Assay Detail
Binding
CHEMBL4007108
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of OG(488) labeled probe binding to GST-tagged EED (unknown origin) after 1 hr by LanthaScreen TR-FRET assay
38
Total Activities
38
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
SAR of amino pyrrolidines as potent and novel protein-protein interaction inhibitors of the PRC2 complex through EED binding.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 38 | 7.66 | 9.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4060827 | — | — | 1 | 9.54 |
| CHEMBL4093096 | — | — | 1 | 9.52 |
| CHEMBL4076017 | — | — | 1 | 9.35 |
| CHEMBL4073166 | — | — | 1 | 9.19 |
| CHEMBL4065766 | — | — | 1 | 9.13 |
| CHEMBL4077363 | — | — | 1 | 9.00 |
| CHEMBL4059553 | — | — | 1 | 8.68 |
| CHEMBL4068192 | — | — | 1 | 8.59 |
| CHEMBL4081496 | — | — | 1 | 8.59 |
| CHEMBL4072329 | — | — | 1 | 8.34 |
| CHEMBL4077273 | — | — | 1 | 8.28 |
| CHEMBL4080018 | — | — | 1 | 7.96 |
| CHEMBL4085428 | — | — | 1 | 7.92 |
| CHEMBL4075197 | — | — | 1 | 7.89 |
| CHEMBL4089371 | — | — | 1 | 7.75 |
| CHEMBL4068811 | — | — | 1 | 7.64 |
| CHEMBL4087904 | — | — | 1 | 7.35 |
| CHEMBL4065124 | — | — | 1 | 7.31 |
| CHEMBL4095605 | — | — | 1 | 7.28 |
| CHEMBL4079061 | — | — | 1 | 7.25 |
| CHEMBL4104796 | — | — | 1 | 7.23 |
| CHEMBL4062773 | — | — | 1 | 7.18 |
| CHEMBL4086916 | — | — | 1 | 7.15 |
| CHEMBL4085375 | — | — | 1 | 7.11 |
| CHEMBL4084449 | — | — | 1 | 7.11 |
| CHEMBL4066584 | — | — | 1 | 6.89 |
| CHEMBL4104253 | — | — | 1 | 6.80 |
| CHEMBL4086565 | — | — | 1 | 6.64 |
| CHEMBL4073650 | — | — | 1 | 6.58 |
| CHEMBL4103354 | — | — | 1 | 6.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4060827 | — | Ki | = | 0.29 | nM | 9.54 |
| CHEMBL4093096 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL4076017 | — | Ki | = | 0.45 | nM | 9.35 |
| CHEMBL4073166 | — | Ki | = | 0.65 | nM | 9.19 |
| CHEMBL4065766 | — | Ki | = | 0.74 | nM | 9.13 |
| CHEMBL4077363 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL4059553 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL4068192 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL4081496 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL4072329 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL4077273 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL4080018 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL4085428 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL4075197 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL4089371 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL4068811 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL4087904 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL4065124 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL4095605 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL4079061 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL4104796 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL4062773 | — | Ki | = | 66.0 | nM | 7.18 |
| CHEMBL4086916 | — | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL4085375 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL4084449 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL4066584 | — | Ki | = | 129.0 | nM | 6.89 |
| CHEMBL4104253 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL4086565 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL4073650 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL4103354 | — | Ki | = | 330.0 | nM | 6.48 |
| CHEMBL4097080 | — | Ki | = | 380.0 | nM | 6.42 |
| CHEMBL4074159 | — | Ki | = | 600.0 | nM | 6.22 |
| CHEMBL4099707 | — | Ki | = | 610.0 | nM | 6.21 |
| CHEMBL4100918 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL4082105 | — | Ki | > | 50000.0 | nM | - |
| CHEMBL4063970 | — | Ki | > | 50000.0 | nM | - |
| CHEMBL4105413 | — | Ki | > | 50000.0 | nM | - |
| CHEMBL4087547 | — | Ki | > | 50000.0 | nM | - |