Assay Detail
Binding
CHEMBL5739406
Review assay metadata, readout intent, target linkage, and publication context from the same page.
LanthaScreen Competitive Binding Assay: Compounds were screened for their ability to displace a fluorescent labelled tracer ERβ ligand via time resolved fluorescent energy transfer using the LanthaScreen Competitive Binding Assay screening service (Thermo Fisher Scientific).
30
Total Activities
7
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Tetrahydro-1H-pyrido [3,4-b]indole anti-estrogenic drugs
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 8.92 | 9.43 |
| kon | 10 | - | - |
| k_off | 10 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3623004 | AZD-9496 | 1.0 | 12 | 9.43 |
| CHEMBL3623003 | — | — | 3 | 9.00 |
| CHEMBL5788675 | — | — | 3 | 8.87 |
| CHEMBL4528514 | — | — | 3 | 8.79 |
| CHEMBL5745979 | — | — | 3 | 8.64 |
| CHEMBL5314475 | PALAZESTRANT | 3.0 | 3 | 8.57 |
| CHEMBL4635493 | — | — | 3 | 8.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3623004 | AZD-9496 | IC50 | = | 0.372 | nM | 9.43 |
| CHEMBL3623004 | AZD-9496 | IC50 | = | 0.372 | nM | 9.43 |
| CHEMBL3623004 | AZD-9496 | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3623003 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5788675 | — | IC50 | = | 1.35 | nM | 8.87 |
| CHEMBL4528514 | — | IC50 | = | 1.62 | nM | 8.79 |
| CHEMBL5745979 | — | IC50 | = | 2.29 | nM | 8.64 |
| CHEMBL5314475 | PALAZESTRANT | IC50 | = | 2.69 | nM | 8.57 |
| CHEMBL4635493 | — | IC50 | = | 2.82 | nM | 8.55 |
| CHEMBL5745979 | — | k_off | = | - | s-1 | - |
| CHEMBL5745979 | — | kon | = | - | — | - |
| CHEMBL3623004 | AZD-9496 | k_off | = | - | s-1 | - |
| CHEMBL3623004 | AZD-9496 | kon | = | - | — | - |
| CHEMBL3623004 | AZD-9496 | k_off | = | - | s-1 | - |
| CHEMBL3623004 | AZD-9496 | kon | = | - | — | - |
| CHEMBL3623003 | — | k_off | = | - | s-1 | - |
| CHEMBL3623003 | — | kon | = | - | — | - |
| CHEMBL3623004 | AZD-9496 | k_off | = | - | s-1 | - |
| CHEMBL3623004 | AZD-9496 | kon | = | - | — | - |
| CHEMBL3623004 | AZD-9496 | kon | = | - | — | - |
| CHEMBL3623004 | AZD-9496 | k_off | = | - | s-1 | - |
| CHEMBL4528514 | — | k_off | = | - | s-1 | - |
| CHEMBL5314475 | PALAZESTRANT | kon | = | - | — | - |
| CHEMBL3623004 | AZD-9496 | IC50 | < | 0.64 | nM | - |
| CHEMBL5314475 | PALAZESTRANT | k_off | = | - | s-1 | - |
| CHEMBL4528514 | — | kon | = | - | — | - |
| CHEMBL4635493 | — | kon | = | - | — | - |
| CHEMBL4635493 | — | k_off | = | - | s-1 | - |
| CHEMBL5788675 | — | k_off | = | - | s-1 | - |
| CHEMBL5788675 | — | kon | = | - | — | - |