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Assay Detail

CHEMBL2329434

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

Binding
Inhibition of human CA2 Ala65Ser and Asn67Gln double mutant expressed in Escherichia coli strain BL21 (DE3) after 6 hrs by stopped-flow CO2 hydration method
4
Total Activities
4
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

Sulfocoumarins (1,2-benzoxathiine-2,2-dioxides): a class of potent and isoform-selective inhibitors of tumor-associated carbonic anhydrases.
Tars K, Vullo D, Kazaks A, Leitans J, Lends A, Grandane A, Zalubovskis R, Scozzafava A, Supuran CT.
J Med Chem (2013) 56 : 293 -300
PubMed 23241068 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 5.86 6.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2326506 1 6.10
CHEMBL2326510 1 6.03
CHEMBL2326507 1 5.69
CHEMBL2326508 1 5.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2326506 Ki = 800.0 nM 6.10
CHEMBL2326510 Ki = 930.0 nM 6.03
CHEMBL2326507 Ki = 2030.0 nM 5.69
CHEMBL2326508 Ki = 2370.0 nM 5.62