Assay Detail
Binding
CHEMBL4201827
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of His-6-tagged human KLK6 R74G/R76Q/N132Q mutant expressed in Escherichia coli DH10 pre-incubated for 30 mins before N-Boc-FSR-AMC substrate addition and measured after 30 mins
43
Total Activities
43
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| 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 | 42 | 5.73 | 7.75 |
| Inhibition | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4217078 | — | — | 1 | 7.75 |
| CHEMBL4212718 | — | — | 1 | 7.00 |
| CHEMBL4216138 | — | — | 1 | 7.00 |
| CHEMBL4218203 | — | — | 1 | 6.89 |
| CHEMBL4210314 | — | — | 1 | 6.89 |
| CHEMBL4203947 | — | — | 1 | 6.82 |
| CHEMBL4211164 | — | — | 1 | 6.72 |
| CHEMBL4214705 | — | — | 1 | 6.60 |
| CHEMBL4207925 | — | — | 1 | 6.60 |
| CHEMBL4218314 | — | — | 1 | 6.54 |
| CHEMBL4211677 | — | — | 1 | 6.31 |
| CHEMBL4212332 | — | — | 1 | 6.19 |
| CHEMBL4208878 | — | — | 1 | 6.05 |
| CHEMBL4204137 | — | — | 1 | 5.92 |
| CHEMBL4218619 | — | — | 1 | 5.92 |
| CHEMBL4215806 | — | — | 1 | 5.85 |
| CHEMBL4203193 | — | — | 1 | 5.64 |
| CHEMBL4203033 | — | — | 1 | 5.55 |
| CHEMBL4215383 | — | — | 1 | 5.36 |
| CHEMBL4206799 | — | — | 1 | 5.22 |
| CHEMBL4205963 | — | — | 1 | 5.21 |
| CHEMBL4210959 | — | — | 1 | 5.16 |
| CHEMBL4212830 | — | — | 1 | 5.12 |
| CHEMBL4206590 | — | — | 1 | 5.12 |
| CHEMBL4211986 | — | — | 1 | 5.05 |
| CHEMBL4217674 | — | — | 1 | 5.05 |
| CHEMBL1883669 | — | — | 1 | 5.00 |
| CHEMBL4210322 | — | — | 1 | 4.89 |
| CHEMBL4205435 | — | — | 1 | 4.82 |
| CHEMBL4206077 | — | — | 1 | 4.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4217078 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4212718 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4216138 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4218203 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4210314 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4203947 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4211164 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4214705 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4207925 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4218314 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL4211677 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL4212332 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL4208878 | — | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL4204137 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4218619 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4215806 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4203193 | — | IC50 | = | 2310.0 | nM | 5.64 |
| CHEMBL4203033 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL4215383 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL4206799 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL4205963 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL4210959 | — | IC50 | = | 6990.0 | nM | 5.16 |
| CHEMBL4206590 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL4212830 | — | IC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL4211986 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL4217674 | — | IC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL1883669 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4210322 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL4205435 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL4206077 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL4214636 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL4212099 | — | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL4216440 | — | IC50 | = | 43000.0 | nM | 4.37 |
| CHEMBL4202434 | — | IC50 | = | 58000.0 | nM | 4.24 |
| CHEMBL4202971 | — | IC50 | = | 110000.0 | nM | - |
| CHEMBL4207321 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4214840 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4206734 | — | IC50 | <= | 2.5 | nM | - |
| CHEMBL4213266 | — | IC50 | - | — | - | |
| CHEMBL4213806 | — | Inhibition | - | % | - | |
| CHEMBL4211470 | — | IC50 | = | 170000.0 | nM | - |
| CHEMBL4213650 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4210437 | — | IC50 | > | 200000.0 | nM | - |