Assay Detail
Functional
CHEMBL1680622
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Antagonist activity at human progesterone receptor expressed in HEK293 cells assessed as inhibition of R5050-induced transcriptional activity by GRE-driven luciferase reporter gene assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel 3-aryl indoles as progesterone receptor antagonists for uterine fibroids.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.29 | 8.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1672547 | — | — | 1 | 8.64 |
| CHEMBL1672541 | — | — | 1 | 8.47 |
| CHEMBL1672548 | — | — | 1 | 8.41 |
| CHEMBL1672545 | — | — | 1 | 8.17 |
| CHEMBL1672546 | — | — | 1 | 8.14 |
| CHEMBL1672549 | — | — | 1 | 8.00 |
| CHEMBL1672544 | — | — | 1 | 7.90 |
| CHEMBL1672543 | — | — | 1 | 6.31 |
| CHEMBL235206 | — | — | 1 | 6.15 |
| CHEMBL1672542 | — | — | 1 | 6.12 |
| CHEMBL391231 | — | — | 1 | 5.70 |
| CHEMBL1672540 | 3-[(4-METHOXYPHENYL)PHENYLMETHYL]INDOLE | — | 1 | 5.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1672547 | — | IC50 | = | 2.29 | nM | 8.64 |
| CHEMBL1672541 | — | IC50 | = | 3.38 | nM | 8.47 |
| CHEMBL1672548 | — | IC50 | = | 3.89 | nM | 8.41 |
| CHEMBL1672545 | — | IC50 | = | 6.81 | nM | 8.17 |
| CHEMBL1672546 | — | IC50 | = | 7.28 | nM | 8.14 |
| CHEMBL1672549 | — | IC50 | = | 9.92 | nM | 8.00 |
| CHEMBL1672544 | — | IC50 | = | 12.6 | nM | 7.90 |
| CHEMBL1672543 | — | IC50 | = | 485.0 | nM | 6.31 |
| CHEMBL235206 | — | IC50 | = | 715.0 | nM | 6.15 |
| CHEMBL1672542 | — | IC50 | = | 765.0 | nM | 6.12 |
| CHEMBL391231 | — | IC50 | = | 2020.0 | nM | 5.70 |
| CHEMBL1672540 | 3-[(4-METHOXYPHENYL)PHENYLMETHYL]INDOLE | IC50 | = | 3720.0 | nM | 5.43 |