Assay Detail
Binding
CHEMBL2168947
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Inhibition of human activated TAFI using Hip-Arg as substrate incubated for 10 mins prior to substrate addition measured after 30 mins by spectrophotometric analysis
14
Total Activities
14
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 |
Publication
Design and characterization of a selenium-containing inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa), a zinc-containing metalloprotease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 6.10 | 8.26 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2164463 | — | — | 1 | 8.26 |
| CHEMBL2164453 | — | — | 1 | 7.47 |
| CHEMBL2164462 | — | — | 1 | 6.70 |
| CHEMBL2164459 | — | — | 1 | 6.12 |
| CHEMBL2164458 | — | — | 1 | 5.85 |
| CHEMBL2164460 | — | — | 1 | 5.80 |
| CHEMBL2164461 | — | — | 1 | 5.70 |
| CHEMBL2164450 | — | — | 1 | 5.48 |
| CHEMBL2164456 | — | — | 1 | 5.42 |
| CHEMBL2164455 | — | — | 1 | 4.21 |
| CHEMBL2164451 | — | — | 1 | - |
| CHEMBL2164452 | — | — | 1 | - |
| CHEMBL2164457 | — | — | 1 | - |
| CHEMBL2164454 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2164463 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL2164453 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL2164462 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL2164459 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL2164458 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL2164460 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL2164461 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL2164450 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL2164456 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL2164455 | — | IC50 | = | 62000.0 | nM | 4.21 |
| CHEMBL2164451 | — | IC50 | > | 3800000.0 | nM | - |
| CHEMBL2164452 | — | IC50 | = | 180000.0 | nM | - |
| CHEMBL2164457 | — | IC50 | > | 3800000.0 | nM | - |
| CHEMBL2164454 | — | IC50 | = | 310000.0 | nM | - |