clobetasol propionate [Ligand Id: 7062] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1159650 (Impoyz, Clobetasol 17-propionate, Cormax, Temovate, Dermovate nn, Etrivex, Embeline, Clobetasol propionate (emollient), CCI 4725, CCI-4725, Temovate e, Impeklo, Olux, Clobetasol, Clarelux, Olux e, GR 2/925, Clobetasol propionate, Dermovate, Embeline e, Clobaderm, Clobex)
  • Androgen receptor/Androgen Receptor in Rat [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 5.6 pKi 2517 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone) B 5.42 pIC50 3775 nM IC50 DrugMatrix in vitro pharmacology data
ABCB11/Bile salt export pump in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6020] [GtoPdb: 778] [UniProtKB: O95342]
ChEMBL Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake B 5.07 pIC50 8500 nM IC50 Drug Metab. Dispos. (2012) 40: 130-138 [PMID:21965623]
ABCB11/Bile salt export pump in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073674] [GtoPdb: 778] [UniProtKB: O70127]
ChEMBL Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake B 4.46 pIC50 35000 nM IC50 Drug Metab. Dispos. (2012) 40: 130-138 [PMID:21965623]
CYP3A5/Cytochrome P450 3A5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3019] [GtoPdb: 1338] [UniProtKB: P20815]
ChEMBL Binding affinity to heme in His-tagged CYP3A5 (unknown origin) expressed in Escherichia coli DH5alpha assessed as changes in absorbance spectra of heme-compound complex by measuring dissociation constant by UV-vis spectrophotometric titration analysis B 7 pKd 100 nM Kd J Med Chem (2020) 63: 1415-1433 [PMID:31965799]
ChEMBL Inhibition of human recombinant CYP3A5 expressed in supersomes assessed as decrease in formation of D-luciferin using luciferin-IPA as substrate incubated for 10 mins in presence of NADPH by P450-Glo luminescence assay B 4.81 pIC50 15600 nM IC50 J Med Chem (2020) 63: 1415-1433 [PMID:31965799]
ChEMBL Inhibition of CYP3A5 in CRISPR/Cas9-mediated CYP3A5 knock-out and doxycycline-induced CYP3A5 overexpressing human AsPC1 cells assessed as decrease in 1-hydroxymidazolam formation using midazolam as substrate pretreated with doxycycline for 24 hrs followed by incubation with compound for 24 hrs by LC-MS/MS analysis B 6.99 pIC50 103 nM IC50 J Med Chem (2020) 63: 1415-1433 [PMID:31965799]
ChEMBL Inhibition of CYP3A5 in lentiviral pLVX-TRE3G-ZsGreen1-CYP3A5 transduced wild type human AsPC1 cells overexpressing CYP3A5 assessed as decrease in 1-hydroxymidazolam formation using midazolam as substrate after 24 hrs by LC-MS/MS analysis B 7.11 pIC50 78 nM IC50 J Med Chem (2020) 63: 1415-1433 [PMID:31965799]
ChEMBL Inhibition of CYP3A5 in wild type human AsPC1 cells assessed as decrease in 1-hydroxymidazolam formation using midazolam as substrate after 24 hrs by LC-MS/MS analysis B 7.36 pIC50 44 nM IC50 J Med Chem (2020) 63: 1415-1433 [PMID:31965799]
ChEMBL Inhibition of CYP3A5 in doxycycline-induced CYP3A5 overexpressing wild type human AsPC1 cells assessed as decrease in 1-hydroxymidazolam formation using midazolam as substrate pretreated with doxycycline for 24 hrs followed by incubation with compound for 24 hrs by LC-MS/MS analysis B 7.68 pIC50 21 nM IC50 J Med Chem (2020) 63: 1415-1433 [PMID:31965799]
Glucocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034] [GtoPdb: 625] [UniProtKB: P04150]
ChEMBL DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone) B 9.18 pKi 0.66 nM Ki DrugMatrix in vitro pharmacology data
GtoPdb - - 9.18 pKi 0.66 nM Ki National Toxicology Program: Dept of Health and Human Services.. DrugMatrix
ChEMBL DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone) B 8.84 pIC50 1.46 nM IC50 DrugMatrix in vitro pharmacology data
Glucocorticoid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3368] [GtoPdb: 625] [UniProtKB: P06536]
ChEMBL Competitive displacement of [3H]dexamethasone from glucocorticoid receptor of rat liver cytosol B 8.5 pIC50 3.17 nM IC50 J. Med. Chem. (1991) 34: 2468-2473 [PMID:1875343]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 infected in RBCs by firefly luciferase reporter gene assay F 6.1 pIC50 797 nM IC50 Antimicrob. Agents Chemother. (2010) 54: 3597-3604 [PMID:20547797]
Progesterone receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1909044] [UniProtKB: Q690N0]
ChEMBL DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020) B 8.82 pKi 1.52 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020) B 7.92 pIC50 12 nM IC50 DrugMatrix in vitro pharmacology data

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]