Assay Detail
Binding
CHEMBL5738512
Review assay metadata, readout intent, target linkage, and publication context from the same page.
KRas G12D Binding Assay: Table 2: The ability of a compound to bind to KRAS G12D was measured using a TR-FRET displacement assay. Biotinylated GDP-loaded recombinant human KRAS G12D (corresponding to amino acids 1:169, produced at Array BioPharma) was incubated with a custom-made Cy5 labelled tracer, europium labelled streptavidin and compound (2% DMSO final) in buffer (50 mM HEPES [pH 7.5], 5mM MgCl2, 0.005% Tween-20 & 1 mM DTT). After a 60 minute incubation at 22° C., the reaction was measured using a PerkinElmer EnVision multimode plate reader via TR-FRET dual wavelength detection, and the percent of control (POC) calculated using a ratiometric emission factor. 100 POC is determined using no test compound and 0 POC is determined using a concentration of control compound that completely inhibits binding of the tracer to KRAS. The POC values were fit to a 4-parameter logistic curve and the IC50 value was determined as the concentration where the curve crosses 50 POC.
2205
Total Activities
449
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
KRas G12D inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 735 | 6.68 | 10.00 |
| kon | 735 | - | - |
| k_off | 735 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5741049 | — | — | 6 | 10.00 |
| CHEMBL4857438 | — | — | 6 | 9.70 |
| CHEMBL4863339 | — | — | 6 | 9.52 |
| CHEMBL4876040 | — | — | 6 | 9.40 |
| CHEMBL4858364 | MRTX-1133 | 1.0 | 6 | 9.40 |
| CHEMBL4859236 | — | — | 6 | 9.40 |
| CHEMBL5905084 | — | — | 6 | 9.40 |
| CHEMBL5776467 | — | — | 6 | 9.40 |
| CHEMBL5996049 | — | — | 6 | 9.40 |
| CHEMBL4857719 | — | — | 6 | 9.30 |
| CHEMBL5856093 | — | — | 12 | 9.30 |
| CHEMBL5948638 | — | — | 6 | 9.30 |
| CHEMBL5187854 | — | — | 6 | 9.30 |
| CHEMBL5829922 | — | — | 6 | 9.30 |
| CHEMBL5840711 | — | — | 6 | 9.22 |
| CHEMBL4867851 | — | — | 6 | 9.22 |
| CHEMBL4876243 | — | — | 6 | 9.22 |
| CHEMBL4874297 | — | — | 6 | 9.22 |
| CHEMBL5863463 | — | — | 12 | 9.15 |
| CHEMBL5953832 | — | — | 12 | 9.15 |
| CHEMBL5932673 | — | — | 6 | 9.15 |
| CHEMBL5883487 | — | — | 6 | 9.15 |
| CHEMBL5889261 | — | — | 6 | 9.15 |
| CHEMBL5979136 | — | — | 6 | 9.15 |
| CHEMBL6028889 | — | — | 6 | 9.15 |
| CHEMBL4863371 | — | — | 6 | 9.10 |
| CHEMBL6048506 | — | — | 6 | 9.10 |
| CHEMBL5977600 | — | — | 6 | 9.10 |
| CHEMBL5881670 | — | — | 6 | 9.05 |
| CHEMBL5862570 | — | — | 6 | 9.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5741049 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL4857438 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4863339 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4858364 | MRTX-1133 | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL5996049 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4876040 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL5905084 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL5776467 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4859236 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4857719 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL5187854 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL5829922 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL5856093 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL5948638 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4876243 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4867851 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4874297 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL5840711 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL5979136 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5863463 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5889261 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL6028889 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5883487 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5856093 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5932673 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5953832 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5977600 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4863371 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4876040 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4858364 | MRTX-1133 | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL6048506 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL5985758 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL5862570 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL5828205 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL5877093 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL5881670 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL5912568 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5762802 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5953832 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5897986 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5815995 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4874297 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5863463 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL5897850 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5798610 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5923638 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL5860569 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL5873176 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL5982761 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5798369 | — | IC50 | = | 1.6 | nM | 8.80 |