Assay Detail
Binding
CHEMBL5735342
Review assay metadata, readout intent, target linkage, and publication context from the same page.
TR FRET Binding Assay: His/Flag epitope tagged CBP was cloned, expressed, and purified to homogeneity. CBP binding and inhibition was assessed by monitoring the engagement of a biotinylated small molecule compound with the target using the TR-FRET assay technology (Perkin-Elmer). Specifically, in a 384 well ProxiPlate CBP (4 nM final) was combined with biotin-ligand (60 nM final) in 50 mM HEPES (pH 7.5), 50 mM NaCl, 1 mM TCEP, 0.01% (w/v) BSA, and 0.008% (w/v) Brij-35 either in the presence of DMSO (final 0.2% DMSO) or compound dilution series in DMSO. After 10 minutes incubation at room temperature, a mixture Eu-W1024 Anti-6×His antibody (6×His is disclosed as SEQ ID NO: 3) (Perkin Elmer AD0110) and SureLight Allophycocyanin-Streptavidin (APC-SA, Perkin Elmer CR130-100) were added to a final concentrations of 0.2 nMolar antibody and 50 nMolar APC-SA, respectively.
375
Total Activities
125
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Therapeutic compounds and uses thereof
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 125 | 7.33 | 8.70 |
| kon | 125 | - | - |
| k_off | 125 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6052218 | — | — | 3 | 8.70 |
| CHEMBL5763461 | — | — | 3 | 8.70 |
| CHEMBL4061254 | — | — | 3 | 8.70 |
| CHEMBL4095153 | — | — | 3 | 8.40 |
| CHEMBL5778256 | — | — | 3 | 8.40 |
| CHEMBL5913995 | — | — | 3 | 8.40 |
| CHEMBL5757014 | — | — | 3 | 8.40 |
| CHEMBL5769692 | — | — | 3 | 8.40 |
| CHEMBL5865121 | — | — | 3 | 8.40 |
| CHEMBL5906625 | — | — | 3 | 8.30 |
| CHEMBL5876479 | — | — | 3 | 8.30 |
| CHEMBL4073812 | — | — | 3 | 8.30 |
| CHEMBL5892494 | — | — | 3 | 8.22 |
| CHEMBL5973330 | — | — | 3 | 8.22 |
| CHEMBL6064436 | — | — | 3 | 8.22 |
| CHEMBL5904357 | — | — | 3 | 8.10 |
| CHEMBL5862734 | — | — | 3 | 8.05 |
| CHEMBL4065346 | — | — | 3 | 8.05 |
| CHEMBL5920528 | — | — | 3 | 8.05 |
| CHEMBL5794727 | — | — | 3 | 8.05 |
| CHEMBL5996168 | — | — | 3 | 8.05 |
| CHEMBL5843430 | — | — | 3 | 8.05 |
| CHEMBL5778843 | — | — | 3 | 8.05 |
| CHEMBL6013728 | — | — | 3 | 8.00 |
| CHEMBL5888782 | — | — | 3 | 8.00 |
| CHEMBL5983379 | — | — | 3 | 7.96 |
| CHEMBL5960518 | — | — | 3 | 7.96 |
| CHEMBL5859034 | — | — | 3 | 7.92 |
| CHEMBL5801650 | — | — | 3 | 7.92 |
| CHEMBL5803431 | — | — | 3 | 7.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6052218 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4061254 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5763461 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5778256 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5913995 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5769692 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4095153 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5757014 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5865121 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5876479 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4073812 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5906625 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5892494 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL6064436 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5973330 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5904357 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4065346 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5862734 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5996168 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5778843 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5843430 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5920528 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5794727 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL6013728 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5888782 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5960518 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5983379 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5801650 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5859034 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5803431 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL6061502 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5841258 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL6036002 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4076254 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5970791 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5969101 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5841703 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL6033005 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL6023676 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5958053 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5875451 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL5921972 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4072630 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL5957898 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5958316 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL5962640 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL5808946 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL5800044 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL5864779 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL5916859 | — | IC50 | = | 26.0 | nM | 7.58 |