Assay Detail
Binding
CHEMBL3868402
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Inhibition of recombinant human AMPA-activated MMP8 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 | 7.75 | 10.01 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL440498 | CTS-1027 | 2.0 | 1 | 10.01 |
| CHEMBL3932562 | — | — | 1 | 9.09 |
| CHEMBL3958969 | — | — | 1 | 8.92 |
| CHEMBL3889936 | — | — | 1 | 8.89 |
| CHEMBL3955430 | — | — | 1 | 8.41 |
| CHEMBL3971135 | — | — | 1 | 8.05 |
| CHEMBL3978380 | — | — | 1 | 7.92 |
| CHEMBL3960062 | — | — | 1 | 7.85 |
| CHEMBL3917494 | — | — | 1 | 7.72 |
| CHEMBL3894181 | — | — | 1 | 7.66 |
| CHEMBL3892938 | — | — | 1 | 7.50 |
| CHEMBL3950850 | — | — | 1 | 7.35 |
| CHEMBL3926071 | — | — | 1 | 7.25 |
| CHEMBL3907007 | — | — | 1 | 6.96 |
| CHEMBL3359091 | — | — | 1 | 6.14 |
| CHEMBL3900916 | — | — | 1 | 6.00 |
| CHEMBL3337869 | — | — | 1 | 5.96 |
| CHEMBL3927817 | — | — | 1 | - |
| CHEMBL3907881 | — | — | 1 | - |
| CHEMBL3965628 | — | — | 1 | - |
| CHEMBL3959990 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL440498 | CTS-1027 | IC50 | = | 0.097 | nM | 10.01 |
| CHEMBL3932562 | — | IC50 | = | 0.82 | nM | 9.09 |
| CHEMBL3958969 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3889936 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3955430 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL3971135 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL3978380 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3960062 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3917494 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3894181 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3892938 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3950850 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL3926071 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL3907007 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3359091 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL3900916 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3337869 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3927817 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL3907881 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL3965628 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3959990 | — | IC50 | > | 10000.0 | nM | - |