Assay Detail
Binding
CHEMBL4010769
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human TACE catalytic domain using Mca-Pro-Leu-Ala-Gln-Ala-Val-Dpa-Arg-Ser-Ser-Ser-Arg-NH2 as substrate after 2 hrs by fluorescence assay
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Disintegrin and metalloproteinase domain-containing protein 17 (CHEMBL3706) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Identification of novel TACE inhibitors compatible with topical application.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 40 | 7.12 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL206815 | APRATASTAT | 2.0 | 1 | 8.40 |
| CHEMBL4065066 | — | — | 1 | 8.22 |
| CHEMBL4102106 | — | — | 1 | 7.92 |
| CHEMBL4069235 | — | — | 1 | 7.89 |
| CHEMBL4096228 | — | — | 1 | 7.85 |
| CHEMBL4084122 | — | — | 1 | 7.80 |
| CHEMBL4082436 | — | — | 1 | 7.80 |
| CHEMBL4093668 | — | — | 1 | 7.72 |
| CHEMBL4095286 | — | — | 1 | 7.64 |
| CHEMBL4072967 | — | — | 1 | 7.64 |
| CHEMBL4067870 | — | — | 1 | 7.58 |
| CHEMBL4064128 | — | — | 1 | 7.54 |
| CHEMBL4090282 | — | — | 1 | 7.52 |
| CHEMBL4067012 | — | — | 1 | 7.46 |
| CHEMBL4060551 | — | — | 1 | 7.46 |
| CHEMBL4091879 | — | — | 1 | 7.40 |
| CHEMBL4097996 | — | — | 1 | 7.40 |
| CHEMBL4071946 | — | — | 1 | 7.38 |
| CHEMBL4066243 | — | — | 1 | 7.22 |
| CHEMBL4067244 | — | — | 1 | 7.15 |
| CHEMBL4093818 | — | — | 1 | 7.08 |
| CHEMBL4099613 | — | — | 1 | 6.96 |
| CHEMBL4061327 | — | — | 1 | 6.82 |
| CHEMBL4072717 | — | — | 1 | 6.80 |
| CHEMBL4088506 | — | — | 1 | 6.75 |
| CHEMBL4072096 | — | — | 1 | 6.70 |
| CHEMBL4076780 | — | — | 1 | 6.68 |
| CHEMBL4078894 | — | — | 1 | 6.46 |
| CHEMBL4092851 | — | — | 1 | 6.12 |
| CHEMBL4078174 | — | — | 1 | 5.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL206815 | APRATASTAT | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4065066 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4102106 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4069235 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4096228 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4084122 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4082436 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4093668 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4095286 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4072967 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4067870 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4064128 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4090282 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4067012 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4060551 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4091879 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4097996 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4071946 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4066243 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4067244 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL4093818 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL4099613 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4061327 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4072717 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4088506 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4072096 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4076780 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4078894 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL4092851 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL4078174 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4068030 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL4103989 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL4089221 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4096921 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4086065 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4070755 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4097872 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4081349 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4105604 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4099110 | — | IC50 | > | 10000.0 | nM | - |