Assay Detail
Binding
CHEMBL1048176
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Inhibition of Mycobacterium tuberculosis recombinant carbonic anhydrase Rv3273 by stopped flow CO2 hydration assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mycobacterium tuberculosis |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
PROBABLE TRANSMEMBRANE CARBONIC ANHYDRASE (CARBONATE DEHYDRATASE) (CARBONIC DEHYDRATASE) (CHEMBL5767) ↗| Type | SINGLE PROTEIN |
| Organism | Mycobacterium tuberculosis |
Publication
Carbonic anhydrase inhibitors. Inhibition of the Rv1284 and Rv3273 beta-carbonic anhydrases from Mycobacterium tuberculosis with diazenylbenzenesulfonamides.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 22 | 5.53 | 6.98 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL20 | ACETAZOLAMIDE | 4.0 | 1 | 6.98 |
| CHEMBL218490 | DORZOLAMIDE | 4.0 | 1 | 6.86 |
| CHEMBL237251 | PRONTOCIL | — | 1 | 6.83 |
| CHEMBL7146 | — | — | 1 | 6.77 |
| CHEMBL220491 | BRINZOLAMIDE | 4.0 | 1 | 6.70 |
| CHEMBL19 | METHAZOLAMIDE | 4.0 | 1 | 6.25 |
| CHEMBL266026 | — | — | 1 | 5.66 |
| CHEMBL7087 | — | — | 1 | 5.47 |
| CHEMBL419 | MAFENIDE | 4.0 | 1 | 5.13 |
| CHEMBL569350 | — | — | 1 | 5.13 |
| CHEMBL570615 | — | — | 1 | 5.06 |
| CHEMBL16909 | — | — | 1 | 5.06 |
| CHEMBL569351 | SODIUM PHENYLAMINOMETHANESULFONATE | — | 1 | 5.05 |
| CHEMBL274704 | — | — | 1 | 5.05 |
| CHEMBL571598 | SODIUM(METHYL(PHENYL)AMINO)METHANESULFONATE | — | 1 | 5.04 |
| CHEMBL571385 | — | — | 1 | 5.04 |
| CHEMBL569804 | — | — | 1 | 5.04 |
| CHEMBL571371 | — | — | 1 | 5.04 |
| CHEMBL570257 | — | — | 1 | 5.03 |
| CHEMBL576908 | — | — | 1 | 5.03 |
| CHEMBL379206 | — | — | 1 | 4.91 |
| CHEMBL277836 | — | — | 1 | 4.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL20 | ACETAZOLAMIDE | Ki | = | 104.0 | nM | 6.98 |
| CHEMBL218490 | DORZOLAMIDE | Ki | = | 137.0 | nM | 6.86 |
| CHEMBL237251 | PRONTOCIL | Ki | = | 148.0 | nM | 6.83 |
| CHEMBL7146 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL220491 | BRINZOLAMIDE | Ki | = | 201.0 | nM | 6.70 |
| CHEMBL19 | METHAZOLAMIDE | Ki | = | 562.0 | nM | 6.25 |
| CHEMBL266026 | — | Ki | = | 2210.0 | nM | 5.66 |
| CHEMBL7087 | — | Ki | = | 3420.0 | nM | 5.47 |
| CHEMBL419 | MAFENIDE | Ki | = | 7330.0 | nM | 5.13 |
| CHEMBL569350 | — | Ki | = | 7400.0 | nM | 5.13 |
| CHEMBL570615 | — | Ki | = | 8680.0 | nM | 5.06 |
| CHEMBL16909 | — | Ki | = | 8780.0 | nM | 5.06 |
| CHEMBL569351 | SODIUM PHENYLAMINOMETHANESULFONATE | Ki | = | 8900.0 | nM | 5.05 |
| CHEMBL274704 | — | Ki | = | 8900.0 | nM | 5.05 |
| CHEMBL571598 | SODIUM(METHYL(PHENYL)AMINO)METHANESULFONATE | Ki | = | 9110.0 | nM | 5.04 |
| CHEMBL571385 | — | Ki | = | 9230.0 | nM | 5.04 |
| CHEMBL569804 | — | Ki | = | 9030.0 | nM | 5.04 |
| CHEMBL571371 | — | Ki | = | 9180.0 | nM | 5.04 |
| CHEMBL570257 | — | Ki | = | 9450.0 | nM | 5.03 |
| CHEMBL576908 | — | Ki | = | 9360.0 | nM | 5.03 |
| CHEMBL379206 | — | Ki | = | 12400.0 | nM | 4.91 |
| CHEMBL277836 | — | Ki | = | 30700.0 | nM | 4.51 |