tazarotene [Ligand Id: 6952] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1657 (AGN 190168, AGN-190168, AGN190168, Arazlo, Avage, Fabior, Idp-123, Tazarotene, Tazarotene component of duobrii, Tazarotene component of idp-118, Tazaroteno, Tazorac, Zorac) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| CYP3A4/Cytochrome P450 3A4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL340] [GtoPdb: 1337] [UniProtKB: P08684] | ||||||||
| ChEMBL | Inhibition Assay: Compounds were assessed for inhibition (IC50, n=2) of CYP2C8, CYP2C9 and CYP3A4 in pooled human liver microsomes using selective probe substrates at their previously determined Km values (CYP2C8: paclitaxel, 4 μM; CYP2C9: diclofenac, 5 μM; CYP3A4: midazolam, 0.5 μM). Incubations contained 0.1 mg/mL human liver microsomes, 3 mM MgCl2, probe substrate and various concentrations of inhibitor (12-point IC50 curve) in 100 mM potassium phosphate buffer (pH 7.4). Concentrations of organic solvents were kept to <1% (v/v). All incubations were pre-incubated at 37° C. for 5 minutes prior to addition of 1 mM NADPH (final concentration). Incubations were stopped after 5 (CYP3A4) or 15 minutes (CYP2C8 and CYP2C9) with one volume (v/v) of ice-cold acetonitrile containing 0.1 μM tolbutamide as an internal standard. All samples were vortexed and centrifuged prior to LC-MS/MS analysis. | B | 5.5 | pIC50 | 3150 | nM | IC50 | US-9963439-B2. Specific inhibitors of cytochrome P450 26 retinoic acid hydroxylase (2018) |
| Retinoic acid receptor-α/Retinoic acid receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2055] [GtoPdb: 590] [UniProtKB: P10276] | ||||||||
| GtoPdb | - | - | 7.2 | pEC50 | 63 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 489-92 [PMID:19058965] |
| ChEMBL | Activity at human RARalpha ligand binding domain expressed in COS7 cells co-transfected with Gal4-DBD assessed as transcriptional activation after 16 hrs by Gal4 response element-driven luciferase reporter gene assay | B | 7.2 | pEC50 | 63 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 489-492 [PMID:19058965] |
| ChEMBL | Affinity On-target Cellular interaction: (Reporter gene assay (HEK293T cells)) EUB0000563a RARA | F | 7.2 | pEC50 | 63 | nM | EC50 | Affinity On-target Cellular Literature for EUbOPEN Chemogenomic Library |
| Retinoic acid receptor-β/Retinoic acid receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2008] [GtoPdb: 591] [UniProtKB: P10826] | ||||||||
| ChEMBL | Activity at human RARbeta ligand binding domain expressed in COS7 cells co-transfected with Gal4-DBD assessed as transcriptional activation after 16 hrs by Gal4 response element-driven luciferase reporter gene assay | B | 9.1 | pEC50 | 0.8 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 489-492 [PMID:19058965] |
| ChEMBL | Affinity On-target Cellular interaction: (Reporter gene assay (HEK293T cells)) EUB0000563a RARB | F | 9.1 | pEC50 | 0.8 | nM | EC50 | Affinity On-target Cellular Literature for EUbOPEN Chemogenomic Library |
| GtoPdb | - | - | 9.1 | pEC50 | 0.8 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 489-92 [PMID:19058965] |
| Retinoic acid receptor-γ/Retinoic acid receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2003] [GtoPdb: 592] [UniProtKB: P13631] | ||||||||
| ChEMBL | Activity at human RARgamma ligand binding domain expressed in COS7 cells co-transfected with Gal4-DBD assessed as transcriptional activation after 16 hrs by Gal4 response element-driven luciferase reporter gene assay | B | 7.4 | pEC50 | 40 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 489-492 [PMID:19058965] |
| ChEMBL | Affinity On-target Cellular interaction: (Reporter gene assay (HEK293T cells)) EUB0000563a RARG | F | 7.4 | pEC50 | 40 | nM | EC50 | Affinity On-target Cellular Literature for EUbOPEN Chemogenomic Library |
| GtoPdb | - | - | 7.4 | pEC50 | 40 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 489-92 [PMID:19058965] |
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]
