Assay Detail
Binding
CHEMBL2393850
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of rat VAP-1 expressed in CHO cells using [14C]-benzylamine as substrate preincubated for 30 mins prior to substrate addition measured after 1 hr by scintillation spectrometric analysis
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Amine oxidase [copper-containing] 3 (CHEMBL4592) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Novel 1H-imidazol-2-amine derivatives as potent and orally active vascular adhesion protein-1 (VAP-1) inhibitors for diabetic macular edema treatment.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 5.73 | 8.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2392121 | — | — | 1 | 8.29 |
| CHEMBL2326864 | — | — | 1 | 7.85 |
| CHEMBL2390968 | — | — | 1 | 7.75 |
| CHEMBL2392120 | — | — | 1 | 6.82 |
| CHEMBL2392118 | — | — | 1 | 6.38 |
| CHEMBL305513 | — | — | 1 | 6.00 |
| CHEMBL2392117 | — | — | 1 | 6.00 |
| CHEMBL2392119 | — | — | 1 | 5.32 |
| CHEMBL2392116 | — | — | 1 | 5.03 |
| CHEMBL1649757 | — | — | 1 | 4.36 |
| CHEMBL2392114 | — | — | 1 | 4.20 |
| CHEMBL14047 | PHENYLGUANIDINE | — | 1 | 4.11 |
| CHEMBL1232570 | — | — | 1 | 4.10 |
| CHEMBL2392115 | — | — | 1 | 4.05 |
| CHEMBL1204384 | — | — | 1 | - |
| CHEMBL543123 | — | — | 1 | - |
| CHEMBL187951 | — | — | 1 | - |
| CHEMBL329785 | — | — | 1 | - |
| CHEMBL306226 | BENZIMIDAZOLE | -1.0 | 1 | - |
| CHEMBL3143911 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2392121 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL2326864 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2390968 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL2392120 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL2392118 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL305513 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL2392117 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL2392119 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL2392116 | — | IC50 | = | 9300.0 | nM | 5.03 |
| CHEMBL1649757 | — | IC50 | = | 44000.0 | nM | 4.36 |
| CHEMBL2392114 | — | IC50 | = | 63000.0 | nM | 4.20 |
| CHEMBL14047 | PHENYLGUANIDINE | IC50 | = | 78000.0 | nM | 4.11 |
| CHEMBL1232570 | — | IC50 | = | 80000.0 | nM | 4.10 |
| CHEMBL2392115 | — | IC50 | = | 90000.0 | nM | 4.05 |
| CHEMBL1204384 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL543123 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL187951 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL329785 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL306226 | BENZIMIDAZOLE | IC50 | > | 100000.0 | nM | - |
| CHEMBL3143911 | — | IC50 | > | 100000.0 | nM | - |