Assay Detail
Binding
CHEMBL5650360
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Inhibition of p300 HAT domain (unknown origin) using Biotin-C6-GRGKGGKGLGKGGAK as substrate pretreated with enzyme for 30 mins followed by incubation with substrate for 1 hr by radiometric scintillation proximity assay
9
Total Activities
9
Compounds Tested
1
Activity Types
4
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 5.99 | 7.51 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| EFO_ID | EFO_ID | - | — | MONDO:0004992 |
| EFO_ID | EFO_ID | - | — | MONDO:0021259 |
| EFO_TERM | EFO_TERM | - | — | cancer |
| EFO_TERM | EFO_TERM | - | — | prostate neoplasm |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4788713 | — | — | 1 | 7.51 |
| CHEMBL505121 | — | — | 1 | 7.30 |
| CHEMBL4282264 | A-485 | — | 1 | 7.22 |
| CHEMBL1797936 | — | — | 1 | 5.80 |
| CHEMBL445599 | — | — | 1 | 5.30 |
| CHEMBL4159813 | — | — | 1 | 5.29 |
| CHEMBL5653591 | — | — | 1 | 4.94 |
| CHEMBL140 | CURCUMIN | 3.0 | 1 | 4.52 |
| CHEMBL4536197 | A-486 | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4788713 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL505121 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4282264 | A-485 | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL1797936 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL445599 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL4159813 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL5653591 | — | IC50 | = | 11500.0 | nM | 4.94 |
| CHEMBL140 | CURCUMIN | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL4536197 | A-486 | IC50 | > | 50000.0 | nM | - |