Assay Detail
Binding
CHEMBL688754
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Tested in vitro for the HMG-CoA reductase inhibitory activity in a microsomal preparation
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Subcellular | Microsome |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
3-hydroxy-3-methylglutaryl-coenzyme A reductase (CHEMBL3247) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Design and biological evaluation of a series of thiophene-based 3-hydroxy-3-methylglutaryl coenzyme a reductase inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 6.86 | 8.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL153492 | — | — | 1 | 8.36 |
| CHEMBL153021 | — | — | 1 | 8.20 |
| CHEMBL152366 | — | — | 1 | 8.01 |
| CHEMBL358623 | — | — | 1 | 7.82 |
| CHEMBL152129 | — | — | 1 | 7.68 |
| CHEMBL151961 | — | — | 1 | 7.58 |
| CHEMBL152551 | — | — | 1 | 7.58 |
| CHEMBL152926 | — | — | 1 | 7.31 |
| CHEMBL346856 | — | — | 1 | 7.03 |
| CHEMBL357515 | COMPACTIN SODIUM | — | 1 | 6.96 |
| CHEMBL152032 | MEVINOLIN | — | 1 | 6.80 |
| CHEMBL152893 | — | — | 1 | 6.70 |
| CHEMBL358245 | — | — | 1 | 6.69 |
| CHEMBL434313 | — | — | 1 | 6.63 |
| CHEMBL347277 | — | — | 1 | 6.49 |
| CHEMBL348225 | — | — | 1 | 6.38 |
| CHEMBL503 | LOVASTATIN | 4.0 | 1 | 6.28 |
| CHEMBL154868 | — | — | 1 | 6.24 |
| CHEMBL154986 | — | — | 1 | 6.00 |
| CHEMBL54440 | MEVASTATIN | 2.0 | 1 | 5.94 |
| CHEMBL152114 | — | — | 1 | 5.85 |
| CHEMBL346635 | — | — | 1 | 5.61 |
| CHEMBL150649 | — | — | 1 | 5.53 |
| CHEMBL152963 | — | — | 1 | - |
| CHEMBL358171 | — | — | 1 | - |
| CHEMBL347095 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL153492 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL153021 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL152366 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL358623 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL152129 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL151961 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL152551 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL152926 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL346856 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL357515 | COMPACTIN SODIUM | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL152032 | MEVINOLIN | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL152893 | — | IC50 | = | 202.0 | nM | 6.70 |
| CHEMBL358245 | — | IC50 | = | 206.0 | nM | 6.69 |
| CHEMBL434313 | — | IC50 | = | 233.0 | nM | 6.63 |
| CHEMBL347277 | — | IC50 | = | 325.0 | nM | 6.49 |
| CHEMBL348225 | — | IC50 | = | 417.0 | nM | 6.38 |
| CHEMBL503 | LOVASTATIN | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL154868 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL154986 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL54440 | MEVASTATIN | IC50 | = | 1150.0 | nM | 5.94 |
| CHEMBL152114 | — | IC50 | = | 1420.0 | nM | 5.85 |
| CHEMBL346635 | — | IC50 | = | 2430.0 | nM | 5.61 |
| CHEMBL150649 | — | IC50 | = | 2980.0 | nM | 5.53 |
| CHEMBL152963 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL358171 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL347095 | — | IC50 | > | 10000.0 | nM | - |