Assay Detail
Binding
CHEMBL2071765
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Inhibition of human CA1 using CO2 as substrate incubated for 6 hrs prior to substrate addition measured for 10 to 100 secs by stopped flow technique
19
Total Activities
19
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
Inhibition of α-class cytosolic human carbonic anhydrases I, II, IX and XII, and β-class fungal enzymes by carboxylic acids and their derivatives: new isoform-I selective nanomolar inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 5.70 | 7.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2070207 | — | — | 1 | 7.38 |
| CHEMBL2070212 | — | — | 1 | 7.31 |
| CHEMBL20 | ACETAZOLAMIDE | 4.0 | 1 | 6.60 |
| CHEMBL2070211 | — | — | 1 | 5.98 |
| CHEMBL23832 | FENAMIC ACID | 1.0 | 1 | 5.92 |
| CHEMBL2070206 | — | — | 1 | 5.92 |
| CHEMBL2070209 | — | — | 1 | 5.78 |
| CHEMBL2070214 | — | — | 1 | 5.73 |
| CHEMBL1673089 | — | — | 1 | 5.56 |
| CHEMBL467389 | — | — | 1 | 5.47 |
| CHEMBL2070202 | — | — | 1 | 5.44 |
| CHEMBL2070205 | — | — | 1 | 5.40 |
| CHEMBL41028 | — | — | 1 | 5.36 |
| CHEMBL499273 | — | — | 1 | 5.29 |
| CHEMBL2070203 | — | — | 1 | 5.26 |
| CHEMBL2070208 | — | — | 1 | 5.21 |
| CHEMBL2070213 | — | — | 1 | 5.12 |
| CHEMBL2070204 | — | — | 1 | 5.12 |
| CHEMBL2070210 | — | — | 1 | 4.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2070207 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL2070212 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL20 | ACETAZOLAMIDE | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL2070211 | — | Ki | = | 1050.0 | nM | 5.98 |
| CHEMBL23832 | FENAMIC ACID | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL2070206 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL2070209 | — | Ki | = | 1650.0 | nM | 5.78 |
| CHEMBL2070214 | — | Ki | = | 1850.0 | nM | 5.73 |
| CHEMBL1673089 | — | Ki | = | 2780.0 | nM | 5.56 |
| CHEMBL467389 | — | Ki | = | 3350.0 | nM | 5.47 |
| CHEMBL2070202 | — | Ki | = | 3600.0 | nM | 5.44 |
| CHEMBL2070205 | — | Ki | = | 4020.0 | nM | 5.40 |
| CHEMBL41028 | — | Ki | = | 4410.0 | nM | 5.36 |
| CHEMBL499273 | — | Ki | = | 5070.0 | nM | 5.29 |
| CHEMBL2070203 | — | Ki | = | 5530.0 | nM | 5.26 |
| CHEMBL2070208 | — | Ki | = | 6200.0 | nM | 5.21 |
| CHEMBL2070213 | — | Ki | = | 7530.0 | nM | 5.12 |
| CHEMBL2070204 | — | Ki | = | 7500.0 | nM | 5.12 |
| CHEMBL2070210 | — | Ki | = | 38000.0 | nM | 4.42 |