Assay Detail
Binding
CHEMBL913225
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Inhibition of Lck by HTRF kinase assay
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 8.73 | 11.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL215969 | — | — | 1 | 11.00 |
| CHEMBL212181 | — | — | 1 | 10.15 |
| CHEMBL215943 | — | — | 1 | 9.70 |
| CHEMBL385937 | — | — | 1 | 9.70 |
| CHEMBL212964 | — | — | 1 | 9.52 |
| CHEMBL427233 | — | — | 1 | 9.52 |
| CHEMBL212128 | — | — | 1 | 9.52 |
| CHEMBL214530 | — | — | 1 | 9.40 |
| CHEMBL213831 | — | — | 1 | 9.40 |
| CHEMBL212900 | — | — | 1 | 9.40 |
| CHEMBL215745 | — | — | 1 | 9.30 |
| CHEMBL215019 | — | — | 1 | 9.30 |
| CHEMBL386661 | — | — | 1 | 9.30 |
| CHEMBL212953 | — | — | 1 | 9.30 |
| CHEMBL215691 | — | — | 1 | 9.22 |
| CHEMBL215813 | — | — | 1 | 9.22 |
| CHEMBL213428 | — | — | 1 | 9.05 |
| CHEMBL215863 | — | — | 1 | 9.00 |
| CHEMBL427226 | — | — | 1 | 9.00 |
| CHEMBL385598 | — | — | 1 | 8.70 |
| CHEMBL385055 | — | — | 1 | 8.70 |
| CHEMBL213290 | — | — | 1 | 8.52 |
| CHEMBL212183 | — | — | 1 | 8.52 |
| CHEMBL384942 | — | — | 1 | 8.22 |
| CHEMBL214556 | — | — | 1 | 8.22 |
| CHEMBL424719 | — | — | 1 | 8.10 |
| CHEMBL386842 | — | — | 1 | 8.00 |
| CHEMBL212195 | — | — | 1 | 7.85 |
| CHEMBL215529 | — | — | 1 | 7.46 |
| CHEMBL214495 | — | — | 1 | 7.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL215969 | — | IC50 | = | 0.01 | nM | 11.00 |
| CHEMBL212181 | — | IC50 | = | 0.07 | nM | 10.15 |
| CHEMBL215943 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL385937 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL212964 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL427233 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL212128 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL214530 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL213831 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL212900 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL215745 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL215019 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL386661 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL212953 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL215813 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL215691 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL213428 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL215863 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL427226 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL385598 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL385055 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL213290 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL212183 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL384942 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL214556 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL424719 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL386842 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL212195 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL215529 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL214495 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL215952 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL385477 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL215892 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL213478 | — | IC50 | = | 297.0 | nM | 6.53 |