Assay Detail
Binding
CHEMBL5629601
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Inhibition of PKC alpha (unknown origin) in presence of ATP at Km
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 | 6.60 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL565612 | SOTRASTAURIN | 2.0 | 1 | 8.70 |
| CHEMBL5631765 | — | — | 1 | 7.60 |
| CHEMBL3798011 | — | — | 1 | 7.37 |
| CHEMBL5631904 | — | — | 1 | 7.31 |
| CHEMBL5631570 | — | — | 1 | 7.31 |
| CHEMBL5631499 | — | — | 1 | 7.25 |
| CHEMBL5632236 | — | — | 1 | 7.24 |
| CHEMBL5633664 | — | — | 1 | 7.23 |
| CHEMBL5632070 | — | — | 1 | 7.19 |
| CHEMBL5631412 | — | — | 1 | 7.17 |
| CHEMBL5632134 | — | — | 1 | 7.09 |
| CHEMBL5633970 | — | — | 1 | 6.87 |
| CHEMBL5633180 | — | — | 1 | 6.85 |
| CHEMBL5632086 | — | — | 1 | 6.59 |
| CHEMBL5631319 | — | — | 1 | 6.58 |
| CHEMBL5632287 | — | — | 1 | 6.57 |
| CHEMBL5631515 | — | — | 1 | 6.50 |
| CHEMBL5631596 | — | — | 1 | 6.43 |
| CHEMBL5631314 | — | — | 1 | 6.36 |
| CHEMBL5633500 | — | — | 1 | 6.20 |
| CHEMBL5633314 | — | — | 1 | 6.14 |
| CHEMBL5631838 | — | — | 1 | 6.11 |
| CHEMBL5633898 | — | — | 1 | 6.09 |
| CHEMBL5633148 | — | — | 1 | 6.06 |
| CHEMBL5632103 | — | — | 1 | 6.04 |
| CHEMBL5631688 | — | — | 1 | 6.01 |
| CHEMBL5633390 | — | — | 1 | 5.96 |
| CHEMBL5633916 | — | — | 1 | 5.72 |
| CHEMBL5631971 | — | — | 1 | 5.54 |
| CHEMBL5632646 | — | — | 1 | 5.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL565612 | SOTRASTAURIN | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5631765 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3798011 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL5631904 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL5631570 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL5631499 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL5632236 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL5633664 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL5632070 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL5631412 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL5632134 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL5633970 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL5633180 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL5632086 | — | IC50 | = | 259.0 | nM | 6.59 |
| CHEMBL5631319 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL5632287 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL5631515 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL5631596 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL5631314 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL5633500 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL5633314 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL5631838 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL5633898 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL5633148 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL5632103 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL5631688 | — | IC50 | = | 980.0 | nM | 6.01 |
| CHEMBL5633390 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL5633916 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL5631971 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL5632646 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL5633746 | — | IC50 | = | 8200.0 | nM | 5.09 |
| CHEMBL5631811 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5632327 | — | IC50 | > | 10000.0 | nM | - |