Assay Detail
Binding
CHEMBL3624758
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Binding affinity to ERalpha receptor (unknown origin)
19
Total Activities
18
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
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 | 19 | 7.79 | 9.84 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL195515 | — | — | 1 | 9.84 |
| CHEMBL2137046 | — | — | 1 | 9.51 |
| CHEMBL3623004 | AZD-9496 | 1.0 | 2 | 9.17 |
| CHEMBL3623002 | — | — | 1 | 9.15 |
| CHEMBL1358 | FULVESTRANT | 4.0 | 1 | 9.09 |
| CHEMBL3623003 | — | — | 1 | 9.00 |
| CHEMBL33899 | — | — | 1 | 8.49 |
| CHEMBL3623001 | — | — | 1 | 8.19 |
| CHEMBL3622996 | — | — | 1 | 7.65 |
| CHEMBL83 | TAMOXIFEN | 4.0 | 1 | 7.61 |
| CHEMBL3622994 | — | — | 1 | 7.40 |
| CHEMBL3622999 | — | — | 1 | 7.16 |
| CHEMBL3622997 | — | — | 1 | 7.15 |
| CHEMBL3623000 | — | — | 1 | 7.01 |
| CHEMBL3622998 | — | — | 1 | 6.16 |
| CHEMBL3622995 | — | — | 1 | 5.75 |
| CHEMBL3622992 | — | — | 1 | 5.69 |
| CHEMBL3622993 | — | — | 1 | 4.86 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL195515 | — | IC50 | = | 0.1445 | nM | 9.84 |
| CHEMBL2137046 | — | IC50 | = | 0.309 | nM | 9.51 |
| CHEMBL3623004 | AZD-9496 | IC50 | = | 0.6761 | nM | 9.17 |
| CHEMBL3623002 | — | IC50 | = | 0.7079 | nM | 9.15 |
| CHEMBL3623004 | AZD-9496 | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL1358 | FULVESTRANT | IC50 | = | 0.8128 | nM | 9.09 |
| CHEMBL3623003 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL33899 | — | IC50 | = | 3.236 | nM | 8.49 |
| CHEMBL3623001 | — | IC50 | = | 6.457 | nM | 8.19 |
| CHEMBL3622996 | — | IC50 | = | 22.39 | nM | 7.65 |
| CHEMBL83 | TAMOXIFEN | IC50 | = | 24.55 | nM | 7.61 |
| CHEMBL3622994 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL3622999 | — | IC50 | = | 69.18 | nM | 7.16 |
| CHEMBL3622997 | — | IC50 | = | 70.79 | nM | 7.15 |
| CHEMBL3623000 | — | IC50 | = | 97.72 | nM | 7.01 |
| CHEMBL3622998 | — | IC50 | = | 691.83 | nM | 6.16 |
| CHEMBL3622995 | — | IC50 | = | 1778.28 | nM | 5.75 |
| CHEMBL3622992 | — | IC50 | = | 2041.74 | nM | 5.69 |
| CHEMBL3622993 | — | IC50 | = | 13803.84 | nM | 4.86 |