Assay Detail
Binding
CHEMBL5629600
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PKC theta (unknown origin) in presence of 1 mM ATP
33
Total Activities
33
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
Discovery of a novel series of selective macrocyclic PKCTheta inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 8.22 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5632236 | — | — | 1 | 10.00 |
| CHEMBL5631570 | — | — | 1 | 9.05 |
| CHEMBL5631319 | — | — | 1 | 9.03 |
| CHEMBL5632134 | — | — | 1 | 9.00 |
| CHEMBL5631499 | — | — | 1 | 8.92 |
| CHEMBL5632287 | — | — | 1 | 8.92 |
| CHEMBL5633180 | — | — | 1 | 8.80 |
| CHEMBL5633500 | — | — | 1 | 8.55 |
| CHEMBL565612 | SOTRASTAURIN | 2.0 | 1 | 8.47 |
| CHEMBL5632086 | — | — | 1 | 8.44 |
| CHEMBL5632070 | — | — | 1 | 8.41 |
| CHEMBL5631314 | — | — | 1 | 8.30 |
| CHEMBL5631596 | — | — | 1 | 8.20 |
| CHEMBL3798011 | — | — | 1 | 8.06 |
| CHEMBL5631811 | — | — | 1 | 8.04 |
| CHEMBL5631515 | — | — | 1 | 8.00 |
| CHEMBL5631838 | — | — | 1 | 7.92 |
| CHEMBL5632103 | — | — | 1 | 7.82 |
| CHEMBL5633148 | — | — | 1 | 7.82 |
| CHEMBL5633970 | — | — | 1 | 7.80 |
| CHEMBL5633898 | — | — | 1 | 7.57 |
| CHEMBL5631971 | — | — | 1 | 7.57 |
| CHEMBL5633314 | — | — | 1 | 7.43 |
| CHEMBL5631688 | — | — | 1 | 7.27 |
| CHEMBL5633916 | — | — | 1 | 7.21 |
| CHEMBL5632646 | — | — | 1 | 7.14 |
| CHEMBL5631412 | — | — | 1 | - |
| CHEMBL5631904 | — | — | 1 | - |
| CHEMBL5633664 | — | — | 1 | - |
| CHEMBL5631765 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5632236 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL5631570 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL5631319 | — | IC50 | = | 0.93 | nM | 9.03 |
| CHEMBL5632134 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5631499 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5632287 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5633180 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5633500 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL565612 | SOTRASTAURIN | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL5632086 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL5632070 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL5631314 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5631596 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL3798011 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL5631811 | — | IC50 | = | 9.2 | nM | 8.04 |
| CHEMBL5631515 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5631838 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5632103 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5633148 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5633970 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5633898 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL5631971 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL5633314 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL5631688 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL5633916 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL5632646 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL5631412 | — | IC50 | < | 0.5 | nM | - |
| CHEMBL5631904 | — | IC50 | < | 0.5 | nM | - |
| CHEMBL5633664 | — | IC50 | < | 0.5 | nM | - |
| CHEMBL5631765 | — | IC50 | < | 0.5 | nM | - |
| CHEMBL5633746 | — | IC50 | - | — | - | |
| CHEMBL5633390 | — | IC50 | - | — | - | |
| CHEMBL5632327 | — | IC50 | - | — | - |