Assay Detail
Binding
CHEMBL5732653
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 disclosed as SEO 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. After twenty minutes of equilibration, the plates were read on an Envision instrument and IC50s calculated using a four parameter non-linear curve fit.
930
Total Activities
308
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 | 310 | 7.39 | 9.00 |
| kon | 310 | - | - |
| k_off | 310 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6044256 | — | — | 3 | 9.00 |
| CHEMBL5794948 | — | — | 3 | 9.00 |
| CHEMBL5822280 | — | — | 3 | 8.70 |
| CHEMBL5811499 | — | — | 3 | 8.70 |
| CHEMBL6025504 | — | — | 3 | 8.70 |
| CHEMBL5753286 | — | — | 3 | 8.70 |
| CHEMBL5975381 | — | — | 3 | 8.70 |
| CHEMBL6021138 | — | — | 3 | 8.52 |
| CHEMBL5948490 | — | — | 3 | 8.52 |
| CHEMBL5867874 | — | — | 3 | 8.52 |
| CHEMBL6034812 | — | — | 3 | 8.40 |
| CHEMBL5890726 | — | — | 3 | 8.40 |
| CHEMBL5970449 | — | — | 3 | 8.30 |
| CHEMBL6010385 | — | — | 3 | 8.30 |
| CHEMBL6013447 | — | — | 3 | 8.15 |
| CHEMBL5962979 | — | — | 3 | 8.15 |
| CHEMBL5763429 | — | — | 3 | 8.10 |
| CHEMBL5920439 | — | — | 3 | 8.00 |
| CHEMBL5946513 | — | — | 3 | 8.00 |
| CHEMBL5988786 | — | — | 3 | 8.00 |
| CHEMBL6036457 | — | — | 3 | 8.00 |
| CHEMBL5994335 | — | — | 3 | 8.00 |
| CHEMBL5806477 | — | — | 3 | 8.00 |
| CHEMBL5797284 | — | — | 3 | 8.00 |
| CHEMBL6030015 | — | — | 3 | 8.00 |
| CHEMBL6024359 | — | — | 3 | 8.00 |
| CHEMBL6051302 | — | — | 3 | 8.00 |
| CHEMBL5819653 | — | — | 3 | 8.00 |
| CHEMBL5978449 | — | — | 3 | 8.00 |
| CHEMBL3962542 | — | — | 3 | 8.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5794948 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL6044256 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5822280 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5975381 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5753286 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5811499 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL6025504 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5948490 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5867874 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL6021138 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5890726 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL6034812 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5970449 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL6010385 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5962979 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL6013447 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5763429 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL5932721 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5757324 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL6024359 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL6030015 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5797284 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5885476 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL6051302 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5819653 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5915732 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5994335 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL6036457 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5978449 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5857985 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5988786 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3892467 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5788497 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5946513 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5994636 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5785255 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3981511 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5850494 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5920439 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5786314 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3962542 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5806477 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5995949 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5983603 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5982481 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5844745 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5839141 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5885467 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL6034588 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL6057802 | — | IC50 | = | 15.0 | nM | 7.82 |