Assay Detail
Binding
CHEMBL3864392
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Inhibition of Halo-tagged histone H3.3 binding to CBP/EP300 (unknown origin) expressed in HEK293 cells measured after overnight incubation by luciferase reporter gene based BRET assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
CREB-binding protein/Histone acetyltransferase p300 (CHEMBL3883300) ↗| Type | PROTEIN FAMILY |
| Organism | Homo sapiens |
Publication
Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 6.12 | 6.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3962542 | — | — | 1 | 6.55 |
| CHEMBL3892467 | — | — | 1 | 6.48 |
| CHEMBL3981511 | — | — | 1 | 6.47 |
| CHEMBL3968533 | — | — | 1 | 6.40 |
| CHEMBL3917504 | — | — | 1 | 6.37 |
| CHEMBL3893541 | — | — | 1 | 6.30 |
| CHEMBL3920459 | — | — | 1 | 6.27 |
| CHEMBL3973515 | — | — | 1 | 6.25 |
| CHEMBL3896323 | — | — | 1 | 6.14 |
| CHEMBL3924330 | — | — | 1 | 6.12 |
| CHEMBL3889679 | — | — | 1 | 6.02 |
| CHEMBL3911524 | — | — | 1 | 6.01 |
| CHEMBL3938408 | — | — | 1 | 6.01 |
| CHEMBL3985118 | — | — | 1 | 6.01 |
| CHEMBL3915331 | — | — | 1 | 5.92 |
| CHEMBL3934488 | — | — | 1 | 5.89 |
| CHEMBL3906525 | — | — | 1 | 5.82 |
| CHEMBL3915504 | — | — | 1 | 5.70 |
| CHEMBL3902514 | — | — | 1 | 5.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3962542 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL3892467 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL3981511 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL3968533 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3917504 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL3893541 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL3920459 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL3973515 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL3896323 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL3924330 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL3889679 | — | IC50 | = | 960.0 | nM | 6.02 |
| CHEMBL3911524 | — | IC50 | = | 980.0 | nM | 6.01 |
| CHEMBL3938408 | — | IC50 | = | 980.0 | nM | 6.01 |
| CHEMBL3985118 | — | IC50 | = | 980.0 | nM | 6.01 |
| CHEMBL3915331 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3934488 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL3906525 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL3915504 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3902514 | — | IC50 | = | 2500.0 | nM | 5.60 |