Assay Detail
Binding
CHEMBL5617823
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Inhibition of full length his-tagged human recombinant cGAS extracted from Escherichia coli BL21 (DE3) incubated for 3 hrs by rapidfire 365 mass spectrometry analysis
6
Total Activities
6
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
Novel Azepino[4,5-<i>b</i>]indolone as cGAS Inhibitors for Treating Immune-Mediated Diseases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 8.24 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5620249 | — | — | 1 | 8.70 |
| CHEMBL5619434 | — | — | 1 | 8.30 |
| CHEMBL5619280 | — | — | 1 | 8.15 |
| CHEMBL5620136 | — | — | 1 | 8.10 |
| CHEMBL5618800 | — | — | 1 | 8.10 |
| CHEMBL5618706 | — | — | 1 | 8.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5620249 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5619434 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5619280 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5620136 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL5618800 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL5618706 | — | IC50 | = | 8.0 | nM | 8.10 |