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Assay Detail

CHEMBL656573

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

Binding
In vitro inhibition against purified human erythrocyte carbonic anhydrase II was determined (acetozolamide used as control.)
17
Total Activities
17
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
IC50 17 7.82 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL18 ETHOXZOLAMIDE 4.0 1 9.40
CHEMBL120418 1 8.46
CHEMBL333193 1 8.35
CHEMBL346810 1 8.30
CHEMBL2092886 1 8.12
CHEMBL158261 1 8.07
CHEMBL348573 1 8.00
CHEMBL314569 1 7.89
CHEMBL1788205 1 7.66
CHEMBL158090 1 7.66
CHEMBL352218 1 7.64
CHEMBL158026 1 7.52
CHEMBL347369 1 7.40
CHEMBL155420 1 7.40
CHEMBL312593 1 7.40
CHEMBL158363 1 7.00
CHEMBL155152 1 6.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL18 ETHOXZOLAMIDE IC50 = 0.4 nM 9.40
CHEMBL120418 IC50 = 3.5 nM 8.46
CHEMBL333193 IC50 = 4.5 nM 8.35
CHEMBL346810 IC50 = 5.0 nM 8.30
CHEMBL2092886 IC50 = 7.5 nM 8.12
CHEMBL158261 IC50 = 8.5 nM 8.07
CHEMBL348573 IC50 = 10.0 nM 8.00
CHEMBL314569 IC50 = 13.0 nM 7.89
CHEMBL1788205 IC50 = 22.0 nM 7.66
CHEMBL158090 IC50 = 22.0 nM 7.66
CHEMBL352218 IC50 = 23.0 nM 7.64
CHEMBL158026 IC50 = 30.0 nM 7.52
CHEMBL347369 IC50 = 40.0 nM 7.40
CHEMBL155420 IC50 = 40.0 nM 7.40
CHEMBL312593 IC50 = 40.0 nM 7.40
CHEMBL158363 IC50 = 100.0 nM 7.00
CHEMBL155152 IC50 = 250.0 nM 6.60