Assay Detail
Binding
CHEMBL2446687
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Inhibition of recombinant human FLAG-tagged ITK using biotinylated GST-SAM68 as substrate after 30 mins
21
Total Activities
21
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
Identification of a Novel and Selective Series of Itk Inhibitors via a Template-Hopping Strategy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 8.17 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2441275 | — | — | 1 | 9.70 |
| CHEMBL2441276 | — | — | 1 | 9.60 |
| CHEMBL2441274 | — | — | 1 | 9.60 |
| CHEMBL2441271 | — | — | 1 | 9.50 |
| CHEMBL2441270 | — | — | 1 | 9.40 |
| CHEMBL2441273 | — | — | 1 | 9.20 |
| CHEMBL2441269 | — | — | 1 | 9.00 |
| CHEMBL2441277 | — | — | 1 | 8.80 |
| CHEMBL2441267 | — | — | 1 | 8.70 |
| CHEMBL2441112 | — | — | 1 | 8.40 |
| CHEMBL2441281 | — | — | 1 | 8.20 |
| CHEMBL2441272 | — | — | 1 | 7.90 |
| CHEMBL2441285 | — | — | 1 | 7.80 |
| CHEMBL2441286 | — | — | 1 | 7.70 |
| CHEMBL2441283 | — | — | 1 | 7.20 |
| CHEMBL2441113 | — | — | 1 | 6.80 |
| CHEMBL2441282 | — | — | 1 | 6.30 |
| CHEMBL2441280 | — | — | 1 | 6.10 |
| CHEMBL2441111 | — | — | 1 | 5.40 |
| CHEMBL2441284 | — | — | 1 | - |
| CHEMBL2441268 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2441275 | — | Ki | = | 0.1995 | nM | 9.70 |
| CHEMBL2441276 | — | Ki | = | 0.2512 | nM | 9.60 |
| CHEMBL2441274 | — | Ki | = | 0.2512 | nM | 9.60 |
| CHEMBL2441271 | — | Ki | = | 0.3162 | nM | 9.50 |
| CHEMBL2441270 | — | Ki | = | 0.3981 | nM | 9.40 |
| CHEMBL2441273 | — | Ki | = | 0.631 | nM | 9.20 |
| CHEMBL2441269 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL2441277 | — | Ki | = | 1.585 | nM | 8.80 |
| CHEMBL2441267 | — | Ki | = | 1.995 | nM | 8.70 |
| CHEMBL2441112 | — | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL2441281 | — | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL2441272 | — | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL2441285 | — | Ki | = | 15.85 | nM | 7.80 |
| CHEMBL2441286 | — | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL2441283 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL2441113 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL2441282 | — | Ki | = | 501.19 | nM | 6.30 |
| CHEMBL2441280 | — | Ki | = | 794.33 | nM | 6.10 |
| CHEMBL2441111 | — | Ki | = | 3981.07 | nM | 5.40 |
| CHEMBL2441284 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2441268 | — | Ki | > | 10000.0 | nM | - |