Assay Detail
Binding
CHEMBL813690
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Inhibitory activity against TACE.
35
Total Activities
35
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 bicyclic heteroaryl hydroxamic acid MMP and TACE inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 6.82 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL36309 | — | — | 1 | 8.22 |
| CHEMBL417144 | — | — | 1 | 7.85 |
| CHEMBL288671 | — | — | 1 | 7.77 |
| CHEMBL289222 | — | — | 1 | 7.52 |
| CHEMBL35989 | — | — | 1 | 7.09 |
| CHEMBL35606 | — | — | 1 | 7.07 |
| CHEMBL290952 | — | — | 1 | 6.92 |
| CHEMBL289604 | — | — | 1 | 6.91 |
| CHEMBL285546 | — | — | 1 | 6.91 |
| CHEMBL287871 | — | — | 1 | 6.91 |
| CHEMBL38352 | — | — | 1 | 6.91 |
| CHEMBL429336 | — | — | 1 | 6.86 |
| CHEMBL34418 | — | — | 1 | 6.83 |
| CHEMBL288670 | — | — | 1 | 6.80 |
| CHEMBL37788 | — | — | 1 | 6.79 |
| CHEMBL34411 | — | — | 1 | 6.72 |
| CHEMBL38106 | — | — | 1 | 6.69 |
| CHEMBL34808 | — | — | 1 | 6.65 |
| CHEMBL37837 | — | — | 1 | 6.53 |
| CHEMBL290948 | — | — | 1 | 6.50 |
| CHEMBL35433 | — | — | 1 | 6.47 |
| CHEMBL286848 | — | — | 1 | 6.45 |
| CHEMBL34660 | — | — | 1 | 6.40 |
| CHEMBL33980 | — | — | 1 | 6.36 |
| CHEMBL35707 | — | — | 1 | 6.27 |
| CHEMBL36999 | — | — | 1 | 6.23 |
| CHEMBL289411 | — | — | 1 | 6.20 |
| CHEMBL287820 | — | — | 1 | 6.00 |
| CHEMBL287823 | — | — | 1 | - |
| CHEMBL36021 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL36309 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL417144 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL288671 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL289222 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL35989 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL35606 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL290952 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL289604 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL285546 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL287871 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL38352 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL429336 | — | IC50 | = | 138.0 | nM | 6.86 |
| CHEMBL34418 | — | IC50 | = | 147.0 | nM | 6.83 |
| CHEMBL288670 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL37788 | — | IC50 | = | 161.0 | nM | 6.79 |
| CHEMBL34411 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL38106 | — | IC50 | = | 205.0 | nM | 6.69 |
| CHEMBL34808 | — | IC50 | = | 226.0 | nM | 6.65 |
| CHEMBL37837 | — | IC50 | = | 296.0 | nM | 6.53 |
| CHEMBL290948 | — | IC50 | = | 314.0 | nM | 6.50 |
| CHEMBL35433 | — | IC50 | = | 336.0 | nM | 6.47 |
| CHEMBL286848 | — | IC50 | = | 356.0 | nM | 6.45 |
| CHEMBL34660 | — | IC50 | = | 401.0 | nM | 6.40 |
| CHEMBL33980 | — | IC50 | = | 435.0 | nM | 6.36 |
| CHEMBL35707 | — | IC50 | = | 535.0 | nM | 6.27 |
| CHEMBL36999 | — | IC50 | = | 589.0 | nM | 6.23 |
| CHEMBL289411 | — | IC50 | = | 627.0 | nM | 6.20 |
| CHEMBL287820 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL287823 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL36021 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL36191 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL38180 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL35059 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL418053 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL34666 | — | IC50 | > | 1000.0 | nM | - |