Assay Detail
Binding
CHEMBL5511282
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Binding affinity to human C-terminal his tagged NSD2 PWWP1 domain (208 to 358 residues) expressed in Escherichia coli Bl21 (DE3) gold cells assessed as dissociation constant measured upto 180 secs by SPR analysis
14
Total Activities
14
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
Histone-lysine N-methyltransferase NSD2 (CHEMBL3108645) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Identification of Novel Potent NSD2-PWWP1 Ligands Using Structure-Based Design and Computational Approaches.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 14 | 6.77 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5559507 | — | — | 1 | 8.60 |
| CHEMBL5562340 | — | — | 1 | 7.90 |
| CHEMBL5562153 | — | — | 1 | 7.40 |
| CHEMBL5517868 | — | — | 1 | 7.40 |
| CHEMBL5200945 | — | — | 1 | 6.90 |
| CHEMBL5557539 | — | — | 1 | 6.90 |
| CHEMBL6067693 | — | — | 1 | 6.90 |
| CHEMBL5557662 | — | — | 1 | 6.80 |
| CHEMBL5555145 | — | — | 1 | 6.70 |
| CHEMBL5562861 | — | — | 1 | 6.60 |
| CHEMBL5562663 | — | — | 1 | 6.60 |
| CHEMBL5561556 | — | — | 1 | 5.60 |
| CHEMBL5565515 | — | — | 1 | 5.30 |
| CHEMBL5563959 | — | — | 1 | 5.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5559507 | — | Kd | = | 2.512 | nM | 8.60 |
| CHEMBL5562340 | — | Kd | = | 12.59 | nM | 7.90 |
| CHEMBL5562153 | — | Kd | = | 39.81 | nM | 7.40 |
| CHEMBL5517868 | — | Kd | = | 39.81 | nM | 7.40 |
| CHEMBL5200945 | — | Kd | = | 125.89 | nM | 6.90 |
| CHEMBL5557539 | — | Kd | = | 125.89 | nM | 6.90 |
| CHEMBL6067693 | — | Kd | = | 125.89 | nM | 6.90 |
| CHEMBL5557662 | — | Kd | = | 158.49 | nM | 6.80 |
| CHEMBL5555145 | — | Kd | = | 199.53 | nM | 6.70 |
| CHEMBL5562861 | — | Kd | = | 251.19 | nM | 6.60 |
| CHEMBL5562663 | — | Kd | = | 251.19 | nM | 6.60 |
| CHEMBL5561556 | — | Kd | = | 2511.89 | nM | 5.60 |
| CHEMBL5565515 | — | Kd | = | 5011.87 | nM | 5.30 |
| CHEMBL5563959 | — | Kd | = | 6309.57 | nM | 5.20 |