Assay Detail
Binding
CHEMBL4188747
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Binding affinity to recombinant human full length PKA-R2beta expressed in Escherichia coli BL21 DE3-RIL cells assessed as reduction in interaction with AKAP by fluorescence polarization analysis
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
cAMP-dependent protein kinase type II-beta regulatory subunit (CHEMBL2270) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Investigating PKA-RII specificity using analogs of the PKA:AKAP peptide inhibitor STAD-2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 13 | 6.77 | 7.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4203735 | — | — | 1 | 7.12 |
| CHEMBL4204708 | — | — | 1 | 6.91 |
| CHEMBL4211508 | — | — | 1 | 6.88 |
| CHEMBL4207455 | — | — | 1 | 6.83 |
| CHEMBL4215761 | — | — | 1 | 6.82 |
| CHEMBL4204281 | — | — | 1 | 6.59 |
| CHEMBL4205523 | — | — | 1 | 6.25 |
| CHEMBL4211816 | — | — | 1 | - |
| CHEMBL4202571 | — | — | 1 | - |
| CHEMBL4209571 | — | — | 1 | - |
| CHEMBL4215956 | — | — | 1 | - |
| CHEMBL4203911 | — | — | 1 | - |
| CHEMBL4213005 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4203735 | — | Kd | = | 75.0 | nM | 7.12 |
| CHEMBL4204708 | — | Kd | = | 124.0 | nM | 6.91 |
| CHEMBL4211508 | — | Kd | = | 131.0 | nM | 6.88 |
| CHEMBL4207455 | — | Kd | = | 147.0 | nM | 6.83 |
| CHEMBL4215761 | — | Kd | = | 152.0 | nM | 6.82 |
| CHEMBL4204281 | — | Kd | = | 257.0 | nM | 6.59 |
| CHEMBL4205523 | — | Kd | = | 557.0 | nM | 6.25 |
| CHEMBL4211816 | — | Kd | - | — | - | |
| CHEMBL4202571 | — | Kd | - | — | - | |
| CHEMBL4209571 | — | Kd | - | — | - | |
| CHEMBL4215956 | — | Kd | - | — | - | |
| CHEMBL4203911 | — | Kd | - | — | - | |
| CHEMBL4213005 | — | Kd | - | — | - |