Assay Detail
Binding
CHEMBL1226686
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]5-[(3-hydroxypropyl)thio]-3-methyl-1-[2-(methyl-t)propyl-2,3-t2]-6-(1-naphthalenylmethyl)-1H-pyrrolo[3,4-d]pyrimidine-2,4(3H,6H)-dione from human MCT1 expressed in INS1 cell membrane
12
Total Activities
11
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | INS1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Monocarboxylate transporter MCT1 is a target for immunosuppression.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 8.57 | 9.52 |
| pKi | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL205526 | — | — | 1 | 9.52 |
| CHEMBL85752 | — | — | 2 | 9.48 |
| CHEMBL204887 | — | — | 1 | 9.30 |
| CHEMBL380192 | — | — | 1 | 9.15 |
| CHEMBL205742 | — | — | 1 | 8.48 |
| CHEMBL383669 | — | — | 1 | 8.25 |
| CHEMBL205807 | — | — | 1 | 8.20 |
| CHEMBL1221551 | — | — | 1 | 7.97 |
| CHEMBL1221509 | — | — | 1 | 7.64 |
| CHEMBL315970 | — | — | 1 | 7.33 |
| CHEMBL1221510 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL205526 | — | Ki | = | 0.302 | nM | 9.52 |
| CHEMBL85752 | — | Ki | = | 0.33 | nM | 9.48 |
| CHEMBL204887 | — | Ki | = | 0.5012 | nM | 9.30 |
| CHEMBL380192 | — | Ki | = | 0.7079 | nM | 9.15 |
| CHEMBL85752 | — | Ki | = | 1.175 | nM | 8.93 |
| CHEMBL205742 | — | Ki | = | 3.311 | nM | 8.48 |
| CHEMBL383669 | — | Ki | = | 5.623 | nM | 8.25 |
| CHEMBL205807 | — | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL1221551 | — | Ki | = | 10.72 | nM | 7.97 |
| CHEMBL1221509 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL315970 | — | Ki | = | 46.77 | nM | 7.33 |
| CHEMBL1221510 | — | pKi | - | — | - |