cortisol [Ligand Id: 2868] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL389621 (Nutracort, Hydrocortisone component of xerese, Hydrocortisone component of calmurid hc, Hydrocortisone component of achromycin, Hydrocortisone component of alphaderm, Ala-scalp, Acetasol hc, Hydrocortisone component of vosol hc, Hydrocortisone component of otobione, Proctofoam hc, Alkindi sprinkle, Efcortelan p, Alphaderm, Texacort, Cortef, Cipro hc, Mildison lipocream, Hc #1, Hydrocort in calamine oily, Hydrocortisone in absorbase, Cortisol, FLEXICORT, Synacort, Hydrocortisone component of otobiotic, U-cort, Anflam, Uniroid, Hydro-rx, Zenoxone, Dioderm, Hc #4, Otosporin, Anusol soothing relief, Exe-cort, Efmody, Anucort-hc, Nogenic hc, Dermacort, Hidrocortisona, Daktacort hydrocort, Hydrocortisone component of oticair, Aeroseb-hc, Tri-cicatrin, Eurax-hc, Gregoderm, H-cort, Quinocort, Penecort, Hytone, Colocort, Hydrocortisone component of cortisporin, Calmurid hc, Cobadex, Ophthocort, Proctosedyl, Corlan, Cort-dome, Eldecort, Dome-cort, Hc (hydrocortisone), Hydrocortisone component of pediotic, Germoloids hc, Hydrocortisone, Terra-cortril nystatin, Cetacort, Perinal, Xyloproct, Uniroid hc, Anusol-hc, Hydrocort in cetomacrogol for a, Daktacort, Hydrocort in wte soft paraf, Flexicort, Hydroderm, Beta-hc, Timodine, Epicort, Alkindi, Topisone, Medicort, Plenadren, Evacort, Eurax-hydrocort, Hydrocortisone component of acetasol hc, Hydrocortisone component of otocort, Hydrocortisone component of orlex hc, Glycort, Hi-cor, Otoseptil, Dermaspray demang, Sential hc, Ala-cort, Cortril, Derma care hydrocort, Cortenema, Nystaform-hc, Anugesic hc, Cortenem, Jungle for, Hydrocortisone component of pyocidin, Proctocream hc, Hydrocortone, Balneol-hc, NSC-10483, Nybadex, Timocort, Econacort, Hydroderm hc, Acticort, Stie-cort, Anusol hc, Anusol plus hc, Proctocort, Canesten hc, Cor-oticin) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| ABCB1/ATP-dependent translocase ABCB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183] | ||||||||
| ChEMBL | Inhibition of P-glycoprotein using calcein-AM assay transfected in porcine PBCEC | F | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2003) 46: 1716-1725 [PMID:12699389] |
| ChEMBL | Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay | F | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2003) 46: 1716-1725 [PMID:12699389] |
| ChEMBL | TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells | F | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2003) 46: 1716-1725 [PMID:12699389] |
| ABCB1/ATP-dependent translocase ABCB1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2573] [GtoPdb: 768] [UniProtKB: P21447] | ||||||||
| ChEMBL | Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay | F | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2003) 46: 1716-1725 [PMID:12699389] |
| ChEMBL | TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells | F | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2003) 46: 1716-1725 [PMID:12699389] |
| Corticosteroid-binding globulin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2421] [UniProtKB: P08185] | ||||||||
| ChEMBL | In silico binding affinity to human corticosteriod binding globulin | B | 6.88 | pKd | 6.88 | - | -Log Kdiss | J Med Chem (1997) 40: 3161-3172 [PMID:9379435] |
| ChEMBL | Binding affinity to human CBG receptor (corticosteroid-binding globulins) | B | 7.88 | pKi | 13.18 | nM | Ki | J Med Chem (2004) 47: 2732-2742 [PMID:15139751] |
| Glucocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034] [GtoPdb: 625] [UniProtKB: P04150] | ||||||||
| ChEMBL | DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone) | B | 7.92 | pKi | 12 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone) | B | 7.59 | pIC50 | 26 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| GtoPdb | - | - | 8 | pIC50 | - | - | - |
Eur J Pharmacol (1993) 247: 145-54 [PMID:8282004]; FEBS Lett (1999) 464: 9-13 [PMID:10611474]; J Biol Chem (2000) 275: 19041-9 [PMID:10747884] |
| Glucocorticoid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3144] [GtoPdb: 625] [UniProtKB: P06537] | ||||||||
