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Assay Detail

CHEMBL1029735

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

Binding
Inhibition of human recombinant full length CA6 by stopped-flow CO2 hydration method
7
Total Activities
7
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 6 (CHEMBL3025)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Carbonic anhydrase inhibitors. Comparison of chlorthalidone, indapamide, trichloromethiazide, and furosemide X-ray crystal structures in adducts with isozyme II, when several water molecules make the difference.
Temperini C, Cecchi A, Scozzafava A, Supuran CT.
Bioorg Med Chem (2009) 17 : 1214 -1221
PubMed 19119014 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 6.74 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL19 METHAZOLAMIDE 4.0 1 8.00
CHEMBL20 ACETAZOLAMIDE 4.0 1 7.96
CHEMBL18 ETHOXZOLAMIDE 4.0 1 7.37
CHEMBL35 FUROSEMIDE 4.0 1 6.61
CHEMBL1055 CHLORTHALIDONE 4.0 1 5.87
CHEMBL406 INDAPAMIDE 4.0 1 5.79
CHEMBL1054 TRICHLORMETHIAZIDE 4.0 1 5.61

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL19 METHAZOLAMIDE Ki = 10.0 nM 8.00
CHEMBL20 ACETAZOLAMIDE Ki = 11.0 nM 7.96
CHEMBL18 ETHOXZOLAMIDE Ki = 43.0 nM 7.37
CHEMBL35 FUROSEMIDE Ki = 245.0 nM 6.61
CHEMBL1055 CHLORTHALIDONE Ki = 1347.0 nM 5.87
CHEMBL406 INDAPAMIDE Ki = 1606.0 nM 5.79
CHEMBL1054 TRICHLORMETHIAZIDE Ki = 2459.0 nM 5.61