Assay Detail
Binding
CHEMBL5047307
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human GDP-bound KRAS G12D mutant assessed as inhibition of SOS1-catalyzed nucleotide exchange by measuring KRAS G12D mutant/GTP/c-Raf1 complex formation incubated for 120 mins followed by incubation with SOS1 and GTP for 60 mins followed by addition of c-Raf1 for 60 mins and measured after 60 mins by AlphaLISA assay
1
Total Activities
1
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
Identification of MRTX1133, a Noncovalent, Potent, and Selective KRAS<sup>G12D</sup> Inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 1 | 8.30 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5081048 | — | — | 1 | 8.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5081048 | — | IC50 | = | 5.0 | nM | 8.30 |