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Assay Detail

CHEMBL3815701

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

Binding
Inhibition of human carbonic anhydrase 2 preincubated for 6 hrs at 4 degC measured for 10 to 100 secs by stopped-flow carbon dioxide hydration assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Kinetic and X-ray crystallographic investigations of substituted 2-thio-6-oxo-1,6-dihydropyrimidine-benzenesulfonamides acting as carbonic anhydrase inhibitors.
Vullo D, Supuran CT, Scozzafava A, De Simone G, Monti SM, Alterio V, Carta F.
Bioorg Med Chem (2016) 24 : 3643 -3648
PubMed 27316543 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 8.17 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2382401 1 8.30
CHEMBL2382402 1 8.29
CHEMBL2382403 1 8.21
CHEMBL2382405 1 8.19
CHEMBL2382337 1 8.12
CHEMBL20 ACETAZOLAMIDE 4.0 1 7.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2382401 Ki = 5.0 nM 8.30
CHEMBL2382402 Ki = 5.1 nM 8.29
CHEMBL2382403 Ki = 6.1 nM 8.21
CHEMBL2382405 Ki = 6.4 nM 8.19
CHEMBL2382337 Ki = 7.6 nM 8.12
CHEMBL20 ACETAZOLAMIDE Ki = 12.0 nM 7.92