Assay Detail
Binding
CHEMBL5731448
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Biacore Assay: The test compounds were dissolved in 1% acetic acid and further complemented with an equal volume of DMSO. The resulting stock solutions were serially diluted in 0.5% acetic acid/50% DMSO. 1 μL aliquots of these solutions were placed into 384 well microplates (Greiner, black, transparent bottom), followed by 30 μL of diluted human citrated plasma (platelet-poor, final concentration: 5%; supplemented with fibrinogen, final concentration: 3 μM; dilution buffer: 20 mM HEPES, 150 mM NaCl, 0.01% Brij (pH 7)). The reactions were started by addition of 20 L of CaCl2 (final concentration: 10 mM), and tPA (tissue plasminogen activator, final concentration: 0.2 nM) in dilution buffer, followed by an additional volume of 20 μL dilution buffer for improved mixing. The reactions were incubated at 37° C. Clot formation and degradation was monitored spectrophotometrically by kinetic optical density measurements at 405 nm.
315
Total Activities
100
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
(Aza)pyridopyrazolopyrimidinones and indazolopyrimidinones and their use
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 105 | 7.56 | 8.00 |
| kon | 105 | - | - |
| k_off | 105 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5897890 | — | — | 6 | 8.00 |
| CHEMBL4536269 | — | — | 3 | 7.96 |
| CHEMBL4578240 | — | — | 3 | 7.96 |
| CHEMBL6062318 | — | — | 3 | 7.89 |
| CHEMBL5928912 | — | — | 3 | 7.89 |
| CHEMBL6011509 | — | — | 3 | 7.89 |
| CHEMBL5980444 | — | — | 3 | 7.89 |
| CHEMBL5933220 | — | — | 6 | 7.89 |
| CHEMBL5872096 | — | — | 3 | 7.85 |
| CHEMBL5896722 | — | — | 6 | 7.85 |
| CHEMBL5774413 | — | — | 3 | 7.85 |
| CHEMBL6031955 | — | — | 3 | 7.85 |
| CHEMBL5977403 | — | — | 3 | 7.85 |
| CHEMBL5901899 | — | — | 3 | 7.82 |
| CHEMBL5976620 | — | — | 3 | 7.82 |
| CHEMBL5791398 | — | — | 3 | 7.82 |
| CHEMBL5803225 | — | — | 3 | 7.82 |
| CHEMBL5315598 | — | — | 6 | 7.82 |
| CHEMBL5838352 | — | — | 3 | 7.82 |
| CHEMBL5957884 | — | — | 3 | 7.82 |
| CHEMBL6040865 | — | — | 3 | 7.82 |
| CHEMBL5754051 | — | — | 3 | 7.82 |
| CHEMBL5818228 | — | — | 3 | 7.80 |
| CHEMBL6020010 | — | — | 3 | 7.80 |
| CHEMBL5756524 | — | — | 3 | 7.80 |
| CHEMBL5908431 | — | — | 3 | 7.77 |
| CHEMBL5765780 | — | — | 3 | 7.75 |
| CHEMBL5853281 | — | — | 3 | 7.75 |
| CHEMBL5998204 | — | — | 3 | 7.75 |
| CHEMBL5826177 | — | — | 3 | 7.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5897890 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4578240 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4536269 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5980444 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL6062318 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL6011509 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5933220 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5928912 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5977403 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL6031955 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5774413 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5872096 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5896722 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5957884 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5838352 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5754051 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5791398 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5901899 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5976620 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5803225 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL6040865 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5315598 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5756524 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5818228 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL6020010 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5908431 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5998204 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5933220 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5765780 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5853281 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5826177 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5774198 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL5987508 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL6002758 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5966749 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5897890 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5989259 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL5928184 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL5777260 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL5745904 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL5886142 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL5787752 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL5753283 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL5976342 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL5822208 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL5930231 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5766019 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5989533 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5778636 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL5847667 | — | IC50 | = | 26.0 | nM | 7.58 |