50 J. Med. Chem. (2017) 60: 8591-8605 [PMID:28937774]
ChEMBL Agonist activity at GR in human SW1353 cells transfected with luciferase gene linked to MMTV promoter assessed as luciferase transactivation activity F 7.91 pEC50 12.4 nM EC50 Bioorg. Med. Chem. Lett. (2011) 21: 5826-5830 [PMID:21880489]
GtoPdb - - 7.91 pEC50 12.4 nM EC50 Bioorg. Med. Chem. Lett. (2011) 21: 5826-30 [PMID:21880489]
ChEMBL Induction of nuclear translocation of human recombinant ProLabel-tagged glucocorticoid receptor expressed in CHO-K1 cells after 3 hrs by luminescence method B 8.46 pEC50 3.5 nM EC50 J Med Chem (2018) 61: 4757-4773 [PMID:29741897]
Glucocorticoid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3368] [GtoPdb: 625] [UniProtKB: P06536]
ChEMBL Steroid binding against the rat thymus glucocorticoid receptor B 8.54 pIC50 2.9 nM IC50 J. Med. Chem. (1996) 39: 4888-4896 [PMID:8960547]
Interleukin-5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1169600] [UniProtKB: P05113]
ChEMBL Inhibition of interleukin-5 B 4.57 pIC50 26800 nM IC50 Bioorg. Med. Chem. (2010) 18: 4625-4629 [PMID:20627591]
Interleukin-5 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163111] [UniProtKB: P04401]
ChEMBL Inhibition of IL-5 in mouse Y16 cells after 48 hrs by WST1 assay B 4.57 pIC50 27100 nM IC50 Bioorg. Med. Chem. (2012) 20: 5757-5762 [PMID:22954899]
ChEMBL Inhibition of IL-5 in mouse pro-B Y16 cells after 48 hrs by WST1 assay B 4.57 pIC50 27100 nM IC50 Eur. J. Med. Chem. (2013) 59: 31-38 [PMID:23202848]
ChEMBL Inhibition interleukin-5 in mouse Y16 cells after 48 hrs by WST-1 assay B 4.57 pIC50 27100 nM IC50 Bioorg. Med. Chem. (2013) 21: 2543-2550 [PMID:23523388]
ChEMBL Inhibition of IL-5 in mouse Y16 cells assessed as reduction in cell proliferation after 48 hrs by WST-1 assay B 4.58 pIC50 26200 nM IC50 Bioorg Med Chem (2017) 25: 4330-4338 [PMID:28651915]
ChEMBL Inhibition of IL5-mediated proliferation of mouse Y16 cells by WST1 assay B 4.58 pIC50 26200 nM IC50 Bioorg. Med. Chem. (2010) 18: 4441-4445 [PMID:20472438]
ChEMBL Inhibition of mouse IL-5-induced cell proliferation in mouse Y16 cells after 48 hrs by WST-1 assay relative to control B 4.58 pIC50 26200 nM IC50 Eur J Med Chem (2017) 139: 290-304 [PMID:28803045]
ChEMBL Inhibition of interleukin-5 in mouse Y16 cells B 4.58 pIC50 26200 nM IC50 Bioorg. Med. Chem. (2010) 18: 4625-4629 [PMID:20627591]
ChEMBL Inhibition of mouse IL5-mediated mouse Y16 cell proliferation after 48 hrs by WST1 assay B 4.58 pIC50 26200 nM IC50 Bioorg. Med. Chem. (2015) 23: 2498-2504 [PMID:25865130]
MMP9/Matrix metalloproteinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL321] [GtoPdb: 1633] [UniProtKB: P14780]
ChEMBL DRUGMATRIX: Protease, Matrix Metalloprotease-9 (MMP-9) enzyme inhibition (substrate: Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2) B 5.7 pIC50 1989 nM IC50 DrugMatrix in vitro pharmacology data
Mineralocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1994] [GtoPdb: 626] [UniProtKB: P08235]
ChEMBL Displacement of [3H]-aldosterone from N terminal maltose binding protein tagged human mineralocorticoid receptor LBD (726 to 984 residues) expressed in baculovirus infected high five cells after 8 hrs by scintillation proximity assay B 7.85 pIC50 14 nM IC50 J Med Chem (2017) 60: 8591-8605 [PMID:28937774]
GtoPdb - - 7.85 pEC50 14 nM EC50 J. Med. Chem. (2017) 60: 8591-8605 [PMID:28937774]
ChEMBL Induction of nuclear translocation of human recombinant ProLabel-tagged mineralocorticoid receptor expressed in CHO-K1 cells after 3 hrs by luminescence method B 8.32 pEC50 4.8 nM EC50 J Med Chem (2018) 61: 4757-4773 [PMID:29741897]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay F 5.3 pIC50 5011.87 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 5.4 pIC50 3981.07 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 5.5 pIC50 3162.28 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay F 5.5 pIC50 3162.28 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 5.6 pIC50 2511.89 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay F 5.8 pIC50 1584.89 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
Progesterone receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL208] [GtoPdb: 627] [UniProtKB: P06401]
ChEMBL Displacement of fluormone labelled PL Red from human recombinant progesterone receptor after 1 to 6 hrs ligand by fluorescence polarization assay B 7.55 pIC50 28 nM IC50 J Med Chem (2017) 60: 8591-8605 [PMID:28937774]
GtoPdb - - 7.15 pEC50 71 nM EC50 J. Med. Chem. (2017) 60: 8591-8605 [PMID:28937774]
GtoPdb - - 7.55 pEC50 28 nM EC50 J. Med. Chem. (2017) 60: 8591-8605 [PMID:28937774]
Progesterone receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1909044] [UniProtKB: Q690N0]
ChEMBL DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020) B 7.57 pKi 27 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020) B 6.68 pIC50 210 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]