Assay Detail
ADMET
CHEMBL3537392
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Inhibition of mouse OAT3 expressed in CHO cells assessed as inhibition of fluorescein uptake over 20 mins
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Mus musculus |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Organic anion transporter 3 interacts selectively with lipophilic β-lactam antibiotics.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 4.53 | 5.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL897 | PROBENECID | 4.0 | 1 | 5.52 |
| CHEMBL893 | DICLOXACILLIN | 4.0 | 1 | 4.78 |
| CHEMBL891 | CLOXACILLIN | 4.0 | 1 | 4.51 |
| CHEMBL617 | CEPHALOTHIN | 4.0 | 1 | 4.48 |
| CHEMBL819 | OXACILLIN | 4.0 | 1 | 4.46 |
| CHEMBL1443 | NAFCILLIN | 4.0 | 1 | 4.46 |
| CHEMBL222913 | CEFTIOFUR | 2.0 | 1 | 4.45 |
| CHEMBL615 | PENICILLIN V | 4.0 | 1 | 4.31 |
| CHEMBL996 | CEFOXITIN | 4.0 | 1 | 4.24 |
| CHEMBL29 | PENICILLIN G | 4.0 | 1 | 4.05 |
| CHEMBL1449 | TICARCILLIN | 4.0 | 1 | - |
| CHEMBL575 | METHICILLIN | 4.0 | 1 | - |
| CHEMBL1201195 | CEFMETAZOLE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL897 | PROBENECID | IC50 | = | 3020.0 | nM | 5.52 |
| CHEMBL893 | DICLOXACILLIN | IC50 | = | 16600.0 | nM | 4.78 |
| CHEMBL891 | CLOXACILLIN | IC50 | = | 30900.0 | nM | 4.51 |
| CHEMBL617 | CEPHALOTHIN | IC50 | = | 33300.0 | nM | 4.48 |
| CHEMBL819 | OXACILLIN | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL1443 | NAFCILLIN | IC50 | = | 34900.0 | nM | 4.46 |
| CHEMBL222913 | CEFTIOFUR | IC50 | = | 35700.0 | nM | 4.45 |
| CHEMBL615 | PENICILLIN V | IC50 | = | 48600.0 | nM | 4.31 |
| CHEMBL996 | CEFOXITIN | IC50 | = | 57000.0 | nM | 4.24 |
| CHEMBL29 | PENICILLIN G | IC50 | = | 89400.0 | nM | 4.05 |
| CHEMBL1449 | TICARCILLIN | IC50 | = | 233000.0 | nM | - |
| CHEMBL575 | METHICILLIN | IC50 | = | 116000.0 | nM | - |
| CHEMBL1201195 | CEFMETAZOLE | IC50 | = | 105000.0 | nM | - |