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Assay Detail

CHEMBL2446522

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

Binding
Inhibition of human recombinant carbonic anhydrase9 transmembrane isoform expressed in Escherichia coli BL21 preincubated for 15 mins by stopped-flow CO2 hydration assay
7
Total Activities
7
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 9 (CHEMBL3594)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Inhibition of human carbonic anhydrase isoforms I-XIV with sulfonamides incorporating fluorine and 1,3,5-triazine moieties.
Ceruso M, Vullo D, Scozzafava A, Supuran CT.
Bioorg Med Chem (2013) 21 : 6929 -6936
PubMed 24103430 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 6.97 7.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2443313 1 7.66
CHEMBL2443314 1 7.65
CHEMBL186716 1 6.82
CHEMBL2443317 1 6.70
CHEMBL2443315 1 6.68
CHEMBL2443318 1 6.67
CHEMBL2443316 1 6.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2443313 Ki = 21.8 nM 7.66
CHEMBL2443314 Ki = 22.3 nM 7.65
CHEMBL186716 Ki = 153.0 nM 6.82
CHEMBL2443317 Ki = 199.0 nM 6.70
CHEMBL2443315 Ki = 208.0 nM 6.68
CHEMBL2443318 Ki = 214.0 nM 6.67
CHEMBL2443316 Ki = 228.0 nM 6.64