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Assay Detail

CHEMBL829116

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Binding
Inhibitory activity against membrane bound tumor associated human carbonic anhydrase IX
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 9 (CHEMBL3594)
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 7.21 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL182455 1 8.40
CHEMBL171476 1 8.15
CHEMBL183701 1 8.02
CHEMBL182440 1 8.00
CHEMBL182276 1 7.88
CHEMBL77517 INDISULAM 2.0 1 7.62
CHEMBL20 ACETAZOLAMIDE 4.0 1 7.60
CHEMBL19 METHAZOLAMIDE 4.0 1 7.57
CHEMBL2113026 1 7.55
CHEMBL361421 1 7.49
CHEMBL18 ETHOXZOLAMIDE 4.0 1 7.47
CHEMBL220491 BRINZOLAMIDE 4.0 1 7.43
CHEMBL68257 1 7.37
CHEMBL17 DICHLORPHENAMIDE 4.0 1 7.30
CHEMBL218490 DORZOLAMIDE 4.0 1 7.28
CHEMBL221802 1 7.24
CHEMBL360714 1 7.21
CHEMBL183240 1 7.15
CHEMBL182429 1 7.00
CHEMBL181753 1 6.28
CHEMBL170139 1 5.88
CHEMBL181357 1 5.70
CHEMBL353258 1 4.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL182455 Ki = 4.0 nM 8.40
CHEMBL171476 Ki = 7.0 nM 8.15
CHEMBL183701 Ki = 9.6 nM 8.02
CHEMBL182440 Ki = 10.1 nM 8.00
CHEMBL182276 Ki = 13.2 nM 7.88
CHEMBL77517 INDISULAM Ki = 24.0 nM 7.62
CHEMBL20 ACETAZOLAMIDE Ki = 25.0 nM 7.60
CHEMBL19 METHAZOLAMIDE Ki = 27.0 nM 7.57
CHEMBL2113026 Ki = 28.0 nM 7.55
CHEMBL361421 Ki = 32.1 nM 7.49
CHEMBL18 ETHOXZOLAMIDE Ki = 34.0 nM 7.47
CHEMBL220491 BRINZOLAMIDE Ki = 37.0 nM 7.43
CHEMBL68257 Ki = 43.1 nM 7.37
CHEMBL17 DICHLORPHENAMIDE Ki = 50.0 nM 7.30
CHEMBL218490 DORZOLAMIDE Ki = 52.0 nM 7.28
CHEMBL221802 Ki = 58.0 nM 7.24
CHEMBL360714 Ki = 61.6 nM 7.21
CHEMBL183240 Ki = 70.8 nM 7.15
CHEMBL182429 Ki = 100.0 nM 7.00
CHEMBL181753 Ki = 525.0 nM 6.28
CHEMBL170139 Ki = 1320.0 nM 5.88
CHEMBL181357 Ki = 2020.0 nM 5.70
CHEMBL353258 Ki = 54000.0 nM 4.27