Assay Detail
Binding
CHEMBL3868403
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Inhibition of recombinant human AMPA-activated MMP9 using Cy3-PLGLK(Cy5Q)AR-NH2 as substrate measured after 40 mins by spectrofluorimetric method
10
Total Activities
10
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 |
Publication
Design, synthesis, and biological activity of novel, potent, and highly selective fused pyrimidine-2-carboxamide-4-one-based matrix metalloproteinase (MMP)-13 zinc-binding inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.09 | 8.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3932562 | — | — | 1 | 8.33 |
| CHEMBL3889936 | — | — | 1 | 8.28 |
| CHEMBL3971135 | — | — | 1 | 7.44 |
| CHEMBL3958969 | — | — | 1 | 7.14 |
| CHEMBL3926071 | — | — | 1 | 5.80 |
| CHEMBL3955430 | — | — | 1 | 5.54 |
| CHEMBL3960062 | — | — | 1 | - |
| CHEMBL3978380 | — | — | 1 | - |
| CHEMBL3337869 | — | — | 1 | - |
| CHEMBL3359091 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3932562 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL3889936 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL3971135 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL3958969 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL3926071 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL3955430 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL3960062 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3978380 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3337869 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3359091 | — | IC50 | > | 10000.0 | nM | - |