Assay Detail
Functional
CHEMBL817437
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibition of TNF-alpha release from human peripheral blood monocytes
12
Total Activities
12
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 | 12 | 6.73 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL146218 | — | — | 1 | 7.96 |
| CHEMBL144287 | — | — | 1 | 7.42 |
| CHEMBL145258 | — | — | 1 | 7.32 |
| CHEMBL343243 | — | — | 1 | 7.10 |
| CHEMBL63 | ROLIPRAM | 2.0 | 1 | 7.08 |
| CHEMBL434516 | — | — | 1 | 6.91 |
| CHEMBL144245 | — | — | 1 | 6.58 |
| CHEMBL342285 | — | — | 1 | 6.47 |
| CHEMBL144570 | — | — | 1 | 6.35 |
| CHEMBL112366 | — | — | 1 | 6.32 |
| CHEMBL111925 | — | — | 1 | 6.00 |
| CHEMBL125123 | — | — | 1 | 5.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL146218 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL144287 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL145258 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL343243 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL63 | ROLIPRAM | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL434516 | — | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL144245 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL342285 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL144570 | — | IC50 | = | 443.0 | nM | 6.35 |
| CHEMBL112366 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL111925 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL125123 | — | IC50 | = | 5350.0 | nM | 5.27 |