Assay Detail
Binding
CHEMBL1048175
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Inhibition of Mycobacterium tuberculosis recombinant carbonic anhydrase Rv1284 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
Beta-carbonic anhydrase 1 (CHEMBL5631) ↗| 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 | 5.43 | 6.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL237251 | PRONTOCIL | — | 1 | 6.90 |
| CHEMBL20 | ACETAZOLAMIDE | 4.0 | 1 | 6.32 |
| CHEMBL266026 | — | — | 1 | 6.21 |
| CHEMBL218490 | DORZOLAMIDE | 4.0 | 1 | 6.13 |
| CHEMBL19 | METHAZOLAMIDE | 4.0 | 1 | 6.11 |
| CHEMBL220491 | BRINZOLAMIDE | 4.0 | 1 | 6.08 |
| CHEMBL7146 | — | — | 1 | 6.07 |
| CHEMBL274704 | — | — | 1 | 5.17 |
| CHEMBL277836 | — | — | 1 | 5.16 |
| CHEMBL570615 | — | — | 1 | 5.16 |
| CHEMBL16909 | — | — | 1 | 5.14 |
| CHEMBL570257 | — | — | 1 | 5.12 |
| CHEMBL576908 | — | — | 1 | 5.12 |
| CHEMBL571598 | SODIUM(METHYL(PHENYL)AMINO)METHANESULFONATE | — | 1 | 5.11 |
| CHEMBL571371 | — | — | 1 | 5.11 |
| CHEMBL569351 | SODIUM PHENYLAMINOMETHANESULFONATE | — | 1 | 5.06 |
| CHEMBL569804 | — | — | 1 | 5.06 |
| CHEMBL419 | MAFENIDE | 4.0 | 1 | 5.06 |
| CHEMBL571385 | — | — | 1 | 5.05 |
| CHEMBL379206 | — | — | 1 | 5.03 |
| CHEMBL7087 | — | — | 1 | 5.02 |
| CHEMBL569350 | — | — | 1 | 4.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL237251 | PRONTOCIL | Ki | = | 126.0 | nM | 6.90 |
| CHEMBL20 | ACETAZOLAMIDE | Ki | = | 481.0 | nM | 6.32 |
| CHEMBL266026 | — | Ki | = | 612.0 | nM | 6.21 |
| CHEMBL218490 | DORZOLAMIDE | Ki | = | 744.0 | nM | 6.13 |
| CHEMBL19 | METHAZOLAMIDE | Ki | = | 781.0 | nM | 6.11 |
| CHEMBL220491 | BRINZOLAMIDE | Ki | = | 839.0 | nM | 6.08 |
| CHEMBL7146 | — | Ki | = | 853.0 | nM | 6.07 |
| CHEMBL274704 | — | Ki | = | 6780.0 | nM | 5.17 |
| CHEMBL277836 | — | Ki | = | 6860.0 | nM | 5.16 |
| CHEMBL570615 | — | Ki | = | 7000.0 | nM | 5.16 |
| CHEMBL16909 | — | Ki | = | 7200.0 | nM | 5.14 |
| CHEMBL570257 | — | Ki | = | 7510.0 | nM | 5.12 |
| CHEMBL576908 | — | Ki | = | 7540.0 | nM | 5.12 |
| CHEMBL571598 | SODIUM(METHYL(PHENYL)AMINO)METHANESULFONATE | Ki | = | 7860.0 | nM | 5.11 |
| CHEMBL571371 | — | Ki | = | 7690.0 | nM | 5.11 |
| CHEMBL569351 | SODIUM PHENYLAMINOMETHANESULFONATE | Ki | = | 8670.0 | nM | 5.06 |
| CHEMBL569804 | — | Ki | = | 8710.0 | nM | 5.06 |
| CHEMBL419 | MAFENIDE | Ki | = | 8690.0 | nM | 5.06 |
| CHEMBL571385 | — | Ki | = | 8970.0 | nM | 5.05 |
| CHEMBL379206 | — | Ki | = | 9270.0 | nM | 5.03 |
| CHEMBL7087 | — | Ki | = | 9560.0 | nM | 5.02 |
| CHEMBL569350 | — | Ki | = | 63000.0 | nM | 4.20 |