Assay Detail
Binding
CHEMBL862671
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Inhibitory activity against human recombinant mitochondrial isozyme CA VB
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Carbonic anhydrase 5B, mitochondrial (CHEMBL3969) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Carbonic anhydrase inhibitors. The mitochondrial isozyme VB as a new target for sulfonamide and sulfamate inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 34 | 6.30 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL26 | SULPIRIDE | 3.0 | 1 | 7.75 |
| CHEMBL18 | ETHOXZOLAMIDE | 4.0 | 1 | 7.72 |
| CHEMBL17 | DICHLORPHENAMIDE | 4.0 | 1 | 7.68 |
| CHEMBL77517 | INDISULAM | 2.0 | 1 | 7.64 |
| CHEMBL266026 | — | — | 1 | 7.62 |
| CHEMBL220492 | TOPIRAMATE | 4.0 | 1 | 7.52 |
| CHEMBL220491 | BRINZOLAMIDE | 4.0 | 1 | 7.52 |
| CHEMBL360356 | — | — | 1 | 7.52 |
| CHEMBL268439 | — | — | 1 | 7.52 |
| CHEMBL218490 | DORZOLAMIDE | 4.0 | 1 | 7.48 |
| CHEMBL73962 | BENZOLAMIDE | — | 1 | 7.47 |
| CHEMBL6685 | — | — | 1 | 7.39 |
| CHEMBL7146 | — | — | 1 | 7.38 |
| CHEMBL20 | ACETAZOLAMIDE | 4.0 | 1 | 7.27 |
| CHEMBL19 | METHAZOLAMIDE | 4.0 | 1 | 7.21 |
| CHEMBL414 | CARZENIDE | 2.0 | 1 | 5.81 |
| CHEMBL6753 | — | — | 1 | 5.68 |
| CHEMBL265674 | — | — | 1 | 5.67 |
| CHEMBL574 | P-TOLUENESULFONAMIDE | 3.0 | 1 | 5.61 |
| CHEMBL268177 | — | — | 1 | 5.48 |
| CHEMBL176495 | — | — | 1 | 5.47 |
| CHEMBL7204 | — | — | 1 | 5.46 |
| CHEMBL6724 | — | — | 1 | 5.45 |
| CHEMBL21 | SULFANILAMIDE | 4.0 | 1 | 5.44 |
| CHEMBL6853 | — | — | 1 | 5.38 |
| CHEMBL7092 | — | — | 1 | 5.37 |
| CHEMBL266240 | — | — | 1 | 5.21 |
| CHEMBL418 | 2,4-DISULFAMYLTRIFLUOROMETHYLANILINE | — | 1 | 5.18 |
| CHEMBL6784 | — | — | 1 | 5.16 |
| CHEMBL6919 | — | — | 1 | 5.13 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL26 | SULPIRIDE | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL18 | ETHOXZOLAMIDE | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL17 | DICHLORPHENAMIDE | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL77517 | INDISULAM | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL266026 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL220492 | TOPIRAMATE | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL220491 | BRINZOLAMIDE | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL360356 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL268439 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL218490 | DORZOLAMIDE | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL73962 | BENZOLAMIDE | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL6685 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL7146 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL20 | ACETAZOLAMIDE | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL19 | METHAZOLAMIDE | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL414 | CARZENIDE | Ki | = | 1560.0 | nM | 5.81 |
| CHEMBL6753 | — | Ki | = | 2075.0 | nM | 5.68 |
| CHEMBL265674 | — | Ki | = | 2150.0 | nM | 5.67 |
| CHEMBL574 | P-TOLUENESULFONAMIDE | Ki | = | 2430.0 | nM | 5.61 |
| CHEMBL268177 | — | Ki | = | 3300.0 | nM | 5.48 |
| CHEMBL176495 | — | Ki | = | 3400.0 | nM | 5.47 |
| CHEMBL7204 | — | Ki | = | 3500.0 | nM | 5.46 |
| CHEMBL6724 | — | Ki | = | 3540.0 | nM | 5.45 |
| CHEMBL21 | SULFANILAMIDE | Ki | = | 3650.0 | nM | 5.44 |
| CHEMBL6853 | — | Ki | = | 4220.0 | nM | 5.38 |
| CHEMBL7092 | — | Ki | = | 4300.0 | nM | 5.37 |
| CHEMBL266240 | — | Ki | = | 6210.0 | nM | 5.21 |
| CHEMBL418 | 2,4-DISULFAMYLTRIFLUOROMETHYLANILINE | Ki | = | 6560.0 | nM | 5.18 |
| CHEMBL6784 | — | Ki | = | 7000.0 | nM | 5.16 |
| CHEMBL6919 | — | Ki | = | 7450.0 | nM | 5.13 |
| CHEMBL7087 | — | Ki | = | 8950.0 | nM | 5.05 |
| CHEMBL6705 | — | Ki | = | 9560.0 | nM | 5.02 |
| CHEMBL6633 | — | Ki | = | 10200.0 | nM | 4.99 |
| CHEMBL419 | MAFENIDE | Ki | = | 12300.0 | nM | 4.91 |