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ChEMBL ligand: CHEMBL1370 (Aircort, Budeflam aquanase, Budelin novolizer, Budenofalk, Budesonide, Cortiment, Duoresp spiromax, Entocort, Entocort cr, Entocort ec, Jorveza, MAP-0010, MAP0010, 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 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]