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ChEMBL ligand: CHEMBL1370 (Aircort, Budeflam aquanase, Budelin novolizer, Budenofalk, Budesonide, Cortiment, Duoresp spiromax, Entocort, Entocort cr, Entocort ec, MAP0010, MAP-0010, NSC-757788, Ortikos, Preferid, Pulmaxan, Pulmicort, Pulmicort flexhaler, Pulmicort l.s., Pulmicort respules, R01AD05, Rhinocort, Rhinocort allergy, Rhinocort aqua, Rhinocort aqua 64, S-1320, Symbicort, Tarpeyo, Uceris) |
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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 | 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] |
ChEMBL | Agonist activity at GR (unknown origin) by Alpha Screen assay | B | 8.7 | pEC50 | 2 | nM | EC50 | Medchemcomm (2019) 10: 1412-1419 [PMID:31673308] |
ChEMBL | Agonist activity at human GR | B | 8.7 | pEC50 | 2 | nM | EC50 | J Med Chem (2016) 59: 9201-9214 [PMID:27652492] |
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] |
Interleukin 5 receptor, α subunit/Interleukin-5 receptor subunit alpha in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523198] [GtoPdb: 1706] [UniProtKB: P21183] | ||||||||
ChEMBL | Inhibition of IL-5 receptor in mouse pro-B Y16 cells assessed as decrease in mIL-5 dependent cell proliferation after 48 hrs in presence of 3 units/ml mIL-5 by WST-1 assay | B | 4.58 | pIC50 | 26200 | nM | IC50 | Eur J Med Chem (2019) 181: 111574-111574 [PMID:31400705] |
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 32:
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]