Assay Detail
Binding
CHEMBL4345255
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant human His-tagged MTH1 expressed in Escherichia coli BL21 (DE3) using 8-oxo-dGTP as substrate incubated for 15 mins followed by substrate addition and measured after 3 hrs by PPiLight Inorganic Pyrophosphate assay kit method
44
Total Activities
44
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 |
Target
Oxidized purine nucleoside triphosphate hydrolase (CHEMBL3708265) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of Potent and Selective MTH1 Inhibitors for Oncology: Enabling Rapid Target (In)Validation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 44 | 7.92 | 10.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4436749 | — | — | 1 | 10.37 |
| CHEMBL4570266 | — | — | 1 | 10.22 |
| CHEMBL4460228 | — | — | 1 | 9.96 |
| CHEMBL4435945 | — | — | 1 | 9.82 |
| CHEMBL4529335 | — | — | 1 | 9.77 |
| CHEMBL4460446 | — | — | 1 | 9.48 |
| CHEMBL4435983 | — | — | 1 | 9.31 |
| CHEMBL4577002 | — | — | 1 | 9.21 |
| CHEMBL4537820 | — | — | 1 | 9.15 |
| CHEMBL4565830 | — | — | 1 | 9.10 |
| CHEMBL4534555 | — | — | 1 | 9.09 |
| CHEMBL4464305 | — | — | 1 | 8.96 |
| CHEMBL4437933 | — | — | 1 | 8.43 |
| CHEMBL3781316 | — | — | 1 | 8.39 |
| CHEMBL4439723 | — | — | 1 | 8.39 |
| CHEMBL4444960 | — | — | 1 | 8.25 |
| CHEMBL4476519 | — | — | 1 | 8.17 |
| CHEMBL4470452 | — | — | 1 | 8.14 |
| CHEMBL4587534 | — | — | 1 | 7.92 |
| CHEMBL4570428 | — | — | 1 | 7.89 |
| CHEMBL4445709 | — | — | 1 | 7.89 |
| CHEMBL4565569 | — | — | 1 | 7.82 |
| CHEMBL4574443 | — | — | 1 | 7.80 |
| CHEMBL4568781 | — | — | 1 | 7.70 |
| CHEMBL4458818 | — | — | 1 | 7.58 |
| CHEMBL3782004 | — | — | 1 | 7.58 |
| CHEMBL4578510 | — | — | 1 | 7.40 |
| CHEMBL4447886 | — | — | 1 | 7.40 |
| CHEMBL4532517 | — | — | 1 | 7.29 |
| CHEMBL4439595 | — | — | 1 | 7.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4436749 | — | IC50 | = | 0.043 | nM | 10.37 |
| CHEMBL4570266 | — | IC50 | = | 0.06 | nM | 10.22 |
| CHEMBL4460228 | — | IC50 | = | 0.11 | nM | 9.96 |
| CHEMBL4435945 | — | IC50 | = | 0.15 | nM | 9.82 |
| CHEMBL4529335 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL4460446 | — | IC50 | = | 0.33 | nM | 9.48 |
| CHEMBL4435983 | — | IC50 | = | 0.49 | nM | 9.31 |
| CHEMBL4577002 | — | IC50 | = | 0.61 | nM | 9.21 |
| CHEMBL4537820 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4565830 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4534555 | — | IC50 | = | 0.82 | nM | 9.09 |
| CHEMBL4464305 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4437933 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL3781316 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL4439723 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL4444960 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL4476519 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL4470452 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL4587534 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4570428 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4445709 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4565569 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4574443 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4568781 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4458818 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3782004 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4578510 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4447886 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4532517 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL4439595 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL4463391 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL4540488 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL4475123 | — | IC50 | = | 207.0 | nM | 6.68 |
| CHEMBL1825141 | — | IC50 | = | 366.0 | nM | 6.44 |
| CHEMBL3793901 | — | IC50 | = | 421.0 | nM | 6.38 |
| CHEMBL4442962 | — | IC50 | = | 467.0 | nM | 6.33 |
| CHEMBL4575540 | — | IC50 | = | 773.0 | nM | 6.11 |
| CHEMBL4452041 | — | IC50 | = | 936.0 | nM | 6.03 |
| CHEMBL4531128 | — | IC50 | = | 946.0 | nM | 6.02 |
| CHEMBL4593996 | — | IC50 | = | 952.0 | nM | 6.02 |
| CHEMBL4517777 | — | IC50 | = | 9077.0 | nM | 5.04 |
| CHEMBL4468099 | — | IC50 | < | 0.05 | nM | - |
| CHEMBL4455353 | — | IC50 | < | 0.05 | nM | - |
| CHEMBL4451394 | — | IC50 | < | 0.05 | nM | - |