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Assay Detail

CHEMBL838677

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Binding
Inhibitory activity against cytosolic human carbonic anhydrase II
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 2 (CHEMBL205)
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 7.61 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL220491 BRINZOLAMIDE 4.0 1 8.52
CHEMBL221802 1 8.30
CHEMBL183701 1 8.22
CHEMBL182440 1 8.10
CHEMBL18 ETHOXZOLAMIDE 4.0 1 8.10
CHEMBL182276 1 8.08
CHEMBL218490 DORZOLAMIDE 4.0 1 8.05
CHEMBL182429 1 8.03
CHEMBL353258 1 8.01
CHEMBL20 ACETAZOLAMIDE 4.0 1 7.92
CHEMBL19 METHAZOLAMIDE 4.0 1 7.85
CHEMBL182455 1 7.84
CHEMBL2113026 1 7.83
CHEMBL77517 INDISULAM 2.0 1 7.82
CHEMBL183240 1 7.82
CHEMBL171476 1 7.61
CHEMBL17 DICHLORPHENAMIDE 4.0 1 7.42
CHEMBL68257 1 7.12
CHEMBL361421 1 7.08
CHEMBL181357 1 6.42
CHEMBL170139 1 6.38
CHEMBL181753 1 6.25
CHEMBL360714 1 6.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL220491 BRINZOLAMIDE Ki = 3.0 nM 8.52
CHEMBL221802 Ki = 5.0 nM 8.30
CHEMBL183701 Ki = 6.0 nM 8.22
CHEMBL182440 Ki = 8.0 nM 8.10
CHEMBL18 ETHOXZOLAMIDE Ki = 8.0 nM 8.10
CHEMBL182276 Ki = 8.3 nM 8.08
CHEMBL218490 DORZOLAMIDE Ki = 9.0 nM 8.05
CHEMBL182429 Ki = 9.4 nM 8.03
CHEMBL353258 Ki = 9.7 nM 8.01
CHEMBL20 ACETAZOLAMIDE Ki = 12.0 nM 7.92
CHEMBL19 METHAZOLAMIDE Ki = 14.0 nM 7.85
CHEMBL182455 Ki = 14.6 nM 7.84
CHEMBL2113026 Ki = 14.7 nM 7.83
CHEMBL77517 INDISULAM Ki = 15.0 nM 7.82
CHEMBL183240 Ki = 15.0 nM 7.82
CHEMBL171476 Ki = 24.5 nM 7.61
CHEMBL17 DICHLORPHENAMIDE Ki = 38.0 nM 7.42
CHEMBL68257 Ki = 76.3 nM 7.12
CHEMBL361421 Ki = 84.2 nM 7.08
CHEMBL181357 Ki = 380.0 nM 6.42
CHEMBL170139 Ki = 417.0 nM 6.38
CHEMBL181753 Ki = 563.0 nM 6.25
CHEMBL360714 Ki = 643.0 nM 6.19