Assay Detail
Binding
CHEMBL4729679
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Inhibition of recombinant human SARM1 TIR domain (561 to 724 residues) expressed in Escherichia coli C43 (DE3) cells lysates using ENAD as substrate preincubated for 20 mins followed by ENAD addition and measured at 15 sec interval for 15 mins
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Subcellular | Lysates |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Identification of the first noncompetitive SARM1 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 4.05 | 4.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL869 | NITROFURAZONE | 4.0 | 1 | 4.05 |
| CHEMBL12089 | BERBERINE CHLORIDE | 1.0 | 1 | - |
| CHEMBL1256723 | DOXYCYCLINE HYDROCHLORIDE | 3.0 | 1 | - |
| CHEMBL1201022 | PHENAZOPYRIDINE HYDROCHLORIDE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL869 | NITROFURAZONE | IC50 | = | 90000.0 | nM | 4.05 |
| CHEMBL12089 | BERBERINE CHLORIDE | IC50 | = | 140000.0 | nM | - |
| CHEMBL1256723 | DOXYCYCLINE HYDROCHLORIDE | IC50 | = | 145000.0 | nM | - |
| CHEMBL1201022 | PHENAZOPYRIDINE HYDROCHLORIDE | IC50 | = | 145000.0 | nM | - |