Assay Detail
Binding
CHEMBL5611673
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal 6His-SUMO tagged human cGAS (1 to 522 residues) extracted from Escherichia coli BL21(DE3)pLysS cells using GTP/ATP as substrate by measuring cGAMP production incubated for 90 mins in presence of 45 base pair DNA by mass spectrometric analysis
10
Total Activities
10
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
Inhibitors of the Cyclic GMP-AMP Synthase (cGAS) as Potential Treatment for Autoimmune and Inflammatory Diseases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 8.03 | 8.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5612485 | — | — | 1 | 8.68 |
| CHEMBL5614320 | — | — | 1 | 8.57 |
| CHEMBL5614182 | — | — | 1 | 8.55 |
| CHEMBL5613252 | — | — | 1 | 8.46 |
| CHEMBL5612416 | — | — | 1 | 8.35 |
| CHEMBL5613515 | — | — | 1 | 8.14 |
| CHEMBL5613451 | — | — | 1 | 7.85 |
| CHEMBL5613424 | — | — | 1 | 7.47 |
| CHEMBL5612358 | — | — | 1 | 7.27 |
| CHEMBL5612787 | — | — | 1 | 7.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5612485 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL5614320 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL5614182 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL5613252 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL5612416 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL5613515 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL5613451 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5613424 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL5612358 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL5612787 | — | IC50 | = | 100.0 | nM | 7.00 |