Assay Detail
Binding
CHEMBL3868397
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Inhibition of recombinant human AMPA-activated MMP13 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 | 9.66 | 11.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL440498 | CTS-1027 | 2.0 | 1 | 11.00 |
| CHEMBL3889936 | — | — | 1 | 10.29 |
| CHEMBL3958969 | — | — | 1 | 10.28 |
| CHEMBL3978380 | — | — | 1 | 10.15 |
| CHEMBL3965628 | — | — | 1 | 10.11 |
| CHEMBL3955430 | — | — | 1 | 9.96 |
| CHEMBL3959990 | — | — | 1 | 9.92 |
| CHEMBL3971135 | — | — | 1 | 9.77 |
| CHEMBL3907881 | — | — | 1 | 9.72 |
| CHEMBL3926071 | — | — | 1 | 9.64 |
| CHEMBL3960062 | — | — | 1 | 9.62 |
| CHEMBL3917494 | — | — | 1 | 9.59 |
| CHEMBL3907007 | — | — | 1 | 9.52 |
| CHEMBL3927817 | — | — | 1 | 9.44 |
| CHEMBL3900916 | — | — | 1 | 9.42 |
| CHEMBL3894181 | — | — | 1 | 9.23 |
| CHEMBL3892938 | — | — | 1 | 8.82 |
| CHEMBL3950850 | — | — | 1 | 8.77 |
| CHEMBL3337869 | — | — | 1 | 8.25 |
| CHEMBL3359091 | — | — | 1 | - |
| CHEMBL3932562 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL440498 | CTS-1027 | IC50 | = | 0.01 | nM | 11.00 |
| CHEMBL3889936 | — | IC50 | = | 0.051 | nM | 10.29 |
| CHEMBL3958969 | — | IC50 | = | 0.052 | nM | 10.28 |
| CHEMBL3978380 | — | IC50 | = | 0.071 | nM | 10.15 |
| CHEMBL3965628 | — | IC50 | = | 0.078 | nM | 10.11 |
| CHEMBL3955430 | — | IC50 | = | 0.11 | nM | 9.96 |
| CHEMBL3959990 | — | IC50 | = | 0.12 | nM | 9.92 |
| CHEMBL3971135 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL3907881 | — | IC50 | = | 0.19 | nM | 9.72 |
| CHEMBL3926071 | — | IC50 | = | 0.23 | nM | 9.64 |
| CHEMBL3960062 | — | IC50 | = | 0.24 | nM | 9.62 |
| CHEMBL3917494 | — | IC50 | = | 0.26 | nM | 9.59 |
| CHEMBL3907007 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3927817 | — | IC50 | = | 0.36 | nM | 9.44 |
| CHEMBL3900916 | — | IC50 | = | 0.38 | nM | 9.42 |
| CHEMBL3894181 | — | IC50 | = | 0.59 | nM | 9.23 |
| CHEMBL3892938 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3950850 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3337869 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL3359091 | — | IC50 | = | 0.0039 | nM | - |
| CHEMBL3932562 | — | IC50 | = | 0.0032 | nM | - |