Assay Detail
Binding
CHEMBL4016543
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3Kdelta in human whole blood assessed as reduction in anti-IgD-mediated B-cell activation by measuring decrease in CD19+ cells expressing CD69 preincubated for 1 hr followed by IgD activation measured after overnight incubation
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 delta isoform (CHEMBL3130) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinase δ (PI3Kδ) Inhibitor for the Treatment of Immunological Disorders.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 37 | 7.08 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4068514 | — | — | 1 | 8.15 |
| CHEMBL4092344 | — | — | 1 | 7.80 |
| CHEMBL4071965 | — | — | 1 | 7.75 |
| CHEMBL4105075 | — | — | 1 | 7.62 |
| CHEMBL4087215 | — | — | 1 | 7.51 |
| CHEMBL4102552 | — | — | 1 | 7.51 |
| CHEMBL4093883 | — | — | 1 | 7.46 |
| CHEMBL4064666 | — | — | 1 | 7.46 |
| CHEMBL4092240 | — | — | 1 | 7.44 |
| CHEMBL4081766 | — | — | 1 | 7.42 |
| CHEMBL4067315 | — | — | 1 | 7.42 |
| CHEMBL4066316 | — | — | 1 | 7.41 |
| CHEMBL4068408 | — | — | 1 | 7.38 |
| CHEMBL4059848 | — | — | 1 | 7.24 |
| CHEMBL4095752 | — | — | 1 | 7.18 |
| CHEMBL4064543 | — | — | 1 | 7.14 |
| CHEMBL4102444 | — | — | 1 | 7.13 |
| CHEMBL4073255 | — | — | 1 | 7.10 |
| CHEMBL4074315 | — | — | 1 | 7.05 |
| CHEMBL4100099 | — | — | 1 | 7.04 |
| CHEMBL4086128 | — | — | 1 | 7.02 |
| CHEMBL4091840 | — | — | 1 | 7.00 |
| CHEMBL4083358 | — | — | 1 | 6.98 |
| CHEMBL4074193 | — | — | 1 | 6.85 |
| CHEMBL4084604 | — | — | 1 | 6.82 |
| CHEMBL4076137 | — | — | 1 | 6.80 |
| CHEMBL4078237 | — | — | 1 | 6.66 |
| CHEMBL4070029 | — | — | 1 | 6.64 |
| CHEMBL4094814 | — | — | 1 | 6.64 |
| CHEMBL4094693 | — | — | 1 | 6.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4068514 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4092344 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4071965 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4105075 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4087215 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4102552 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4093883 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4064666 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4092240 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4067315 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL4081766 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL4066316 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4068408 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4059848 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL4095752 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL4064543 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL4102444 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL4073255 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL4074315 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL4100099 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL4086128 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL4091840 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4083358 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL4074193 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4084604 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4076137 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4078237 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL4094814 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL4070029 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL4094693 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4097222 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL4070164 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL4087001 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4096288 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL4104044 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL4088567 | — | IC50 | - | — | - | |
| CHEMBL4084490 | — | IC50 | - | — | - |