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Assay Detail

CHEMBL1821328

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

Binding
Inhibition of human cloned carbonic anhydrase 2 preincubated for 15 mins by stopped flow CO2 hydration assay
15
Total Activities
15
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 2 (CHEMBL205)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Carbonic anhydrase inhibitors. Synthesis, molecular structures, and inhibition of the human cytosolic isozymes I and II and transmembrane isozymes IX, XII (cancer-associated) and XIV with novel 3-pyridinesulfonamide derivatives.
Brzozowski Z, Sławiński J, Gdaniec M, Innocenti A, Supuran CT.
Eur J Med Chem (2011) 46 : 4403 -4410
PubMed 21820216 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 7.16 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL18 ETHOXZOLAMIDE 4.0 1 8.10
CHEMBL20 ACETAZOLAMIDE 4.0 1 7.92
CHEMBL19 METHAZOLAMIDE 4.0 1 7.85
CHEMBL77517 INDISULAM 2.0 1 7.82
CHEMBL17 DICHLORPHENAMIDE 4.0 1 7.42
CHEMBL1242890 1 7.30
CHEMBL1817908 1 7.26
CHEMBL1817672 1 7.05
CHEMBL1817905 1 7.01
CHEMBL1817901 1 6.99
CHEMBL1817904 1 6.83
CHEMBL1817906 1 6.66
CHEMBL1817902 1 6.47
CHEMBL1817903 1 6.41
CHEMBL1817907 1 6.31

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL18 ETHOXZOLAMIDE Ki = 8.0 nM 8.10
CHEMBL20 ACETAZOLAMIDE Ki = 12.0 nM 7.92
CHEMBL19 METHAZOLAMIDE Ki = 14.0 nM 7.85
CHEMBL77517 INDISULAM Ki = 15.0 nM 7.82
CHEMBL17 DICHLORPHENAMIDE Ki = 38.0 nM 7.42
CHEMBL1242890 Ki = 50.5 nM 7.30
CHEMBL1817908 Ki = 54.6 nM 7.26
CHEMBL1817672 Ki = 90.0 nM 7.05
CHEMBL1817905 Ki = 98.3 nM 7.01
CHEMBL1817901 Ki = 102.0 nM 6.99
CHEMBL1817904 Ki = 149.0 nM 6.83
CHEMBL1817906 Ki = 220.0 nM 6.66
CHEMBL1817902 Ki = 336.0 nM 6.47
CHEMBL1817903 Ki = 391.0 nM 6.41
CHEMBL1817907 Ki = 487.0 nM 6.31