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Assay Detail

CHEMBL938975

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

Binding
Inhibition of Cryptococcus neoformans recombinant Carbonic anhydrase 2 pre-incubated for 15 mins by CO2 hydration stopped-flow assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cryptococcus neoformans
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Carbonic anhydrase inhibitors. Inhibition of the fungal beta-carbonic anhydrases from Candida albicans and Cryptococcus neoformans with boronic acids.
Innocenti A, Winum JY, Hall RA, Mühlschlegel FA, Scozzafava A, Supuran CT.
Bioorg Med Chem Lett (2009) 19 : 2642 -2645
PubMed 19375309 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 5.54 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL20 ACETAZOLAMIDE 4.0 1 8.00
CHEMBL18 ETHOXZOLAMIDE 4.0 1 7.06
CHEMBL17 DICHLORPHENAMIDE 4.0 1 5.92
CHEMBL453758 1 5.07
CHEMBL140780 TOLYL BORONIC ACID 1 5.05
CHEMBL20866 1 5.02
CHEMBL485742 BIPHENYLBORONIC ACID 1 5.00
CHEMBL555064 1 4.96
CHEMBL141079 1 4.96
CHEMBL459151 1 4.94
CHEMBL21427 1 4.94
CHEMBL559289 STYRYLBORONIC ACID 1 -
CHEMBL551649 1 -
CHEMBL561852 1 -
CHEMBL20461 PHENETHYLBORONIC ACID 1 -
CHEMBL539140 1 -
CHEMBL21485 PHENYLBORONIC ACID 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL20 ACETAZOLAMIDE Ki = 10.0 nM 8.00
CHEMBL18 ETHOXZOLAMIDE Ki = 87.0 nM 7.06
CHEMBL17 DICHLORPHENAMIDE Ki = 1200.0 nM 5.92
CHEMBL453758 Ki = 8500.0 nM 5.07
CHEMBL140780 TOLYL BORONIC ACID Ki = 8900.0 nM 5.05
CHEMBL20866 Ki = 9600.0 nM 5.02
CHEMBL485742 BIPHENYLBORONIC ACID Ki = 9900.0 nM 5.00
CHEMBL555064 Ki = 10900.0 nM 4.96
CHEMBL141079 Ki = 11000.0 nM 4.96
CHEMBL459151 Ki = 11500.0 nM 4.94
CHEMBL21427 Ki = 11400.0 nM 4.94
CHEMBL559289 STYRYLBORONIC ACID Ki = 490000.0 nM -
CHEMBL551649 Ki = 521000.0 nM -
CHEMBL561852 Ki = 3040000.0 nM -
CHEMBL20461 PHENETHYLBORONIC ACID Ki = 428000.0 nM -
CHEMBL539140 Ki = 506000.0 nM -
CHEMBL21485 PHENYLBORONIC ACID Ki = 810000.0 nM -