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Assay Detail

CHEMBL839012

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Binding
Inhibitory activity against human carbonic anhydrase II (hCAII)
21
Total Activities
21
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 2 (CHEMBL205)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Carbonic anhydrase inhibitors. Inhibition of the membrane-bound human and bovine isozymes IV with sulfonamides.
Innocenti A, Firnges MA, Antel J, Wurl M, Scozzafava A, Supuran CT.
Bioorg Med Chem Lett (2005) 15 : 1149 -1154
PubMed 15686931 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 7.30 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL220492 TOPIRAMATE 4.0 1 8.30
CHEMBL18 ETHOXZOLAMIDE 4.0 1 8.10
CHEMBL218490 DORZOLAMIDE 4.0 1 8.05
CHEMBL20 ACETAZOLAMIDE 4.0 1 7.92
CHEMBL19 METHAZOLAMIDE 4.0 1 7.85
CHEMBL266026 1 7.48
CHEMBL17 DICHLORPHENAMIDE 4.0 1 7.42
CHEMBL6724 1 7.40
CHEMBL865 VALDECOXIB 4.0 1 7.37
CHEMBL265674 1 7.22
CHEMBL6853 1 7.22
CHEMBL418 2,4-DISULFAMYLTRIFLUOROMETHYLANILINE 1 7.20
CHEMBL268177 1 7.16
CHEMBL266240 1 7.12
CHEMBL7092 1 6.96
CHEMBL7087 1 6.80
CHEMBL419 MAFENIDE 4.0 1 6.77
CHEMBL6852 1 6.62
CHEMBL21 SULFANILAMIDE 4.0 1 6.52
CHEMBL7204 1 6.50
CHEMBL118 CELECOXIB 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL220492 TOPIRAMATE Ki = 5.0 nM 8.30
CHEMBL18 ETHOXZOLAMIDE Ki = 8.0 nM 8.10
CHEMBL218490 DORZOLAMIDE Ki = 9.0 nM 8.05
CHEMBL20 ACETAZOLAMIDE Ki = 12.0 nM 7.92
CHEMBL19 METHAZOLAMIDE Ki = 14.0 nM 7.85
CHEMBL266026 Ki = 33.0 nM 7.48
CHEMBL17 DICHLORPHENAMIDE Ki = 38.0 nM 7.42
CHEMBL6724 Ki = 40.0 nM 7.40
CHEMBL865 VALDECOXIB Ki = 43.0 nM 7.37
CHEMBL265674 Ki = 60.0 nM 7.22
CHEMBL6853 Ki = 60.0 nM 7.22
CHEMBL418 2,4-DISULFAMYLTRIFLUOROMETHYLANILINE Ki = 63.0 nM 7.20
CHEMBL268177 Ki = 70.0 nM 7.16
CHEMBL266240 Ki = 75.0 nM 7.12
CHEMBL7092 Ki = 110.0 nM 6.96
CHEMBL7087 Ki = 160.0 nM 6.80
CHEMBL419 MAFENIDE Ki = 170.0 nM 6.77
CHEMBL6852 Ki = 240.0 nM 6.62
CHEMBL21 SULFANILAMIDE Ki = 300.0 nM 6.52
CHEMBL7204 Ki = 320.0 nM 6.50
CHEMBL118 CELECOXIB Ki = 21.0 nM -