Assay Detail
Binding
CHEMBL3865469
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Binding affinity to human His6-tagged SETD8 (192 to 352 residues) C302S mutant in PBS buffer in presence of SAM by ITC assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Turning a Substrate Peptide into a Potent Inhibitor for the Histone Methyltransferase SETD8.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 15 | 5.94 | 6.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3979628 | — | — | 1 | 6.92 |
| CHEMBL3934996 | — | — | 1 | 6.85 |
| CHEMBL3909400 | — | — | 1 | 6.68 |
| CHEMBL3894573 | — | — | 1 | 6.50 |
| CHEMBL3961424 | — | — | 1 | 6.46 |
| CHEMBL3918322 | — | — | 1 | 6.24 |
| CHEMBL3960411 | — | — | 1 | 6.10 |
| CHEMBL3986240 | — | — | 1 | 5.74 |
| CHEMBL3957541 | — | — | 1 | 5.52 |
| CHEMBL3891356 | — | — | 1 | 5.33 |
| CHEMBL3933297 | — | — | 1 | 5.25 |
| CHEMBL3905280 | — | — | 1 | 4.83 |
| CHEMBL3933942 | — | — | 1 | 4.82 |
| CHEMBL3954512 | — | — | 1 | - |
| CHEMBL3971503 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3979628 | — | Kd | = | 120.0 | nM | 6.92 |
| CHEMBL3934996 | — | Kd | = | 140.0 | nM | 6.85 |
| CHEMBL3909400 | — | Kd | = | 210.0 | nM | 6.68 |
| CHEMBL3894573 | — | Kd | = | 320.0 | nM | 6.50 |
| CHEMBL3961424 | — | Kd | = | 350.0 | nM | 6.46 |
| CHEMBL3918322 | — | Kd | = | 580.0 | nM | 6.24 |
| CHEMBL3960411 | — | Kd | = | 800.0 | nM | 6.10 |
| CHEMBL3986240 | — | Kd | = | 1840.0 | nM | 5.74 |
| CHEMBL3957541 | — | Kd | = | 3040.0 | nM | 5.52 |
| CHEMBL3891356 | — | Kd | = | 4640.0 | nM | 5.33 |
| CHEMBL3933297 | — | Kd | = | 5570.0 | nM | 5.25 |
| CHEMBL3905280 | — | Kd | = | 14800.0 | nM | 4.83 |
| CHEMBL3933942 | — | Kd | = | 15000.0 | nM | 4.82 |
| CHEMBL3954512 | — | Kd | - | — | - | |
| CHEMBL3971503 | — | Kd | - | — | - |