Assay Detail
Binding
CHEMBL4223773
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human TGase 2 using R-I-Cad/DMC as substrate preincubated for 5 mins followed by substrate addition measured at 30 secs interval over 900 secs by fluorescence anisotropy assay
12
Total Activities
12
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 |
Target
Protein-glutamine gamma-glutamyltransferase (CHEMBL2730) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 11 | 6.74 | 7.05 |
| Ki | 1 | 5.17 | 5.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4228875 | — | — | 1 | 7.05 |
| CHEMBL4227301 | — | — | 1 | 7.00 |
| CHEMBL4228168 | — | — | 1 | 6.96 |
| CHEMBL4227835 | — | — | 1 | 6.85 |
| CHEMBL4228542 | — | — | 1 | 6.77 |
| CHEMBL4227328 | — | — | 1 | 6.75 |
| CHEMBL4226785 | — | — | 1 | 6.70 |
| CHEMBL4228671 | — | — | 1 | 6.66 |
| CHEMBL2203451 | — | — | 1 | 6.51 |
| CHEMBL4225490 | — | — | 1 | 6.47 |
| CHEMBL4228146 | — | — | 1 | 6.41 |
| CHEMBL4226594 | — | — | 1 | 5.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4228875 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL4227301 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4228168 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4227835 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4228542 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4227328 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4226785 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4228671 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL2203451 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL4225490 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL4228146 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL4226594 | — | Ki | = | 6810.0 | nM | 5.17 |