Assay Detail
Binding
CHEMBL2019836
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Inhibition of cytosolic human carbonic anhydrase 1 preincubated for 15 mins by stopped flow CO2 hydration assay
26
Total Activities
24
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Flavones and structurally related 4-chromenones inhibit carbonic anhydrases by a different mechanism of action compared to coumarins.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 4.98 | 5.34 |
| Ki | 7 | 5.56 | 5.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2019140 | — | — | 2 | 5.90 |
| CHEMBL275638 | FLAVONE | 2.0 | 1 | 5.72 |
| CHEMBL2019155 | — | — | 1 | 5.66 |
| CHEMBL2019143 | — | — | 2 | 5.65 |
| CHEMBL276915 | 7-HYDROXYFLAVONE | — | 1 | 5.47 |
| CHEMBL2019154 | — | — | 1 | 5.32 |
| CHEMBL2019136 | — | — | 1 | 5.31 |
| CHEMBL294009 | FLAVONOL | — | 1 | 5.28 |
| CHEMBL117 | CHRYSIN | — | 1 | 5.26 |
| CHEMBL2019150 | — | — | 1 | 5.23 |
| CHEMBL2019144 | — | — | 1 | 5.15 |
| CHEMBL2019146 | — | — | 1 | 5.12 |
| CHEMBL2019139 | — | — | 1 | 5.12 |
| CHEMBL2019141 | — | — | 1 | 5.09 |
| CHEMBL2019142 | — | — | 1 | 5.09 |
| CHEMBL2019145 | — | — | 1 | 5.08 |
| CHEMBL2019151 | — | — | 1 | 5.08 |
| CHEMBL2019153 | — | — | 1 | 5.07 |
| CHEMBL2019138 | — | — | 1 | 5.04 |
| CHEMBL2019148 | — | — | 1 | 5.01 |
| CHEMBL2019152 | — | — | 1 | 5.01 |
| CHEMBL2019137 | — | — | 1 | 4.33 |
| CHEMBL2019147 | — | — | 1 | 4.27 |
| CHEMBL2019149 | — | — | 1 | 4.02 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2019140 | — | Ki | = | 1250.0 | nM | 5.90 |
| CHEMBL275638 | FLAVONE | Ki | = | 1890.0 | nM | 5.72 |
| CHEMBL2019155 | — | Ki | = | 2180.0 | nM | 5.66 |
| CHEMBL2019143 | — | Ki | = | 2260.0 | nM | 5.65 |
| CHEMBL276915 | 7-HYDROXYFLAVONE | Ki | = | 3370.0 | nM | 5.47 |
| CHEMBL2019140 | — | IC50 | = | 4610.0 | nM | 5.34 |
| CHEMBL2019154 | — | IC50 | = | 4810.0 | nM | 5.32 |
| CHEMBL2019136 | — | IC50 | = | 4870.0 | nM | 5.31 |
| CHEMBL294009 | FLAVONOL | Ki | = | 5210.0 | nM | 5.28 |
| CHEMBL117 | CHRYSIN | Ki | = | 5490.0 | nM | 5.26 |
| CHEMBL2019150 | — | IC50 | = | 5850.0 | nM | 5.23 |
| CHEMBL2019144 | — | IC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL2019139 | — | IC50 | = | 7660.0 | nM | 5.12 |
| CHEMBL2019146 | — | IC50 | = | 7680.0 | nM | 5.12 |
| CHEMBL2019142 | — | IC50 | = | 8060.0 | nM | 5.09 |
| CHEMBL2019141 | — | IC50 | = | 8120.0 | nM | 5.09 |
| CHEMBL2019145 | — | IC50 | = | 8370.0 | nM | 5.08 |
| CHEMBL2019151 | — | IC50 | = | 8300.0 | nM | 5.08 |
| CHEMBL2019153 | — | IC50 | = | 8510.0 | nM | 5.07 |
| CHEMBL2019138 | — | IC50 | = | 9070.0 | nM | 5.04 |
| CHEMBL2019143 | — | IC50 | = | 9560.0 | nM | 5.02 |
| CHEMBL2019148 | — | IC50 | = | 9850.0 | nM | 5.01 |
| CHEMBL2019152 | — | IC50 | = | 9720.0 | nM | 5.01 |
| CHEMBL2019137 | — | IC50 | = | 46200.0 | nM | 4.33 |
| CHEMBL2019147 | — | IC50 | = | 54100.0 | nM | 4.27 |
| CHEMBL2019149 | — | IC50 | = | 95700.0 | nM | 4.02 |