Assay Detail
Binding
CHEMBL2168708
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant CatK assessed as suppression of enzyme-mediated Z-Phe-Arg-AMC cleavage incubated for 1 hrs by QFRET assay
38
Total Activities
38
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 |
Publication
(1R,2R)-N-(1-cyanocyclopropyl)-2-(6-methoxy-1,3,4,5-tetrahydropyrido[4,3-b]indole-2-carbonyl)cyclohexanecarboxamide (AZD4996): a potent and highly selective cathepsin K inhibitor for the treatment of osteoarthritis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 38 | 8.01 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2164670 | — | — | 1 | 9.00 |
| CHEMBL2163360 | — | — | 1 | 9.00 |
| CHEMBL2164682 | — | — | 1 | 9.00 |
| CHEMBL2163582 | — | — | 1 | 8.70 |
| CHEMBL2164674 | — | — | 1 | 8.70 |
| CHEMBL2163589 | — | — | 1 | 8.70 |
| CHEMBL2163585 | — | — | 1 | 8.70 |
| CHEMBL2164669 | — | — | 1 | 8.52 |
| CHEMBL2164686 | — | — | 1 | 8.52 |
| CHEMBL2164687 | — | — | 1 | 8.52 |
| CHEMBL2163583 | — | — | 1 | 8.52 |
| CHEMBL2163584 | — | — | 1 | 8.40 |
| CHEMBL2163588 | — | — | 1 | 8.40 |
| CHEMBL2164684 | — | — | 1 | 8.40 |
| CHEMBL371064 | BALICATIB | 2.0 | 1 | 8.30 |
| CHEMBL2163586 | — | — | 1 | 8.30 |
| CHEMBL2164676 | — | — | 1 | 8.15 |
| CHEMBL2164685 | — | — | 1 | 8.00 |
| CHEMBL2164679 | — | — | 1 | 7.79 |
| CHEMBL2163591 | — | — | 1 | 7.77 |
| CHEMBL2164680 | — | — | 1 | 7.76 |
| CHEMBL2164673 | — | — | 1 | 7.75 |
| CHEMBL2164668 | — | — | 1 | 7.60 |
| CHEMBL2163349 | — | — | 1 | 7.47 |
| CHEMBL2164675 | — | — | 1 | 7.43 |
| CHEMBL2164688 | — | — | 1 | 7.39 |
| CHEMBL2164689 | — | — | 1 | 7.38 |
| CHEMBL2164690 | — | — | 1 | 7.30 |
| CHEMBL2164672 | — | — | 1 | 7.14 |
| CHEMBL2163581 | — | — | 1 | 7.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2164670 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL2164682 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL2163360 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL2163582 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2164674 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2163589 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2163585 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2164669 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2164686 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2164687 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2163583 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2163584 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2164684 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2163588 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2163586 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL371064 | BALICATIB | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2164676 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL2164685 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2164679 | — | IC50 | = | 16.2 | nM | 7.79 |
| CHEMBL2163591 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL2164680 | — | IC50 | = | 17.3 | nM | 7.76 |
| CHEMBL2164673 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL2164668 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL2163349 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL2164675 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL2164688 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL2164689 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL2164690 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL2164672 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL2163581 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL2164671 | — | IC50 | = | 257.0 | nM | 6.59 |
| CHEMBL2164681 | — | IC50 | = | 785.0 | nM | 6.11 |
| CHEMBL2164683 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL2164678 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL2164677 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL2163587 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL2163590 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL481611 | ODANACATIB | IC50 | < | 1.0 | nM | - |