Assay Detail
Binding
CHEMBL5504664
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Inhibition of PI3Kdelta/AKT pathway in M-CSF stimulated human THP-1 cells assessed as decrease in AKT phosphorylation preincubated for 60 mins followed by M-CSF stimulation and measured after 10 mins by HTRF analysis
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | THP-1 |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Discovery and Optimization of Pyridazinones as PI3Kδ Selective Inhibitors for Administration by Inhalation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 7.53 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5558448 | — | — | 1 | 9.30 |
| CHEMBL5555605 | — | — | 1 | 8.90 |
| CHEMBL5531964 | — | — | 1 | 8.60 |
| CHEMBL5555403 | — | — | 1 | 8.30 |
| CHEMBL5542678 | — | — | 1 | 8.10 |
| CHEMBL5527852 | — | — | 1 | 8.00 |
| CHEMBL5517938 | — | — | 1 | 7.80 |
| CHEMBL5543016 | — | — | 1 | 7.70 |
| CHEMBL5512440 | — | — | 1 | 7.70 |
| CHEMBL5559126 | — | — | 1 | 7.60 |
| CHEMBL5559413 | — | — | 1 | 7.30 |
| CHEMBL5512540 | — | — | 1 | 7.00 |
| CHEMBL1213083 | — | — | 1 | 7.00 |
| CHEMBL5558076 | — | — | 1 | 7.00 |
| CHEMBL5518064 | — | — | 1 | 6.90 |
| CHEMBL5542223 | — | — | 1 | 6.70 |
| CHEMBL5557135 | — | — | 1 | 6.60 |
| CHEMBL5517641 | — | — | 1 | 6.30 |
| CHEMBL5555181 | — | — | 1 | 6.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5558448 | — | IC50 | = | 0.5012 | nM | 9.30 |
| CHEMBL5555605 | — | IC50 | = | 1.259 | nM | 8.90 |
| CHEMBL5531964 | — | IC50 | = | 2.512 | nM | 8.60 |
| CHEMBL5555403 | — | IC50 | = | 5.012 | nM | 8.30 |
| CHEMBL5542678 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL5527852 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5517938 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL5543016 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL5512440 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL5559126 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL5559413 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL5512540 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL1213083 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5558076 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5518064 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL5542223 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL5557135 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL5517641 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL5555181 | — | IC50 | = | 501.19 | nM | 6.30 |