Assay Detail
Binding
CHEMBL4386801
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Cis-inhibition of human LAT1 expressed in TREx HEK293 cells assessed as inhibition of [3H]-gabapentin uptake preincubated for 3 mins at 37 degC followed by washing with choline buffer and measured after 3 hrs by scintillation counting analysis
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Large neutral amino acids transporter small subunit 1 (CHEMBL4459) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
l-Type amino acid transporter 1 activity of 1,2,3-triazolyl analogs of l-histidine and l-tryptophan.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 4.11 | 4.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL301523 | PHENYLALANINE | 3.0 | 1 | 4.16 |
| CHEMBL4242404 | — | — | 1 | 4.16 |
| CHEMBL4249170 | — | — | 1 | 4.00 |
| CHEMBL4464816 | — | — | 1 | - |
| CHEMBL4448346 | — | — | 1 | - |
| CHEMBL4569744 | — | — | 1 | - |
| CHEMBL4586342 | — | — | 1 | - |
| CHEMBL4587818 | — | — | 1 | - |
| CHEMBL4457506 | — | — | 1 | - |
| CHEMBL4570233 | — | — | 1 | - |
| CHEMBL17962 | HISTIDINE | 2.0 | 1 | - |
| CHEMBL1233327 | — | — | 1 | - |
| CHEMBL4240267 | — | — | 1 | - |
| CHEMBL4243343 | — | — | 1 | - |
| CHEMBL54976 | TRYPTOPHAN | 4.0 | 1 | - |
| CHEMBL4559029 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL301523 | PHENYLALANINE | IC50 | = | 69000.0 | nM | 4.16 |
| CHEMBL4242404 | — | IC50 | = | 69000.0 | nM | 4.16 |
| CHEMBL4249170 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL4464816 | — | IC50 | = | 160000.0 | nM | - |
| CHEMBL4448346 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL4569744 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL4586342 | — | IC50 | = | 440000.0 | nM | - |
| CHEMBL4587818 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL4457506 | — | IC50 | - | — | - | |
| CHEMBL4570233 | — | IC50 | - | — | - | |
| CHEMBL17962 | HISTIDINE | IC50 | = | 110000.0 | nM | - |
| CHEMBL1233327 | — | IC50 | = | 190000.0 | nM | - |
| CHEMBL4240267 | — | IC50 | = | 170000.0 | nM | - |
| CHEMBL4243343 | — | IC50 | = | 160000.0 | nM | - |
| CHEMBL54976 | TRYPTOPHAN | IC50 | = | 160000.0 | nM | - |
| CHEMBL4559029 | — | IC50 | = | 340000.0 | nM | - |