Assay Detail
Binding
CHEMBL4223774
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of guinea pig TGase 2 using F-Cad/DMC as substrate preincubated for 30 mins followed by substrate addition measured at 30 secs interval over 900 secs by fluorescence anisotropy assay
15
Total Activities
15
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Nε-Acryloyllysine Piperazides as Irreversible Inhibitors of Transglutaminase 2: Synthesis, Structure-Activity Relationships, and Pharmacokinetic Profiling.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 6.65 | 6.92 |
| Ki | 2 | 5.10 | 5.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4227301 | — | — | 1 | 6.92 |
| CHEMBL4226785 | — | — | 1 | 6.82 |
| CHEMBL4228875 | — | — | 1 | 6.82 |
| CHEMBL4227328 | — | — | 1 | 6.80 |
| CHEMBL4228468 | — | — | 1 | 6.80 |
| CHEMBL4228542 | — | — | 1 | 6.77 |
| CHEMBL4228168 | — | — | 1 | 6.70 |
| CHEMBL4228671 | — | — | 1 | 6.70 |
| CHEMBL2203451 | — | — | 1 | 6.57 |
| CHEMBL4228146 | — | — | 1 | 6.57 |
| CHEMBL4225490 | — | — | 1 | 6.51 |
| CHEMBL4227594 | — | — | 1 | 6.34 |
| CHEMBL4225338 | — | — | 1 | 6.10 |
| CHEMBL4226594 | — | — | 1 | 5.15 |
| CHEMBL4226019 | — | — | 1 | 5.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4227301 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4226785 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4228875 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4227328 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4228468 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4228542 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4228168 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4228671 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL2203451 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4228146 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4225490 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL4227594 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL4225338 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL4226594 | — | Ki | = | 7140.0 | nM | 5.15 |
| CHEMBL4226019 | — | Ki | = | 9150.0 | nM | 5.04 |