Assay Detail
Binding
CHEMBL4223792
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Reversible inhibition of human TGase 2 using Z-Glu(HMC)-Gly-OH as substrate measured at 20 secs interval over 900 secs by fluorimetric assay
12
Total Activities
12
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 |
|---|---|---|---|
| Ki | 12 | 5.17 | 5.65 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4227301 | — | — | 1 | 5.65 |
| CHEMBL4227835 | — | — | 1 | 5.54 |
| CHEMBL4228542 | — | — | 1 | 5.46 |
| CHEMBL4227328 | — | — | 1 | 5.35 |
| CHEMBL4228671 | — | — | 1 | 5.25 |
| CHEMBL2203451 | — | — | 1 | 5.24 |
| CHEMBL4228168 | — | — | 1 | 5.20 |
| CHEMBL4228146 | — | — | 1 | 5.13 |
| CHEMBL4226785 | — | — | 1 | 5.11 |
| CHEMBL4225490 | — | — | 1 | 5.08 |
| CHEMBL4229246 | — | — | 1 | 4.82 |
| CHEMBL4227629 | — | — | 1 | 4.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4227301 | — | Ki | = | 2260.0 | nM | 5.65 |
| CHEMBL4227835 | — | Ki | = | 2920.0 | nM | 5.54 |
| CHEMBL4228542 | — | Ki | = | 3500.0 | nM | 5.46 |
| CHEMBL4227328 | — | Ki | = | 4430.0 | nM | 5.35 |
| CHEMBL4228671 | — | Ki | = | 5650.0 | nM | 5.25 |
| CHEMBL2203451 | — | Ki | = | 5730.0 | nM | 5.24 |
| CHEMBL4228168 | — | Ki | = | 6280.0 | nM | 5.20 |
| CHEMBL4228146 | — | Ki | = | 7320.0 | nM | 5.13 |
| CHEMBL4226785 | — | Ki | = | 7760.0 | nM | 5.11 |
| CHEMBL4225490 | — | Ki | = | 8420.0 | nM | 5.08 |
| CHEMBL4229246 | — | Ki | = | 15000.0 | nM | 4.82 |
| CHEMBL4227629 | — | Ki | = | 64300.0 | nM | 4.19 |