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Assay Detail

CHEMBL869403

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Binding
Inhibition of recombinant human mitochondrial isozyme CA VA
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Carbonic anhydrase inhibitors: inhibition of the human isozymes I, II, VA, and IX with a library of substituted difluoromethanesulfonamides.
Cecchi A, Taylor SD, Liu Y, Hill B, Vullo D, Scozzafava A, Supuran CT.
Bioorg Med Chem Lett (2005) 15 : 5192 -5196
PubMed 16203142 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 6.28 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL20 ACETAZOLAMIDE 4.0 1 7.22
CHEMBL199464 1 6.89
CHEMBL1628004 1 6.89
CHEMBL370159 1 6.82
CHEMBL200673 1 6.80
CHEMBL199493 1 6.15
CHEMBL371870 PHENYLDIFLUOROMETHANESULFONAMIDE 1 6.11
CHEMBL370854 1 6.01
CHEMBL1628081 1 5.83
CHEMBL198891 1 5.82
CHEMBL369953 PHENYLMETHANESULFONAMIDE 1 5.80
CHEMBL198913 1 5.07
CHEMBL24259 PHENYLSULFAMATE 1 -
CHEMBL11185 1 -
CHEMBL122708 EMATE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL20 ACETAZOLAMIDE Ki = 60.0 nM 7.22
CHEMBL199464 Ki = 128.0 nM 6.89
CHEMBL1628004 Ki = 129.0 nM 6.89
CHEMBL370159 Ki = 153.0 nM 6.82
CHEMBL200673 Ki = 160.0 nM 6.80
CHEMBL199493 Ki = 714.0 nM 6.15
CHEMBL371870 PHENYLDIFLUOROMETHANESULFONAMIDE Ki = 785.0 nM 6.11
CHEMBL370854 Ki = 982.0 nM 6.01
CHEMBL1628081 Ki = 1464.0 nM 5.83
CHEMBL198891 Ki = 1516.0 nM 5.82
CHEMBL369953 PHENYLMETHANESULFONAMIDE Ki = 1580.0 nM 5.80
CHEMBL198913 Ki = 8600.0 nM 5.07
CHEMBL24259 PHENYLSULFAMATE Ki - -
CHEMBL11185 Ki - -
CHEMBL122708 EMATE Ki - -