Assay Detail
Binding
CHEMBL897360
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of TACE in human whole blood
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Blood |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Disintegrin and metalloproteinase domain-containing protein 17 (CHEMBL3706) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
A new 4-(2-methylquinolin-4-ylmethyl)phenyl P1' group for the beta-amino hydroxamic acid derived TACE inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 6.75 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL233844 | — | — | 1 | 7.30 |
| CHEMBL391873 | — | — | 1 | 7.17 |
| CHEMBL234604 | — | — | 1 | 7.14 |
| CHEMBL235997 | — | — | 1 | 7.12 |
| CHEMBL392894 | — | — | 1 | 7.11 |
| CHEMBL234225 | — | — | 1 | 7.11 |
| CHEMBL234417 | — | — | 1 | 7.07 |
| CHEMBL233629 | — | — | 1 | 7.07 |
| CHEMBL234605 | — | — | 1 | 7.06 |
| CHEMBL399604 | — | — | 1 | 7.02 |
| CHEMBL429444 | — | — | 1 | 7.02 |
| CHEMBL401453 | — | — | 1 | 7.02 |
| CHEMBL392686 | — | — | 1 | 7.01 |
| CHEMBL233842 | — | — | 1 | 6.96 |
| CHEMBL233843 | — | — | 1 | 6.92 |
| CHEMBL234034 | — | — | 1 | 6.89 |
| CHEMBL234033 | — | — | 1 | 6.89 |
| CHEMBL392312 | — | — | 1 | 6.66 |
| CHEMBL234416 | — | — | 1 | 6.64 |
| CHEMBL234224 | — | — | 1 | 6.58 |
| CHEMBL401455 | — | — | 1 | 6.38 |
| CHEMBL234415 | — | — | 1 | 6.34 |
| CHEMBL401454 | — | — | 1 | 6.25 |
| CHEMBL234199 | — | — | 1 | 6.16 |
| CHEMBL234226 | — | — | 1 | 6.14 |
| CHEMBL398371 | — | — | 1 | 6.12 |
| CHEMBL236204 | — | — | 1 | 6.04 |
| CHEMBL234603 | — | — | 1 | 5.92 |
| CHEMBL234032 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL233844 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL391873 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL234604 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL235997 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL392894 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL234225 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL234417 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL233629 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL234605 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL399604 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL429444 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL401453 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL392686 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL233842 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL233843 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL234034 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL234033 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL392312 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL234416 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL234224 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL401455 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL234415 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL401454 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL234199 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL234226 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL398371 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL236204 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL234603 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL234032 | — | IC50 | > | 3000.0 | nM | - |