Assay Detail
Binding
CHEMBL3292802
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Inhibition of human recombinant carbonic anhydrase 2 pretreated for 15 mins by stopped flow CO2 hydrase assay
17
Total Activities
17
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 | 17 | 6.33 | 7.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL20 | ACETAZOLAMIDE | 4.0 | 1 | 7.64 |
| CHEMBL4303669 | ZOLEDRONIC ACID | 4.0 | 1 | 7.21 |
| CHEMBL3291012 | — | — | 1 | 7.16 |
| CHEMBL3291013 | — | — | 1 | 7.15 |
| CHEMBL3291010 | — | — | 1 | 6.30 |
| CHEMBL3291009 | — | — | 1 | 5.85 |
| CHEMBL3291007 | — | — | 1 | 5.74 |
| CHEMBL3291011 | — | — | 1 | 5.58 |
| CHEMBL3291008 | — | — | 1 | 5.42 |
| CHEMBL3291001 | — | — | 1 | 5.21 |
| CHEMBL3291005 | — | — | 1 | - |
| CHEMBL3291006 | — | — | 1 | - |
| CHEMBL3291004 | — | — | 1 | - |
| CHEMBL3291003 | — | — | 1 | - |
| CHEMBL3291002 | — | — | 1 | - |
| CHEMBL3291000 | — | — | 1 | - |
| CHEMBL180570 | MEDRONIC ACID | 3.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL20 | ACETAZOLAMIDE | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4303669 | ZOLEDRONIC ACID | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL3291012 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL3291013 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL3291010 | — | IC50 | = | 504.0 | nM | 6.30 |
| CHEMBL3291009 | — | IC50 | = | 1410.0 | nM | 5.85 |
| CHEMBL3291007 | — | IC50 | = | 1830.0 | nM | 5.74 |
| CHEMBL3291011 | — | IC50 | = | 2660.0 | nM | 5.58 |
| CHEMBL3291008 | — | IC50 | = | 3820.0 | nM | 5.42 |
| CHEMBL3291001 | — | IC50 | = | 6160.0 | nM | 5.21 |
| CHEMBL3291005 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3291006 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3291004 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3291003 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3291002 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3291000 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL180570 | MEDRONIC ACID | IC50 | = | 1250000.0 | nM | - |