Assay Detail
Binding
CHEMBL5047301
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Binding affinity to human AviTEV6His-tagged KRAS isoform 4B G12D mutant (1 to 169 residues) expressed in Escherichia coli BL21 (DE3) assessed as dissociation constant by SPR analysis
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| 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 |
|---|---|---|---|
| Kd | 12 | 6.70 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5080840 | — | — | 1 | 9.10 |
| CHEMBL5091481 | — | — | 1 | 8.05 |
| CHEMBL5075989 | — | — | 1 | 7.14 |
| CHEMBL5093896 | — | — | 1 | 7.02 |
| CHEMBL5090910 | — | — | 1 | 6.72 |
| CHEMBL5081048 | — | — | 1 | 6.70 |
| CHEMBL5080165 | — | — | 1 | 6.55 |
| CHEMBL5076492 | — | — | 1 | 6.42 |
| CHEMBL5091167 | — | — | 1 | 6.38 |
| CHEMBL5072416 | — | — | 1 | 5.82 |
| CHEMBL5084171 | — | — | 1 | 5.46 |
| CHEMBL5085395 | — | — | 1 | 5.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5080840 | — | Kd | = | 0.8 | nM | 9.10 |
| CHEMBL5091481 | — | Kd | = | 9.0 | nM | 8.05 |
| CHEMBL5075989 | — | Kd | = | 73.0 | nM | 7.14 |
| CHEMBL5093896 | — | Kd | = | 96.0 | nM | 7.02 |
| CHEMBL5090910 | — | Kd | = | 190.0 | nM | 6.72 |
| CHEMBL5081048 | — | Kd | = | 200.0 | nM | 6.70 |
| CHEMBL5080165 | — | Kd | = | 280.0 | nM | 6.55 |
| CHEMBL5076492 | — | Kd | = | 380.0 | nM | 6.42 |
| CHEMBL5091167 | — | Kd | = | 420.0 | nM | 6.38 |
| CHEMBL5072416 | — | Kd | = | 1500.0 | nM | 5.82 |
| CHEMBL5084171 | — | Kd | = | 3500.0 | nM | 5.46 |
| CHEMBL5085395 | — | Kd | = | 8700.0 | nM | 5.06 |