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Assay Detail

CHEMBL659853

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

Binding
In vitro binding to human erythrocyte carbonic anhydrase was determined by fluorescence competition assay employing the fluorescent CA inhibitor dansylamide
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Thienothiopyran-2-sulfonamides: a novel class of water-soluble carbonic anhydrase inhibitors.
Ponticello GS, Freedman MB, Habecker CN, Lyle PA, Schwam H, Varga SL, Christy ME, Randall WC, Baldwin JJ.
J Med Chem (1987) 30 : 591 -597
PubMed 3560154 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 7.89 9.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL18 ETHOXZOLAMIDE 4.0 1 9.31
CHEMBL333193 1 8.48
CHEMBL2092886 1 8.17
CHEMBL348573 1 8.15
CHEMBL1788205 1 7.81
CHEMBL155420 1 7.74
CHEMBL158363 1 6.98
CHEMBL155152 1 6.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL18 ETHOXZOLAMIDE Ki = 0.49 nM 9.31
CHEMBL333193 Ki = 3.3 nM 8.48
CHEMBL2092886 Ki = 6.7 nM 8.17
CHEMBL348573 Ki = 7.11 nM 8.15
CHEMBL1788205 Ki = 15.4 nM 7.81
CHEMBL155420 Ki = 18.2 nM 7.74
CHEMBL158363 Ki = 104.0 nM 6.98
CHEMBL155152 Ki = 309.0 nM 6.51