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Assay Detail

CHEMBL840039

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Binding
Inhibitory constant value for Carbonic anhydrase II in human determined in esterase assay
7
Total Activities
5
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 2 (CHEMBL205)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Comparison of sulfamate and sulfamide groups for the inhibition of carbonic anhydrase-II by using topiramate as a structural platform.
Maryanoff BE, McComsey DF, Costanzo MJ, Hochman C, Smith-Swintosky V, Shank RP.
J Med Chem (2005) 48 : 1941 -1947
PubMed 15771438 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 6.23 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL20 ACETAZOLAMIDE 4.0 1 7.75
CHEMBL417656 2 7.42
CHEMBL220492 TOPIRAMATE 4.0 2 6.37
CHEMBL177425 1 4.60
CHEMBL283695 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL20 ACETAZOLAMIDE Ki = 18.0 nM 7.75
CHEMBL417656 Ki = 38.0 nM 7.42
CHEMBL220492 TOPIRAMATE Ki = 430.0 nM 6.37
CHEMBL417656 Ki = 750.0 nM 6.12
CHEMBL220492 TOPIRAMATE Ki = 7700.0 nM 5.11
CHEMBL177425 Ki = 25000.0 nM 4.60
CHEMBL283695 Ki = 340000.0 nM -