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Assay Detail

CHEMBL4391785

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Binding
Inhibition of human CA 12 catalytic domain
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Carbonic anhydrase 12 (CHEMBL3242)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Pyridazinone-substituted benzenesulfonamides display potent inhibition of membrane-bound human carbonic anhydrase IX and promising antiproliferative activity against cancer cell lines.
Krasavin M, Shetnev A, Baykov S, Kalinin S, Nocentini A, Sharoyko V, Poli G, Tuccinardi T, Korsakov M, Tennikova TB, Supuran CT.
Eur J Med Chem (2019) 168 : 301 -314
PubMed 30826507 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 8.44 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL77517 INDISULAM 2.0 1 8.52
CHEMBL220491 BRINZOLAMIDE 4.0 1 8.52
CHEMBL19 METHAZOLAMIDE 4.0 1 8.47
CHEMBL218490 DORZOLAMIDE 4.0 1 8.46
CHEMBL20 ACETAZOLAMIDE 4.0 1 8.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL77517 INDISULAM Ki = 3.0 nM 8.52
CHEMBL220491 BRINZOLAMIDE Ki = 3.0 nM 8.52
CHEMBL19 METHAZOLAMIDE Ki = 3.4 nM 8.47
CHEMBL218490 DORZOLAMIDE Ki = 3.5 nM 8.46
CHEMBL20 ACETAZOLAMIDE Ki = 5.7 nM 8.24