Assay Detail
Binding
CHEMBL4704018
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Inhibition of full-length C-terminal his-tagged mouse AMCase expressed in expressed in CHO-K1 cells assessed as reduction in chitinolytic activity using 4-methylumbelliferyl-beta-D-N,N'-diacetylchitobioside hydrate as substrate after 60 mins by fluorometric assay
19
Total Activities
18
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of OATD-01, a First-in-Class Chitinase Inhibitor as Potential New Therapeutics for Idiopathic Pulmonary Fibrosis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.21 | 9.00 |
| Ki | 1 | 8.24 | 8.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4756869 | — | — | 1 | 9.00 |
| CHEMBL4776610 | — | — | 1 | 8.89 |
| CHEMBL4794014 | — | — | 1 | 8.68 |
| CHEMBL4764430 | — | — | 1 | 8.26 |
| CHEMBL4788866 | 5-(4-((2S,5S)-5-(4-CHLOROBENZYL)-2-METHYLMORPHOLINO)PIPERIDIN-1-YL)-1H-1,2,4-TRIAZOL-3-AMINE | 2.0 | 2 | 8.24 |
| CHEMBL4789376 | — | — | 1 | 8.17 |
| CHEMBL4749391 | — | — | 1 | 8.11 |
| CHEMBL4755139 | — | — | 1 | 8.11 |
| CHEMBL4076989 | — | — | 1 | 7.73 |
| CHEMBL4461925 | — | — | 1 | 7.52 |
| CHEMBL4640857 | — | — | 1 | 7.23 |
| CHEMBL4580568 | — | — | 1 | 7.09 |
| CHEMBL4758240 | — | — | 1 | 6.18 |
| CHEMBL4742167 | — | — | 1 | 6.00 |
| CHEMBL4791640 | — | — | 1 | 5.52 |
| CHEMBL4206372 | — | — | 1 | 5.38 |
| CHEMBL4209364 | — | — | 1 | 5.12 |
| CHEMBL4758850 | — | — | 1 | 4.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4756869 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4776610 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4794014 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL4764430 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL4788866 | 5-(4-((2S,5S)-5-(4-CHLOROBENZYL)-2-METHYLMORPHOLINO)PIPERIDIN-1-YL)-1H-1,2,4-TRIAZOL-3-AMINE | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL4789376 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL4788866 | 5-(4-((2S,5S)-5-(4-CHLOROBENZYL)-2-METHYLMORPHOLINO)PIPERIDIN-1-YL)-1H-1,2,4-TRIAZOL-3-AMINE | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL4749391 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL4755139 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL4076989 | — | IC50 | = | 18.8 | nM | 7.73 |
| CHEMBL4461925 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4640857 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL4580568 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL4758240 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL4742167 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4791640 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL4206372 | — | IC50 | = | 4170.0 | nM | 5.38 |
| CHEMBL4209364 | — | IC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL4758850 | — | IC50 | = | 22000.0 | nM | 4.66 |