Assay Detail
Binding
CHEMBL4026560
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Inhibition of D5D in human HepG2 cells assessed as [14C]AA formation from [14C]DGLA preincubated for 30 mins followed by [14C]eicosatrienoic acid addition measured after 3 hrs by TLC analysis
20
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of 3,5-Diphenyl-4-methyl-1,3-oxazolidin-2-ones as Novel, Potent, and Orally Available Δ-5 Desaturase (D5D) Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 7.59 | 9.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4084502 | — | — | 1 | 9.28 |
| CHEMBL4064555 | — | — | 1 | 8.82 |
| CHEMBL4102458 | — | — | 1 | 8.43 |
| CHEMBL4060775 | — | — | 1 | 8.39 |
| CHEMBL4070383 | — | — | 2 | 8.06 |
| CHEMBL4090490 | — | — | 1 | 7.75 |
| CHEMBL4104260 | — | — | 1 | 7.26 |
| CHEMBL4066595 | — | — | 1 | 7.22 |
| CHEMBL4069465 | — | — | 1 | 6.82 |
| CHEMBL4087912 | — | — | 1 | 6.77 |
| CHEMBL4080025 | — | — | 1 | 6.77 |
| CHEMBL4085437 | — | — | 1 | 6.72 |
| CHEMBL4063561 | — | — | 1 | 5.96 |
| CHEMBL4084463 | — | — | 1 | - |
| CHEMBL4062788 | — | — | 1 | - |
| CHEMBL4073142 | — | — | 1 | - |
| CHEMBL4069792 | — | — | 1 | - |
| CHEMBL4091399 | — | — | 1 | - |
| CHEMBL4072166 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4084502 | — | IC50 | = | 0.52 | nM | 9.28 |
| CHEMBL4064555 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4102458 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL4060775 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL4070383 | — | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL4070383 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL4090490 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4104260 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL4066595 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4069465 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4087912 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4080025 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4085437 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4063561 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4084463 | — | IC50 | - | — | - | |
| CHEMBL4062788 | — | IC50 | - | — | - | |
| CHEMBL4073142 | — | IC50 | - | — | - | |
| CHEMBL4069792 | — | IC50 | - | — | - | |
| CHEMBL4091399 | — | IC50 | - | — | - | |
| CHEMBL4072166 | — | IC50 | - | — | - |