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

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ChEMBL ligand: CHEMBL1159650 (CCI 4725, CCI-4725, Clarelux, Clobaderm, Clobecort amex, Clobetasol, Clobetasol 17-propionate, Clobetasol propionate, Clobetasol propionate (emollient), Clobex, Cormax, Dermovate, Dermovate nn, Dovate, Embeline, Embeline e, Etrivex, GR 2/925, Impeklo, Impoyz, NSC-758634, Olux, Olux e, Psorex, Temovate, Temovate e)
  • 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 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]