Assay Detail
Binding
CHEMBL3705624
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition Assay: Inhibition of human FIIa was determined by the method described in [0092]-[0098] using human alpha-thrombin from Enzyme Research Laboratories at 0.1 NIH U/mL and Mes-d-Cha-Gly-Arg-pNA (Pefachrome tPA) at 2 mM, 1 mM, and 0.5 mM as substrate; results are reported as Ki values (nanomolar).
23
Total Activities
21
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 |
Target
Transcription initiation factor IIA subunit 1 (CHEMBL4832) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Trypsin-like serine protease inhibitors, and their preparation and use
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 5.36 | 6.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3660186 | — | — | 1 | 6.62 |
| CHEMBL3660173 | — | — | 1 | 6.10 |
| CHEMBL3660191 | — | — | 1 | 5.92 |
| CHEMBL3660187 | — | — | 1 | 5.77 |
| CHEMBL3660189 | — | — | 1 | 5.44 |
| CHEMBL3660176 | — | — | 1 | 5.42 |
| CHEMBL3660179 | — | — | 1 | 5.41 |
| CHEMBL3660177 | — | — | 1 | 5.38 |
| CHEMBL3660171 | — | — | 1 | 5.36 |
| CHEMBL3660178 | — | — | 1 | 5.35 |
| CHEMBL3660192 | — | — | 1 | 5.33 |
| CHEMBL3660181 | — | — | 1 | 5.32 |
| CHEMBL3660184 | — | — | 2 | 5.31 |
| CHEMBL3660182 | — | — | 1 | 5.26 |
| CHEMBL3660175 | — | — | 1 | 5.25 |
| CHEMBL3660172 | — | — | 1 | 5.10 |
| CHEMBL3660174 | — | — | 1 | 5.07 |
| CHEMBL3660188 | — | — | 1 | 5.05 |
| CHEMBL3660180 | — | — | 1 | 4.89 |
| CHEMBL3660183 | — | — | 1 | 4.89 |
| CHEMBL3660185 | — | — | 2 | 4.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3660186 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL3660173 | — | Ki | = | 800.0 | nM | 6.10 |
| CHEMBL3660191 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL3660187 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL3660189 | — | Ki | = | 3600.0 | nM | 5.44 |
| CHEMBL3660176 | — | Ki | = | 3800.0 | nM | 5.42 |
| CHEMBL3660179 | — | Ki | = | 3900.0 | nM | 5.41 |
| CHEMBL3660177 | — | Ki | = | 4200.0 | nM | 5.38 |
| CHEMBL3660171 | — | Ki | = | 4400.0 | nM | 5.36 |
| CHEMBL3660178 | — | Ki | = | 4500.0 | nM | 5.35 |
| CHEMBL3660192 | — | Ki | = | 4700.0 | nM | 5.33 |
| CHEMBL3660181 | — | Ki | = | 4800.0 | nM | 5.32 |
| CHEMBL3660184 | — | Ki | = | 4900.0 | nM | 5.31 |
| CHEMBL3660184 | — | Ki | = | 4900.0 | nM | 5.31 |
| CHEMBL3660182 | — | Ki | = | 5500.0 | nM | 5.26 |
| CHEMBL3660175 | — | Ki | = | 5600.0 | nM | 5.25 |
| CHEMBL3660172 | — | Ki | = | 8000.0 | nM | 5.10 |
| CHEMBL3660174 | — | Ki | = | 8500.0 | nM | 5.07 |
| CHEMBL3660188 | — | Ki | = | 9000.0 | nM | 5.05 |
| CHEMBL3660185 | — | Ki | = | 13000.0 | nM | 4.89 |
| CHEMBL3660183 | — | Ki | = | 13000.0 | nM | 4.89 |
| CHEMBL3660185 | — | Ki | = | 13000.0 | nM | 4.89 |
| CHEMBL3660180 | — | Ki | = | 13000.0 | nM | 4.89 |