Assay Detail
ADMET
CHEMBL4405045
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of MSGRGK(Ac)-GGK(Ac)GLGK(Ac)GGAKRHR-biotin binding to EP300 (1040 to 1160 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) by Alphascreen assay
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| 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 | 5.03 | 7.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3987016 | MIVEBRESIB | 2.0 | 1 | 7.20 |
| CHEMBL4543167 | — | — | 1 | 5.66 |
| CHEMBL4440098 | — | — | 1 | 5.41 |
| CHEMBL4524758 | — | — | 1 | 5.40 |
| CHEMBL4539863 | — | — | 1 | 5.27 |
| CHEMBL4579454 | — | — | 1 | 4.90 |
| CHEMBL4579222 | — | — | 1 | 4.81 |
| CHEMBL4461077 | — | — | 1 | 4.78 |
| CHEMBL4441348 | — | — | 1 | 4.75 |
| CHEMBL4522212 | — | — | 1 | 4.73 |
| CHEMBL4445399 | — | — | 1 | 4.60 |
| CHEMBL4461662 | — | — | 1 | 4.60 |
| CHEMBL4473292 | — | — | 1 | 4.57 |
| CHEMBL4470170 | — | — | 1 | 4.46 |
| CHEMBL4550412 | — | — | 1 | 4.24 |
| CHEMBL4567383 | — | — | 1 | - |
| CHEMBL4441706 | — | — | 1 | - |
| CHEMBL4449279 | — | — | 1 | - |
| CHEMBL4474369 | — | — | 1 | - |
| CHEMBL4462005 | — | — | 1 | - |
| CHEMBL4564804 | — | — | 1 | - |
| CHEMBL4542938 | — | — | 1 | - |
| CHEMBL4466659 | — | — | 1 | - |
| CHEMBL4467880 | — | — | 1 | - |
| CHEMBL4546494 | — | — | 1 | - |
| CHEMBL4553526 | — | — | 1 | - |
| CHEMBL4562592 | — | — | 1 | - |
| CHEMBL3581647 | BIRABRESIB | 2.0 | 1 | - |
| CHEMBL4470237 | — | — | 1 | - |
| CHEMBL4557084 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3987016 | MIVEBRESIB | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL4543167 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL4440098 | — | IC50 | = | 3857.0 | nM | 5.41 |
| CHEMBL4524758 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL4539863 | — | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL4579454 | — | IC50 | = | 12600.0 | nM | 4.90 |
| CHEMBL4579222 | — | IC50 | = | 15600.0 | nM | 4.81 |
| CHEMBL4461077 | — | IC50 | = | 16500.0 | nM | 4.78 |
| CHEMBL4441348 | — | IC50 | = | 17800.0 | nM | 4.75 |
| CHEMBL4522212 | — | IC50 | = | 18600.0 | nM | 4.73 |
| CHEMBL4445399 | — | IC50 | = | 25100.0 | nM | 4.60 |
| CHEMBL4461662 | — | IC50 | = | 25100.0 | nM | 4.60 |
| CHEMBL4473292 | — | IC50 | = | 26900.0 | nM | 4.57 |
| CHEMBL4470170 | — | IC50 | = | 34700.0 | nM | 4.46 |
| CHEMBL4550412 | — | IC50 | = | 57000.0 | nM | 4.24 |
| CHEMBL4567383 | — | IC50 | > | 33000.0 | nM | - |
| CHEMBL4441706 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4449279 | — | IC50 | > | 33000.0 | nM | - |
| CHEMBL4474369 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4462005 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4564804 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4542938 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4466659 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4467880 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4546494 | — | IC50 | - | — | - | |
| CHEMBL4553526 | — | IC50 | - | — | - | |
| CHEMBL4562592 | — | IC50 | - | — | - | |
| CHEMBL3581647 | BIRABRESIB | IC50 | > | 33000.0 | nM | - |
| CHEMBL4470237 | — | IC50 | > | 33000.0 | nM | - |
| CHEMBL4557084 | — | IC50 | > | 33000.0 | nM | - |