Assay Detail
Binding
CHEMBL3259186
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Competitive reversible inhibition of bovine thrombin using alpha-N-benzoyl-DL-arginine-p-nitroanilide hydrochloride as substrate after 15 to 40 mins by Michaelis-Menten plot analysis
62
Total Activities
62
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Bos taurus |
| 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 | 62 | 5.04 | 5.86 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3251534 | — | — | 1 | 5.86 |
| CHEMBL3251191 | — | — | 1 | 5.85 |
| CHEMBL352553 | — | — | 1 | 5.70 |
| CHEMBL102148 | — | — | 1 | 5.68 |
| CHEMBL101672 | — | — | 1 | 5.65 |
| CHEMBL165312 | — | — | 1 | 5.61 |
| CHEMBL101261 | — | — | 1 | 5.56 |
| CHEMBL3251186 | — | — | 1 | 5.52 |
| CHEMBL168077 | — | — | 1 | 5.51 |
| CHEMBL103649 | — | — | 1 | 5.51 |
| CHEMBL52393 | — | — | 1 | 5.49 |
| CHEMBL3251527 | — | — | 1 | 5.41 |
| CHEMBL279962 | — | — | 1 | 5.38 |
| CHEMBL99951 | — | — | 1 | 5.38 |
| CHEMBL167255 | — | — | 1 | 5.38 |
| CHEMBL297809 | — | — | 1 | 5.37 |
| CHEMBL563834 | — | — | 1 | 5.33 |
| CHEMBL3251192 | — | — | 1 | 5.31 |
| CHEMBL289577 | — | — | 1 | 5.28 |
| CHEMBL3244501 | — | — | 1 | 5.27 |
| CHEMBL167761 | — | — | 1 | 5.19 |
| CHEMBL1233459 | — | — | 1 | 5.18 |
| CHEMBL167762 | — | — | 1 | 5.16 |
| CHEMBL352923 | — | — | 1 | 5.12 |
| CHEMBL417907 | — | — | 1 | 5.11 |
| CHEMBL48217 | DAPI | — | 1 | 5.08 |
| CHEMBL297403 | — | — | 1 | 5.01 |
| CHEMBL167845 | — | — | 1 | 5.00 |
| CHEMBL3251535 | — | — | 1 | 5.00 |
| CHEMBL352718 | — | — | 1 | 4.98 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3251534 | — | Ki | = | 1390.0 | nM | 5.86 |
| CHEMBL3251191 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL352553 | — | Ki | = | 2020.0 | nM | 5.70 |
| CHEMBL102148 | — | Ki | = | 2090.0 | nM | 5.68 |
| CHEMBL101672 | — | Ki | = | 2240.0 | nM | 5.65 |
| CHEMBL165312 | — | Ki | = | 2450.0 | nM | 5.61 |
| CHEMBL101261 | — | Ki | = | 2730.0 | nM | 5.56 |
| CHEMBL3251186 | — | Ki | = | 3020.0 | nM | 5.52 |
| CHEMBL168077 | — | Ki | = | 3120.0 | nM | 5.51 |
| CHEMBL103649 | — | Ki | = | 3080.0 | nM | 5.51 |
| CHEMBL52393 | — | Ki | = | 3220.0 | nM | 5.49 |
| CHEMBL3251527 | — | Ki | = | 3940.0 | nM | 5.41 |
| CHEMBL167255 | — | Ki | = | 4130.0 | nM | 5.38 |
| CHEMBL99951 | — | Ki | = | 4150.0 | nM | 5.38 |
| CHEMBL279962 | — | Ki | = | 4170.0 | nM | 5.38 |
| CHEMBL297809 | — | Ki | = | 4280.0 | nM | 5.37 |
| CHEMBL563834 | — | Ki | = | 4730.0 | nM | 5.33 |
| CHEMBL3251192 | — | Ki | = | 4880.0 | nM | 5.31 |
| CHEMBL289577 | — | Ki | = | 5220.0 | nM | 5.28 |
| CHEMBL3244501 | — | Ki | = | 5400.0 | nM | 5.27 |
| CHEMBL167761 | — | Ki | = | 6450.0 | nM | 5.19 |
| CHEMBL1233459 | — | Ki | = | 6670.0 | nM | 5.18 |
| CHEMBL167762 | — | Ki | = | 6880.0 | nM | 5.16 |
| CHEMBL352923 | — | Ki | = | 7680.0 | nM | 5.12 |
| CHEMBL417907 | — | Ki | = | 7830.0 | nM | 5.11 |
| CHEMBL48217 | DAPI | Ki | = | 8370.0 | nM | 5.08 |
| CHEMBL297403 | — | Ki | = | 9870.0 | nM | 5.01 |
| CHEMBL167845 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL3251535 | — | Ki | = | 10100.0 | nM | 5.00 |
| CHEMBL352718 | — | Ki | = | 10400.0 | nM | 4.98 |
| CHEMBL3251190 | — | Ki | = | 10500.0 | nM | 4.98 |
| CHEMBL354342 | — | Ki | = | 11300.0 | nM | 4.95 |
| CHEMBL356487 | — | Ki | = | 11600.0 | nM | 4.94 |
| CHEMBL3251187 | — | Ki | = | 11800.0 | nM | 4.93 |
| CHEMBL164947 | — | Ki | = | 14200.0 | nM | 4.85 |
| CHEMBL3251185 | — | Ki | = | 16100.0 | nM | 4.79 |
| CHEMBL164489 | — | Ki | = | 17700.0 | nM | 4.75 |
| CHEMBL3251528 | — | Ki | = | 19600.0 | nM | 4.71 |
| CHEMBL3251188 | — | Ki | = | 22700.0 | nM | 4.64 |
| CHEMBL3251537 | — | Ki | = | 23900.0 | nM | 4.62 |
| CHEMBL1688696 | — | Ki | = | 24600.0 | nM | 4.61 |
| CHEMBL167801 | — | Ki | = | 24400.0 | nM | 4.61 |
| CHEMBL3251538 | — | Ki | = | 27700.0 | nM | 4.56 |
| CHEMBL166236 | — | Ki | = | 28100.0 | nM | 4.55 |
| CHEMBL3251536 | — | Ki | = | 40700.0 | nM | 4.39 |
| CHEMBL168138 | — | Ki | = | 44700.0 | nM | 4.35 |
| CHEMBL3251194 | — | Ki | = | 53800.0 | nM | 4.27 |
| CHEMBL500330 | — | Ki | = | 53500.0 | nM | 4.27 |
| CHEMBL3251533 | — | Ki | = | 56700.0 | nM | 4.25 |
| CHEMBL388768 | — | Ki | = | 66200.0 | nM | 4.18 |