Assay Detail
Binding
CHEMBL3428280
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GST-tagged recombinant full length human ITK using AcEFPIYDFLPAKKK-NH2 as substrate after 35 mins by Morrison plot analysis
18
Total Activities
12
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 |
Publication
Tetrahydroindazoles as Interleukin-2 Inducible T-Cell Kinase Inhibitors. Part II. Second-Generation Analogues with Enhanced Potency, Selectivity, and Pharmacodynamic Modulation in Vivo.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 9.10 | 10.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3426309 | — | — | 1 | 10.05 |
| CHEMBL3426308 | — | — | 1 | 9.70 |
| CHEMBL3426302 | — | — | 2 | 9.70 |
| CHEMBL3426305 | — | — | 2 | 9.70 |
| CHEMBL3426307 | — | — | 2 | 9.52 |
| CHEMBL3426303 | — | — | 2 | 9.52 |
| CHEMBL3426304 | — | — | 1 | 9.52 |
| CHEMBL3426301 | — | — | 2 | 9.30 |
| CHEMBL3426306 | — | — | 1 | 9.30 |
| CHEMBL3298369 | — | — | 2 | 8.52 |
| CHEMBL3298288 | — | — | 1 | 8.28 |
| CHEMBL3298374 | — | — | 1 | 8.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3426309 | — | Ki | = | 0.09 | nM | 10.05 |
| CHEMBL3426308 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3426305 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3426302 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3426307 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3426304 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3426305 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3426303 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3426303 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3426306 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL3426301 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL3426301 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL3426302 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL3298369 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL3298288 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL3298374 | — | Ki | = | 6.2 | nM | 8.21 |
| CHEMBL3298369 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL3426307 | — | Ki | > | 400.0 | nM | - |