Assay Detail
Binding
CHEMBL4008166
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant N-terminal GST-tagged EED (76 to 441 residues) (unknown origin) expressed in Escherichia coli BL21-CodonPlus(DE3)-RIL assessed as reduction in SAH production using H3[21-44,K27Me0) peptide as substrate measured after 20 mins by LC/MS/MS method
39
Total Activities
39
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 First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 39 | 6.58 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3414621 | TAZEMETOSTAT | 4.0 | 1 | 8.70 |
| CHEMBL4103319 | — | — | 1 | 8.15 |
| CHEMBL4079806 | — | — | 1 | 8.05 |
| CHEMBL4088683 | — | — | 1 | 8.05 |
| CHEMBL4081748 | — | — | 1 | 7.89 |
| CHEMBL4105572 | — | — | 1 | 7.72 |
| CHEMBL4099766 | — | — | 1 | 7.70 |
| CHEMBL4065484 | — | — | 1 | 7.66 |
| CHEMBL4093147 | — | — | 1 | 7.52 |
| CHEMBL4076858 | — | — | 1 | 7.31 |
| CHEMBL4066526 | — | — | 1 | 7.31 |
| CHEMBL4081454 | — | — | 1 | 7.28 |
| CHEMBL4105039 | — | — | 1 | 7.28 |
| CHEMBL4067448 | — | — | 1 | 7.21 |
| CHEMBL4095382 | — | — | 1 | 7.16 |
| CHEMBL4103134 | — | — | 1 | 7.16 |
| CHEMBL4097833 | — | — | 1 | 7.03 |
| CHEMBL4085389 | — | — | 1 | 7.03 |
| CHEMBL4086716 | — | — | 1 | 6.89 |
| CHEMBL4104753 | — | — | 1 | 6.82 |
| CHEMBL4087691 | — | — | 1 | 6.82 |
| CHEMBL4070157 | — | — | 1 | 6.58 |
| CHEMBL4067992 | — | — | 1 | 6.54 |
| CHEMBL4065278 | — | — | 1 | 6.29 |
| CHEMBL4078858 | — | — | 1 | 6.11 |
| CHEMBL4063655 | — | — | 1 | 6.00 |
| CHEMBL4061496 | — | — | 1 | 5.66 |
| CHEMBL4086879 | — | — | 1 | 5.65 |
| CHEMBL4064552 | — | — | 1 | 5.63 |
| CHEMBL4089623 | — | — | 1 | 5.45 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3414621 | TAZEMETOSTAT | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4103319 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4088683 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4079806 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4081748 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4105572 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4099766 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4065484 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4093147 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4076858 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL4066526 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL4081454 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL4105039 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL4067448 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL4103134 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL4095382 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL4097833 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL4085389 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL4086716 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4104753 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4087691 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4070157 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL4067992 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL4065278 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL4078858 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL4063655 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4061496 | — | IC50 | = | 2180.0 | nM | 5.66 |
| CHEMBL4086879 | — | IC50 | = | 2220.0 | nM | 5.65 |
| CHEMBL4064552 | — | IC50 | = | 2340.0 | nM | 5.63 |
| CHEMBL4089623 | — | IC50 | = | 3520.0 | nM | 5.45 |
| CHEMBL4096234 | — | IC50 | = | 4030.0 | nM | 5.39 |
| CHEMBL310238 | — | IC50 | = | 6040.0 | nM | 5.22 |
| CHEMBL4097028 | — | IC50 | = | 12400.0 | nM | 4.91 |
| CHEMBL4097339 | — | IC50 | = | 14080.0 | nM | 4.85 |
| CHEMBL4101492 | — | IC50 | = | 14900.0 | nM | 4.83 |
| CHEMBL4080815 | — | IC50 | = | 20490.0 | nM | 4.69 |
| CHEMBL4079016 | — | IC50 | = | 21800.0 | nM | 4.66 |
| CHEMBL4059484 | — | IC50 | = | 21800.0 | nM | 4.66 |
| CHEMBL4085277 | — | IC50 | > | 100000.0 | nM | - |