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Assay Detail

CHEMBL657818

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Binding
Inhibition of human carbonic anhydrase I
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Carbonic anhydrase 1 (CHEMBL261)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Carbonic anhydrase inhibitors: N-(p-sulfamoylphenyl)-alpha-D-glycopyranosylamines as topically acting antiglaucoma agents in hypertensive rabbits.
Winum JY, Casini A, Mincione F, Starnotti M, Montero JL, Scozzafava A, Supuran CT.
Bioorg Med Chem Lett (2004) 14 : 225 -229
PubMed 14684332 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 5.95 6.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2112278 1 6.29
CHEMBL1089967 1 6.20
CHEMBL2111555 1 6.17
CHEMBL2111556 1 6.12
CHEMBL19 METHAZOLAMIDE 4.0 1 6.11
CHEMBL1089637 1 6.08
CHEMBL20 ACETAZOLAMIDE 4.0 1 6.05
CHEMBL2111554 1 6.03
CHEMBL2114130 1 6.00
CHEMBL2112277 1 5.92
CHEMBL17 DICHLORPHENAMIDE 4.0 1 5.92
CHEMBL21 SULFANILAMIDE 4.0 1 4.55
CHEMBL220491 BRINZOLAMIDE 4.0 1 -
CHEMBL218490 DORZOLAMIDE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2112278 Ki = 510.0 nM 6.29
CHEMBL1089967 Ki = 630.0 nM 6.20
CHEMBL2111555 Ki = 680.0 nM 6.17
CHEMBL2111556 Ki = 750.0 nM 6.12
CHEMBL19 METHAZOLAMIDE Ki = 780.0 nM 6.11
CHEMBL1089637 Ki = 840.0 nM 6.08
CHEMBL20 ACETAZOLAMIDE Ki = 900.0 nM 6.05
CHEMBL2111554 Ki = 930.0 nM 6.03
CHEMBL2114130 Ki = 1000.0 nM 6.00
CHEMBL2112277 Ki = 1200.0 nM 5.92
CHEMBL17 DICHLORPHENAMIDE Ki = 1200.0 nM 5.92
CHEMBL21 SULFANILAMIDE Ki = 28000.0 nM 4.55
CHEMBL220491 BRINZOLAMIDE Ki - nM -
CHEMBL218490 DORZOLAMIDE Ki > 50000.0 nM -