Assay Detail
Binding
CHEMBL3259188
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Competitive reversible inhibition of porcine pancreatic kallikrein using alpha-N-benzoyl-DL-arginine-p-nitroanilide hydrochloride as substrate after 15 to 180 mins by Michaelis-Menten plot analysis
59
Total Activities
59
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Sus scrofa |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Diarylamidine derivatives with one or both of the aryl moieties consisting of an indole or indole-like ring. Inhibitors of arginine-specific esteroproteases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 59 | 4.79 | 6.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL352923 | — | — | 1 | 6.14 |
| CHEMBL167255 | — | — | 1 | 5.62 |
| CHEMBL48217 | DAPI | — | 1 | 5.57 |
| CHEMBL102148 | — | — | 1 | 5.40 |
| CHEMBL1233459 | — | — | 1 | 5.39 |
| CHEMBL3251534 | — | — | 1 | 5.33 |
| CHEMBL164489 | — | — | 1 | 5.33 |
| CHEMBL101672 | — | — | 1 | 5.29 |
| CHEMBL167762 | — | — | 1 | 5.29 |
| CHEMBL103649 | — | — | 1 | 5.22 |
| CHEMBL167801 | — | — | 1 | 5.13 |
| CHEMBL164947 | — | — | 1 | 5.11 |
| CHEMBL352553 | — | — | 1 | 5.06 |
| CHEMBL388768 | — | — | 1 | 5.05 |
| CHEMBL354342 | — | — | 1 | 5.04 |
| CHEMBL279962 | — | — | 1 | 5.02 |
| CHEMBL167845 | — | — | 1 | 4.97 |
| CHEMBL167761 | — | — | 1 | 4.96 |
| CHEMBL101261 | — | — | 1 | 4.95 |
| CHEMBL165312 | — | — | 1 | 4.91 |
| CHEMBL3251194 | — | — | 1 | 4.91 |
| CHEMBL297809 | — | — | 1 | 4.87 |
| CHEMBL417907 | — | — | 1 | 4.82 |
| CHEMBL99951 | — | — | 1 | 4.76 |
| CHEMBL3251190 | — | — | 1 | 4.75 |
| CHEMBL52393 | — | — | 1 | 4.74 |
| CHEMBL3251186 | — | — | 1 | 4.72 |
| CHEMBL3251192 | — | — | 1 | 4.65 |
| CHEMBL3251187 | — | — | 1 | 4.64 |
| CHEMBL3251185 | — | — | 1 | 4.59 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL352923 | — | Ki | = | 730.0 | nM | 6.14 |
| CHEMBL167255 | — | Ki | = | 2370.0 | nM | 5.62 |
| CHEMBL48217 | DAPI | Ki | = | 2700.0 | nM | 5.57 |
| CHEMBL102148 | — | Ki | = | 3980.0 | nM | 5.40 |
| CHEMBL1233459 | — | Ki | = | 4110.0 | nM | 5.39 |
| CHEMBL3251534 | — | Ki | = | 4670.0 | nM | 5.33 |
| CHEMBL164489 | — | Ki | = | 4650.0 | nM | 5.33 |
| CHEMBL101672 | — | Ki | = | 5160.0 | nM | 5.29 |
| CHEMBL167762 | — | Ki | = | 5070.0 | nM | 5.29 |
| CHEMBL103649 | — | Ki | = | 6050.0 | nM | 5.22 |
| CHEMBL167801 | — | Ki | = | 7360.0 | nM | 5.13 |
| CHEMBL164947 | — | Ki | = | 7760.0 | nM | 5.11 |
| CHEMBL352553 | — | Ki | = | 8680.0 | nM | 5.06 |
| CHEMBL388768 | — | Ki | = | 8910.0 | nM | 5.05 |
| CHEMBL354342 | — | Ki | = | 9080.0 | nM | 5.04 |
| CHEMBL279962 | — | Ki | = | 9530.0 | nM | 5.02 |
| CHEMBL167845 | — | Ki | = | 10600.0 | nM | 4.97 |
| CHEMBL167761 | — | Ki | = | 11000.0 | nM | 4.96 |
| CHEMBL101261 | — | Ki | = | 11300.0 | nM | 4.95 |
| CHEMBL165312 | — | Ki | = | 12260.0 | nM | 4.91 |
| CHEMBL3251194 | — | Ki | = | 12300.0 | nM | 4.91 |
| CHEMBL297809 | — | Ki | = | 13500.0 | nM | 4.87 |
| CHEMBL417907 | — | Ki | = | 15300.0 | nM | 4.82 |
| CHEMBL99951 | — | Ki | = | 17300.0 | nM | 4.76 |
| CHEMBL3251190 | — | Ki | = | 17600.0 | nM | 4.75 |
| CHEMBL52393 | — | Ki | = | 18100.0 | nM | 4.74 |
| CHEMBL3251186 | — | Ki | = | 18900.0 | nM | 4.72 |
| CHEMBL3251192 | — | Ki | = | 22500.0 | nM | 4.65 |
| CHEMBL3251187 | — | Ki | = | 23000.0 | nM | 4.64 |
| CHEMBL3251185 | — | Ki | = | 25700.0 | nM | 4.59 |
| CHEMBL168138 | — | Ki | = | 29100.0 | nM | 4.54 |
| CHEMBL297403 | — | Ki | = | 31400.0 | nM | 4.50 |
| CHEMBL3251528 | — | Ki | = | 35600.0 | nM | 4.45 |
| CHEMBL356487 | — | Ki | = | 36500.0 | nM | 4.44 |
| CHEMBL168077 | — | Ki | = | 38000.0 | nM | 4.42 |
| CHEMBL3251537 | — | Ki | = | 39300.0 | nM | 4.41 |
| CHEMBL1688696 | — | Ki | = | 39700.0 | nM | 4.40 |
| CHEMBL3244501 | — | Ki | = | 40000.0 | nM | 4.40 |
| CHEMBL3251535 | — | Ki | = | 46100.0 | nM | 4.34 |
| CHEMBL3251188 | — | Ki | = | 48300.0 | nM | 4.32 |
| CHEMBL352718 | — | Ki | = | 52900.0 | nM | 4.28 |
| CHEMBL500330 | — | Ki | = | 56200.0 | nM | 4.25 |
| CHEMBL3251536 | — | Ki | = | 61200.0 | nM | 4.21 |
| CHEMBL3251529 | — | Ki | = | 61300.0 | nM | 4.21 |
| CHEMBL563834 | — | Ki | = | 64500.0 | nM | 4.19 |
| CHEMBL166236 | — | Ki | = | 71700.0 | nM | 4.14 |
| CHEMBL3251533 | — | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL145735 | — | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL353802 | — | Ki | = | 104000.0 | nM | - |
| CHEMBL145656 | — | Ki | = | 141000.0 | nM | - |