Assay Detail
Binding
CHEMBL4835313
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Inhibition of recombinant human activated TAFI incubated for 45 mins using hippuryl-arginine as substrate by spectrophotometry
56
Total Activities
55
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Phosphinanes and Azaphosphinanes as Potent and Selective Inhibitors of Activated Thrombin-Activatable Fibrinolysis Inhibitor (TAFIa).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 55 | 6.62 | 9.00 |
| Ki | 1 | 9.12 | 9.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4878039 | — | — | 2 | 9.12 |
| CHEMBL4868605 | — | — | 1 | 9.00 |
| CHEMBL4846664 | — | — | 1 | 8.70 |
| CHEMBL4858095 | — | — | 1 | 8.30 |
| CHEMBL4861532 | — | — | 1 | 8.30 |
| CHEMBL4853133 | — | — | 1 | 8.15 |
| CHEMBL4852722 | — | — | 1 | 8.10 |
| CHEMBL4858909 | — | — | 1 | 8.10 |
| CHEMBL4875723 | — | — | 1 | 8.05 |
| CHEMBL4852607 | — | — | 1 | 8.05 |
| CHEMBL4861840 | — | — | 1 | 8.00 |
| CHEMBL4854445 | — | — | 1 | 7.96 |
| CHEMBL4866725 | — | — | 1 | 7.77 |
| CHEMBL4868496 | — | — | 1 | 7.51 |
| CHEMBL4858525 | — | — | 1 | 7.06 |
| CHEMBL4861694 | — | — | 1 | 7.00 |
| CHEMBL4856598 | — | — | 1 | 7.00 |
| CHEMBL4846016 | — | — | 1 | 6.90 |
| CHEMBL4855391 | — | — | 1 | 6.79 |
| CHEMBL4847492 | — | — | 1 | 6.74 |
| CHEMBL4869435 | — | — | 1 | 6.70 |
| CHEMBL4862631 | — | — | 1 | 6.70 |
| CHEMBL4857164 | — | — | 1 | 6.70 |
| CHEMBL4861443 | — | — | 1 | 6.30 |
| CHEMBL4855720 | — | — | 1 | 6.30 |
| CHEMBL4848798 | — | — | 1 | 6.29 |
| CHEMBL4864051 | — | — | 1 | 6.12 |
| CHEMBL4858857 | — | — | 1 | 5.96 |
| CHEMBL4851707 | — | — | 1 | 5.96 |
| CHEMBL4879366 | — | — | 1 | 5.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4878039 | — | Ki | = | 0.75 | nM | 9.12 |
| CHEMBL4868605 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4846664 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4861532 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4858095 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4878039 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4853133 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4858909 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4852722 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4852607 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4875723 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4861840 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4854445 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4866725 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4868496 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4858525 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL4861694 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL4856598 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4846016 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL4855391 | — | IC50 | = | 161.0 | nM | 6.79 |
| CHEMBL4847492 | — | IC50 | = | 183.0 | nM | 6.74 |
| CHEMBL4857164 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4869435 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4862631 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4855720 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4861443 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4848798 | — | IC50 | = | 515.0 | nM | 6.29 |
| CHEMBL4864051 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL4851707 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4858857 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4879366 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4861262 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4877745 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4851494 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL4850188 | — | IC50 | = | 3104.0 | nM | 5.51 |
| CHEMBL4860221 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL4850416 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL4868220 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL4872299 | — | IC50 | = | 8700.0 | nM | 5.06 |
| CHEMBL4865984 | — | IC50 | = | 9300.0 | nM | 5.03 |
| CHEMBL4864497 | — | IC50 | = | 10700.0 | nM | 4.97 |
| CHEMBL4878365 | — | IC50 | = | 11700.0 | nM | 4.93 |
| CHEMBL4871500 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL4856209 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL4877082 | — | IC50 | = | 20100.0 | nM | 4.70 |
| CHEMBL4857886 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4848329 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4864625 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4867193 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4870502 | — | IC50 | > | 30000.0 | nM | - |