ChEMBL ligand: CHEMBL389433 (Liarozole, Liazal, R-75251)
CYP19A1/Cytochrome P450 19A1 in Human [ChEMBL: CHEMBL1978] [GtoPdb: 1362] [UniProtKB: P11511] There should be some charts here, you may need to enable JavaScript!
CYP24A1/Cytochrome P450 24A1 in Human [ChEMBL: CHEMBL4521] [GtoPdb: 1365] [UniProtKB: Q07973] There should be some charts here, you may need to enable JavaScript!
CYP26A1/Cytochrome P450 26A1 in Human [ChEMBL: CHEMBL5141] [GtoPdb: 1366] [UniProtKB: O43174] There should be some charts here, you may need to enable JavaScript!
CYP26B1/Cytochrome P450 26B1 in Human [ChEMBL: CHEMBL3713687] [GtoPdb: 1367] [UniProtKB: Q9NR63] There should be some charts here, you may need to enable JavaScript!
CYP3A4/Cytochrome P450 3A4 in Human [ChEMBL: CHEMBL340] [GtoPdb: 1337] [UniProtKB: P08684] 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
CYP19A1/Cytochrome P450 19A1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1978] [GtoPdb: 1362] [UniProtKB: P11511]
ChEMBL	Inhibition of human placental microsome CYP19	B	7.35	pIC50	44.67	nM	IC50	J Med Chem (2005) 48: 7282-7289 [PMID:16279787]
ChEMBL	Inhibition of human placental microsome CYP19	B	8.3	pIC50	5	nM	IC50	Bioorg Med Chem Lett (2010) 20: 3050-3064 [PMID:20413308]
CYP24A1/Cytochrome P450 24A1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4521] [GtoPdb: 1365] [UniProtKB: Q07973]
ChEMBL	Inhibition of human MBP-tagged CYP24A1 expressed in Escherichia coli using 1,25(OH)2D3 substrate in presence of bovine adrenodoxin, adrenodoxin reductase and NADPH incubated at 37 degC for 25 mins by HPLC method	B	8.64	pIC50	2.3	nM	IC50	J Med Chem (2014) 57: 7702-7715 [PMID:25148392]
CYP26A1/Cytochrome P450 26A1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5141] [GtoPdb: 1366] [UniProtKB: O43174]
ChEMBL	Inhibition of CYP26A1 in human MCF7 cells	B	5.15	pIC50	7000	nM	IC50	Bioorg Med Chem (2008) 16: 8301-8313 [PMID:18722776]
ChEMBL	Potency towards cytochrome P 450 26 enzyme activity	B	5.22	pIC50	6000	nM	IC50	Bioorg Med Chem Lett (2005) 15: 1669-1673 [PMID:15745819]
ChEMBL	Inhibition of CYP26A1 in ATRA-induced human HL60 cell microsomes incubated for 30 mins using ATRA and NADPH by HPLC method	B	5.61	pIC50	2450	nM	IC50	Bioorg Med Chem (2015) 23: 1356-1365 [PMID:25684424]
GtoPdb	-	-	5.7	pIC50	-	-	-	Mol Pharmacol (2011) 80: 228-39 [PMID:21521770]
ChEMBL	Inhibition of microsomal fraction of human CYP26A1 expressed in Sf9 cells using 9-cis-RA as substrate preincubated for 5 mins followed by NADPH addition measured after 1 min by HPLC analysis in presence of rat P450 reductase	B	5.72	pIC50	1900	nM	IC50	J Med Chem (2016) 59: 2579-2595 [PMID:26918322]
ChEMBL	Inhibition of CYP26A1 in ATRA-induced human HL60 cell microsomes incubated for 30 mins in dark condition with NADPH and ATRA by HPLC method	B	6.05	pIC50	890	nM	IC50	Bioorg Med Chem (2015) 23: 6763-6773 [PMID:26365710]
ChEMBL	Inhibition of human CYP26A1 assessed using [11,12-3H]ATRA as substrate by scintillation counting	B	6.27	pIC50	540	nM	IC50	J Med Chem (2011) 54: 6803-6811 [PMID:21838328]
ChEMBL	Inhibition of CYP26A1 in human MCF7 cell microsomes using [3H]ATRA after 1 hr by scintillation counting	B	6.27	pIC50	540	nM	IC50	J Med Chem (2011) 54: 2778-2791 [PMID:21428449]
CYP26B1/Cytochrome P450 26B1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3713687] [GtoPdb: 1367] [UniProtKB: Q9NR63]
ChEMBL	Inhibition of microsomal fraction of human CYP26B1 expressed in Sf9 cells using 9-cis-RA as substrate preincubated for 5 mins followed by NADPH addition measured after 5 mins by HPLC analysis in presence of rat P450 reductase	B	7.74	pIC50	18	nM	IC50	J Med Chem (2016) 59: 2579-2595 [PMID:26918322]
CYP3A4/Cytochrome P450 3A4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL340] [GtoPdb: 1337] [UniProtKB: P08684]
ChEMBL	null: A commercially available P450-GLO Assay kit (Promega Corporation, Madison Wis.) is used to screen various compounds for CYP3A4A inhibition activity. CYP3A4A is thought to be one of the primary CYP isoforms responsible for retinoic acid metabolism in the skin. Three benchmark agents, liarozole, climbazole, and ketoconazole, were assessed for CYP3A4 inhibition to confirm that the inhibition activity (the IC50 for CYP3A4 inhibition) measured by the assay corresponds to the activity reported by the published literature. The results show that the substituted azole compounds having the specific structure set forth herein are CYP inhibitors, and thus function as RAMBAs.	B	7	pIC50	<100	nM	IC50	US-9138393-B2. Cosmetic compositions containing substituted azole and methods for improving the appearance of aging skin (2015)
ChEMBL	In vitro CYP3A4 Inhibition Assay: Cytochrome P450 is a large and diverse group of enzymes that catalyze the oxidation of organic substances. Some members of the CYP family contribute to the elimination of ATRA by catalyzing its 4-hydroxylation in the mammalian liver and skin, including that of humans as well as swine. Applicant evaluated the potential RAMBA activity of several azoles using pig liver microsomes, a rich source of CYP activity, comprising many different CYP 450 isoforms. Therefore, this approach, while a reasonable way to assess CYP inhibitors with broad activities may or may not be the best way to discover RAMBAs with selectivity for the skin, which has a much more narrow complement of CYP expression. As understanding in this area has progressed, a more specific CYP inhibition assay can be used to provide better predictivity of activity in human skin. Nevertheless, this assay may still be used as a general predictor of overall CYP activity.	B	7	pIC50	<100	nM	IC50	US-9144538-B2. Cosmetic compositions containing substituted azole and methods for alleviating the signs of photoaged skin (2015)

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]