Assay Detail
Binding
CHEMBL3587455
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal His-tagged human p110delta expressed in Sf9 cells co-expressing p85alpha regulatory subunit using phosphatidylinositol substrate and [gamma-33P]-ATP by basic thin layer chromatography technique based lipid kinase assay
45
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (CHEMBL3130) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 6.38 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3585619 | — | — | 1 | 7.52 |
| CHEMBL3585612 | — | — | 1 | 6.85 |
| CHEMBL3218574 | — | — | 1 | 6.85 |
| CHEMBL1972466 | — | — | 1 | 6.85 |
| CHEMBL3585609 | — | — | 1 | 6.82 |
| CHEMBL3585602 | — | — | 1 | 6.70 |
| CHEMBL3585581 | — | — | 1 | 6.66 |
| CHEMBL3585616 | — | — | 1 | 6.66 |
| CHEMBL3585601 | — | — | 1 | 6.64 |
| CHEMBL3585588 | — | — | 1 | 6.62 |
| CHEMBL3585607 | — | — | 1 | 6.57 |
| CHEMBL3585617 | — | — | 1 | 6.57 |
| CHEMBL3585583 | — | — | 1 | 6.57 |
| CHEMBL3585611 | — | — | 1 | 6.52 |
| CHEMBL3585597 | — | — | 1 | 6.51 |
| CHEMBL3585595 | — | — | 1 | 6.39 |
| CHEMBL3585605 | — | — | 1 | 6.35 |
| CHEMBL3585593 | — | — | 1 | 6.34 |
| CHEMBL3585598 | — | — | 1 | 6.33 |
| CHEMBL3585584 | — | — | 1 | 6.33 |
| CHEMBL3585582 | — | — | 1 | 6.33 |
| CHEMBL3585591 | — | — | 1 | 6.33 |
| CHEMBL3585618 | — | — | 1 | 6.33 |
| CHEMBL3585621 | — | — | 1 | 6.32 |
| CHEMBL3585600 | — | — | 1 | 6.30 |
| CHEMBL3585610 | — | — | 1 | 6.28 |
| CHEMBL3585592 | — | — | 1 | 6.26 |
| CHEMBL3585590 | — | — | 1 | 6.24 |
| CHEMBL3585589 | — | — | 1 | 6.22 |
| CHEMBL3585603 | — | — | 1 | 6.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3585619 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3585612 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3218574 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL1972466 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3585609 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3585602 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3585581 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL3585616 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL3585601 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL3585588 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL3585607 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL3585583 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL3585617 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL3585611 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL3585597 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL3585595 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL3585605 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL3585593 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL3585618 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL3585591 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL3585584 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL3585598 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL3585582 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL3585621 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL3585600 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL3585610 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL3585592 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL3585590 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL3585589 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL3585603 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL3585606 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL3585586 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL3585608 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL3585604 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL3585585 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL3585596 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL3585599 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3585587 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3585594 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL3585620 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL3585622 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL3585615 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3585614 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3585613 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3585351 | — | IC50 | > | 10000.0 | nM | - |