Assay Detail
Binding
CHEMBL3868404
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human AMPA-activated MMP10 using Cy3-PLGLK(Cy5Q)AR-NH2 as substrate measured after 40 mins by spectrofluorimetric method
21
Total Activities
21
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 | 21 | 7.25 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3932562 | — | — | 1 | 9.52 |
| CHEMBL3889936 | — | — | 1 | 9.46 |
| CHEMBL440498 | CTS-1027 | 2.0 | 1 | 9.27 |
| CHEMBL3971135 | — | — | 1 | 8.62 |
| CHEMBL3958969 | — | — | 1 | 8.59 |
| CHEMBL3955430 | — | — | 1 | 8.21 |
| CHEMBL3900916 | — | — | 1 | 7.47 |
| CHEMBL3907007 | — | — | 1 | 7.19 |
| CHEMBL3978380 | — | — | 1 | 6.82 |
| CHEMBL3359091 | — | — | 1 | 6.80 |
| CHEMBL3894181 | — | — | 1 | 6.66 |
| CHEMBL3960062 | — | — | 1 | 6.62 |
| CHEMBL3950850 | — | — | 1 | 6.34 |
| CHEMBL3892938 | — | — | 1 | 6.19 |
| CHEMBL3965628 | — | — | 1 | 6.09 |
| CHEMBL3926071 | — | — | 1 | 6.03 |
| CHEMBL3337869 | — | — | 1 | 5.47 |
| CHEMBL3959990 | — | — | 1 | 5.20 |
| CHEMBL3927817 | — | — | 1 | - |
| CHEMBL3907881 | — | — | 1 | - |
| CHEMBL3917494 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3932562 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3889936 | — | IC50 | = | 0.35 | nM | 9.46 |
| CHEMBL440498 | CTS-1027 | IC50 | = | 0.54 | nM | 9.27 |
| CHEMBL3971135 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL3958969 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3955430 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL3900916 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL3907007 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL3978380 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3359091 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3894181 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL3960062 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL3950850 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL3892938 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL3965628 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL3926071 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL3337869 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL3959990 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL3927817 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL3907881 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL3917494 | — | IC50 | < | 10.0 | nM | - |