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Assay Detail

CHEMBL657848

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

Binding
Inhibitory activity against human carbonic anhydrase II (hCA II) by using esterase assay method
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Carbonic anhydrase 2 (CHEMBL205)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Carbonic anhydrase inhibitors. Inhibition of cytosolic isozyme XIII with aromatic and heterocyclic sulfonamides: a novel target for the drug design.
Lehtonen JM, Parkkila S, Vullo D, Casini A, Scozzafava A, Supuran CT.
Bioorg Med Chem Lett (2004) 14 : 3757 -3762
PubMed 15203157 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 7.35 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL268439 1 8.70
CHEMBL218490 DORZOLAMIDE 4.0 1 8.05
CHEMBL20 ACETAZOLAMIDE 4.0 1 7.92
CHEMBL19 METHAZOLAMIDE 4.0 1 7.85
CHEMBL7146 1 7.52
CHEMBL266026 1 7.48
CHEMBL17 DICHLORPHENAMIDE 4.0 1 7.42
CHEMBL6724 1 7.40
CHEMBL865 VALDECOXIB 4.0 1 7.37
CHEMBL269122 1 7.34
CHEMBL6853 1 7.22
CHEMBL268177 1 7.16
CHEMBL7092 1 6.96
CHEMBL7087 1 6.80
CHEMBL419 MAFENIDE 4.0 1 6.77
CHEMBL6705 1 6.53
CHEMBL21 SULFANILAMIDE 4.0 1 6.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL268439 Ki = 2.0 nM 8.70
CHEMBL218490 DORZOLAMIDE Ki = 9.0 nM 8.05
CHEMBL20 ACETAZOLAMIDE Ki = 12.0 nM 7.92
CHEMBL19 METHAZOLAMIDE Ki = 14.0 nM 7.85
CHEMBL7146 Ki = 30.0 nM 7.52
CHEMBL266026 Ki = 33.0 nM 7.48
CHEMBL17 DICHLORPHENAMIDE Ki = 38.0 nM 7.42
CHEMBL6724 Ki = 40.0 nM 7.40
CHEMBL865 VALDECOXIB Ki = 43.0 nM 7.37
CHEMBL269122 Ki = 46.0 nM 7.34
CHEMBL6853 Ki = 60.0 nM 7.22
CHEMBL268177 Ki = 70.0 nM 7.16
CHEMBL7092 Ki = 110.0 nM 6.96
CHEMBL7087 Ki = 160.0 nM 6.80
CHEMBL419 MAFENIDE Ki = 170.0 nM 6.77
CHEMBL6705 Ki = 295.0 nM 6.53
CHEMBL21 SULFANILAMIDE Ki = 300.0 nM 6.52