Assay Detail
Binding
CHEMBL3887413
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Morpholino compounds, uses and methods
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 5.40 | 5.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3946661 | — | — | 1 | 5.64 |
| CHEMBL3946540 | — | — | 1 | 5.38 |
| CHEMBL3986651 | — | — | 1 | 5.19 |
| CHEMBL4110261 | — | — | 1 | - |
| CHEMBL3897835 | — | — | 1 | - |
| CHEMBL4114519 | — | — | 1 | - |
| CHEMBL4109218 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3946661 | — | Ki | = | 2307.0 | nM | 5.64 |
| CHEMBL3946540 | — | Ki | = | 4181.0 | nM | 5.38 |
| CHEMBL3986651 | — | Ki | = | 6448.0 | nM | 5.19 |
| CHEMBL4110261 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3897835 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4114519 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4109218 | — | Ki | > | 10000.0 | nM | - |