Assay Detail
Binding
CHEMBL1104614
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Inhibition of PI3Kalpha by DELFIA assay
49
Total Activities
49
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (CHEMBL4005) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of 4-morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as highly potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): optimization of the 6-aryl substituent.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 49 | 6.69 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1098245 | — | — | 1 | 8.00 |
| CHEMBL550972 | — | — | 1 | 7.85 |
| CHEMBL556947 | — | — | 1 | 7.82 |
| CHEMBL1097900 | — | — | 1 | 7.78 |
| CHEMBL1098244 | — | — | 1 | 7.77 |
| CHEMBL1098247 | — | — | 1 | 7.68 |
| CHEMBL1097898 | — | — | 1 | 7.54 |
| CHEMBL1097902 | — | — | 1 | 7.52 |
| CHEMBL1098246 | — | — | 1 | 7.47 |
| CHEMBL1095627 | — | — | 1 | 7.39 |
| CHEMBL1098248 | — | — | 1 | 7.39 |
| CHEMBL551440 | — | — | 1 | 7.39 |
| CHEMBL1097901 | — | — | 1 | 7.26 |
| CHEMBL1095618 | — | — | 1 | 7.23 |
| CHEMBL1095933 | — | — | 1 | 7.10 |
| CHEMBL1098305 | — | — | 1 | 7.08 |
| CHEMBL1097896 | — | — | 1 | 7.07 |
| CHEMBL563985 | — | — | 1 | 7.00 |
| CHEMBL1098619 | — | — | 1 | 6.86 |
| CHEMBL1095932 | — | — | 1 | 6.72 |
| CHEMBL1097261 | — | — | 1 | 6.64 |
| CHEMBL1097893 | — | — | 1 | 6.63 |
| CHEMBL1098306 | — | — | 1 | 6.59 |
| CHEMBL1097894 | — | — | 1 | 6.57 |
| CHEMBL552532 | — | — | 1 | 6.55 |
| CHEMBL1097263 | — | — | 1 | 6.54 |
| CHEMBL1095945 | — | — | 1 | 6.50 |
| CHEMBL1097895 | — | — | 1 | 6.49 |
| CHEMBL1097897 | — | — | 1 | 6.40 |
| CHEMBL1097262 | — | — | 1 | 6.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1098245 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL550972 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL556947 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1097900 | — | IC50 | = | 16.5 | nM | 7.78 |
| CHEMBL1098244 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL1098247 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL1097898 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL1097902 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1098246 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL1095627 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL1098248 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL551440 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL1097901 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL1095618 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL1095933 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL1098305 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL1097896 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL563985 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL1098619 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL1095932 | — | IC50 | = | 189.0 | nM | 6.72 |
| CHEMBL1097261 | — | IC50 | = | 231.0 | nM | 6.64 |
| CHEMBL1097893 | — | IC50 | = | 234.0 | nM | 6.63 |
| CHEMBL1098306 | — | IC50 | = | 257.0 | nM | 6.59 |
| CHEMBL1097894 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL552532 | — | IC50 | = | 284.0 | nM | 6.55 |
| CHEMBL1097263 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL1095945 | — | IC50 | = | 317.0 | nM | 6.50 |
| CHEMBL1097895 | — | IC50 | = | 323.0 | nM | 6.49 |
| CHEMBL1097897 | — | IC50 | = | 401.0 | nM | 6.40 |
| CHEMBL1097262 | — | IC50 | = | 436.0 | nM | 6.36 |
| CHEMBL1098301 | — | IC50 | = | 486.0 | nM | 6.31 |
| CHEMBL1098300 | — | IC50 | = | 493.0 | nM | 6.31 |
| CHEMBL561907 | — | IC50 | = | 505.0 | nM | 6.30 |
| CHEMBL1097603 | — | IC50 | = | 589.0 | nM | 6.23 |
| CHEMBL562999 | — | IC50 | = | 661.0 | nM | 6.18 |
| CHEMBL1097899 | — | IC50 | = | 708.0 | nM | 6.15 |
| CHEMBL1098242 | — | IC50 | = | 786.0 | nM | 6.11 |
| CHEMBL1095626 | — | IC50 | = | 801.0 | nM | 6.10 |
| CHEMBL1095281 | — | IC50 | = | 792.0 | nM | 6.10 |
| CHEMBL561103 | — | IC50 | = | 801.0 | nM | 6.10 |
| CHEMBL1098243 | — | IC50 | = | 898.0 | nM | 6.05 |
| CHEMBL1098310 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL1095946 | — | IC50 | = | 1005.0 | nM | 6.00 |
| CHEMBL1098311 | — | IC50 | = | 1050.0 | nM | 5.98 |
| CHEMBL1094981 | — | IC50 | = | 1207.0 | nM | 5.92 |
| CHEMBL1095625 | — | IC50 | = | 1368.0 | nM | 5.86 |
| CHEMBL1097942 | — | IC50 | = | 1782.0 | nM | 5.75 |
| CHEMBL1097561 | — | IC50 | = | 1935.0 | nM | 5.71 |
| CHEMBL1095623 | — | IC50 | = | 4058.0 | nM | 5.39 |