Assay Detail
Binding
CHEMBL3615645
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3Kalpha (unknown origin) by radiometric assay
37
Total Activities
37
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 |
Target
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (CHEMBL4005) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery and SAR of novel pyrazolo[1,5-a]pyrimidines as inhibitors of CDK9.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 37 | 6.21 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL393525 | — | — | 1 | 9.30 |
| CHEMBL3612501 | — | — | 1 | 7.54 |
| CHEMBL3612502 | — | — | 1 | 7.09 |
| CHEMBL3612622 | — | — | 1 | 6.79 |
| CHEMBL3612514 | — | — | 1 | 6.71 |
| CHEMBL3612507 | — | — | 1 | 6.70 |
| CHEMBL3612504 | — | — | 1 | 6.63 |
| CHEMBL3612482 | — | — | 1 | 6.57 |
| CHEMBL3612508 | — | — | 1 | 6.49 |
| CHEMBL3612511 | — | — | 1 | 6.05 |
| CHEMBL3612503 | — | — | 1 | 6.04 |
| CHEMBL3612506 | — | — | 1 | 5.99 |
| CHEMBL3612515 | — | — | 1 | 5.97 |
| CHEMBL3612505 | — | — | 1 | 5.91 |
| CHEMBL3612512 | — | — | 1 | 5.73 |
| CHEMBL3612499 | — | — | 1 | 5.53 |
| CHEMBL3612498 | — | — | 1 | 5.53 |
| CHEMBL3612485 | — | — | 1 | 5.36 |
| CHEMBL3612490 | — | — | 1 | 5.34 |
| CHEMBL3612491 | — | — | 1 | 5.27 |
| CHEMBL3612493 | — | — | 1 | 5.11 |
| CHEMBL3612500 | — | — | 1 | 5.03 |
| CHEMBL3612513 | — | — | 1 | - |
| CHEMBL3612484 | — | — | 1 | - |
| CHEMBL3612510 | — | — | 1 | - |
| CHEMBL3612509 | — | — | 1 | - |
| CHEMBL3612489 | — | — | 1 | - |
| CHEMBL3612483 | — | — | 1 | - |
| CHEMBL3612486 | — | — | 1 | - |
| CHEMBL3612487 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL393525 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3612501 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL3612502 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL3612622 | — | IC50 | = | 164.0 | nM | 6.79 |
| CHEMBL3612514 | — | IC50 | = | 194.0 | nM | 6.71 |
| CHEMBL3612507 | — | IC50 | = | 198.0 | nM | 6.70 |
| CHEMBL3612504 | — | IC50 | = | 233.0 | nM | 6.63 |
| CHEMBL3612482 | — | IC50 | = | 271.0 | nM | 6.57 |
| CHEMBL3612508 | — | IC50 | = | 327.0 | nM | 6.49 |
| CHEMBL3612511 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL3612503 | — | IC50 | = | 902.0 | nM | 6.04 |
| CHEMBL3612506 | — | IC50 | = | 1030.0 | nM | 5.99 |
| CHEMBL3612515 | — | IC50 | = | 1070.0 | nM | 5.97 |
| CHEMBL3612505 | — | IC50 | = | 1240.0 | nM | 5.91 |
| CHEMBL3612512 | — | IC50 | = | 1870.0 | nM | 5.73 |
| CHEMBL3612499 | — | IC50 | = | 2963.0 | nM | 5.53 |
| CHEMBL3612498 | — | IC50 | = | 2960.0 | nM | 5.53 |
| CHEMBL3612485 | — | IC50 | = | 4350.0 | nM | 5.36 |
| CHEMBL3612490 | — | IC50 | = | 4544.0 | nM | 5.34 |
| CHEMBL3612491 | — | IC50 | = | 5373.0 | nM | 5.27 |
| CHEMBL3612493 | — | IC50 | = | 7840.0 | nM | 5.11 |
| CHEMBL3612500 | — | IC50 | = | 9430.0 | nM | 5.03 |
| CHEMBL3612492 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3612494 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3612495 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3612496 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3612497 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3612072 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3612488 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3612487 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3612486 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3612483 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3612489 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3612509 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3612510 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3612484 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3612513 | — | IC50 | > | 10000.0 | nM | - |