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Assay Detail

CHEMBL839585

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Binding
Inhibitory activity against cytosolic human carbonic anhydrase I
23
Total Activities
23
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 1 (CHEMBL261)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with bis-sulfamates.
Winum JY, Pastorekova S, Jakubickova L, Montero JL, Scozzafava A, Pastorek J, Vullo D, Innocenti A, Supuran CT.
Bioorg Med Chem Lett (2005) 15 : 579 -584
PubMed 15664816 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 6.32 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL18 ETHOXZOLAMIDE 4.0 1 7.60
CHEMBL77517 INDISULAM 2.0 1 7.51
CHEMBL182429 1 7.10
CHEMBL183701 1 7.03
CHEMBL68257 1 6.98
CHEMBL2113026 1 6.97
CHEMBL182276 1 6.87
CHEMBL182440 1 6.84
CHEMBL183240 1 6.57
CHEMBL182455 1 6.42
CHEMBL353258 1 6.26
CHEMBL19 METHAZOLAMIDE 4.0 1 6.11
CHEMBL181357 1 6.06
CHEMBL20 ACETAZOLAMIDE 4.0 1 6.05
CHEMBL171476 1 6.05
CHEMBL17 DICHLORPHENAMIDE 4.0 1 5.92
CHEMBL361421 1 5.87
CHEMBL170139 1 5.19
CHEMBL181753 1 4.78
CHEMBL218490 DORZOLAMIDE 4.0 1 4.30
CHEMBL220491 BRINZOLAMIDE 4.0 1 -
CHEMBL221802 1 -
CHEMBL360714 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL18 ETHOXZOLAMIDE Ki = 25.0 nM 7.60
CHEMBL77517 INDISULAM Ki = 31.0 nM 7.51
CHEMBL182429 Ki = 79.0 nM 7.10
CHEMBL183701 Ki = 93.0 nM 7.03
CHEMBL68257 Ki = 105.0 nM 6.98
CHEMBL2113026 Ki = 108.0 nM 6.97
CHEMBL182276 Ki = 136.0 nM 6.87
CHEMBL182440 Ki = 145.0 nM 6.84
CHEMBL183240 Ki = 267.0 nM 6.57
CHEMBL182455 Ki = 378.0 nM 6.42
CHEMBL353258 Ki = 548.0 nM 6.26
CHEMBL19 METHAZOLAMIDE Ki = 780.0 nM 6.11
CHEMBL181357 Ki = 872.0 nM 6.06
CHEMBL20 ACETAZOLAMIDE Ki = 900.0 nM 6.05
CHEMBL171476 Ki = 890.0 nM 6.05
CHEMBL17 DICHLORPHENAMIDE Ki = 1200.0 nM 5.92
CHEMBL361421 Ki = 1350.0 nM 5.87
CHEMBL170139 Ki = 6490.0 nM 5.19
CHEMBL181753 Ki = 16450.0 nM 4.78
CHEMBL218490 DORZOLAMIDE Ki = 50000.0 nM 4.30
CHEMBL220491 BRINZOLAMIDE Ki - nM -
CHEMBL221802 Ki = 6000.0 nM -
CHEMBL360714 Ki > 20.0 nM -