Assay Detail
Binding
CHEMBL4405044
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of SGRG-K(Ac)-GG-K(Ac)-GLG-K(Ac)-GGA-K(Ac)-RHRKVGG-K-Biotin binding to N-terminal His6-tagged BRD4 bromodomain 2 (344 to 455 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) preincubated for 15 mins followed by biotin-labeled H4 peptide addition and measured after 10 mins by Alphascreen assay
30
Total Activities
30
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
Discovery of 8-Methyl-pyrrolo[1,2-a]pyrazin-1(2H)-one Derivatives as Highly Potent and Selective Bromodomain and Extra-Terminal (BET) Bromodomain Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 7.18 | 8.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4440098 | — | — | 1 | 8.66 |
| CHEMBL3987016 | MIVEBRESIB | 2.0 | 1 | 8.57 |
| CHEMBL4543167 | — | — | 1 | 8.46 |
| CHEMBL4461077 | — | — | 1 | 8.15 |
| CHEMBL4522212 | — | — | 1 | 8.13 |
| CHEMBL4441348 | — | — | 1 | 7.93 |
| CHEMBL4524758 | — | — | 1 | 7.89 |
| CHEMBL4474369 | — | — | 1 | 7.79 |
| CHEMBL4579454 | — | — | 1 | 7.59 |
| CHEMBL4461662 | — | — | 1 | 7.58 |
| CHEMBL4449279 | — | — | 1 | 7.55 |
| CHEMBL4567383 | — | — | 1 | 7.17 |
| CHEMBL4466659 | — | — | 1 | 7.15 |
| CHEMBL4445399 | — | — | 1 | 7.11 |
| CHEMBL4539863 | — | — | 1 | 7.03 |
| CHEMBL4542938 | — | — | 1 | 7.01 |
| CHEMBL4470237 | — | — | 1 | 6.93 |
| CHEMBL4470170 | — | — | 1 | 6.89 |
| CHEMBL4550412 | — | — | 1 | 6.75 |
| CHEMBL3581647 | BIRABRESIB | 2.0 | 1 | 6.71 |
| CHEMBL4557084 | — | — | 1 | 6.64 |
| CHEMBL4467880 | — | — | 1 | 6.38 |
| CHEMBL4462005 | — | — | 1 | 6.32 |
| CHEMBL4473292 | — | — | 1 | 6.17 |
| CHEMBL4564804 | — | — | 1 | 6.11 |
| CHEMBL4553526 | — | — | 1 | 5.80 |
| CHEMBL4562592 | — | — | 1 | 5.44 |
| CHEMBL4579222 | — | — | 1 | - |
| CHEMBL4441706 | — | — | 1 | - |
| CHEMBL4546494 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4440098 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL3987016 | MIVEBRESIB | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL4543167 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL4461077 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4522212 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL4441348 | — | IC50 | = | 11.7 | nM | 7.93 |
| CHEMBL4524758 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4474369 | — | IC50 | = | 16.2 | nM | 7.79 |
| CHEMBL4579454 | — | IC50 | = | 25.9 | nM | 7.59 |
| CHEMBL4461662 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4449279 | — | IC50 | = | 28.4 | nM | 7.55 |
| CHEMBL4567383 | — | IC50 | = | 67.3 | nM | 7.17 |
| CHEMBL4466659 | — | IC50 | = | 71.3 | nM | 7.15 |
| CHEMBL4445399 | — | IC50 | = | 77.2 | nM | 7.11 |
| CHEMBL4539863 | — | IC50 | = | 93.7 | nM | 7.03 |
| CHEMBL4542938 | — | IC50 | = | 97.9 | nM | 7.01 |
| CHEMBL4470237 | — | IC50 | = | 117.0 | nM | 6.93 |
| CHEMBL4470170 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4550412 | — | IC50 | = | 178.0 | nM | 6.75 |
| CHEMBL3581647 | BIRABRESIB | IC50 | = | 197.0 | nM | 6.71 |
| CHEMBL4557084 | — | IC50 | = | 229.0 | nM | 6.64 |
| CHEMBL4467880 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL4462005 | — | IC50 | = | 478.0 | nM | 6.32 |
| CHEMBL4473292 | — | IC50 | = | 669.0 | nM | 6.17 |
| CHEMBL4564804 | — | IC50 | = | 772.0 | nM | 6.11 |
| CHEMBL4553526 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4562592 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL4579222 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4441706 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4546494 | — | IC50 | > | 2000.0 | nM | - |