Assay Detail
Binding
CHEMBL833550
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Inhibitory concentration against TNF-alpha converting enzyme at 1 uM
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Disintegrin and metalloproteinase domain-containing protein 17 (CHEMBL3706) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and SAR of diazepine and thiazepine TACE and MMP inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 7.68 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL180891 | — | — | 1 | 8.40 |
| CHEMBL181317 | — | — | 1 | 8.30 |
| CHEMBL369574 | — | — | 1 | 8.15 |
| CHEMBL361809 | — | — | 1 | 8.00 |
| CHEMBL369302 | — | — | 1 | 8.00 |
| CHEMBL359920 | — | — | 1 | 7.96 |
| CHEMBL180410 | — | — | 1 | 7.92 |
| CHEMBL180181 | — | — | 1 | 7.89 |
| CHEMBL180627 | — | — | 1 | 7.85 |
| CHEMBL178929 | — | — | 1 | 7.82 |
| CHEMBL180484 | — | — | 1 | 7.77 |
| CHEMBL181328 | — | — | 1 | 7.72 |
| CHEMBL178732 | — | — | 1 | 7.72 |
| CHEMBL362797 | — | — | 1 | 7.70 |
| CHEMBL361959 | — | — | 1 | 7.64 |
| CHEMBL180130 | — | — | 1 | 7.64 |
| CHEMBL181094 | — | — | 1 | 7.62 |
| CHEMBL360257 | — | — | 1 | 7.62 |
| CHEMBL180047 | — | — | 1 | 7.55 |
| CHEMBL181365 | — | — | 1 | 7.52 |
| CHEMBL180245 | — | — | 1 | 7.46 |
| CHEMBL181208 | — | — | 1 | 7.43 |
| CHEMBL180333 | — | — | 1 | 7.21 |
| CHEMBL180197 | — | — | 1 | 7.17 |
| CHEMBL359502 | — | — | 1 | 7.13 |
| CHEMBL181110 | — | — | 1 | 7.12 |
| CHEMBL183132 | — | — | 1 | 7.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL180891 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL181317 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL369574 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL361809 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL369302 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL359920 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL180410 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL180181 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL180627 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL178929 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL180484 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL181328 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL178732 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL362797 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL361959 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL180130 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL181094 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL360257 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL180047 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL181365 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL180245 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL181208 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL180333 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL180197 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL359502 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL181110 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL183132 | — | IC50 | = | 83.0 | nM | 7.08 |