Assay Detail
Binding
CHEMBL938995
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Inhibition of Mycobacterium tuberculosis recombinant carbonic anhydrase Rv3273 by by stopped flow CO2 hydration assay
20
Total Activities
20
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
Discovery of low nanomolar and subnanomolar inhibitors of the mycobacterial beta-carbonic anhydrases Rv1284 and Rv3273.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 7.14 | 9.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL501294 | — | — | 1 | 9.03 |
| CHEMBL512633 | — | — | 1 | 8.14 |
| CHEMBL20 | ACETAZOLAMIDE | 4.0 | 1 | 7.92 |
| CHEMBL77517 | INDISULAM | 2.0 | 1 | 7.82 |
| CHEMBL6633 | — | — | 1 | 7.48 |
| CHEMBL467897 | — | — | 1 | 7.42 |
| CHEMBL6724 | — | — | 1 | 7.40 |
| CHEMBL468294 | — | — | 1 | 7.19 |
| CHEMBL468946 | — | — | 1 | 7.17 |
| CHEMBL466832 | — | — | 1 | 7.15 |
| CHEMBL467898 | — | — | 1 | 7.13 |
| CHEMBL513854 | — | — | 1 | 7.11 |
| CHEMBL511239 | — | — | 1 | 7.07 |
| CHEMBL469126 | — | — | 1 | 7.04 |
| CHEMBL513835 | — | — | 1 | 7.00 |
| CHEMBL468945 | — | — | 1 | 6.98 |
| CHEMBL466234 | — | — | 1 | 6.97 |
| CHEMBL467258 | — | — | 1 | 5.75 |
| CHEMBL521690 | — | — | 1 | 5.55 |
| CHEMBL468094 | — | — | 1 | 5.47 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL501294 | — | Ki | = | 0.93 | nM | 9.03 |
| CHEMBL512633 | — | Ki | = | 7.2 | nM | 8.14 |
| CHEMBL20 | ACETAZOLAMIDE | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL77517 | INDISULAM | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL6633 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL467897 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL6724 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL468294 | — | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL468946 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL466832 | — | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL467898 | — | Ki | = | 74.0 | nM | 7.13 |
| CHEMBL513854 | — | Ki | = | 77.0 | nM | 7.11 |
| CHEMBL511239 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL469126 | — | Ki | = | 91.0 | nM | 7.04 |
| CHEMBL513835 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL468945 | — | Ki | = | 104.0 | nM | 6.98 |
| CHEMBL466234 | — | Ki | = | 106.0 | nM | 6.97 |
| CHEMBL467258 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL521690 | — | Ki | = | 2840.0 | nM | 5.55 |
| CHEMBL468094 | — | Ki | = | 3380.0 | nM | 5.47 |