Assay Detail
Functional
CHEMBL934255
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human PR expressed in human T47D cells assessed as inhibition of progesterone induced alkaline phosphatase
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | T47D |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 7.74 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1276308 | MIFEPRISTONE | 4.0 | 1 | 9.70 |
| CHEMBL407847 | — | — | 1 | 8.49 |
| CHEMBL272663 | — | — | 1 | 8.48 |
| CHEMBL429572 | — | — | 1 | 8.35 |
| CHEMBL429928 | — | — | 1 | 8.31 |
| CHEMBL407848 | — | — | 1 | 8.30 |
| CHEMBL270714 | — | — | 1 | 8.23 |
| CHEMBL270908 | — | — | 1 | 8.00 |
| CHEMBL271804 | — | — | 1 | 7.89 |
| CHEMBL271552 | — | — | 1 | 7.82 |
| CHEMBL308938 | — | — | 1 | 7.82 |
| CHEMBL270052 | — | — | 1 | 7.70 |
| CHEMBL406235 | — | — | 1 | 7.69 |
| CHEMBL271149 | — | — | 1 | 7.60 |
| CHEMBL117187 | — | — | 1 | 7.57 |
| CHEMBL437801 | — | — | 1 | 7.57 |
| CHEMBL405428 | — | — | 1 | 7.54 |
| CHEMBL271175 | — | — | 1 | 7.52 |
| CHEMBL437622 | — | — | 1 | 7.52 |
| CHEMBL407622 | — | — | 1 | 7.52 |
| CHEMBL271336 | — | — | 1 | 7.32 |
| CHEMBL271835 | — | — | 1 | 6.79 |
| CHEMBL408696 | — | — | 1 | 6.71 |
| CHEMBL270909 | — | — | 1 | 6.52 |
| CHEMBL409147 | — | — | 1 | 6.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1276308 | MIFEPRISTONE | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL407847 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL272663 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL429572 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL429928 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL407848 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL270714 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL270908 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL271804 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL271552 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL308938 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL270052 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL406235 | — | IC50 | = | 20.3 | nM | 7.69 |
| CHEMBL271149 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL117187 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL437801 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL405428 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL271175 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL437622 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL407622 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL271336 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL271835 | — | IC50 | = | 164.0 | nM | 6.79 |
| CHEMBL408696 | — | IC50 | = | 194.0 | nM | 6.71 |
| CHEMBL270909 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL409147 | — | IC50 | = | 351.0 | nM | 6.46 |