Assay Detail
Binding
CHEMBL4201828
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Inhibition of trypsin (unknown origin) pre-incubated for 30 mins before N-Boc-FSR-AMC substrate addition and measured after 30 mins
41
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Intermediate |
Publication
Depsipeptides Featuring a Neutral P1 Are Potent Inhibitors of Kallikrein-Related Peptidase 6 with On-Target Cellular Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 41 | 4.98 | 6.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4208878 | — | — | 1 | 6.75 |
| CHEMBL4216138 | — | — | 1 | 6.48 |
| CHEMBL4217078 | — | — | 1 | 6.42 |
| CHEMBL4218619 | — | — | 1 | 5.60 |
| CHEMBL4203033 | — | — | 1 | 5.07 |
| CHEMBL4212718 | — | — | 1 | 4.72 |
| CHEMBL4218203 | — | — | 1 | 4.68 |
| CHEMBL4210314 | — | — | 1 | 4.62 |
| CHEMBL4211677 | — | — | 1 | 4.60 |
| CHEMBL4214705 | — | — | 1 | 4.58 |
| CHEMBL4218314 | — | — | 1 | 4.47 |
| CHEMBL4207925 | — | — | 1 | 4.47 |
| CHEMBL4212332 | — | — | 1 | 4.42 |
| CHEMBL4204137 | — | — | 1 | 4.30 |
| CHEMBL4203193 | — | — | 1 | 4.21 |
| CHEMBL4206799 | — | — | 1 | 4.21 |
| CHEMBL4213650 | — | — | 1 | - |
| CHEMBL4203947 | — | — | 1 | - |
| CHEMBL1883669 | — | — | 1 | - |
| CHEMBL4216440 | — | — | 1 | - |
| CHEMBL4211470 | — | — | 1 | - |
| CHEMBL4206734 | — | — | 1 | - |
| CHEMBL4217674 | — | — | 1 | - |
| CHEMBL4215806 | — | — | 1 | - |
| CHEMBL4206590 | — | — | 1 | - |
| CHEMBL4211986 | — | — | 1 | - |
| CHEMBL4215383 | — | — | 1 | - |
| CHEMBL4210959 | — | — | 1 | - |
| CHEMBL4206077 | — | — | 1 | - |
| CHEMBL4210437 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4208878 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4216138 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL4217078 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL4218619 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL4203033 | — | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL4212718 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL4218203 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL4210314 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL4211677 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL4214705 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL4218314 | — | IC50 | = | 34000.0 | nM | 4.47 |
| CHEMBL4207925 | — | IC50 | = | 34000.0 | nM | 4.47 |
| CHEMBL4212332 | — | IC50 | = | 38000.0 | nM | 4.42 |
| CHEMBL4204137 | — | IC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL4206799 | — | IC50 | = | 61000.0 | nM | 4.21 |
| CHEMBL4203193 | — | IC50 | = | 61000.0 | nM | 4.21 |
| CHEMBL4212830 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4210322 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4211164 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4205435 | — | IC50 | = | 150000.0 | nM | - |
| CHEMBL4207321 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4202434 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4202971 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4214636 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4205963 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4212099 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4214840 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4210437 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4206077 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4210959 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4215383 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4211986 | — | IC50 | = | 190000.0 | nM | - |
| CHEMBL4206590 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4215806 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4217674 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4206734 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL4211470 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4216440 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL1883669 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4203947 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4213650 | — | IC50 | > | 50000.0 | nM | - |