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Assay Detail

CHEMBL1059705

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

Binding
Inhibition of mouse carbonic anhydrase 15 by stopped flow CO2 hydration assay
4
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Carbonic anhydrase 15 (CHEMBL5973)
Type SINGLE PROTEIN
Organism Mus musculus

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 7.12 7.14
IC50 1 4.03 4.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL20 ACETAZOLAMIDE 4.0 1 7.14
CHEMBL941 IMATINIB 4.0 1 7.11
CHEMBL255863 NILOTINIB 4.0 1 7.10
CHEMBL560175 1 4.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL20 ACETAZOLAMIDE Ki = 72.0 nM 7.14
CHEMBL941 IMATINIB Ki = 78.0 nM 7.11
CHEMBL255863 NILOTINIB Ki = 79.0 nM 7.10
CHEMBL560175 IC50 = 93100.0 nM 4.03