Assay Detail
Binding
CHEMBL805974
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In vitro inhibition of TNF-alpha converting enzyme (TACE)
20
Total Activities
20
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
The discovery of anthranilic acid-based MMP inhibitors. Part 2: SAR of the 5-position and P1(1) groups.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 6.84 | 7.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL71227 | — | — | 1 | 7.64 |
| CHEMBL305499 | — | — | 1 | 7.55 |
| CHEMBL71725 | — | — | 1 | 7.37 |
| CHEMBL71436 | — | — | 1 | 7.25 |
| CHEMBL67590 | — | — | 1 | 7.24 |
| CHEMBL69268 | — | — | 1 | 7.21 |
| CHEMBL303666 | — | — | 1 | 7.19 |
| CHEMBL307079 | — | — | 1 | 7.16 |
| CHEMBL68271 | — | — | 1 | 6.88 |
| CHEMBL70957 | — | — | 1 | 6.76 |
| CHEMBL68542 | — | — | 1 | 6.71 |
| CHEMBL70176 | — | — | 1 | 6.64 |
| CHEMBL514138 | CGS-27023A | — | 1 | 6.64 |
| CHEMBL69569 | — | — | 1 | 6.54 |
| CHEMBL304730 | — | — | 1 | 6.53 |
| CHEMBL307990 | — | — | 1 | 6.42 |
| CHEMBL70207 | — | — | 1 | 6.37 |
| CHEMBL71007 | — | — | 1 | 6.33 |
| CHEMBL419995 | — | — | 1 | 6.20 |
| CHEMBL71686 | — | — | 1 | 6.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL71227 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL305499 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL71725 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL71436 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL67590 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL69268 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL303666 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL307079 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL68271 | — | IC50 | = | 133.0 | nM | 6.88 |
| CHEMBL70957 | — | IC50 | = | 173.0 | nM | 6.76 |
| CHEMBL68542 | — | IC50 | = | 194.0 | nM | 6.71 |
| CHEMBL70176 | — | IC50 | = | 231.0 | nM | 6.64 |
| CHEMBL514138 | CGS-27023A | IC50 | = | 231.0 | nM | 6.64 |
| CHEMBL69569 | — | IC50 | = | 285.0 | nM | 6.54 |
| CHEMBL304730 | — | IC50 | = | 294.0 | nM | 6.53 |
| CHEMBL307990 | — | IC50 | = | 377.0 | nM | 6.42 |
| CHEMBL70207 | — | IC50 | = | 429.0 | nM | 6.37 |
| CHEMBL71007 | — | IC50 | = | 467.0 | nM | 6.33 |
| CHEMBL419995 | — | IC50 | = | 633.0 | nM | 6.20 |
| CHEMBL71686 | — | IC50 | = | 727.0 | nM | 6.14 |