A series of N-(2-(1H-imidazol-1-yl)-2-phenylethyl)arylamides were prepared, using an efficient three- to five-step synthesis, and evaluated for their inhibitory activity against human cytochrome P450C24A1 (CYP24A1) hydroxylase. Inhibition ranged from IC50 0.3-72 microM compared with the standard ketoconazole IC50 0.52 microM, with the styryl derivative (11c) displaying enhanced activity (IC50=0.3 microM) compared with the standard, providing a useful preliminary lead for drug development. ..more
BioActive Compound: 1
Description:
Title: Synthesis and CYP24A1 inhibitory activity of N-(2-(1H-imidazol-1-yl)-2-phenylethyl)arylamides.
Abstract: A series of N-(2-(1H-imidazol-1-yl)-2-phenylethyl)arylamides were prepared, using an efficient three- to five-step synthesis, and evaluated for their inhibitory activity against human cytochrome P450C24A1 (CYP24A1) hydroxylase. Inhibition ranged from IC50 0.3-72 microM compared with the standard ketoconazole IC50 0.52 microM, with the styryl derivative (11c) displaying enhanced activity (IC50=0.3 microM) compared with the standard, providing a useful preliminary lead for drug development.
(PMID: 20594862)
Abstract: A series of N-(2-(1H-imidazol-1-yl)-2-phenylethyl)arylamides were prepared, using an efficient three- to five-step synthesis, and evaluated for their inhibitory activity against human cytochrome P450C24A1 (CYP24A1) hydroxylase. Inhibition ranged from IC50 0.3-72 microM compared with the standard ketoconazole IC50 0.52 microM, with the styryl derivative (11c) displaying enhanced activity (IC50=0.3 microM) compared with the standard, providing a useful preliminary lead for drug development.
(PMID: 20594862)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.
Putative Target:
ChEMBL Target ID: 100474
Target Type: SINGLE PROTEIN
Pref Name: Cytochrome P450 24A1
Description: 1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrial
Organism: Homo sapiens
Tax ID: 9606
Confidence: Homologous single protein target assigned
Relationship Type: Homologous protein target assigned
ChEMBL target type: Target is a single protein chain
Putative Target:
ChEMBL Target ID: 100474
Target Type: SINGLE PROTEIN
Pref Name: Cytochrome P450 24A1
Description: 1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrial
Organism: Homo sapiens
Tax ID: 9606
Confidence: Homologous single protein target assigned
Relationship Type: Homologous protein target assigned
ChEMBL target type: Target is a single protein chain
Categorized Comment
ChEMBL Assay Type: ADMET
ChEMBL Assay Data Source: Scientific Literature
ChEMBL Assay Data Source: Scientific Literature
Result Definitions
| TID | Name | Description | Histogram | Type | Unit | |
|---|---|---|---|---|---|---|
| Outcome | The BioAssay activity outcome | Outcome | ||||
| 1 | IC50* | IC50 PubChem standard value |  | Float | μM | |
| 2 | IC50 activity comment | IC50 activity comment | String | |||
| 3 | IC50 standard flag | IC50 standard flag | | Integer | ||
| 4 | IC50 qualifier | IC50 qualifier | String | |||
| 5 | IC50 published value | IC50 published value | | Float | nM | |
| 6 | IC50 standard value | IC50 standard value | | Float | nM |
* Activity Concentration.
Data Table (Concise)
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