Assay Detail
Binding
CHEMBL4718896
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human LAT1 expressed in HEK293-T-Rex cells assessed as inhibition of [3H]-gabapentin uptake by scintillation counting cis-inhibition assay relative to BCH inhibition (RV = 100%)
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293-T-REx |
| 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
LAT1 activity of carboxylic acid bioisosteres: Evaluation of hydroxamic acids as substrates.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 4.06 | 4.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL291962 | LEUCINE | 3.0 | 1 | 4.06 |
| CHEMBL4760569 | — | — | 1 | - |
| CHEMBL4757756 | — | — | 1 | - |
| CHEMBL216796 | — | — | 1 | - |
| CHEMBL4749347 | — | — | 1 | - |
| CHEMBL4755600 | — | — | 1 | - |
| CHEMBL4742824 | — | — | 1 | - |
| CHEMBL42336 | METHIONINE | 3.0 | 1 | - |
| CHEMBL1233584 | ISOLEUCINE | 2.0 | 1 | - |
| CHEMBL773 | GLYCINE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL291962 | LEUCINE | IC50 | = | 87000.0 | nM | 4.06 |
| CHEMBL4760569 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4757756 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL216796 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4749347 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4755600 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4742824 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL42336 | METHIONINE | IC50 | = | 180000.0 | nM | - |
| CHEMBL1233584 | ISOLEUCINE | IC50 | = | 150000.0 | nM | - |
| CHEMBL773 | GLYCINE | IC50 | > | 200000.0 | nM | - |