Assay Detail
Binding
CHEMBL5162522
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of C-terminal His6-tagged BRD4 BD1 (unknown origin) using H-YSGRGK(Ac)GGK(Ac)GLGK(Ac)-GGAK(Ac)RHRK-Biotin-OH as substrate incubated for 1 hrs by HTRF assay
43
Total Activities
43
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
Structure-Based Discovery and Optimization of Furo[3,2-<i>c</i>]pyridin-4(5<i>H</i>)-one Derivatives as Potent and Second Bromodomain (BD2)-Selective Bromo and Extra Terminal Domain (BET) Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 43 | 8.28 | 9.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5171062 | — | — | 1 | 9.48 |
| CHEMBL5171510 | — | — | 1 | 9.41 |
| CHEMBL5176955 | — | — | 1 | 9.37 |
| CHEMBL5202705 | — | — | 1 | 9.28 |
| CHEMBL5171591 | — | — | 1 | 9.28 |
| CHEMBL5200542 | — | — | 1 | 9.25 |
| CHEMBL5184079 | — | — | 1 | 9.25 |
| CHEMBL5191078 | — | — | 1 | 9.24 |
| CHEMBL5206375 | — | — | 1 | 9.15 |
| CHEMBL5175082 | — | — | 1 | 9.14 |
| CHEMBL5171031 | — | — | 1 | 9.12 |
| CHEMBL5206261 | — | — | 1 | 9.03 |
| CHEMBL5199360 | — | — | 1 | 9.02 |
| CHEMBL5174374 | — | — | 1 | 9.00 |
| CHEMBL5172345 | — | — | 1 | 8.92 |
| CHEMBL5209398 | — | — | 1 | 8.92 |
| CHEMBL5196207 | — | — | 1 | 8.85 |
| CHEMBL5177436 | — | — | 1 | 8.80 |
| CHEMBL5173301 | — | — | 1 | 8.70 |
| CHEMBL5190094 | — | — | 1 | 8.64 |
| CHEMBL5200884 | — | — | 1 | 8.62 |
| CHEMBL5183265 | — | — | 1 | 8.48 |
| CHEMBL5189967 | — | — | 1 | 8.39 |
| CHEMBL5205435 | — | — | 1 | 8.39 |
| CHEMBL5204275 | — | — | 1 | 8.22 |
| CHEMBL5176332 | — | — | 1 | 8.21 |
| CHEMBL5176176 | — | — | 1 | 8.19 |
| CHEMBL5204795 | — | — | 1 | 8.17 |
| CHEMBL5181765 | — | — | 1 | 8.11 |
| CHEMBL5207143 | — | — | 1 | 8.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5171062 | — | IC50 | = | 0.33 | nM | 9.48 |
| CHEMBL5171510 | — | IC50 | = | 0.39 | nM | 9.41 |
| CHEMBL5176955 | — | IC50 | = | 0.43 | nM | 9.37 |
| CHEMBL5202705 | — | IC50 | = | 0.52 | nM | 9.28 |
| CHEMBL5171591 | — | IC50 | = | 0.53 | nM | 9.28 |
| CHEMBL5200542 | — | IC50 | = | 0.56 | nM | 9.25 |
| CHEMBL5184079 | — | IC50 | = | 0.56 | nM | 9.25 |
| CHEMBL5191078 | — | IC50 | = | 0.57 | nM | 9.24 |
| CHEMBL5206375 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5175082 | — | IC50 | = | 0.72 | nM | 9.14 |
| CHEMBL5171031 | — | IC50 | = | 0.75 | nM | 9.12 |
| CHEMBL5206261 | — | IC50 | = | 0.94 | nM | 9.03 |
| CHEMBL5199360 | — | IC50 | = | 0.95 | nM | 9.02 |
| CHEMBL5174374 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5209398 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5172345 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5196207 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL5177436 | — | IC50 | = | 1.57 | nM | 8.80 |
| CHEMBL5173301 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5190094 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL5200884 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL5183265 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL5205435 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL5189967 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL5204275 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5176332 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL5176176 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL5204795 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL5181765 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL5207143 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL5169842 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1957266 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5192071 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL5200030 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL5179959 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL5186717 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL5180474 | — | IC50 | = | 121.0 | nM | 6.92 |
| CHEMBL5205742 | — | IC50 | = | 153.0 | nM | 6.82 |
| CHEMBL5178480 | — | IC50 | = | 162.0 | nM | 6.79 |
| CHEMBL5173426 | — | IC50 | = | 192.0 | nM | 6.72 |
| CHEMBL4297454 | ABBV-744 | IC50 | = | 238.0 | nM | 6.62 |
| CHEMBL5206088 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL5204783 | — | IC50 | = | 326.0 | nM | 6.49 |