Assay Detail
Binding
CHEMBL3136682
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Inhibition of MBTD1 (130 to 566) (unknown origin) expressed in Escherichia coli BL21 Rosetta DE3 using H4K20Me1 as substrate incubated for 30 mins at room temperature followed by incubation under dark condition for 30 mins by AlphaScreen assay
25
Total Activities
25
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 |
Publication
The structure-activity relationships of L3MBTL3 inhibitors: flexibility of the dimer interface.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 4.18 | 4.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2426474 | — | — | 1 | 4.30 |
| CHEMBL3134131 | — | — | 1 | 4.28 |
| CHEMBL3134141 | — | — | 1 | 4.24 |
| CHEMBL2426364 | — | — | 1 | 4.11 |
| CHEMBL3134136 | — | — | 1 | 4.11 |
| CHEMBL3134137 | — | — | 1 | 4.03 |
| CHEMBL3134129 | — | — | 1 | - |
| CHEMBL3134128 | — | — | 1 | - |
| CHEMBL3134127 | — | — | 1 | - |
| CHEMBL3134126 | — | — | 1 | - |
| CHEMBL3134125 | — | — | 1 | - |
| CHEMBL3134146 | — | — | 1 | - |
| CHEMBL3134145 | — | — | 1 | - |
| CHEMBL3134144 | — | — | 1 | - |
| CHEMBL3134143 | — | — | 1 | - |
| CHEMBL3134142 | — | — | 1 | - |
| CHEMBL3134130 | — | — | 1 | - |
| CHEMBL3134139 | — | — | 1 | - |
| CHEMBL3134138 | — | — | 1 | - |
| CHEMBL3134135 | — | — | 1 | - |
| CHEMBL3134134 | — | — | 1 | - |
| CHEMBL3134133 | — | — | 1 | - |
| CHEMBL3134132 | — | — | 1 | - |
| CHEMBL1235119 | — | — | 1 | - |
| CHEMBL3134140 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2426474 | — | IC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL3134131 | — | IC50 | = | 53000.0 | nM | 4.28 |
| CHEMBL3134141 | — | IC50 | = | 58000.0 | nM | 4.24 |
| CHEMBL2426364 | — | IC50 | = | 78000.0 | nM | 4.11 |
| CHEMBL3134136 | — | IC50 | = | 78000.0 | nM | 4.11 |
| CHEMBL3134137 | — | IC50 | = | 94000.0 | nM | 4.03 |
| CHEMBL3134129 | — | IC50 | = | 247000.0 | nM | - |
| CHEMBL3134128 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL3134127 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL3134126 | — | IC50 | = | 290000.0 | nM | - |
| CHEMBL3134125 | — | IC50 | = | 249000.0 | nM | - |
| CHEMBL3134146 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL3134145 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL3134144 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL3134143 | — | IC50 | = | 166000.0 | nM | - |
| CHEMBL3134142 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL3134130 | — | IC50 | = | 176000.0 | nM | - |
| CHEMBL3134139 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL3134138 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL3134135 | — | IC50 | = | 261000.0 | nM | - |
| CHEMBL3134134 | — | IC50 | = | 135000.0 | nM | - |
| CHEMBL3134133 | — | IC50 | = | 157000.0 | nM | - |
| CHEMBL3134132 | — | IC50 | = | 170000.0 | nM | - |
| CHEMBL1235119 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL3134140 | — | IC50 | = | 149000.0 | nM | - |