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Assay Detail

CHEMBL841779

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Binding
Inhibitory activity against human carbonic anhydrase II
30
Total Activities
30
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: design of thioureido sulfonamides with potent isozyme II and XII inhibitory properties and intraocular pressure lowering activity in a rabbit model of glaucoma.
Mincione F, Starnotti M, Masini E, Bacciottini L, Scrivanti C, Casini A, Vullo D, Scozzafava A, Supuran CT.
Bioorg Med Chem Lett (2005) 15 : 3821 -3827
PubMed 16039853 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 30 7.72 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL220491 BRINZOLAMIDE 4.0 1 8.52
CHEMBL179355 1 8.22
CHEMBL181082 1 8.22
CHEMBL180177 THIOUREIDO SULFONAMIDE 1 8.15
CHEMBL178403 1 8.15
CHEMBL178560 1 8.10
CHEMBL18 ETHOXZOLAMIDE 4.0 1 8.10
CHEMBL538564 1 8.05
CHEMBL218490 DORZOLAMIDE 4.0 1 8.05
CHEMBL182197 1 8.00
CHEMBL181422 1 7.96
CHEMBL180506 1 7.92
CHEMBL20 ACETAZOLAMIDE 4.0 1 7.92
CHEMBL182135 1 7.89
CHEMBL181825 1 7.89
CHEMBL178603 1 7.85
CHEMBL19 METHAZOLAMIDE 4.0 1 7.85
CHEMBL180936 1 7.80
CHEMBL361955 1 7.75
CHEMBL362636 1 7.72
CHEMBL361827 1 7.60
CHEMBL413357 1 7.57
CHEMBL179218 1 7.48
CHEMBL17 DICHLORPHENAMIDE 4.0 1 7.42
CHEMBL360254 1 7.32
CHEMBL181716 1 7.12
CHEMBL178664 THIOUREIDO SULFONAMIDE 1 6.82
CHEMBL180195 1 6.80
CHEMBL180675 THIOUREIDO SULFONAMIDE 1 6.73
CHEMBL21 SULFANILAMIDE 4.0 1 6.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL220491 BRINZOLAMIDE Ki = 3.0 nM 8.52
CHEMBL179355 Ki = 6.0 nM 8.22
CHEMBL181082 Ki = 6.0 nM 8.22
CHEMBL180177 THIOUREIDO SULFONAMIDE Ki = 7.0 nM 8.15
CHEMBL178403 Ki = 7.0 nM 8.15
CHEMBL178560 Ki = 8.0 nM 8.10
CHEMBL18 ETHOXZOLAMIDE Ki = 8.0 nM 8.10
CHEMBL538564 Ki = 9.0 nM 8.05
CHEMBL218490 DORZOLAMIDE Ki = 9.0 nM 8.05
CHEMBL182197 Ki = 10.0 nM 8.00
CHEMBL181422 Ki = 11.0 nM 7.96
CHEMBL180506 Ki = 12.0 nM 7.92
CHEMBL20 ACETAZOLAMIDE Ki = 12.0 nM 7.92
CHEMBL182135 Ki = 13.0 nM 7.89
CHEMBL181825 Ki = 13.0 nM 7.89
CHEMBL178603 Ki = 14.0 nM 7.85
CHEMBL19 METHAZOLAMIDE Ki = 14.0 nM 7.85
CHEMBL180936 Ki = 16.0 nM 7.80
CHEMBL361955 Ki = 18.0 nM 7.75
CHEMBL362636 Ki = 19.0 nM 7.72
CHEMBL361827 Ki = 25.0 nM 7.60
CHEMBL413357 Ki = 27.0 nM 7.57
CHEMBL179218 Ki = 33.0 nM 7.48
CHEMBL17 DICHLORPHENAMIDE Ki = 38.0 nM 7.42
CHEMBL360254 Ki = 48.0 nM 7.32
CHEMBL181716 Ki = 75.0 nM 7.12
CHEMBL178664 THIOUREIDO SULFONAMIDE Ki = 150.0 nM 6.82
CHEMBL180195 Ki = 159.0 nM 6.80
CHEMBL180675 THIOUREIDO SULFONAMIDE Ki = 185.0 nM 6.73
CHEMBL21 SULFANILAMIDE Ki = 300.0 nM 6.52