Assay Detail
Binding
CHEMBL4704015
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Inhibition of recombinant full-length C-terminal his-tagged mouse CHIT1 expressed in CHO-K1 cells assessed as reduction in chitinolytic activity using 4-methylumbelliferyl-beta-D-N,N',N"-triacetylchitotrioside 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 | 6.76 | 7.85 |
| Ki | 1 | 7.58 | 7.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4776610 | — | — | 1 | 7.85 |
| CHEMBL4756869 | — | — | 1 | 7.82 |
| CHEMBL4794014 | — | — | 1 | 7.72 |
| CHEMBL4789376 | — | — | 1 | 7.60 |
| CHEMBL4788866 | 5-(4-((2S,5S)-5-(4-CHLOROBENZYL)-2-METHYLMORPHOLINO)PIPERIDIN-1-YL)-1H-1,2,4-TRIAZOL-3-AMINE | 2.0 | 2 | 7.58 |
| CHEMBL4206372 | — | — | 1 | 7.54 |
| CHEMBL4764430 | — | — | 1 | 7.54 |
| CHEMBL4755139 | — | — | 1 | 7.52 |
| CHEMBL4749391 | — | — | 1 | 7.31 |
| CHEMBL4461925 | — | — | 1 | 7.13 |
| CHEMBL4580568 | — | — | 1 | 7.06 |
| CHEMBL4640857 | — | — | 1 | 6.86 |
| CHEMBL4209364 | — | — | 1 | 5.80 |
| CHEMBL4791640 | — | — | 1 | 5.77 |
| CHEMBL4076989 | — | — | 1 | 5.53 |
| CHEMBL4758240 | — | — | 1 | 5.28 |
| CHEMBL4742167 | — | — | 1 | 5.14 |
| CHEMBL4758850 | — | — | 1 | 4.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4776610 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4756869 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4794014 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4789376 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4788866 | 5-(4-((2S,5S)-5-(4-CHLOROBENZYL)-2-METHYLMORPHOLINO)PIPERIDIN-1-YL)-1H-1,2,4-TRIAZOL-3-AMINE | Ki | = | 26.05 | nM | 7.58 |
| CHEMBL4788866 | 5-(4-((2S,5S)-5-(4-CHLOROBENZYL)-2-METHYLMORPHOLINO)PIPERIDIN-1-YL)-1H-1,2,4-TRIAZOL-3-AMINE | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4206372 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4764430 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4755139 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4749391 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL4461925 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL4580568 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL4640857 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL4209364 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4791640 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4076989 | — | IC50 | = | 2955.0 | nM | 5.53 |
| CHEMBL4758240 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL4742167 | — | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL4758850 | — | IC50 | = | 27000.0 | nM | 4.57 |