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Assay Detail

CHEMBL2019843

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of transmembrane tumor-associated human carbonic anhydrase 12 preincubated for 12 hrs by stopped flow CO2 hydration assay
4
Total Activities
4
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

Target

Carbonic anhydrase 12 (CHEMBL3242)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Flavones and structurally related 4-chromenones inhibit carbonic anhydrases by a different mechanism of action compared to coumarins.
Balboni G, Congiu C, Onnis V, Maresca A, Scozzafava A, Winum JY, Maietti A, Supuran CT.
Bioorg Med Chem Lett (2012) 22 : 3063 -3066
PubMed 22487176 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 5.11 5.18

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL294009 FLAVONOL 1 5.18
CHEMBL275638 FLAVONE 2.0 1 5.13
CHEMBL276915 7-HYDROXYFLAVONE 1 5.07
CHEMBL117 CHRYSIN 1 5.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL294009 FLAVONOL Ki = 6650.0 nM 5.18
CHEMBL275638 FLAVONE Ki = 7330.0 nM 5.13
CHEMBL276915 7-HYDROXYFLAVONE Ki = 8510.0 nM 5.07
CHEMBL117 CHRYSIN Ki = 9070.0 nM 5.04