Assay Detail
Binding
CHEMBL3240043
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Inhibition of human recombinant carbonic anhydrase 1 preincubated for 15 mins by stopped flow CO2 hydration method
22
Total Activities
22
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
Arylamino bisphosphonates: potent and selective inhibitors of the tumor-associated carbonic anhydrase XII.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 5.50 | 7.32 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL20 | ACETAZOLAMIDE | 4.0 | 1 | 7.32 |
| CHEMBL450938 | (3-NITROPHENYLAMINO)METHYLENEDIPHOSPHONIC ACID | — | 1 | 6.09 |
| CHEMBL2440438 | — | — | 1 | 5.34 |
| CHEMBL2440434 | — | — | 1 | 5.26 |
| CHEMBL2440439 | (P-TOLYLAMINO)METHYLENEDIPHOSPHONIC ACID | — | 1 | 5.23 |
| CHEMBL2440435 | — | — | 1 | 5.23 |
| CHEMBL2440440 | — | — | 1 | 5.22 |
| CHEMBL191613 | 2,4-DICHLOROPHENYLAMINOMETHYLENEBISPHOSPHONIC ACID | — | 1 | 5.15 |
| CHEMBL2440578 | — | — | 1 | 5.10 |
| CHEMBL370662 | — | — | 1 | 5.08 |
| CHEMBL4303669 | ZOLEDRONIC ACID | 4.0 | 1 | - |
| CHEMBL2440580 | (PHENYLAMINO)METHYLENEDIPHOSPHONIC ACID | — | 1 | - |
| CHEMBL2440581 | — | — | 1 | - |
| CHEMBL2440436 | — | — | 1 | - |
| CHEMBL2440441 | — | — | 1 | - |
| CHEMBL2440433 | 3,4-DICHLOROPHENYLAMINOMETHYLENEBISPHOSPHONIC ACID | — | 1 | - |
| CHEMBL293479 | — | — | 1 | - |
| CHEMBL55371 | — | — | 1 | - |
| CHEMBL2440430 | — | — | 1 | - |
| CHEMBL2440431 | — | — | 1 | - |
| CHEMBL2440432 | — | — | 1 | - |
| CHEMBL2440429 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL20 | ACETAZOLAMIDE | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL450938 | (3-NITROPHENYLAMINO)METHYLENEDIPHOSPHONIC ACID | IC50 | = | 814.0 | nM | 6.09 |
| CHEMBL2440438 | — | IC50 | = | 4570.0 | nM | 5.34 |
| CHEMBL2440434 | — | IC50 | = | 5535.0 | nM | 5.26 |
| CHEMBL2440439 | (P-TOLYLAMINO)METHYLENEDIPHOSPHONIC ACID | IC50 | = | 5932.0 | nM | 5.23 |
| CHEMBL2440435 | — | IC50 | = | 5830.0 | nM | 5.23 |
| CHEMBL2440440 | — | IC50 | = | 6082.0 | nM | 5.22 |
| CHEMBL191613 | 2,4-DICHLOROPHENYLAMINOMETHYLENEBISPHOSPHONIC ACID | IC50 | = | 7136.0 | nM | 5.15 |
| CHEMBL2440578 | — | IC50 | = | 7977.0 | nM | 5.10 |
| CHEMBL370662 | — | IC50 | = | 8285.0 | nM | 5.08 |
| CHEMBL4303669 | ZOLEDRONIC ACID | IC50 | > | 10000.0 | nM | - |
| CHEMBL2440580 | (PHENYLAMINO)METHYLENEDIPHOSPHONIC ACID | IC50 | > | 10000.0 | nM | - |
| CHEMBL2440581 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2440436 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2440441 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2440433 | 3,4-DICHLOROPHENYLAMINOMETHYLENEBISPHOSPHONIC ACID | IC50 | > | 10000.0 | nM | - |
| CHEMBL293479 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL55371 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2440430 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2440431 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2440432 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2440429 | — | IC50 | > | 10000.0 | nM | - |