Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL659667

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

Binding
Evaluated for its activity against carbonic anhydrase (CA) in anesthetized rabbits
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Carbonic anhydrase (CHEMBL2095180)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Synthesis and physicochemical properties of thiadiazolo[3,2-a]pyrimidinesulfonamides and thiadiazolo[3,2-a]triazinesulfonamides as candidates for topically effective carbonic anhydrase inhibitors.
Katritzky AR, Caster KC, Maren TH, Conroy CW, Bar-Ilan A.
J Med Chem (1987) 30 : 2058 -2062
PubMed 3669014 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.62 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL65455 1 7.85
CHEMBL423848 1 7.75
CHEMBL19 METHAZOLAMIDE 4.0 1 7.70
CHEMBL294799 1 7.70
CHEMBL65604 1 7.70
CHEMBL20 ACETAZOLAMIDE 4.0 1 7.70
CHEMBL64055 1 7.70
CHEMBL293684 1 7.70
CHEMBL303108 1 7.43
CHEMBL62782 1 7.30
CHEMBL430596 1 7.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL65455 IC50 = 14.0 nM 7.85
CHEMBL423848 IC50 = 18.0 nM 7.75
CHEMBL19 METHAZOLAMIDE IC50 = 20.0 nM 7.70
CHEMBL294799 IC50 = 20.0 nM 7.70
CHEMBL65604 IC50 = 20.0 nM 7.70
CHEMBL20 ACETAZOLAMIDE IC50 = 20.0 nM 7.70
CHEMBL64055 IC50 = 20.0 nM 7.70
CHEMBL293684 IC50 = 20.0 nM 7.70
CHEMBL303108 IC50 = 37.0 nM 7.43
CHEMBL62782 IC50 = 50.0 nM 7.30
CHEMBL430596 IC50 = 50.0 nM 7.30