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Assay Detail

CHEMBL1053955

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

Binding
Inhibition of human carbonic anhydrase 5A by stopped flow CO2 hydration assay
4
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Carbonic anhydrase 5A, mitochondrial (CHEMBL4789)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The protein tyrosine kinase inhibitors imatinib and nilotinib strongly inhibit several mammalian alpha-carbonic anhydrase isoforms.
Parkkila S, Innocenti A, Kallio H, Hilvo M, Scozzafava A, Supuran CT.
Bioorg Med Chem Lett (2009) 19 : 4102 -4106
PubMed 19527930 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 5.72 7.20
IC50 1 5.02 5.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL20 ACETAZOLAMIDE 4.0 1 7.20
CHEMBL255863 NILOTINIB 4.0 1 5.26
CHEMBL560175 1 5.02
CHEMBL941 IMATINIB 4.0 1 4.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL20 ACETAZOLAMIDE Ki = 63.0 nM 7.20
CHEMBL255863 NILOTINIB Ki = 5485.0 nM 5.26
CHEMBL560175 IC50 = 9600.0 nM 5.02
CHEMBL941 IMATINIB Ki = 20200.0 nM 4.70