Assay Detail
Functional
CHEMBL2078569
Review assay metadata, readout intent, target linkage, and publication context from the same page.
TP_TRANSPORTER: inhibition of MTX uptake in OAT-K1-expressing MDCK cells
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | MDCK |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Solute carrier organic anion transporter family member 1A3 (CHEMBL2073707) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Trans-stimulation effects of folic acid derivatives on methotrexate transport by rat renal organic anion transporter, OAT-K1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 5.37 | 6.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL376180 | AMINOPTERIN | 2.0 | 1 | 6.30 |
| CHEMBL1231574 | LEVOMEFOLIC ACID | 4.0 | 1 | 5.92 |
| CHEMBL1679 | LEUCOVORIN | 4.0 | 1 | 5.09 |
| CHEMBL1622 | FOLIC ACID | 4.0 | 1 | 4.85 |
| CHEMBL453904 | SULFOBROMOPHTHALEIN SODIUM | -1.0 | 1 | 4.68 |
| CHEMBL224867 | TAUROCHOLIC ACID | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL376180 | AMINOPTERIN | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL1231574 | LEVOMEFOLIC ACID | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL1679 | LEUCOVORIN | Ki | = | 8200.0 | nM | 5.09 |
| CHEMBL1622 | FOLIC ACID | Ki | = | 14100.0 | nM | 4.85 |
| CHEMBL453904 | SULFOBROMOPHTHALEIN SODIUM | Ki | = | 21000.0 | nM | 4.68 |
| CHEMBL224867 | TAUROCHOLIC ACID | Ki | = | 183000.0 | nM | - |