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Assay Detail

CHEMBL883496

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

Binding
In vitro concentration that causes 50% inhibition of carbonic anhydrase carbonate hydro-lyase (EC.4.2.1.1) isolated from bovine erythrocyte
11
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Carbonic anhydrase (CHEMBL2096971)
Type PROTEIN FAMILY
Organism Bos taurus

Publication

Synthesis of 2-substituted-1,3,4-thiadiazole-5-sulphonamides as novel water-soluble inhibitors of carbonic anhydrase
Jayaweera GA, MacNeil SA, Trager SF, Blackburn G
Bioorg Med Chem Lett (1991) 1 : 407 -410
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.38 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL130950 1 8.30
CHEMBL129880 1 8.15
CHEMBL335243 1 8.10
CHEMBL336554 1 8.05
CHEMBL131496 1 8.00
CHEMBL20 ACETAZOLAMIDE 4.0 1 7.80
CHEMBL133619 1 7.52
CHEMBL91302 2 6.43
CHEMBL129895 2 6.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL130950 IC50 = 5.0 nM 8.30
CHEMBL129880 IC50 = 7.0 nM 8.15
CHEMBL335243 IC50 = 8.0 nM 8.10
CHEMBL336554 IC50 = 9.0 nM 8.05
CHEMBL131496 IC50 = 10.0 nM 8.00
CHEMBL20 ACETAZOLAMIDE IC50 = 16.0 nM 7.80
CHEMBL133619 IC50 = 30.0 nM 7.52
CHEMBL91302 IC50 = 370.0 nM 6.43
CHEMBL91302 IC50 = 440.0 nM 6.36
CHEMBL129895 IC50 = 550.0 nM 6.26
CHEMBL129895 IC50 = 570.0 nM 6.24