Assay Detail
Binding
CHEMBL4839364
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of 5-TAMRA-labelled Tracer A from human GST-fused/FLAG-tagged full length ATR/human N-terminal FLAG-tagged full length ATRIP expressed in HEK293-6E cells preincubated for 15 mins followed by tracer A addition and measured after 30 mins by TR-FRET based competition binding assay
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK2936E |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
BAY-8400: A Novel Potent and Selective DNA-PK Inhibitor which Shows Synergistic Efficacy in Combination with Targeted Alpha Therapies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 5.88 | 7.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4870563 | — | — | 1 | 7.05 |
| CHEMBL4860637 | — | — | 1 | 6.93 |
| CHEMBL4860779 | — | — | 1 | 6.85 |
| CHEMBL4869632 | — | — | 1 | 6.71 |
| CHEMBL4875626 | — | — | 1 | 6.57 |
| CHEMBL4868400 | — | — | 1 | 6.50 |
| CHEMBL4851439 | — | — | 1 | 6.41 |
| CHEMBL4852502 | — | — | 1 | 6.39 |
| CHEMBL4849035 | — | — | 1 | 6.26 |
| CHEMBL4871998 | — | — | 1 | 6.10 |
| CHEMBL4850640 | — | — | 1 | 6.04 |
| CHEMBL4855691 | — | — | 1 | 5.93 |
| CHEMBL4862738 | — | — | 1 | 5.91 |
| CHEMBL4860129 | — | — | 1 | 5.88 |
| CHEMBL4877926 | — | — | 1 | 5.78 |
| CHEMBL4857669 | — | — | 1 | 5.75 |
| CHEMBL4873263 | — | — | 1 | 5.67 |
| CHEMBL4863567 | — | — | 1 | 5.54 |
| CHEMBL4867528 | — | — | 1 | 5.31 |
| CHEMBL4878956 | — | — | 1 | 5.24 |
| CHEMBL4864349 | — | — | 1 | 5.17 |
| CHEMBL4865476 | — | — | 1 | 4.89 |
| CHEMBL4873491 | — | — | 1 | 4.77 |
| CHEMBL4851045 | — | — | 1 | 4.76 |
| CHEMBL4850455 | — | — | 1 | 4.71 |
| CHEMBL4847559 | — | — | 1 | - |
| CHEMBL4879247 | — | — | 1 | - |
| CHEMBL4868065 | — | — | 1 | - |
| CHEMBL4865490 | — | — | 1 | - |
| CHEMBL4876439 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4870563 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL4860637 | — | IC50 | = | 117.0 | nM | 6.93 |
| CHEMBL4860779 | — | IC50 | = | 141.0 | nM | 6.85 |
| CHEMBL4869632 | — | IC50 | = | 197.0 | nM | 6.71 |
| CHEMBL4875626 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4868400 | — | IC50 | = | 314.0 | nM | 6.50 |
| CHEMBL4851439 | — | IC50 | = | 394.0 | nM | 6.41 |
| CHEMBL4852502 | — | IC50 | = | 407.0 | nM | 6.39 |
| CHEMBL4849035 | — | IC50 | = | 551.0 | nM | 6.26 |
| CHEMBL4871998 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL4850640 | — | IC50 | = | 907.0 | nM | 6.04 |
| CHEMBL4855691 | — | IC50 | = | 1180.0 | nM | 5.93 |
| CHEMBL4862738 | — | IC50 | = | 1220.0 | nM | 5.91 |
| CHEMBL4860129 | — | IC50 | = | 1320.0 | nM | 5.88 |
| CHEMBL4877926 | — | IC50 | = | 1660.0 | nM | 5.78 |
| CHEMBL4857669 | — | IC50 | = | 1770.0 | nM | 5.75 |
| CHEMBL4873263 | — | IC50 | = | 2160.0 | nM | 5.67 |
| CHEMBL4863567 | — | IC50 | = | 2880.0 | nM | 5.54 |
| CHEMBL4867528 | — | IC50 | = | 4920.0 | nM | 5.31 |
| CHEMBL4878956 | — | IC50 | = | 5750.0 | nM | 5.24 |
| CHEMBL4864349 | — | IC50 | = | 6750.0 | nM | 5.17 |
| CHEMBL4865476 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL4873491 | — | IC50 | = | 16900.0 | nM | 4.77 |
| CHEMBL4851045 | — | IC50 | = | 17200.0 | nM | 4.76 |
| CHEMBL4850455 | — | IC50 | = | 19700.0 | nM | 4.71 |
| CHEMBL4847559 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4879247 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4868065 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4865490 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4876439 | — | IC50 | > | 10000.0 | nM | - |