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Assay Detail

CHEMBL830081

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition constant against human (cloned) isozyme (hCA II) by CO2 hydration method
17
Total Activities
17
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 fluorescent sulfonamides as probes of tumor-associated carbonic anhydrase IX that inhibit isozyme IX-mediated acidification of hypoxic tumors.
Cecchi A, Hulikova A, Pastorek J, Pastoreková S, Scozzafava A, Winum JY, Montero JL, Supuran CT.
J Med Chem (2005) 48 : 4834 -4841
PubMed 16033263 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 7.47 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL18 ETHOXZOLAMIDE 4.0 1 8.10
CHEMBL20 ACETAZOLAMIDE 4.0 1 7.92
CHEMBL19 METHAZOLAMIDE 4.0 1 7.85
CHEMBL77517 INDISULAM 2.0 1 7.82
CHEMBL361496 1 7.57
CHEMBL360604 1 7.47
CHEMBL17 DICHLORPHENAMIDE 4.0 1 7.42
CHEMBL187947 1 7.40
CHEMBL191109 1 7.39
CHEMBL187919 1 7.37
CHEMBL372888 1 7.36
CHEMBL186522 1 7.35
CHEMBL187974 1 7.33
CHEMBL188750 1 7.30
CHEMBL188002 1 7.28
CHEMBL366082 1 7.28
CHEMBL7087 1 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL18 ETHOXZOLAMIDE Ki = 8.0 nM 8.10
CHEMBL20 ACETAZOLAMIDE Ki = 12.0 nM 7.92
CHEMBL19 METHAZOLAMIDE Ki = 14.0 nM 7.85
CHEMBL77517 INDISULAM Ki = 15.0 nM 7.82
CHEMBL361496 Ki = 27.0 nM 7.57
CHEMBL360604 Ki = 34.0 nM 7.47
CHEMBL17 DICHLORPHENAMIDE Ki = 38.0 nM 7.42
CHEMBL187947 Ki = 40.0 nM 7.40
CHEMBL191109 Ki = 41.0 nM 7.39
CHEMBL187919 Ki = 43.0 nM 7.37
CHEMBL372888 Ki = 44.0 nM 7.36
CHEMBL186522 Ki = 45.0 nM 7.35
CHEMBL187974 Ki = 47.0 nM 7.33
CHEMBL188750 Ki = 50.0 nM 7.30
CHEMBL188002 Ki = 52.0 nM 7.28
CHEMBL366082 Ki = 52.0 nM 7.28
CHEMBL7087 Ki = 160.0 nM 6.80