Assay Detail
Binding
CHEMBL2393976
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Inhibition of human 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 | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
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 | 5.56 | 7.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2392121 | — | — | 1 | 7.72 |
| CHEMBL2326864 | — | — | 1 | 6.64 |
| CHEMBL2390968 | — | — | 1 | 5.66 |
| CHEMBL305513 | — | — | 1 | 5.39 |
| CHEMBL2392120 | — | — | 1 | 4.89 |
| CHEMBL2392118 | — | — | 1 | 4.50 |
| CHEMBL2392114 | — | — | 1 | 4.13 |
| CHEMBL2392119 | — | — | 1 | - |
| CHEMBL1649757 | — | — | 1 | - |
| CHEMBL2392117 | — | — | 1 | - |
| CHEMBL2392116 | — | — | 1 | - |
| CHEMBL1232570 | — | — | 1 | - |
| CHEMBL2392115 | — | — | 1 | - |
| CHEMBL3143911 | — | — | 1 | - |
| CHEMBL306226 | BENZIMIDAZOLE | -1.0 | 1 | - |
| CHEMBL329785 | — | — | 1 | - |
| CHEMBL543123 | — | — | 1 | - |
| CHEMBL1204384 | — | — | 1 | - |
| CHEMBL14047 | PHENYLGUANIDINE | — | 1 | - |
| CHEMBL187951 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2392121 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL2326864 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL2390968 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL305513 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL2392120 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL2392118 | — | IC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL2392114 | — | IC50 | = | 74000.0 | nM | 4.13 |
| CHEMBL2392119 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1649757 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2392117 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2392116 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1232570 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2392115 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3143911 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL306226 | BENZIMIDAZOLE | IC50 | > | 100000.0 | nM | - |
| CHEMBL329785 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL543123 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1204384 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL14047 | PHENYLGUANIDINE | IC50 | > | 100000.0 | nM | - |
| CHEMBL187951 | — | IC50 | > | 100000.0 | nM | - |