Assay Detail
Binding
CHEMBL4189551
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full-length N-terminal GST-fused human PKC-iota expressed in baculovirus expression system using (5FAM) RFARKGSLRQKNV as substrate after 60 mins by caliper assay
52
Total Activities
52
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 Drug Discovery of Potent Protein Kinase C Iota Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 52 | 4.83 | 8.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4212424 | — | — | 1 | 8.57 |
| CHEMBL4202753 | — | — | 1 | 8.55 |
| CHEMBL4208685 | — | — | 1 | 8.42 |
| CHEMBL4206065 | — | — | 1 | 8.30 |
| CHEMBL4216507 | — | — | 1 | 8.19 |
| CHEMBL4208028 | — | — | 1 | 7.52 |
| CHEMBL4213984 | — | — | 1 | 7.32 |
| CHEMBL4212934 | — | — | 1 | 7.19 |
| CHEMBL4211722 | — | — | 1 | 6.96 |
| CHEMBL4208982 | — | — | 1 | 6.92 |
| CHEMBL4215492 | — | — | 1 | 6.54 |
| CHEMBL4206023 | — | — | 1 | 6.24 |
| CHEMBL4205851 | — | — | 1 | 6.10 |
| CHEMBL4211820 | — | — | 1 | 5.96 |
| CHEMBL4214431 | — | — | 1 | 5.32 |
| CHEMBL4217980 | — | — | 1 | 5.22 |
| CHEMBL4215555 | — | — | 1 | 5.16 |
| CHEMBL4214403 | — | — | 1 | 5.12 |
| CHEMBL4216980 | — | — | 1 | 5.11 |
| CHEMBL4208713 | — | — | 1 | 5.02 |
| CHEMBL4204387 | — | — | 1 | 4.70 |
| CHEMBL4216587 | — | — | 1 | 4.43 |
| CHEMBL4215391 | — | — | 1 | 4.42 |
| CHEMBL4212132 | — | — | 1 | 4.39 |
| CHEMBL4205739 | — | — | 1 | 4.12 |
| CHEMBL4218133 | — | — | 1 | 4.02 |
| CHEMBL4202899 | — | — | 1 | 3.98 |
| CHEMBL4210601 | — | — | 1 | 3.83 |
| CHEMBL4203835 | — | — | 1 | 3.73 |
| CHEMBL4218913 | — | — | 1 | 3.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4212424 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL4202753 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL4208685 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL4206065 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4216507 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL4208028 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4213984 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL4212934 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL4211722 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4208982 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4215492 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL4206023 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL4205851 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL4211820 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4214431 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL4217980 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL4215555 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL4214403 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL4216980 | — | IC50 | = | 7700.0 | nM | 5.11 |
| CHEMBL4208713 | — | IC50 | = | 9500.0 | nM | 5.02 |
| CHEMBL4204387 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL4216587 | — | IC50 | = | 37000.0 | nM | 4.43 |
| CHEMBL4215391 | — | IC50 | = | 38000.0 | nM | 4.42 |
| CHEMBL4212132 | — | IC50 | = | 41000.0 | nM | 4.39 |
| CHEMBL4205739 | — | IC50 | = | 75000.0 | nM | 4.12 |
| CHEMBL4218133 | — | IC50 | = | 95000.0 | nM | 4.02 |
| CHEMBL4202899 | — | IC50 | = | 105000.0 | nM | 3.98 |
| CHEMBL4210601 | — | IC50 | = | 148000.0 | nM | 3.83 |
| CHEMBL4203835 | — | IC50 | = | 188000.0 | nM | 3.73 |
| CHEMBL4218913 | — | IC50 | = | 201000.0 | nM | 3.70 |
| CHEMBL4204384 | — | IC50 | = | 215000.0 | nM | 3.67 |
| CHEMBL4206942 | — | IC50 | = | 221000.0 | nM | 3.66 |
| CHEMBL4207793 | — | IC50 | = | 229000.0 | nM | 3.64 |
| CHEMBL4207181 | — | IC50 | = | 371000.0 | nM | 3.43 |
| CHEMBL4214498 | — | IC50 | = | 374000.0 | nM | 3.43 |
| CHEMBL4203838 | — | IC50 | = | 424000.0 | nM | 3.37 |
| CHEMBL4204389 | — | IC50 | = | 452000.0 | nM | 3.35 |
| CHEMBL124706 | PHTHALAZINONE | IC50 | = | 589000.0 | nM | 3.23 |
| CHEMBL4206553 | — | IC50 | = | 615000.0 | nM | 3.21 |
| CHEMBL1617811 | — | IC50 | = | 728000.0 | nM | 3.14 |
| CHEMBL4212691 | — | IC50 | = | 927000.0 | nM | 3.03 |
| CHEMBL4204893 | — | IC50 | = | 1300000.0 | nM | 2.89 |
| CHEMBL4216063 | — | IC50 | = | 1312000.0 | nM | 2.88 |
| CHEMBL4204735 | — | IC50 | = | 1423000.0 | nM | 2.85 |
| CHEMBL3274344 | — | IC50 | = | 1556000.0 | nM | 2.81 |
| CHEMBL4215993 | — | IC50 | = | 1570000.0 | nM | 2.80 |
| CHEMBL3288306 | — | IC50 | = | 1677000.0 | nM | 2.77 |
| CHEMBL4211034 | — | IC50 | = | 2216000.0 | nM | 2.65 |
| CHEMBL4202835 | — | IC50 | > | 384000.0 | nM | - |
| CHEMBL4203536 | — | IC50 | > | 384000.0 | nM | - |