Assay Detail
Binding
CHEMBL4845002
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of FITC-labelled 5-(((8-Chloro-9-(3-methylpyridin-4-yl)-5-oxo-5,6-dihydro-[1,2,4]triazolo[1,5-c]quinazolin-2-yl)methyl)carbamoyl)-2-(6-hydroxy-3-oxo-3H-xanthen-9-yl)benzoic acid probe from human TIM-3 IgV domain (residues 22 to 130) expressed in Escherichia coli BL21 (DE3) by FPA competition assay
14
Total Activities
13
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Hepatitis A virus cellular receptor 2 (CHEMBL4630879) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Fragment-Based Discovery of Small Molecules Bound to T-Cell Immunoglobulin and Mucin Domain-Containing Molecule 3 (TIM-3).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 5.80 | 6.26 |
| IC50 | 1 | 4.28 | 4.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4873816 | — | — | 1 | 6.26 |
| CHEMBL4863017 | — | — | 1 | 6.12 |
| CHEMBL4868118 | — | — | 1 | 6.01 |
| CHEMBL4875904 | — | — | 1 | 5.89 |
| CHEMBL4874818 | — | — | 1 | 5.82 |
| CHEMBL4846039 | — | — | 1 | 5.82 |
| CHEMBL4859588 | — | — | 1 | 5.80 |
| CHEMBL4851756 | — | — | 1 | 5.75 |
| CHEMBL4860976 | — | — | 1 | 5.68 |
| CHEMBL4872496 | — | — | 1 | 5.66 |
| CHEMBL4876721 | — | — | 1 | 5.64 |
| CHEMBL4864303 | — | — | 1 | 5.58 |
| CHEMBL4863477 | — | — | 2 | 5.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4873816 | — | Ki | = | 550.0 | nM | 6.26 |
| CHEMBL4863017 | — | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL4868118 | — | Ki | = | 970.0 | nM | 6.01 |
| CHEMBL4875904 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL4874818 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL4846039 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL4859588 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL4851756 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL4860976 | — | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL4872496 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL4876721 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL4864303 | — | Ki | = | 2600.0 | nM | 5.58 |
| CHEMBL4863477 | — | Ki | = | 4900.0 | nM | 5.31 |
| CHEMBL4863477 | — | IC50 | = | 53000.0 | nM | 4.28 |