Assay Detail
Binding
CHEMBL3706209
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition Assay: The prepared substances were tested for TAFIa inhibition using the Actichrome plasma TAFI activity kit from American Diagnostica (Pr. No. 874). This entailed adding 29 μl of assay buffer (20 mM Hepes, 150 mM NaCl, pH 7.4) and 10 μl of TAFIa (American Diagnostica Pr. No. 874TAFIA; 2.5/ml) to 1 μl of 5 mM DMSO solution of the substance and incubating in a 96 half-well microtiter plate at room temperature for 15 minutes. The enzymic reaction was started by adding 10 μl of TAFIa developer (prediluted 1:2 with water). The time course of the reaction was followed at 420 nm in a microtiter plate reader (SpectraMax plus 384; Molecular Devices) for 15 minutes.
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Plasma |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Imidazole derivatives used as TAFIa inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 7.10 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3694281 | — | — | 1 | 8.52 |
| CHEMBL3694275 | — | — | 1 | 7.96 |
| CHEMBL3694272 | — | — | 1 | 7.92 |
| CHEMBL3694273 | — | — | 1 | 7.92 |
| CHEMBL3694271 | — | — | 1 | 7.82 |
| CHEMBL3694267 | — | — | 1 | 7.80 |
| CHEMBL3694276 | — | — | 1 | 7.68 |
| CHEMBL3694270 | — | — | 1 | 7.64 |
| CHEMBL3694266 | — | — | 1 | 7.52 |
| CHEMBL3694274 | — | — | 1 | 7.42 |
| CHEMBL3694282 | — | — | 1 | 7.31 |
| CHEMBL3694269 | — | — | 1 | 6.36 |
| CHEMBL3694280 | — | — | 1 | 6.06 |
| CHEMBL3694278 | — | — | 1 | 5.96 |
| CHEMBL3694268 | — | — | 1 | 5.95 |
| CHEMBL3694279 | — | — | 1 | 5.84 |
| CHEMBL3694277 | — | — | 1 | 4.98 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3694281 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3694275 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3694272 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3694273 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3694271 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3694267 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3694276 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3694270 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3694266 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3694274 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL3694282 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL3694269 | — | IC50 | = | 439.0 | nM | 6.36 |
| CHEMBL3694280 | — | IC50 | = | 870.0 | nM | 6.06 |
| CHEMBL3694278 | — | IC50 | = | 1110.0 | nM | 5.96 |
| CHEMBL3694268 | — | IC50 | = | 1130.0 | nM | 5.95 |
| CHEMBL3694279 | — | IC50 | = | 1440.0 | nM | 5.84 |
| CHEMBL3694277 | — | IC50 | = | 10510.0 | nM | 4.98 |