Assay Detail
Binding
CHEMBL1003624
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Inhibition of TACE
38
Total Activities
37
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
Disintegrin and metalloproteinase domain-containing protein 17 (CHEMBL3706) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Current perspective of TACE inhibitors: a review.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 37 | 8.12 | 10.59 |
| Ki | 1 | 8.64 | 8.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL391851 | — | — | 1 | 10.59 |
| CHEMBL271235 | — | — | 1 | 9.85 |
| CHEMBL489100 | — | — | 1 | 9.70 |
| CHEMBL193316 | — | — | 1 | 9.00 |
| CHEMBL184885 | — | — | 1 | 9.00 |
| CHEMBL524092 | — | — | 1 | 9.00 |
| CHEMBL148169 | — | — | 2 | 9.00 |
| CHEMBL491287 | — | — | 1 | 9.00 |
| CHEMBL209970 | — | — | 1 | 8.82 |
| CHEMBL99995 | — | — | 1 | 8.70 |
| CHEMBL144320 | — | — | 1 | 8.70 |
| CHEMBL61193 | — | — | 1 | 8.64 |
| CHEMBL474339 | — | — | 1 | 8.52 |
| CHEMBL203160 | — | — | 1 | 8.43 |
| CHEMBL279785 | MARIMASTAT | 3.0 | 1 | 8.42 |
| CHEMBL374219 | — | — | 1 | 8.40 |
| CHEMBL357675 | — | — | 1 | 8.40 |
| CHEMBL36309 | — | — | 1 | 8.22 |
| CHEMBL134908 | — | — | 1 | 8.21 |
| CHEMBL491084 | — | — | 1 | 8.10 |
| CHEMBL207729 | — | — | 1 | 8.08 |
| CHEMBL183924 | — | — | 1 | 7.92 |
| CHEMBL288671 | — | — | 1 | 7.77 |
| CHEMBL75094 | PRINOMASTAT | 3.0 | 1 | 7.66 |
| CHEMBL474140 | — | — | 1 | 7.60 |
| CHEMBL455409 | — | — | 1 | 7.55 |
| CHEMBL18614 | — | — | 1 | 7.50 |
| CHEMBL291361 | — | — | 1 | 7.12 |
| CHEMBL290952 | — | — | 1 | 6.92 |
| CHEMBL34418 | — | — | 1 | 6.83 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL391851 | — | IC50 | = | 0.026 | nM | 10.59 |
| CHEMBL271235 | — | IC50 | = | 0.14 | nM | 9.85 |
| CHEMBL489100 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL184885 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL524092 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL148169 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL193316 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL148169 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL491287 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL209970 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL99995 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL144320 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL61193 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL474339 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL203160 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL279785 | MARIMASTAT | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL357675 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL374219 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL36309 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL134908 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL491084 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL207729 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL183924 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL288671 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL75094 | PRINOMASTAT | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL474140 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL455409 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL18614 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL291361 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL290952 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL34418 | — | IC50 | = | 147.0 | nM | 6.83 |
| CHEMBL144049 | — | IC50 | = | 185.0 | nM | 6.73 |
| CHEMBL206815 | APRATASTAT | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL148118 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL515390 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL253088 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL491286 | — | IC50 | = | 110000.0 | nM | - |
| CHEMBL100570 | — | IC50 | > | 1000.0 | nM | - |