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Assay Detail

CHEMBL873716

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Binding
Inhibitory activity against human carbonic anhydrase I
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Carbonic anhydrase 1 (CHEMBL261)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Carbonic anhydrase inhibitors: inhibition of the tumor-associated isozyme IX with fluorine-containing sulfonamides. The first subnanomolar CA IX inhibitor discovered.
Vullo D, Scozzafava A, Pastorekova S, Pastorek J, Supuran CT.
Bioorg Med Chem Lett (2004) 14 : 2351 -2356
PubMed 15081039 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 6.08 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL307939 1 7.89
CHEMBL18 ETHOXZOLAMIDE 4.0 1 7.60
CHEMBL77517 INDISULAM 2.0 1 7.51
CHEMBL75855 1 6.60
CHEMBL76607 1 6.57
CHEMBL74491 1 6.12
CHEMBL305726 1 6.12
CHEMBL19 METHAZOLAMIDE 4.0 1 6.11
CHEMBL265534 1 6.07
CHEMBL77284 1 6.05
CHEMBL20 ACETAZOLAMIDE 4.0 1 6.05
CHEMBL308631 1 6.01
CHEMBL76563 1 6.01
CHEMBL309592 1 5.97
CHEMBL17 DICHLORPHENAMIDE 4.0 1 5.92
CHEMBL75747 1 5.82
CHEMBL76956 1 5.77
CHEMBL75620 1 5.73
CHEMBL76626 1 5.22
CHEMBL306118 1 5.21
CHEMBL77359 1 5.20
CHEMBL218490 DORZOLAMIDE 4.0 1 4.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL307939 Ki = 13.0 nM 7.89
CHEMBL18 ETHOXZOLAMIDE Ki = 25.0 nM 7.60
CHEMBL77517 INDISULAM Ki = 31.0 nM 7.51
CHEMBL75855 Ki = 250.0 nM 6.60
CHEMBL76607 Ki = 270.0 nM 6.57
CHEMBL74491 Ki = 760.0 nM 6.12
CHEMBL305726 Ki = 750.0 nM 6.12
CHEMBL19 METHAZOLAMIDE Ki = 780.0 nM 6.11
CHEMBL265534 Ki = 860.0 nM 6.07
CHEMBL77284 Ki = 900.0 nM 6.05
CHEMBL20 ACETAZOLAMIDE Ki = 900.0 nM 6.05
CHEMBL308631 Ki = 980.0 nM 6.01
CHEMBL76563 Ki = 975.0 nM 6.01
CHEMBL309592 Ki = 1080.0 nM 5.97
CHEMBL17 DICHLORPHENAMIDE Ki = 1200.0 nM 5.92
CHEMBL75747 Ki = 1500.0 nM 5.82
CHEMBL76956 Ki = 1700.0 nM 5.77
CHEMBL75620 Ki = 1870.0 nM 5.73
CHEMBL76626 Ki = 6000.0 nM 5.22
CHEMBL306118 Ki = 6100.0 nM 5.21
CHEMBL77359 Ki = 6300.0 nM 5.20
CHEMBL218490 DORZOLAMIDE Ki = 50000.0 nM 4.30