Assay Detail
Binding
CHEMBL5156554
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Inhibition of His6-tagged human CBP bromodomain (1081 to 1197 residues) expressed in Escherichia coli BL21 (DE3) incubated for 30 mins by HTRF assay
31
Total Activities
31
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
Design, Synthesis, and Biological Evaluation of 1-(Indolizin-3-yl)ethan-1-ones as CBP Bromodomain Inhibitors for the Treatment of Prostate Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 7.80 | 8.83 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5204688 | — | — | 1 | 8.83 |
| CHEMBL5191045 | — | — | 1 | 8.72 |
| CHEMBL4785363 | INOBRODIB | 1.0 | 1 | 8.69 |
| CHEMBL5179328 | — | — | 1 | 8.68 |
| CHEMBL5179809 | — | — | 1 | 8.53 |
| CHEMBL5179520 | — | — | 1 | 8.38 |
| CHEMBL5205974 | — | — | 1 | 8.01 |
| CHEMBL5198394 | — | — | 1 | 7.92 |
| CHEMBL5195756 | — | — | 1 | 7.89 |
| CHEMBL5191527 | — | — | 1 | 7.86 |
| CHEMBL3814752 | — | — | 1 | 7.86 |
| CHEMBL5192803 | — | — | 1 | 7.67 |
| CHEMBL5195875 | — | — | 1 | 7.66 |
| CHEMBL5198835 | — | — | 1 | 7.61 |
| CHEMBL5192405 | — | — | 1 | 7.58 |
| CHEMBL5208356 | — | — | 1 | 7.58 |
| CHEMBL5200678 | — | — | 1 | 7.38 |
| CHEMBL5207470 | — | — | 1 | 7.26 |
| CHEMBL5204233 | — | — | 1 | 7.25 |
| CHEMBL5179738 | — | — | 1 | 7.16 |
| CHEMBL5181127 | — | — | 1 | 7.11 |
| CHEMBL5192554 | — | — | 1 | 7.10 |
| CHEMBL4171749 | — | — | 1 | 6.75 |
| CHEMBL5202460 | — | — | 1 | - |
| CHEMBL5193196 | — | — | 1 | - |
| CHEMBL5201144 | — | — | 1 | - |
| CHEMBL5185538 | — | — | 1 | - |
| CHEMBL5174255 | — | — | 1 | - |
| CHEMBL5196089 | — | — | 1 | - |
| CHEMBL5189533 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5204688 | — | IC50 | = | 1.48 | nM | 8.83 |
| CHEMBL5191045 | — | IC50 | = | 1.89 | nM | 8.72 |
| CHEMBL4785363 | INOBRODIB | IC50 | = | 2.05 | nM | 8.69 |
| CHEMBL5179328 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL5179809 | — | IC50 | = | 2.96 | nM | 8.53 |
| CHEMBL5179520 | — | IC50 | = | 4.21 | nM | 8.38 |
| CHEMBL5205974 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL5198394 | — | IC50 | = | 12.04 | nM | 7.92 |
| CHEMBL5195756 | — | IC50 | = | 13.01 | nM | 7.89 |
| CHEMBL5191527 | — | IC50 | = | 13.95 | nM | 7.86 |
| CHEMBL3814752 | — | IC50 | = | 13.95 | nM | 7.86 |
| CHEMBL5192803 | — | IC50 | = | 21.32 | nM | 7.67 |
| CHEMBL5195875 | — | IC50 | = | 21.77 | nM | 7.66 |
| CHEMBL5198835 | — | IC50 | = | 24.84 | nM | 7.61 |
| CHEMBL5192405 | — | IC50 | = | 26.37 | nM | 7.58 |
| CHEMBL5208356 | — | IC50 | = | 26.22 | nM | 7.58 |
| CHEMBL5200678 | — | IC50 | = | 41.95 | nM | 7.38 |
| CHEMBL5207470 | — | IC50 | = | 55.23 | nM | 7.26 |
| CHEMBL5204233 | — | IC50 | = | 55.63 | nM | 7.25 |
| CHEMBL5179738 | — | IC50 | = | 69.65 | nM | 7.16 |
| CHEMBL5181127 | — | IC50 | = | 78.46 | nM | 7.11 |
| CHEMBL5192554 | — | IC50 | = | 79.01 | nM | 7.10 |
| CHEMBL4171749 | — | IC50 | = | 178.15 | nM | 6.75 |
| CHEMBL5202460 | — | IC50 | - | — | - | |
| CHEMBL5193196 | — | IC50 | - | — | - | |
| CHEMBL5201144 | — | IC50 | - | — | - | |
| CHEMBL5185538 | — | IC50 | - | — | - | |
| CHEMBL5174255 | — | IC50 | - | — | - | |
| CHEMBL5196089 | — | IC50 | - | — | - | |
| CHEMBL5189533 | — | IC50 | - | — | - | |
| CHEMBL5208083 | — | IC50 | - | — | - |