Assay Detail
Binding
CHEMBL4402363
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Inhibition of recombinant human full length N-terminal GST-fused PKCi (1 to 587 residues) expressed in baculovirus expression system using 5-FAM-RFARKGSLRQKNV as substrate measured after 60 mins by caliper microfluidic mobility shift assay
20
Total Activities
20
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
Fragment-based Discovery of a Small-Molecule Protein Kinase C-iota Inhibitor Binding Post-kinase Domain Residues.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 4.74 | 6.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4517782 | — | — | 1 | 6.57 |
| CHEMBL4471416 | — | — | 1 | 6.47 |
| CHEMBL4441139 | — | — | 1 | 6.15 |
| CHEMBL4520505 | — | — | 1 | 4.71 |
| CHEMBL4543879 | — | — | 1 | 4.66 |
| CHEMBL4450200 | — | — | 1 | 4.64 |
| CHEMBL4547613 | — | — | 1 | 4.62 |
| CHEMBL4440509 | — | — | 1 | 4.50 |
| CHEMBL4584982 | — | — | 1 | 4.47 |
| CHEMBL4540971 | — | — | 1 | 4.38 |
| CHEMBL4446447 | — | — | 1 | 4.12 |
| CHEMBL4551875 | — | — | 1 | 4.11 |
| CHEMBL4450468 | — | — | 1 | 3.58 |
| CHEMBL4203838 | — | — | 1 | 3.37 |
| CHEMBL4552099 | — | — | 1 | - |
| CHEMBL4459501 | — | — | 1 | - |
| CHEMBL4566521 | — | — | 1 | - |
| CHEMBL4454756 | — | — | 1 | - |
| CHEMBL4459301 | — | — | 1 | - |
| CHEMBL4450572 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4517782 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4471416 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL4441139 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL4520505 | — | IC50 | = | 19600.0 | nM | 4.71 |
| CHEMBL4543879 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL4450200 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL4547613 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL4440509 | — | IC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL4584982 | — | IC50 | = | 34000.0 | nM | 4.47 |
| CHEMBL4540971 | — | IC50 | = | 42200.0 | nM | 4.38 |
| CHEMBL4446447 | — | IC50 | = | 76000.0 | nM | 4.12 |
| CHEMBL4551875 | — | IC50 | = | 77000.0 | nM | 4.11 |
| CHEMBL4450468 | — | IC50 | = | 263000.0 | nM | 3.58 |
| CHEMBL4203838 | — | IC50 | = | 424000.0 | nM | 3.37 |
| CHEMBL4552099 | — | IC50 | > | 384000.0 | nM | - |
| CHEMBL4459501 | — | IC50 | > | 384000.0 | nM | - |
| CHEMBL4566521 | — | IC50 | > | 384000.0 | nM | - |
| CHEMBL4454756 | — | IC50 | > | 384000.0 | nM | - |
| CHEMBL4459301 | — | IC50 | > | 384000.0 | nM | - |
| CHEMBL4450572 | — | IC50 | > | 384000.0 | nM | - |