Assay Detail
Binding
CHEMBL5732363
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition Assay: The dose dependent inhibition of OCT2 mediated uptake of a model substrate 14C-Tetraethylammonium (TEA) by test compounds was studied in wild-type and OCT2-transfected MDCKII cells at 7 concentrations from 0.014 μM to 10 μM.MDCKII cells were maintained in minimal essential medium (MEM) with 1% Pen/Strep, 10% fetal bovine serum, and 0.25 mg/mL hygromycin B in an incubator set at 37° C., 90% humidity and 5% CO2. 24 hours prior to assay, media containing 5 mM sodium butyrate were added to MDCKII cells in flasks, and cells were grown to 80-90% confluence. On assay day, cells were trypsinized and resuspended in Krebs-Henseleit Buffer (KHB), pH 7.4 at 5×106 million cells/mL. Cells were preincubated for 15 min in assay plate before addition of test compound or substrate.
69
Total Activities
21
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Solute carrier family 22 member 2 (CHEMBL1743122) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Substituted 1,2,3,4,6,8,12,12a-octahydro-1,4-methanodipyrido[1,2-a:1',2'-d]pyrazines and methods for treating viral infections
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 5.96 | 7.38 |
| kon | 23 | - | - |
| k_off | 23 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5864617 | — | — | 3 | 7.38 |
| CHEMBL5870848 | — | — | 3 | 7.03 |
| CHEMBL6000266 | — | — | 3 | 6.86 |
| CHEMBL6049097 | — | — | 6 | 6.69 |
| CHEMBL5819083 | — | — | 3 | 6.62 |
| CHEMBL6066002 | — | — | 3 | 6.60 |
| CHEMBL5843001 | — | — | 3 | 6.35 |
| CHEMBL5792941 | — | — | 6 | 6.32 |
| CHEMBL3989866 | BICTEGRAVIR | 4.0 | 3 | 6.31 |
| CHEMBL5882513 | — | — | 3 | 6.21 |
| CHEMBL5916318 | — | — | 3 | 5.82 |
| CHEMBL5827479 | — | — | 3 | 5.65 |
| CHEMBL5932213 | — | — | 3 | 5.55 |
| CHEMBL5758649 | — | — | 3 | 5.43 |
| CHEMBL6003192 | — | — | 3 | 5.42 |
| CHEMBL5777750 | — | — | 3 | 5.31 |
| CHEMBL5883252 | — | — | 3 | 5.21 |
| CHEMBL5998444 | — | — | 3 | 5.00 |
| CHEMBL5991232 | — | — | 3 | 5.00 |
| CHEMBL5960223 | — | — | 3 | 5.00 |
| CHEMBL5817410 | — | — | 3 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5864617 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL5870848 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL6000266 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL6049097 | — | IC50 | = | 204.0 | nM | 6.69 |
| CHEMBL5819083 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL6066002 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL6049097 | — | IC50 | = | 358.0 | nM | 6.45 |
| CHEMBL5843001 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL5792941 | — | IC50 | = | 476.0 | nM | 6.32 |
| CHEMBL3989866 | BICTEGRAVIR | IC50 | = | 487.0 | nM | 6.31 |
| CHEMBL5882513 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL5792941 | — | IC50 | = | 1357.0 | nM | 5.87 |
| CHEMBL5916318 | — | IC50 | = | 1506.0 | nM | 5.82 |
| CHEMBL5827479 | — | IC50 | = | 2230.0 | nM | 5.65 |
| CHEMBL5932213 | — | IC50 | = | 2823.0 | nM | 5.55 |
| CHEMBL5758649 | — | IC50 | = | 3726.0 | nM | 5.43 |
| CHEMBL6003192 | — | IC50 | = | 3830.0 | nM | 5.42 |
| CHEMBL5777750 | — | IC50 | = | 4909.0 | nM | 5.31 |
| CHEMBL5883252 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL5817410 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL5960223 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL5998444 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL5991232 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL5792941 | — | k_off | = | - | s-1 | - |
| CHEMBL5758649 | — | kon | = | - | — | - |
| CHEMBL5758649 | — | k_off | = | - | s-1 | - |
| CHEMBL5916318 | — | kon | = | - | — | - |
| CHEMBL5916318 | — | k_off | = | - | s-1 | - |
| CHEMBL6049097 | — | k_off | = | - | s-1 | - |
| CHEMBL5819083 | — | kon | = | - | — | - |
| CHEMBL5819083 | — | k_off | = | - | s-1 | - |
| CHEMBL6066002 | — | kon | = | - | — | - |
| CHEMBL6066002 | — | k_off | = | - | s-1 | - |
| CHEMBL5827479 | — | kon | = | - | — | - |
| CHEMBL5827479 | — | k_off | = | - | s-1 | - |
| CHEMBL5991232 | — | kon | = | - | — | - |
| CHEMBL5792941 | — | kon | = | - | — | - |
| CHEMBL5817410 | — | k_off | = | - | s-1 | - |
| CHEMBL5817410 | — | kon | = | - | — | - |
| CHEMBL5883252 | — | kon | = | - | — | - |
| CHEMBL5960223 | — | kon | = | - | — | - |
| CHEMBL6003192 | — | k_off | = | - | s-1 | - |
| CHEMBL6003192 | — | kon | = | - | — | - |
| CHEMBL5843001 | — | k_off | = | - | s-1 | - |
| CHEMBL5843001 | — | kon | = | - | — | - |
| CHEMBL5870848 | — | k_off | = | - | s-1 | - |
| CHEMBL5960223 | — | k_off | = | - | s-1 | - |
| CHEMBL5864617 | — | kon | = | - | — | - |
| CHEMBL5864617 | — | k_off | = | - | s-1 | - |
| CHEMBL5870848 | — | kon | = | - | — | - |