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ChEMBL ligand: CHEMBL389621 (Acetasol hc, Acticort, Aeroseb-hc, Ala-cort, Ala-scalp, Alkindi sprinkle, Alphaderm, Anflam, Anucort-Hc, Anugesic hc, Anusol hc, Anusol-Hc, Anusol plus hc, Anusol soothing relief, Balneol-hc, Beta-hc, Calmurid hc, Canesten hc, Cetacort, Cipro hc, Cobadex, Colocort, Corlan, Cor-Oticin, Cort-dome, Cortef, Cortenem, Cortenema, Cortifoam, Cortisol, Cortril, Daktacort, Daktacort hydrocort, Derma care hydrocort, Dermacort, Dermaspray demang, Dioderm, Dome-cort, Econacort, Efcortelan p, Eldecort, Epicort, Eurax-hc, Eurax-hydrocort, Evacort, Exe-cort, Flexicort, FLEXICORT, Germoloids hc, Glycort, Gregoderm, Hc #1, Hc #4, Hc (hydrocortisone), H-cort, Hi-cor, Hydrocort in calamine oily, Hydrocort in cetomacrogol for a, Hydrocort in wte soft paraf, Hydrocortisone, Hydrocortisone in absorbase, Hydrocortone, Hydroderm, Hydroderm hc, Hydro-rx, Hytone, Jungle for, Locoid, Medicort, Micort-HC, Mildison lipocream, Neo-Cortef, Nogenic hc, NSC-10483, Nutracort, Nybadex, Nystaform-hc, Ophthocort, Otoseptil, Otosporin, Penecort, Perinal, Plenadren, Proctocort, Proctocream hc, Proctofoam hc, Proctosedyl, Quinocort, Sential hc, Stie-cort, Synacort, Terra-Cortril, Terra-cortril nystatin, Texacort, Timocort, Timodine, Topisone, Tri-cicatrin, U-Cort, Uniroid, Uniroid hc, Xyloproct, Zenoxone) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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] |
ABCB1/P-glycoprotein 1 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] |
P-glycoprotein 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3467] [UniProtKB: P06795] | ||||||||
ChEMBL | Inhibition of P-glycoprotein, mouse L-mdr1b 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 Mdr1b-expressing LLC-PK1 cells | F | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2003) 46: 1716-1725 [PMID:12699389] |
ABCB1/P-glycoprotein 3 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] |
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] |
Testis-specific androgen-binding protein 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] |
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]