Assay Detail
Binding
CHEMBL908767
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Inhibition of [3H]methyl dThd phosphorylation by TK2
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
N1-substituted thymine derivatives as mitochondrial thymidine kinase (TK-2) inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 5.43 | 6.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL219299 | — | — | 1 | 6.41 |
| CHEMBL220459 | — | — | 1 | 6.33 |
| CHEMBL216998 | — | — | 1 | 6.30 |
| CHEMBL101135 | — | — | 1 | 5.82 |
| CHEMBL373998 | — | — | 1 | 5.75 |
| CHEMBL385954 | — | — | 1 | 5.72 |
| CHEMBL219960 | — | — | 1 | 5.72 |
| CHEMBL373997 | — | — | 1 | 5.62 |
| CHEMBL216997 | — | — | 1 | 5.60 |
| CHEMBL219367 | — | — | 1 | 5.33 |
| CHEMBL219458 | — | — | 1 | 5.28 |
| CHEMBL219905 | — | — | 1 | 5.01 |
| CHEMBL438603 | — | — | 1 | 4.64 |
| CHEMBL219510 | — | — | 1 | 4.64 |
| CHEMBL374244 | — | — | 1 | 4.35 |
| CHEMBL384435 | — | — | 1 | 4.35 |
| CHEMBL219908 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL219299 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL220459 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL216998 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL101135 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL373998 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL385954 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL219960 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL373997 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL216997 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL219367 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL219458 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL219905 | — | IC50 | = | 9700.0 | nM | 5.01 |
| CHEMBL438603 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL219510 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL374244 | — | IC50 | = | 45000.0 | nM | 4.35 |
| CHEMBL384435 | — | IC50 | = | 45000.0 | nM | 4.35 |
| CHEMBL219908 | — | IC50 | = | 114000.0 | nM | - |