Assay Detail
Binding
CHEMBL3830587
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Alexa Fluor 647-tagged I-BET762 binding to recombinant truncated 6H-Thr BRD4 BD1 Y97A mutant (1 to 477 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) cells after 30 mins by TR-FRET assay
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | BL21-DE3 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 4.80 | 5.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3827767 | — | — | 1 | 5.10 |
| CHEMBL3828194 | — | — | 1 | 5.00 |
| CHEMBL3356145 | — | — | 1 | 5.00 |
| CHEMBL3828311 | — | — | 1 | 5.00 |
| CHEMBL3827114 | — | — | 1 | 5.00 |
| CHEMBL3828008 | — | — | 1 | 4.90 |
| CHEMBL3827280 | — | — | 1 | 4.70 |
| CHEMBL3828191 | — | — | 1 | 4.70 |
| CHEMBL3827276 | — | — | 1 | 4.60 |
| CHEMBL3827927 | — | — | 1 | 4.40 |
| CHEMBL3828061 | — | — | 1 | 4.40 |
| CHEMBL3827629 | — | — | 1 | - |
| CHEMBL3828186 | — | — | 1 | - |
| CHEMBL3827941 | — | — | 1 | - |
| CHEMBL3828546 | — | — | 1 | - |
| CHEMBL3827710 | — | — | 1 | - |
| CHEMBL3828299 | — | — | 1 | - |
| CHEMBL3356143 | — | — | 1 | - |
| CHEMBL3827158 | — | — | 1 | - |
| CHEMBL3828504 | — | — | 1 | - |
| CHEMBL3827434 | — | — | 1 | - |
| CHEMBL3828357 | — | — | 1 | - |
| CHEMBL3828426 | — | — | 1 | - |
| CHEMBL3828684 | — | — | 1 | - |
| CHEMBL3828026 | — | — | 1 | - |
| CHEMBL3828354 | — | — | 1 | - |
| CHEMBL3356146 | — | — | 1 | - |
| CHEMBL3827560 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3827767 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL3828194 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3356145 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3828311 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3827114 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3828008 | — | IC50 | = | 12589.25 | nM | 4.90 |
| CHEMBL3827280 | — | IC50 | = | 19952.62 | nM | 4.70 |
| CHEMBL3828191 | — | IC50 | = | 19952.62 | nM | 4.70 |
| CHEMBL3827276 | — | IC50 | = | 25118.86 | nM | 4.60 |
| CHEMBL3827927 | — | IC50 | = | 39810.72 | nM | 4.40 |
| CHEMBL3828061 | — | IC50 | = | 39810.72 | nM | 4.40 |
| CHEMBL3827629 | — | IC50 | > | 50118.72 | nM | - |
| CHEMBL3828186 | — | IC50 | > | 50118.72 | nM | - |
| CHEMBL3827941 | — | IC50 | > | 50118.72 | nM | - |
| CHEMBL3828546 | — | IC50 | > | 50118.72 | nM | - |
| CHEMBL3827710 | — | IC50 | > | 50118.72 | nM | - |
| CHEMBL3828299 | — | IC50 | > | 50118.72 | nM | - |
| CHEMBL3356143 | — | IC50 | > | 50118.72 | nM | - |
| CHEMBL3827158 | — | IC50 | > | 50118.72 | nM | - |
| CHEMBL3828504 | — | IC50 | > | 50118.72 | nM | - |
| CHEMBL3827434 | — | IC50 | > | 50118.72 | nM | - |
| CHEMBL3828357 | — | IC50 | > | 50118.72 | nM | - |
| CHEMBL3828426 | — | IC50 | > | 50118.72 | nM | - |
| CHEMBL3828684 | — | IC50 | > | 50118.72 | nM | - |
| CHEMBL3828026 | — | IC50 | > | 50118.72 | nM | - |
| CHEMBL3828354 | — | IC50 | > | 50118.72 | nM | - |
| CHEMBL3356146 | — | IC50 | > | 50118.72 | nM | - |
| CHEMBL3827560 | — | IC50 | > | 50118.72 | nM | - |