Assay Detail
Binding
CHEMBL5734658
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Suv 39H2 Assay: Assay buffer (4 μL) was added into all the wells, including test compound and control wells (except for Sinefungin control wells), using the Multidrop Combi. The plate was centrifuged at 1000 rpm for 1 min. Substrate mix (8 μL) containing radiolabelled 3H-SAM (final conc: 100 nM) and H3 Histone Peptide (final conc: 350 nM) was added to all wells using Multidrop Combi and centrifuged at 1000 rpm for 1 min. SUV39H2 (8 μL, final conc: optimized for each lot of the enzyme based on specific activity) was added by using the Multidrop Combi. The assay plate was centrifuged at 1000 rpm for 1 min. Assay buffer was used as background control, and incubated at room temperature for 3 hours. The reaction was stopped with 20 μL of 2.5 mg/mL Streptavidin SPA beads (final conc. 50 μg/well) in buffer using the Multidrop Combi and centrifuged for 1 min. The plate was loaded into the Trilux-Microbeta counter and a delayed read of 10 hours was made. The radioactive signal was measured at 1 min/well. Sinefungin and the internal standard compound were used as tool compounds to determine assay performance.
918
Total Activities
303
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Histone-lysine N-methyltransferase SUV39H2 (CHEMBL1795177) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Bicyclic compound and use thereof for inhibiting SUV39H2
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 306 | 7.75 | 8.75 |
| kon | 306 | - | - |
| k_off | 306 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5917854 | — | — | 3 | 8.75 |
| CHEMBL4556599 | — | — | 3 | 8.68 |
| CHEMBL5889747 | — | — | 3 | 8.66 |
| CHEMBL5813669 | — | — | 3 | 8.57 |
| CHEMBL5889567 | — | — | 3 | 8.54 |
| CHEMBL5833321 | — | — | 3 | 8.52 |
| CHEMBL5802370 | — | — | 3 | 8.51 |
| CHEMBL5821250 | — | — | 3 | 8.48 |
| CHEMBL6039206 | — | — | 3 | 8.48 |
| CHEMBL6002706 | — | — | 3 | 8.47 |
| CHEMBL5882142 | — | — | 3 | 8.46 |
| CHEMBL5990392 | — | — | 3 | 8.45 |
| CHEMBL5752280 | — | — | 3 | 8.43 |
| CHEMBL6058730 | — | — | 3 | 8.42 |
| CHEMBL5778265 | — | — | 3 | 8.40 |
| CHEMBL5982126 | — | — | 3 | 8.39 |
| CHEMBL6035731 | — | — | 3 | 8.38 |
| CHEMBL5783478 | — | — | 3 | 8.37 |
| CHEMBL6054950 | — | — | 3 | 8.36 |
| CHEMBL6019346 | — | — | 3 | 8.36 |
| CHEMBL5874588 | — | — | 3 | 8.36 |
| CHEMBL6033942 | — | — | 3 | 8.36 |
| CHEMBL5755050 | — | — | 3 | 8.34 |
| CHEMBL5794968 | — | — | 3 | 8.31 |
| CHEMBL5813364 | — | — | 3 | 8.31 |
| CHEMBL5975952 | — | — | 3 | 8.29 |
| CHEMBL5813687 | — | — | 3 | 8.29 |
| CHEMBL4543399 | — | — | 3 | 8.28 |
| CHEMBL5840209 | — | — | 3 | 8.28 |
| CHEMBL5976455 | — | — | 3 | 8.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5917854 | — | IC50 | = | 1.77 | nM | 8.75 |
| CHEMBL4556599 | — | IC50 | = | 2.07 | nM | 8.68 |
| CHEMBL5889747 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL5813669 | — | IC50 | = | 2.71 | nM | 8.57 |
| CHEMBL5889567 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL5833321 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5802370 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL6039206 | — | IC50 | = | 3.33 | nM | 8.48 |
| CHEMBL5821250 | — | IC50 | = | 3.27 | nM | 8.48 |
| CHEMBL6002706 | — | IC50 | = | 3.35 | nM | 8.47 |
| CHEMBL5882142 | — | IC50 | = | 3.49 | nM | 8.46 |
| CHEMBL5990392 | — | IC50 | = | 3.53 | nM | 8.45 |
| CHEMBL5752280 | — | IC50 | = | 3.71 | nM | 8.43 |
| CHEMBL6058730 | — | IC50 | = | 3.81 | nM | 8.42 |
| CHEMBL5778265 | — | IC50 | = | 3.95 | nM | 8.40 |
| CHEMBL5982126 | — | IC50 | = | 4.11 | nM | 8.39 |
| CHEMBL6035731 | — | IC50 | = | 4.16 | nM | 8.38 |
| CHEMBL5783478 | — | IC50 | = | 4.31 | nM | 8.37 |
| CHEMBL6019346 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL6054950 | — | IC50 | = | 4.35 | nM | 8.36 |
| CHEMBL5874588 | — | IC50 | = | 4.33 | nM | 8.36 |
| CHEMBL6033942 | — | IC50 | = | 4.35 | nM | 8.36 |
| CHEMBL5755050 | — | IC50 | = | 4.54 | nM | 8.34 |
| CHEMBL5794968 | — | IC50 | = | 4.89 | nM | 8.31 |
| CHEMBL5813364 | — | IC50 | = | 4.88 | nM | 8.31 |
| CHEMBL5813687 | — | IC50 | = | 5.14 | nM | 8.29 |
| CHEMBL5975952 | — | IC50 | = | 5.15 | nM | 8.29 |
| CHEMBL4543399 | — | IC50 | = | 5.31 | nM | 8.28 |
| CHEMBL5840209 | — | IC50 | = | 5.24 | nM | 8.28 |
| CHEMBL5976455 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL4554934 | — | IC50 | = | 5.38 | nM | 8.27 |
| CHEMBL5919082 | — | IC50 | = | 5.44 | nM | 8.26 |
| CHEMBL5811206 | — | IC50 | = | 5.61 | nM | 8.25 |
| CHEMBL5786923 | — | IC50 | = | 5.75 | nM | 8.24 |
| CHEMBL5934131 | — | IC50 | = | 5.74 | nM | 8.24 |
| CHEMBL6001781 | — | IC50 | = | 5.85 | nM | 8.23 |
| CHEMBL5968613 | — | IC50 | = | 6.08 | nM | 8.22 |
| CHEMBL6056074 | — | IC50 | = | 6.06 | nM | 8.22 |
| CHEMBL5815685 | — | IC50 | = | 5.97 | nM | 8.22 |
| CHEMBL6007204 | — | IC50 | = | 6.35 | nM | 8.20 |
| CHEMBL5808722 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL5764876 | — | IC50 | = | 6.37 | nM | 8.20 |
| CHEMBL6042902 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL5952813 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL5928778 | — | IC50 | = | 6.49 | nM | 8.19 |
| CHEMBL5767518 | — | IC50 | = | 6.66 | nM | 8.18 |
| CHEMBL6008212 | — | IC50 | = | 6.55 | nM | 8.18 |
| CHEMBL5826640 | — | IC50 | = | 6.74 | nM | 8.17 |
| CHEMBL6037469 | — | IC50 | = | 6.72 | nM | 8.17 |
| CHEMBL4483443 | — | IC50 | = | 6.72 | nM | 8.17 |