Assay Detail
Binding
CHEMBL4612347
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Inhibition of KRAS G12C mutant in human NCI-H358 cells assessed as reduction in ERK phosphorylation incubated for 3 hrs by in-cell western method
26
Total Activities
25
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | NCI-H358 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Identification of the Clinical Development Candidate MRTX849, a Covalent KRASG12C Inhibitor for the Treatment of Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 6.96 | 9.00 |
| fIC50 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4648852 | — | — | 1 | 9.00 |
| CHEMBL4632935 | — | — | 1 | 9.00 |
| CHEMBL4640636 | — | — | 1 | 8.52 |
| CHEMBL4636611 | — | — | 1 | 8.40 |
| CHEMBL4646899 | — | — | 1 | 8.22 |
| CHEMBL4645376 | — | — | 1 | 8.05 |
| CHEMBL4648671 | — | — | 2 | 8.00 |
| CHEMBL4594350 | ADAGRASIB | 4.0 | 1 | 7.85 |
| CHEMBL4648056 | — | — | 1 | 7.85 |
| CHEMBL4648124 | — | — | 1 | 7.66 |
| CHEMBL4640234 | — | — | 1 | 7.19 |
| CHEMBL4456598 | — | — | 1 | 6.85 |
| CHEMBL4645768 | — | — | 1 | 6.59 |
| CHEMBL4642659 | — | — | 1 | 6.46 |
| CHEMBL4649703 | — | — | 1 | 5.99 |
| CHEMBL4637314 | — | — | 1 | 5.97 |
| CHEMBL4642347 | — | — | 1 | 5.93 |
| CHEMBL4637434 | — | — | 1 | 5.82 |
| CHEMBL4639210 | — | — | 1 | 5.48 |
| CHEMBL4647242 | — | — | 1 | 5.36 |
| CHEMBL4649174 | — | — | 1 | 5.34 |
| CHEMBL4643600 | — | — | 1 | 5.33 |
| CHEMBL4638484 | — | — | 1 | 5.32 |
| CHEMBL4649393 | — | — | 1 | - |
| CHEMBL4635454 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4632935 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4648852 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4640636 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4636611 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4646899 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4645376 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4648671 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4594350 | ADAGRASIB | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4648056 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4648124 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4640234 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL4456598 | — | IC50 | = | 142.0 | nM | 6.85 |
| CHEMBL4645768 | — | IC50 | = | 254.0 | nM | 6.59 |
| CHEMBL4642659 | — | IC50 | = | 351.0 | nM | 6.46 |
| CHEMBL4649703 | — | IC50 | = | 1020.0 | nM | 5.99 |
| CHEMBL4637314 | — | IC50 | = | 1080.0 | nM | 5.97 |
| CHEMBL4642347 | — | IC50 | = | 1180.0 | nM | 5.93 |
| CHEMBL4637434 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4639210 | — | IC50 | = | 3320.0 | nM | 5.48 |
| CHEMBL4647242 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL4649174 | — | IC50 | = | 4530.0 | nM | 5.34 |
| CHEMBL4643600 | — | IC50 | = | 4630.0 | nM | 5.33 |
| CHEMBL4638484 | — | IC50 | = | 4840.0 | nM | 5.32 |
| CHEMBL4649393 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4635454 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4648671 | — | fIC50 | = | 200.0 | nM | - |