Assay Detail
Functional
CHEMBL817438
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibition of TNF-alpha-release from human whole blood
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Synthesis, structure-activity relationships, and pharmacological profile of 9-amino-4-oxo-1-phenyl-3,4,6,7-tetrahydro[1,4]diazepino[6, 7,1-hi]indoles: discovery of potent, selective phosphodiesterase type 4 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 5.84 | 6.67 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL144287 | — | — | 1 | 6.67 |
| CHEMBL343243 | — | — | 1 | 6.40 |
| CHEMBL146218 | — | — | 1 | 6.36 |
| CHEMBL144245 | — | — | 1 | 6.12 |
| CHEMBL63 | ROLIPRAM | 2.0 | 1 | 6.03 |
| CHEMBL434516 | — | — | 1 | 5.97 |
| CHEMBL112366 | — | — | 1 | 5.96 |
| CHEMBL342285 | — | — | 1 | 5.91 |
| CHEMBL144570 | — | — | 1 | 5.82 |
| CHEMBL145258 | — | — | 1 | 5.47 |
| CHEMBL511115 | CILOMILAST | 3.0 | 1 | 5.14 |
| CHEMBL111925 | — | — | 1 | 4.21 |
| CHEMBL125123 | — | — | 1 | - |
| CHEMBL341671 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL144287 | — | IC50 | = | 213.0 | nM | 6.67 |
| CHEMBL343243 | — | IC50 | = | 398.0 | nM | 6.40 |
| CHEMBL146218 | — | IC50 | = | 438.0 | nM | 6.36 |
| CHEMBL144245 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL63 | ROLIPRAM | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL434516 | — | IC50 | = | 1061.0 | nM | 5.97 |
| CHEMBL112366 | — | IC50 | = | 1090.0 | nM | 5.96 |
| CHEMBL342285 | — | IC50 | = | 1240.0 | nM | 5.91 |
| CHEMBL144570 | — | IC50 | = | 1520.0 | nM | 5.82 |
| CHEMBL145258 | — | IC50 | = | 3366.0 | nM | 5.47 |
| CHEMBL511115 | CILOMILAST | IC50 | = | 7300.0 | nM | 5.14 |
| CHEMBL111925 | — | IC50 | = | 61000.0 | nM | 4.21 |
| CHEMBL125123 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL341671 | — | IC50 | = | - | nM | - |