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Assay Detail

CHEMBL827204

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Binding
Inhibitory activity against alpha carbonic anhydrase (Co-Cam) from Methanosarcina thermophila
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Methanosarcina thermophila
Confidence 9 — Direct single protein target
Curated By Expert

Target

Carbonic anhydrase (CHEMBL3932)
Type SINGLE PROTEIN
Organism Methanosarcina thermophila

Publication

Carbonic anhydrase inhibitors. Inhibition of the prokariotic beta and gamma-class enzymes from Archaea with sulfonamides.
Zimmerman S, Innocenti A, Casini A, Ferry JG, Scozzafava A, Supuran CT.
Bioorg Med Chem Lett (2004) 14 : 6001 -6006
PubMed 15546717 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 6.10 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL220492 TOPIRAMATE 4.0 1 6.92
CHEMBL7087 1 6.89
CHEMBL17 DICHLORPHENAMIDE 4.0 1 6.82
CHEMBL19 METHAZOLAMIDE 4.0 1 6.77
CHEMBL7204 1 6.66
CHEMBL865 VALDECOXIB 4.0 1 6.62
CHEMBL6724 1 6.55
CHEMBL6853 1 6.38
CHEMBL266240 1 6.21
CHEMBL268177 1 6.18
CHEMBL7092 1 6.13
CHEMBL18 ETHOXZOLAMIDE 4.0 1 6.13
CHEMBL418 2,4-DISULFAMYLTRIFLUOROMETHYLANILINE 1 6.02
CHEMBL118 CELECOXIB 4.0 1 6.00
CHEMBL6852 1 5.91
CHEMBL20 ACETAZOLAMIDE 4.0 1 5.84
CHEMBL218490 DORZOLAMIDE 4.0 1 5.77
CHEMBL68253 SULFAMATE 1 5.47
CHEMBL21 SULFANILAMIDE 4.0 1 5.41
CHEMBL355001 SULFAMIDE 1 5.22
CHEMBL266026 1 5.20
CHEMBL419 MAFENIDE 4.0 1 5.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL220492 TOPIRAMATE Ki = 120.0 nM 6.92
CHEMBL7087 Ki = 130.0 nM 6.89
CHEMBL17 DICHLORPHENAMIDE Ki = 150.0 nM 6.82
CHEMBL19 METHAZOLAMIDE Ki = 170.0 nM 6.77
CHEMBL7204 Ki = 220.0 nM 6.66
CHEMBL865 VALDECOXIB Ki = 240.0 nM 6.62
CHEMBL6724 Ki = 280.0 nM 6.55
CHEMBL6853 Ki = 420.0 nM 6.38
CHEMBL266240 Ki = 610.0 nM 6.21
CHEMBL268177 Ki = 660.0 nM 6.18
CHEMBL7092 Ki = 740.0 nM 6.13
CHEMBL18 ETHOXZOLAMIDE Ki = 740.0 nM 6.13
CHEMBL418 2,4-DISULFAMYLTRIFLUOROMETHYLANILINE Ki = 950.0 nM 6.02
CHEMBL118 CELECOXIB Ki = 1010.0 nM 6.00
CHEMBL6852 Ki = 1240.0 nM 5.91
CHEMBL20 ACETAZOLAMIDE Ki = 1430.0 nM 5.84
CHEMBL218490 DORZOLAMIDE Ki = 1710.0 nM 5.77
CHEMBL68253 SULFAMATE Ki = 3360.0 nM 5.47
CHEMBL21 SULFANILAMIDE Ki = 3930.0 nM 5.41
CHEMBL355001 SULFAMIDE Ki = 5960.0 nM 5.22
CHEMBL266026 Ki = 6360.0 nM 5.20
CHEMBL419 MAFENIDE Ki = 8500.0 nM 5.07