Assay Detail
Binding
CHEMBL5374157
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Inhibition of wild-type GDP-bound biotinylated-KRAS (unknown origin) assessed as suppression of SOS1-mediated nucleotide exchange by measuring reduction in KRAS-RAF RBD complex formation preincubated for 60 mins followed by SOS1 addition and further incubated for 60 mins and subsequent addition of KRAS-RAF RBD mixture measured after 30 to 60 mins by FRET assay
13
Total Activities
13
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
Structure-Based Design and Synthesis of Potent and Selective KRAS G12D Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 7.68 | 8.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5408369 | — | — | 1 | 8.41 |
| CHEMBL5428238 | — | — | 1 | 8.38 |
| CHEMBL5405632 | — | — | 1 | 8.04 |
| CHEMBL5393883 | — | — | 1 | 7.94 |
| CHEMBL5430198 | — | — | 1 | 7.77 |
| CHEMBL5397425 | — | — | 1 | 7.40 |
| CHEMBL5410609 | — | — | 1 | 6.82 |
| CHEMBL5410069 | — | — | 1 | 6.67 |
| CHEMBL5424715 | — | — | 1 | - |
| CHEMBL5418527 | — | — | 1 | - |
| CHEMBL5418176 | — | — | 1 | - |
| CHEMBL5426739 | — | — | 1 | - |
| CHEMBL5431156 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5408369 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL5428238 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL5405632 | — | IC50 | = | 9.2 | nM | 8.04 |
| CHEMBL5393883 | — | IC50 | = | 11.6 | nM | 7.94 |
| CHEMBL5430198 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5397425 | — | IC50 | = | 39.6 | nM | 7.40 |
| CHEMBL5410609 | — | IC50 | = | 153.0 | nM | 6.82 |
| CHEMBL5410069 | — | IC50 | = | 214.0 | nM | 6.67 |
| CHEMBL5424715 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5418527 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5418176 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5426739 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5431156 | — | IC50 | > | 1000.0 | nM | - |