Assay Detail
Binding
CHEMBL4223780
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of TGase 2 in human A375 cells 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
3
Total Activities
3
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 |
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 | 3 | 6.15 | 6.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4227301 | — | — | 1 | 6.40 |
| CHEMBL2203451 | — | — | 1 | 6.10 |
| CHEMBL4228168 | — | — | 1 | 5.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4227301 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL2203451 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL4228168 | — | IC50 | = | 1100.0 | nM | 5.96 |