Assay Detail
Binding
CHEMBL3887404
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.
23
Total Activities
23
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 | 23 | 5.96 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3946661 | — | — | 1 | 9.22 |
| CHEMBL3986651 | — | — | 1 | 6.76 |
| CHEMBL3900699 | — | — | 1 | 6.43 |
| CHEMBL4112056 | — | — | 1 | 6.42 |
| CHEMBL4110261 | — | — | 1 | 6.27 |
| CHEMBL3946540 | — | — | 1 | 6.26 |
| CHEMBL3941579 | — | — | 1 | 6.23 |
| CHEMBL3897835 | — | — | 1 | 6.19 |
| CHEMBL3915107 | — | — | 1 | 5.86 |
| CHEMBL4109801 | — | — | 1 | 5.83 |
| CHEMBL4115493 | — | — | 1 | 5.73 |
| CHEMBL4112007 | — | — | 1 | 5.64 |
| CHEMBL4108986 | — | — | 1 | 5.54 |
| CHEMBL4112610 | — | — | 1 | 5.30 |
| CHEMBL4112412 | — | — | 1 | 5.20 |
| CHEMBL4115017 | — | — | 1 | 5.18 |
| CHEMBL4107302 | — | — | 1 | 5.13 |
| CHEMBL4109218 | — | — | 1 | 5.12 |
| CHEMBL3936595 | — | — | 1 | 5.00 |
| CHEMBL4114519 | — | — | 1 | - |
| CHEMBL4112009 | — | — | 1 | - |
| CHEMBL4110219 | — | — | 1 | - |
| CHEMBL4115505 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3946661 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL3986651 | — | Ki | = | 174.0 | nM | 6.76 |
| CHEMBL3900699 | — | Ki | = | 371.0 | nM | 6.43 |
| CHEMBL4112056 | — | Ki | = | 384.0 | nM | 6.42 |
| CHEMBL4110261 | — | Ki | = | 540.0 | nM | 6.27 |
| CHEMBL3946540 | — | Ki | = | 545.0 | nM | 6.26 |
| CHEMBL3941579 | — | Ki | = | 592.0 | nM | 6.23 |
| CHEMBL3897835 | — | Ki | = | 644.0 | nM | 6.19 |
| CHEMBL3915107 | — | Ki | = | 1388.0 | nM | 5.86 |
| CHEMBL4109801 | — | Ki | = | 1469.0 | nM | 5.83 |
| CHEMBL4115493 | — | Ki | = | 1848.0 | nM | 5.73 |
| CHEMBL4112007 | — | Ki | = | 2298.0 | nM | 5.64 |
| CHEMBL4108986 | — | Ki | = | 2883.0 | nM | 5.54 |
| CHEMBL4112610 | — | Ki | = | 5024.0 | nM | 5.30 |
| CHEMBL4112412 | — | Ki | = | 6374.0 | nM | 5.20 |
| CHEMBL4115017 | — | Ki | = | 6591.0 | nM | 5.18 |
| CHEMBL4107302 | — | Ki | = | 7324.0 | nM | 5.13 |
| CHEMBL4109218 | — | Ki | = | 7535.0 | nM | 5.12 |
| CHEMBL3936595 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL4114519 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4112009 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4110219 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4115505 | — | Ki | > | 10000.0 | nM | - |