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Assay Detail

CHEMBL893568

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Binding
Inhibition of human recombinant CA9 after 15 mins by CO2 hydration stopped flow assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Carbonic anhydrase 9 (CHEMBL3594)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Carbonic anhydrase inhibitors. Inhibition of isoforms I, II, IV, VA, VII, IX, and XIV with sulfonamides incorporating fructopyranose-thioureido tails.
Winum JY, Thiry A, Cheikh KE, Dogné JM, Montero JL, Vullo D, Scozzafava A, Masereel B, Supuran CT.
Bioorg Med Chem Lett (2007) 17 : 2685 -2691
PubMed 17376683 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 6.97 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL390035 1 8.00
CHEMBL395734 1 7.96
CHEMBL20 ACETAZOLAMIDE 4.0 1 7.60
CHEMBL395981 1 7.12
CHEMBL232616 1 7.09
CHEMBL233019 1 6.96
CHEMBL232816 1 6.87
CHEMBL220492 TOPIRAMATE 4.0 1 5.80
CHEMBL232617 1 5.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL390035 Ki = 10.0 nM 8.00
CHEMBL395734 Ki = 11.0 nM 7.96
CHEMBL20 ACETAZOLAMIDE Ki = 25.0 nM 7.60
CHEMBL395981 Ki = 76.0 nM 7.12
CHEMBL232616 Ki = 82.0 nM 7.09
CHEMBL233019 Ki = 110.0 nM 6.96
CHEMBL232816 Ki = 134.0 nM 6.87
CHEMBL220492 TOPIRAMATE Ki = 1590.0 nM 5.80
CHEMBL232617 Ki = 4500.0 nM 5.35