Assay Detail
Binding
CHEMBL3292807
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant MMP-2 pretreated for 30 mins measured 2 to 4 hrs after Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 substrate addition by fluorescence analysis
16
Total Activities
16
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
Dual carbonic anhydrase/matrix metalloproteinase inhibitors incorporating bisphosphonic acid moieties targeting bone tumors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 5.47 | 7.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3291011 | — | — | 1 | 7.43 |
| CHEMBL3291012 | — | — | 1 | 6.96 |
| CHEMBL3291009 | — | — | 1 | 6.85 |
| CHEMBL3291013 | — | — | 1 | 6.72 |
| CHEMBL3291010 | — | — | 1 | 6.64 |
| CHEMBL3291002 | — | — | 1 | 5.32 |
| CHEMBL3291007 | — | — | 1 | 5.31 |
| CHEMBL4303669 | ZOLEDRONIC ACID | 4.0 | 1 | 5.16 |
| CHEMBL3291001 | — | — | 1 | 5.02 |
| CHEMBL3291000 | — | — | 1 | 4.80 |
| CHEMBL3291008 | — | — | 1 | 4.80 |
| CHEMBL3291005 | — | — | 1 | 4.75 |
| CHEMBL3291006 | — | — | 1 | 4.72 |
| CHEMBL3291003 | — | — | 1 | 4.52 |
| CHEMBL180570 | MEDRONIC ACID | 3.0 | 1 | 4.31 |
| CHEMBL3291004 | — | — | 1 | 4.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3291011 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL3291012 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3291009 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3291013 | — | IC50 | = | 192.0 | nM | 6.72 |
| CHEMBL3291010 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL3291002 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL3291007 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL4303669 | ZOLEDRONIC ACID | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL3291001 | — | IC50 | = | 9500.0 | nM | 5.02 |
| CHEMBL3291000 | — | IC50 | = | 15800.0 | nM | 4.80 |
| CHEMBL3291008 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL3291005 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL3291006 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL3291003 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL180570 | MEDRONIC ACID | IC50 | = | 49000.0 | nM | 4.31 |
| CHEMBL3291004 | — | IC50 | = | 52000.0 | nM | 4.28 |