Assay Detail
Binding
CHEMBL4056973
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Inhibition of human Factor XIa using S-2366 as chromogenic substrate after 60 mins by Lineweaver-Burk plot analysis
29
Total Activities
25
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
Macrocyclic inhibitors of Factor XIa: Discovery of alkyl-substituted macrocyclic amide linkers with improved potency.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 29 | 8.70 | 10.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4060950 | — | — | 1 | 10.52 |
| CHEMBL4097522 | — | — | 1 | 10.22 |
| CHEMBL4083769 | — | — | 1 | 10.15 |
| CHEMBL4063677 | — | — | 1 | 9.89 |
| CHEMBL4103982 | — | — | 1 | 9.85 |
| CHEMBL4071545 | — | — | 1 | 9.80 |
| CHEMBL4089185 | — | — | 1 | 9.74 |
| CHEMBL4063746 | — | — | 2 | 9.48 |
| CHEMBL4101766 | — | — | 1 | 9.41 |
| CHEMBL4062923 | — | — | 1 | 9.33 |
| CHEMBL4070961 | — | — | 1 | 9.16 |
| CHEMBL3676167 | — | — | 1 | 9.00 |
| CHEMBL4076558 | — | — | 1 | 8.96 |
| CHEMBL4077140 | — | — | 1 | 8.70 |
| CHEMBL4090854 | — | — | 1 | 8.49 |
| CHEMBL3699199 | — | — | 2 | 8.23 |
| CHEMBL4059590 | — | — | 2 | 8.19 |
| CHEMBL4080459 | — | — | 1 | 8.15 |
| CHEMBL4078696 | — | — | 1 | 8.00 |
| CHEMBL4086540 | — | — | 1 | 7.92 |
| CHEMBL4105168 | — | — | 1 | 7.80 |
| CHEMBL4095227 | — | — | 1 | 7.68 |
| CHEMBL4098046 | — | — | 1 | 7.68 |
| CHEMBL4067808 | — | — | 2 | 7.46 |
| CHEMBL4065103 | — | — | 1 | 7.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4060950 | — | Ki | = | 0.03 | nM | 10.52 |
| CHEMBL4097522 | — | Ki | = | 0.06 | nM | 10.22 |
| CHEMBL4083769 | — | Ki | = | 0.07 | nM | 10.15 |
| CHEMBL4063677 | — | Ki | = | 0.13 | nM | 9.89 |
| CHEMBL4103982 | — | Ki | = | 0.14 | nM | 9.85 |
| CHEMBL4071545 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL4089185 | — | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL4063746 | — | Ki | = | 0.33 | nM | 9.48 |
| CHEMBL4101766 | — | Ki | = | 0.39 | nM | 9.41 |
| CHEMBL4062923 | — | Ki | = | 0.47 | nM | 9.33 |
| CHEMBL4070961 | — | Ki | = | 0.69 | nM | 9.16 |
| CHEMBL3676167 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL4076558 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL4077140 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL4063746 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL4090854 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL3699199 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL4059590 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL4080459 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL4078696 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL4086540 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL4105168 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL3699199 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL4095227 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL4098046 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL4059590 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL4067808 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL4067808 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL4065103 | — | Ki | = | 44.0 | nM | 7.36 |