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Assay Detail

CHEMBL2019838

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

Binding
Inhibition of cytosolic human carbonic anhydrase 2 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

Target

Carbonic anhydrase 2 (CHEMBL205)
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
IC50 19 5.05 5.44
Ki 7 5.51 6.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2019140 2 6.04
CHEMBL2019155 1 5.76
CHEMBL2019143 2 5.70
CHEMBL276915 7-HYDROXYFLAVONE 1 5.65
CHEMBL117 CHRYSIN 1 5.36
CHEMBL2019142 1 5.19
CHEMBL2019153 1 5.19
CHEMBL2019138 1 5.17
CHEMBL2019146 1 5.12
CHEMBL2019148 1 5.10
CHEMBL2019144 1 5.09
CHEMBL2019151 1 5.08
CHEMBL2019141 1 5.08
CHEMBL2019145 1 5.08
CHEMBL2019150 1 5.06
CHEMBL275638 FLAVONE 2.0 1 5.06
CHEMBL2019139 1 5.06
CHEMBL2019152 1 5.04
CHEMBL2019136 1 5.03
CHEMBL2019154 1 5.03
CHEMBL294009 FLAVONOL 1 5.03
CHEMBL2019147 1 4.86
CHEMBL2019137 1 4.44
CHEMBL2019149 1 4.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2019140 Ki = 910.0 nM 6.04
CHEMBL2019155 Ki = 1750.0 nM 5.76
CHEMBL2019143 Ki = 2010.0 nM 5.70
CHEMBL276915 7-HYDROXYFLAVONE Ki = 2240.0 nM 5.65
CHEMBL2019140 IC50 = 3620.0 nM 5.44
CHEMBL2019143 IC50 = 3660.0 nM 5.44
CHEMBL117 CHRYSIN Ki = 4380.0 nM 5.36
CHEMBL2019142 IC50 = 6510.0 nM 5.19
CHEMBL2019153 IC50 = 6440.0 nM 5.19
CHEMBL2019138 IC50 = 6790.0 nM 5.17
CHEMBL2019146 IC50 = 7590.0 nM 5.12
CHEMBL2019148 IC50 = 7870.0 nM 5.10
CHEMBL2019144 IC50 = 8070.0 nM 5.09
CHEMBL2019141 IC50 = 8250.0 nM 5.08
CHEMBL2019151 IC50 = 8350.0 nM 5.08
CHEMBL2019145 IC50 = 8280.0 nM 5.08
CHEMBL2019139 IC50 = 8660.0 nM 5.06
CHEMBL275638 FLAVONE Ki = 8710.0 nM 5.06
CHEMBL2019150 IC50 = 8740.0 nM 5.06
CHEMBL2019152 IC50 = 9020.0 nM 5.04
CHEMBL2019154 IC50 = 9330.0 nM 5.03
CHEMBL2019136 IC50 = 9430.0 nM 5.03
CHEMBL294009 FLAVONOL Ki = 9300.0 nM 5.03
CHEMBL2019147 IC50 = 13700.0 nM 4.86
CHEMBL2019137 IC50 = 36200.0 nM 4.44
CHEMBL2019149 IC50 = 36700.0 nM 4.43