ChEMBL ligand: CHEMBL1370 (Cortiment, Rhinocort, Entocort cr, Budesonida, Pulmicort, MAP0010, Entocort ec, Duoresp spiromax, Pulmicort flexhaler, Rhinocort aqua 64, Budelin novolizer, Pulmaxan, R01AD05, Ortikos, Budesonide component of symbicort, Budesonide component of airsupra, S-1320, Budesonide component of breztri, Pulmicort respules, Aircort, Symbicort, Entocort, Pulmicort l.s., Rhinocort aqua, MAP-0010, Tarpeyo, Jorveza, Kinpeygo, Budesonide, Uceris, Preferid, NSC-757788, Budeflam aquanase, Budenofalk, Rhinocort allergy, Budesonide component of uceris, Eohilia)
Androgen receptor in Rat [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207] There should be some charts here, you may need to enable JavaScript!
Estrogen receptor-α/Estrogen receptor in Human [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372] There should be some charts here, you may need to enable JavaScript!
Estrogen receptor-β/Estrogen receptor beta in Human [ChEMBL: CHEMBL242] [GtoPdb: 621] [UniProtKB: Q92731] There should be some charts here, you may need to enable JavaScript!
Glucocorticoid receptor in Human [ChEMBL: CHEMBL2034] [GtoPdb: 625] [UniProtKB: P04150] Glucocorticoid receptor in Rat [ChEMBL: CHEMBL3368] [GtoPdb: 625] [UniProtKB: P06536] There should be some charts here, you may need to enable JavaScript!
Interleukin-5 in Human [ChEMBL: CHEMBL1169600] [UniProtKB: P05113] Interleukin-5 in Mouse [ChEMBL: CHEMBL1163111] [UniProtKB: P04401] There should be some charts here, you may need to enable JavaScript!
Interleukin 5 receptor, α subunit/Interleukin-5 receptor subunit alpha in Mouse [ChEMBL: CHEMBL4523198] [GtoPdb: 1706] [UniProtKB: P21183] There should be some charts here, you may need to enable JavaScript!
MMP9/Matrix metalloproteinase-9 in Human [ChEMBL: CHEMBL321] [GtoPdb: 1633] [UniProtKB: P14780] There should be some charts here, you may need to enable JavaScript!
Mineralocorticoid receptor in Human [ChEMBL: CHEMBL1994] [GtoPdb: 626] [UniProtKB: P08235] There should be some charts here, you may need to enable JavaScript!
Plasmodium falciparum [ChEMBL: CHEMBL364] There should be some charts here, you may need to enable JavaScript!
Progesterone receptor in Human [ChEMBL: CHEMBL208] [GtoPdb: 627] [UniProtKB: P06401] Progesterone receptor in Bovine [ChEMBL: CHEMBL1909044] [UniProtKB: Q690N0] 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 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 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	Glucocorticoid Receptor Competitor Assay: The potency of binding to gucocorticoid receptor by small molecule compounds was measured with the PolarScreen™ Glucocorticoid Receptor Competitor Assay Kit, Red (Life Technology, Catalog #A15898) according to the procedure in the kit. In brief, after compounds were diluted and transferred into assay plates, the fluormone GS red and GR full length protein were subsequently added into the assay plates, along with the positive and negative controls. The samples were mixed on a shaker for 1 minute and then the plates were incubated at room temperature for 2-4 hours with minimal light exposure. The plates were read with an Envision and the relative fluorescent signals were calculated. The data were plotted in GraphPad Prism and the EC50 values were calculated with non-linear regression curve fit of the data in GraphPad Prism.	B	9.05	pIC50	0.9	nM	IC50	US-11554172-B2. Phosphonate linkers and their use to facilitate cellular retention of compounds (2023)
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 36:

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]