Assay Detail
Binding
CHEMBL3624761
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Antagonist activity at progesterone receptor in human MCF cells assessed as estradiol-induced receptor response
18
Total Activities
18
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MCF |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic Acid (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor Downregulator and Antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 7.30 | 9.68 |
| pIC50 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1358 | FULVESTRANT | 4.0 | 1 | 9.68 |
| CHEMBL3623004 | AZD-9496 | 1.0 | 1 | 9.55 |
| CHEMBL2137046 | — | — | 1 | 9.10 |
| CHEMBL3623002 | — | — | 1 | 9.08 |
| CHEMBL3623003 | — | — | 1 | 8.46 |
| CHEMBL3623001 | — | — | 1 | 8.44 |
| CHEMBL195515 | — | — | 1 | 7.92 |
| CHEMBL3622999 | — | — | 1 | 7.31 |
| CHEMBL3623000 | — | — | 1 | 7.30 |
| CHEMBL83 | TAMOXIFEN | 4.0 | 1 | 6.89 |
| CHEMBL3622994 | — | — | 1 | 6.14 |
| CHEMBL3622996 | — | — | 1 | 6.04 |
| CHEMBL3622995 | — | — | 1 | 5.82 |
| CHEMBL3622997 | — | — | 1 | 5.68 |
| CHEMBL3622998 | — | — | 1 | 5.64 |
| CHEMBL3622992 | — | — | 1 | 5.57 |
| CHEMBL33899 | — | — | 1 | 5.40 |
| CHEMBL3622993 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1358 | FULVESTRANT | IC50 | = | 0.2089 | nM | 9.68 |
| CHEMBL3623004 | AZD-9496 | IC50 | = | 0.2818 | nM | 9.55 |
| CHEMBL2137046 | — | IC50 | = | 0.7943 | nM | 9.10 |
| CHEMBL3623002 | — | IC50 | = | 0.8318 | nM | 9.08 |
| CHEMBL3623003 | — | IC50 | = | 3.467 | nM | 8.46 |
| CHEMBL3623001 | — | IC50 | = | 3.631 | nM | 8.44 |
| CHEMBL195515 | — | IC50 | = | 12.02 | nM | 7.92 |
| CHEMBL3622999 | — | IC50 | = | 48.98 | nM | 7.31 |
| CHEMBL3623000 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL83 | TAMOXIFEN | IC50 | = | 128.82 | nM | 6.89 |
| CHEMBL3622994 | — | IC50 | = | 724.44 | nM | 6.14 |
| CHEMBL3622996 | — | IC50 | = | 912.01 | nM | 6.04 |
| CHEMBL3622995 | — | IC50 | = | 1513.56 | nM | 5.82 |
| CHEMBL3622997 | — | IC50 | = | 2089.3 | nM | 5.68 |
| CHEMBL3622998 | — | IC50 | = | 2290.87 | nM | 5.64 |
| CHEMBL3622992 | — | IC50 | = | 2691.53 | nM | 5.57 |
| CHEMBL33899 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL3622993 | — | pIC50 | - | — | - |