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Assay Detail

CHEMBL5112293

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

Binding
Inhibition of human recombinant CA5A assessed as inhibition constant pre-incubated for 15 mins measured by phenol red dye based stopped flow CO2 hydration assay
17
Total Activities
17
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 5A, mitochondrial (CHEMBL4789)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a Potent and Highly Selective Dipeptidyl Peptidase IV and Carbonic Anhydrase Inhibitor as "Antidiabesity" Agents Based on Repurposing and Morphing of WB-4101.
Artasensi A, Angeli A, Lammi C, Bollati C, Gervasoni S, Baron G, Matucci R, Supuran CT, Vistoli G, Fumagalli L.
J Med Chem (2022) 65 : 13946 -13966
PubMed 36201615 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 6.67 7.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL20 ACETAZOLAMIDE 4.0 1 7.20
CHEMBL5206696 1 7.11
CHEMBL5171860 1 7.11
CHEMBL5198237 1 7.05
CHEMBL5177166 1 7.03
CHEMBL5193531 1 6.34
CHEMBL5191973 1 6.18
CHEMBL5205289 1 5.36
CHEMBL5201114 1 -
CHEMBL1422 SITAGLIPTIN 4.0 1 -
CHEMBL25554 1 -
CHEMBL5191609 1 -
CHEMBL5193118 1 -
CHEMBL5184240 1 -
CHEMBL5194237 1 -
CHEMBL5203377 1 -
CHEMBL5176469 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL20 ACETAZOLAMIDE Ki = 63.0 nM 7.20
CHEMBL5206696 Ki = 77.5 nM 7.11
CHEMBL5171860 Ki = 77.9 nM 7.11
CHEMBL5198237 Ki = 89.6 nM 7.05
CHEMBL5177166 Ki = 94.1 nM 7.03
CHEMBL5193531 Ki = 456.0 nM 6.34
CHEMBL5191973 Ki = 658.8 nM 6.18
CHEMBL5205289 Ki = 4346.0 nM 5.36
CHEMBL5201114 Ki > 10000.0 nM -
CHEMBL1422 SITAGLIPTIN Ki > 10000.0 nM -
CHEMBL25554 Ki > 10000.0 nM -
CHEMBL5191609 Ki > 10000.0 nM -
CHEMBL5193118 Ki > 10000.0 nM -
CHEMBL5184240 Ki > 10000.0 nM -
CHEMBL5194237 Ki > 10000.0 nM -
CHEMBL5203377 Ki > 10000.0 nM -
CHEMBL5176469 Ki > 10000.0 nM -