Assay Detail
Binding
CHEMBL5164055
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Induction of degradation of hamster HMGCR (TM1-8)-GFP (1 to 346 residues) transfected in CHO-7 cells incubated for 16 hrs in sterol-depleted medium by fluorescence based microplate reader assay
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cricetulus griseus |
| Cell Type | CHO-7 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
3-hydroxy-3-methylglutaryl-coenzyme A reductase (CHEMBL5169105) ↗| Type | SINGLE PROTEIN |
| Organism | Cricetulus griseus |
Publication
Synthesis of heterocyclic ring-fused analogs of HMG499 as novel degraders of HMG-CoA reductase that lower cholesterol.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 43 | 5.79 | 6.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5179808 | — | — | 1 | 6.66 |
| CHEMBL5209354 | — | — | 1 | 6.55 |
| CHEMBL5198179 | — | — | 1 | 6.39 |
| CHEMBL5201524 | — | — | 1 | 6.39 |
| CHEMBL5177065 | — | — | 1 | 6.39 |
| CHEMBL5203338 | — | — | 1 | 6.39 |
| CHEMBL5172178 | — | — | 1 | 6.39 |
| CHEMBL5200363 | — | — | 1 | 6.39 |
| CHEMBL5181250 | — | — | 1 | 6.37 |
| CHEMBL5178222 | — | — | 1 | 6.37 |
| CHEMBL5190867 | — | — | 1 | 6.37 |
| CHEMBL5170642 | — | — | 1 | 6.32 |
| CHEMBL5175711 | — | — | 1 | 6.28 |
| CHEMBL5199638 | — | — | 1 | 6.28 |
| CHEMBL5188312 | — | — | 1 | 6.20 |
| CHEMBL5183387 | — | — | 1 | 6.19 |
| CHEMBL5184418 | — | — | 1 | 6.14 |
| CHEMBL5203822 | — | — | 1 | 6.12 |
| CHEMBL5173477 | — | — | 1 | 6.09 |
| CHEMBL5194591 | — | — | 1 | 6.08 |
| CHEMBL5176116 | — | — | 1 | 6.01 |
| CHEMBL5208996 | — | — | 1 | 5.96 |
| CHEMBL5207190 | — | — | 1 | 5.90 |
| CHEMBL5189735 | — | — | 1 | 5.79 |
| CHEMBL5170366 | — | — | 1 | 5.74 |
| CHEMBL5191772 | — | — | 1 | 5.69 |
| CHEMBL5202652 | — | — | 1 | 5.58 |
| CHEMBL5207917 | — | — | 1 | 5.56 |
| CHEMBL5174649 | — | — | 1 | 5.47 |
| CHEMBL2205896 | — | — | 1 | 5.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5179808 | — | EC50 | = | 220.0 | nM | 6.66 |
| CHEMBL5209354 | — | EC50 | = | 280.0 | nM | 6.55 |
| CHEMBL5201524 | — | EC50 | = | 410.0 | nM | 6.39 |
| CHEMBL5177065 | — | EC50 | = | 410.0 | nM | 6.39 |
| CHEMBL5203338 | — | EC50 | = | 410.0 | nM | 6.39 |
| CHEMBL5172178 | — | EC50 | = | 410.0 | nM | 6.39 |
| CHEMBL5200363 | — | EC50 | = | 410.0 | nM | 6.39 |
| CHEMBL5198179 | — | EC50 | = | 410.0 | nM | 6.39 |
| CHEMBL5181250 | — | EC50 | = | 430.0 | nM | 6.37 |
| CHEMBL5178222 | — | EC50 | = | 430.0 | nM | 6.37 |
| CHEMBL5190867 | — | EC50 | = | 430.0 | nM | 6.37 |
| CHEMBL5170642 | — | EC50 | = | 480.0 | nM | 6.32 |
| CHEMBL5175711 | — | EC50 | = | 520.0 | nM | 6.28 |
| CHEMBL5199638 | — | EC50 | = | 530.0 | nM | 6.28 |
| CHEMBL5188312 | — | EC50 | = | 630.0 | nM | 6.20 |
| CHEMBL5183387 | — | EC50 | = | 650.0 | nM | 6.19 |
| CHEMBL5184418 | — | EC50 | = | 730.0 | nM | 6.14 |
| CHEMBL5203822 | — | EC50 | = | 760.0 | nM | 6.12 |
| CHEMBL5173477 | — | EC50 | = | 820.0 | nM | 6.09 |
| CHEMBL5194591 | — | EC50 | = | 830.0 | nM | 6.08 |
| CHEMBL5176116 | — | EC50 | = | 980.0 | nM | 6.01 |
| CHEMBL5208996 | — | EC50 | = | 1090.0 | nM | 5.96 |
| CHEMBL5207190 | — | EC50 | = | 1260.0 | nM | 5.90 |
| CHEMBL5189735 | — | EC50 | = | 1630.0 | nM | 5.79 |
| CHEMBL5170366 | — | EC50 | = | 1840.0 | nM | 5.74 |
| CHEMBL5191772 | — | EC50 | = | 2030.0 | nM | 5.69 |
| CHEMBL5202652 | — | EC50 | = | 2660.0 | nM | 5.58 |
| CHEMBL5207917 | — | EC50 | = | 2730.0 | nM | 5.56 |
| CHEMBL5174649 | — | EC50 | = | 3370.0 | nM | 5.47 |
| CHEMBL2205896 | — | EC50 | = | 3990.0 | nM | 5.40 |
| CHEMBL5170746 | — | EC50 | = | 4470.0 | nM | 5.35 |
| CHEMBL5195488 | — | EC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL5202075 | — | EC50 | = | 4940.0 | nM | 5.31 |
| CHEMBL2205888 | — | EC50 | = | 5020.0 | nM | 5.30 |
| CHEMBL5203106 | — | EC50 | = | 5410.0 | nM | 5.27 |
| CHEMBL5169927 | — | EC50 | = | 5810.0 | nM | 5.24 |
| CHEMBL5209055 | — | EC50 | = | 8160.0 | nM | 5.09 |
| CHEMBL5195715 | — | EC50 | = | 8250.0 | nM | 5.08 |
| CHEMBL2205895 | — | EC50 | = | 8800.0 | nM | 5.06 |
| CHEMBL5190100 | — | EC50 | = | 12580.0 | nM | 4.90 |
| CHEMBL5176196 | — | EC50 | = | 28080.0 | nM | 4.55 |
| CHEMBL5193383 | — | EC50 | = | 31360.0 | nM | 4.50 |
| CHEMBL5188933 | — | EC50 | = | 43880.0 | nM | 4.36 |