Assay Detail
Binding
CHEMBL660503
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Inhibition of [3H]-choline brain uptake was determined by in situ brain perfusion studies in male rats
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sodium- and chloride-dependent creatine transporter 1 (CHEMBL3814) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Molecular modeling studies on the active binding site of the blood-brain barrier choline transporter.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 30 | 4.55 | 5.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL53882 | — | — | 1 | 5.64 |
| CHEMBL105218 | — | — | 1 | 4.50 |
| CHEMBL105546 | — | — | 1 | 4.40 |
| CHEMBL920 | CHOLINE | 0.5 | 1 | 4.38 |
| CHEMBL105667 | — | — | 1 | 4.35 |
| CHEMBL105536 | — | — | 1 | 4.03 |
| CHEMBL102289 | — | — | 1 | - |
| CHEMBL276310 | — | — | 1 | - |
| CHEMBL102781 | — | — | 1 | - |
| CHEMBL104586 | — | — | 1 | - |
| CHEMBL104083 | — | — | 1 | - |
| CHEMBL103052 | — | — | 1 | - |
| CHEMBL317449 | — | — | 1 | - |
| CHEMBL104529 | — | — | 1 | - |
| CHEMBL104898 | — | — | 1 | - |
| CHEMBL103048 | — | — | 1 | - |
| CHEMBL104549 | — | — | 1 | - |
| CHEMBL104154 | — | — | 1 | - |
| CHEMBL104897 | — | — | 1 | - |
| CHEMBL316976 | — | — | 1 | - |
| CHEMBL277871 | — | — | 1 | - |
| CHEMBL555023 | — | — | 1 | - |
| CHEMBL104207 | — | — | 1 | - |
| CHEMBL318178 | — | — | 1 | - |
| CHEMBL10731 | — | — | 1 | - |
| CHEMBL105901 | — | — | 1 | - |
| CHEMBL302326 | — | — | 1 | - |
| CHEMBL104943 | MONOETHANOLAMINE | 2.0 | 1 | - |
| CHEMBL107582 | — | — | 1 | - |
| CHEMBL105059 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL53882 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL105218 | — | Ki | = | 32000.0 | nM | 4.50 |
| CHEMBL105546 | — | Ki | = | 40000.0 | nM | 4.40 |
| CHEMBL920 | CHOLINE | Ki | = | 42000.0 | nM | 4.38 |
| CHEMBL105667 | — | Ki | = | 45000.0 | nM | 4.35 |
| CHEMBL105536 | — | Ki | = | 94000.0 | nM | 4.03 |
| CHEMBL102289 | — | Ki | > | 10000000.0 | nM | - |
| CHEMBL276310 | — | Ki | = | 200000.0 | nM | - |
| CHEMBL102781 | — | Ki | > | 10000000.0 | nM | - |
| CHEMBL104586 | — | Ki | = | 117000.0 | nM | - |
| CHEMBL104083 | — | Ki | = | 127000.0 | nM | - |
| CHEMBL103052 | — | Ki | > | 10000000.0 | nM | - |
| CHEMBL317449 | — | Ki | = | 162000.0 | nM | - |
| CHEMBL104529 | — | Ki | = | 495000.0 | nM | - |
| CHEMBL104898 | — | Ki | > | 10000000.0 | nM | - |
| CHEMBL103048 | — | Ki | > | 10000000.0 | nM | - |
| CHEMBL104549 | — | Ki | > | 10000000.0 | nM | - |
| CHEMBL104154 | — | Ki | > | 10000000.0 | nM | - |
| CHEMBL104897 | — | Ki | = | 4698000.0 | nM | - |
| CHEMBL316976 | — | Ki | = | 737000.0 | nM | - |
| CHEMBL277871 | — | Ki | > | 10000000.0 | nM | - |
| CHEMBL555023 | — | Ki | = | 1903000.0 | nM | - |
| CHEMBL104207 | — | Ki | = | 5369000.0 | nM | - |
| CHEMBL318178 | — | Ki | = | 574000.0 | nM | - |
| CHEMBL10731 | — | Ki | = | 384000.0 | nM | - |
| CHEMBL105901 | — | Ki | > | 10000000.0 | nM | - |
| CHEMBL302326 | — | Ki | > | 10000000.0 | nM | - |
| CHEMBL104943 | MONOETHANOLAMINE | Ki | = | 903000.0 | nM | - |
| CHEMBL107582 | — | Ki | = | 200000.0 | nM | - |
| CHEMBL105059 | — | Ki | = | 190000.0 | nM | - |