| ChEMBL | Displacement of 1 x 10'-8 M of [1,2,3-3H]-triamcinolone acetonide from glucocorticoid receptor in soluble fraction of mouse L929 cells after 20 hrs | B | 7.37 | pKd | 43 | nM | Kd | J Med Chem (1977) 20: 1134-1139 [PMID:926113] |
| Glucocorticoid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3368] [GtoPdb: 625] [UniProtKB: P06536] | ||||||||
| ChEMBL | Agonist activity at glucocorticoid receptor in rat INS-1 832/13 cells transfected with CCL2-promoter luciferase plasmid construct assessed as reduction in IL-1 beta induced inflammation by luciferase reporter gene assay | B | 6.5 | pIC50 | 316.23 | nM | IC50 | ACS Med Chem Lett (2022) 13: 1493-1499 [PMID:36105346] |
| ChEMBL | Agonist activity at glucocorticoid receptor in rat INS-1 832/13 cells transfected with CCL2-promoter luciferase plasmid construct assessed as reduction in IL-1 beta induced inflammation by luciferase reporter gene assay | B | 7.6 | pIC50 | 25.12 | nM | IC50 | ACS Med Chem Lett (2021) 12: 1568-1577 [PMID:34676039] |
| ChEMBL | Agonist activity at glucocorticoid receptor in rat INS-1 832/13 cells transfected with 3XGRE-promoter luciferase plasmid construct assessed as induction of receptor transactivation by luciferase reporter gene assay | B | 5.6 | pEC50 | 2511.89 | nM | EC50 | ACS Med Chem Lett (2021) 12: 1568-1577 [PMID:34676039] |
| ChEMBL | Agonist activity at glucocorticoid receptor in rat INS-1 832/13 cells transfected with 3XGRE-promoter luciferase plasmid construct assessed as induction of receptor transactivation by luciferase reporter gene assay | B | 7 | pEC50 | 100 | nM | EC50 | ACS Med Chem Lett (2022) 13: 1493-1499 [PMID:36105346] |
| Mineralocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1994] [GtoPdb: 626] [UniProtKB: P08235] | ||||||||
| ChEMBL | Binding affinity to MR (unknown origin) | B | 9.3 | pKd | 0.5 | nM | Kd | J Med Chem (2017) 60: 2629-2650 [PMID:28051871] |
| GtoPdb | - | - | 9.95 | pIC50 | - | - | - |
Eur J Pharmacol (1993) 247: 145-54 [PMID:8282004]; FEBS Lett (1999) 464: 9-13 [PMID:10611474] |
| ChEMBL | Mineralocorticoid Receptor Transactivation Potencies for Cortisol and 17-ester Derivatives: Mineralocorticoid receptor (MR) activation potency was assessed using a HEK 293T cell line containing the UAS-bla reporter (UAS-bla HEK 293T CELLSENSOR®). This cell line was stably cotransfected with an expression construct containing β-lactamase cDNA under control of the GAL4 Upstream Activator Sequence (UAS) and another expression construct encoding for the fusion protein GAL4(DBD)-MR(LBD). Results for one experiment performed in duplicate for 9 compounds and the control compound, aldosterone, in agonist mode are summarized in Table 4. All assays were performed as 10-point dose responses using a half log-fold dilution series starting with a maximum compound concentration of 100 nM. The compounds were incubated for 16 hours. The activation of the fusion protein GAL4(DBD)-MR(LBD) leads to expression of the reporter β-lactamase which is detected by the conversion of a FRET substrate in a ratiometric assay format. This functional assay allows for measurement of receptor agonism by compounds and can be used to determine compound potency and selectivity. Assay reproducibility was determined by calculating Z′ values for untreated versus maximum stimulation. The Z′ value was greater than 0.6, indicating good reproducibility of the assay format. | B | 8.54 | pEC50 | 2.9 | nM | EC50 | US-10188667-B2. Pharmaceutical compositions and methods of use of 4-pregenen-11β-17-21-triol-3,20-dione derivatives (2019) |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| Sex hormone-binding globulin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3305] [UniProtKB: P04278] | ||||||||
| ChEMBL | Binding affinity towards human testosterone binding globulin. | B | 5.2 | pKd | 5.2 | - | -Log Kdiss | J Med Chem (1997) 40: 3161-3172 [PMID:9379435] |
| ChEMBL | Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | B | 6.2 | pKd | 630.96 | nM | Kd | J Med Chem (2008) 51: 2047-2056 [PMID:18330978] |
| GPR33 in Human [GtoPdb: 100] [UniProtKB: Q49SQ1] | ||||||||
| GtoPdb | Binding affinity of purified mouse Gpr33 oligomers | - | 7.92 | pKd | 11.9 | nM | Kd | Biochem Biophys Res Commun (2025) 764: 151845 [PMID:40253912] |
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]
