Assay Detail
Binding
CHEMBL5736830
Review assay metadata, readout intent, target linkage, and publication context from the same page.
TR-FRET Assay: The TR-FRET method was used to measure the PRC2 enzyme activity. First, the enzyme was mixed with compounds at different concentrations and incubated for 30 min at room temperature. The biotin-labeled histone H3 peptide substrate and the cofactor S-adenosylmethionine (SAM) were added to initiate the enzymatic reaction. After reaction was performed at room temperature for 4 hour, Acceptor and Donor were added and incubated for half an hour. The multifunctional microplate reader EnVision (Perkin Elmer Inc.) was used to detect the fluorescence signal.
240
Total Activities
79
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Histone-binding protein RBBP4/Histone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12 (CHEMBL6066587) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Triazolopyrimidine, triazolopyridine compounds, and the composition thereof for treating PRC2-mediated diseases
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 80 | 7.56 | 8.77 |
| kon | 80 | - | - |
| k_off | 80 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6031570 | — | — | 3 | 8.77 |
| CHEMBL5830594 | — | — | 3 | 8.66 |
| CHEMBL5755546 | — | — | 3 | 8.60 |
| CHEMBL5744415 | — | — | 3 | 8.54 |
| CHEMBL5921456 | — | — | 3 | 8.49 |
| CHEMBL6026043 | — | — | 3 | 8.48 |
| CHEMBL5850167 | — | — | 3 | 8.47 |
| CHEMBL5757741 | — | — | 3 | 8.46 |
| CHEMBL5903614 | — | — | 3 | 8.44 |
| CHEMBL5981172 | — | — | 3 | 8.41 |
| CHEMBL5873219 | — | — | 6 | 8.39 |
| CHEMBL5993160 | — | — | 3 | 8.38 |
| CHEMBL5938838 | — | — | 3 | 8.35 |
| CHEMBL5790437 | — | — | 3 | 8.33 |
| CHEMBL5989347 | — | — | 3 | 8.33 |
| CHEMBL6020239 | — | — | 3 | 8.32 |
| CHEMBL5885689 | — | — | 3 | 8.28 |
| CHEMBL6019980 | — | — | 3 | 8.28 |
| CHEMBL5799894 | — | — | 3 | 8.27 |
| CHEMBL5970917 | — | — | 3 | 8.25 |
| CHEMBL5899703 | — | — | 3 | 8.21 |
| CHEMBL5846743 | — | — | 3 | 8.18 |
| CHEMBL5837429 | — | — | 3 | 8.14 |
| CHEMBL5985124 | — | — | 3 | 8.11 |
| CHEMBL5901505 | — | — | 3 | 8.10 |
| CHEMBL5814258 | — | — | 3 | 8.08 |
| CHEMBL5817076 | — | — | 3 | 8.08 |
| CHEMBL5757987 | — | — | 3 | 8.07 |
| CHEMBL6020675 | — | — | 3 | 8.05 |
| CHEMBL5812331 | — | — | 3 | 8.03 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6031570 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5830594 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL5755546 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL5744415 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL5921456 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL6026043 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL5850167 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL5757741 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL5903614 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL5981172 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL5873219 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL5993160 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL5938838 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL5989347 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL5790437 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL6020239 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL5873219 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL6019980 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL5885689 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL5799894 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL5970917 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL5899703 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL5846743 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL5837429 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL5985124 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL5901505 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL5817076 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL5814258 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL5757987 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL6020675 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL5812331 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL5798344 | — | IC50 | = | 10.7 | nM | 7.97 |
| CHEMBL5850078 | — | IC50 | = | 11.9 | nM | 7.92 |
| CHEMBL5773639 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5746890 | — | IC50 | = | 14.1 | nM | 7.85 |
| CHEMBL5895393 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5923740 | — | IC50 | = | 16.1 | nM | 7.79 |
| CHEMBL5835604 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL6027526 | — | IC50 | = | 17.7 | nM | 7.75 |
| CHEMBL5894410 | — | IC50 | = | 17.9 | nM | 7.75 |
| CHEMBL5848949 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL5752294 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5795067 | — | IC50 | = | 22.3 | nM | 7.65 |
| CHEMBL5826494 | — | IC50 | = | 22.5 | nM | 7.65 |
| CHEMBL5874166 | — | IC50 | = | 23.3 | nM | 7.63 |
| CHEMBL6017307 | — | IC50 | = | 32.8 | nM | 7.48 |
| CHEMBL5949102 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL5884531 | — | IC50 | = | 40.8 | nM | 7.39 |
| CHEMBL5909807 | — | IC50 | = | 47.6 | nM | 7.32 |
| CHEMBL5837241 | — | IC50 | = | 54.5 | nM | 7.26 |