Assay Detail
Binding
CHEMBL4190835
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Inhibition of human recombinant FLAG-tagged full length ATR expressed in mammalian cell line co-expressing human recombinant cMyc-tagged full length ATRIP
24
Total Activities
21
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
Discovery of pyrazolopyrimidine derivatives as novel inhibitors of ataxia telangiectasia and rad3 related protein (ATR).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 6.05 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3989870 | BERZOSERTIB | 2.0 | 1 | 7.82 |
| CHEMBL4207014 | — | — | 1 | 7.18 |
| CHEMBL4211377 | — | — | 1 | 7.07 |
| CHEMBL4207265 | — | — | 3 | 6.80 |
| CHEMBL4207205 | — | — | 2 | 6.57 |
| CHEMBL4213994 | — | — | 1 | 6.24 |
| CHEMBL4210861 | — | — | 1 | 6.18 |
| CHEMBL4215278 | — | — | 1 | 5.88 |
| CHEMBL1081312 | — | — | 1 | 5.85 |
| CHEMBL4209086 | — | — | 1 | 5.80 |
| CHEMBL4211185 | — | — | 1 | 5.73 |
| CHEMBL4216036 | — | — | 1 | 5.58 |
| CHEMBL3964073 | — | — | 1 | 5.45 |
| CHEMBL4210228 | — | — | 1 | 5.33 |
| CHEMBL4215814 | — | — | 1 | 4.72 |
| CHEMBL4204301 | — | — | 1 | 4.71 |
| CHEMBL4209026 | — | — | 1 | 4.65 |
| CHEMBL4212315 | — | — | 1 | - |
| CHEMBL4203385 | — | — | 1 | - |
| CHEMBL4212747 | — | — | 1 | - |
| CHEMBL4206529 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3989870 | BERZOSERTIB | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4207014 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL4211377 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL4207265 | — | IC50 | = | 158.0 | nM | 6.80 |
| CHEMBL4207265 | — | IC50 | = | 212.0 | nM | 6.67 |
| CHEMBL4207205 | — | IC50 | = | 269.0 | nM | 6.57 |
| CHEMBL4207265 | — | IC50 | = | 304.0 | nM | 6.52 |
| CHEMBL4207205 | — | IC50 | = | 547.0 | nM | 6.26 |
| CHEMBL4213994 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL4210861 | — | IC50 | = | 654.0 | nM | 6.18 |
| CHEMBL4215278 | — | IC50 | = | 1320.0 | nM | 5.88 |
| CHEMBL1081312 | — | IC50 | = | 1420.0 | nM | 5.85 |
| CHEMBL4209086 | — | IC50 | = | 1590.0 | nM | 5.80 |
| CHEMBL4211185 | — | IC50 | = | 1860.0 | nM | 5.73 |
| CHEMBL4216036 | — | IC50 | = | 2630.0 | nM | 5.58 |
| CHEMBL3964073 | — | IC50 | = | 3560.0 | nM | 5.45 |
| CHEMBL4210228 | — | IC50 | = | 4620.0 | nM | 5.33 |
| CHEMBL4215814 | — | IC50 | = | 19100.0 | nM | 4.72 |
| CHEMBL4204301 | — | IC50 | = | 19300.0 | nM | 4.71 |
| CHEMBL4209026 | — | IC50 | = | 22400.0 | nM | 4.65 |
| CHEMBL4212747 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4212315 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4203385 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4206529 | — | IC50 | > | 30000.0 | nM | - |