Assay Detail
Functional
CHEMBL3587456
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of cell proliferation of human NZB5 cells containing wild-type p110alpha gene incubated for 5 days by [3H]thymidine incorporation assay
45
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | NZB5 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Exploring the isoform selectivity of TGX-221 related pyrido[1,2-a]pyrimidinone-based Class IA PI 3-kinase inhibitors: synthesis, biological evaluation and molecular modelling.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 45 | 5.48 | 7.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3585601 | — | — | 1 | 7.00 |
| CHEMBL3585588 | — | — | 1 | 6.47 |
| CHEMBL3585602 | — | — | 1 | 6.40 |
| CHEMBL3585603 | — | — | 1 | 6.40 |
| CHEMBL3585608 | — | — | 1 | 6.16 |
| CHEMBL3585607 | — | — | 1 | 6.16 |
| CHEMBL3585598 | — | — | 1 | 6.05 |
| CHEMBL3585619 | — | — | 1 | 6.05 |
| CHEMBL3585599 | — | — | 1 | 6.00 |
| CHEMBL3585595 | — | — | 1 | 5.92 |
| CHEMBL3585600 | — | — | 1 | 5.82 |
| CHEMBL3218574 | — | — | 1 | 5.82 |
| CHEMBL3585609 | — | — | 1 | 5.70 |
| CHEMBL3585596 | — | — | 1 | 5.70 |
| CHEMBL3585604 | — | — | 1 | 5.62 |
| CHEMBL1972466 | — | — | 1 | 5.55 |
| CHEMBL3585585 | — | — | 1 | 5.52 |
| CHEMBL3585617 | — | — | 1 | 5.26 |
| CHEMBL3585586 | — | — | 1 | 5.26 |
| CHEMBL3585618 | — | — | 1 | 5.22 |
| CHEMBL3585620 | — | — | 1 | 5.22 |
| CHEMBL3585622 | — | — | 1 | 5.16 |
| CHEMBL3585621 | — | — | 1 | 5.14 |
| CHEMBL3585590 | — | — | 1 | 5.11 |
| CHEMBL3585611 | — | — | 1 | 5.10 |
| CHEMBL3585605 | — | — | 1 | 5.09 |
| CHEMBL3585616 | — | — | 1 | 5.00 |
| CHEMBL3585583 | — | — | 1 | 4.92 |
| CHEMBL3585615 | — | — | 1 | 4.92 |
| CHEMBL3585593 | — | — | 1 | 4.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3585601 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3585588 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL3585603 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3585602 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3585608 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL3585607 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL3585598 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL3585619 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL3585599 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3585595 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3585600 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL3218574 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL3585609 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3585596 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3585604 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL1972466 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL3585585 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL3585617 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL3585586 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL3585618 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL3585620 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL3585622 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL3585621 | — | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL3585590 | — | IC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL3585611 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL3585605 | — | IC50 | = | 8200.0 | nM | 5.09 |
| CHEMBL3585616 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3585583 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL3585615 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL3585593 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL3585592 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL3585606 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL3585591 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL3585614 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL3585589 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL3585613 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL3585584 | — | IC50 | - | — | - | |
| CHEMBL3585581 | — | IC50 | - | — | - | |
| CHEMBL3585582 | — | IC50 | - | — | - | |
| CHEMBL3585597 | — | IC50 | - | — | - | |
| CHEMBL3585587 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL3585612 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL3585610 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL3585351 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL3585594 | — | IC50 | > | 20000.0 | nM | - |