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Assay Detail

CHEMBL932210

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

Binding
Inhibition of human recombinant CA12 by CO2 hydration stopped flow assay
15
Total Activities
15
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

Carbonic anhydrase inhibitors: copper(II) complexes of polyamino-polycarboxylamido aromatic/heterocyclic sulfonamides are very potent inhibitors of the tumor-associated isoforms IX and XII.
Rami M, Winum JY, Innocenti A, Montero JL, Scozzafava A, Supuran CT.
Bioorg Med Chem Lett (2008) 18 : 836 -841
PubMed 18042384 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 8.16 8.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL34546 1 8.68
CHEMBL432083 1 8.55
CHEMBL34526 1 8.55
CHEMBL285436 1 8.52
CHEMBL34016 1 8.49
CHEMBL19 METHAZOLAMIDE 4.0 1 8.47
CHEMBL286862 1 8.41
CHEMBL286449 1 8.40
CHEMBL284694 1 8.36
CHEMBL285962 1 8.32
CHEMBL20 ACETAZOLAMIDE 4.0 1 8.24
CHEMBL287145 1 8.17
CHEMBL18 ETHOXZOLAMIDE 4.0 1 7.66
CHEMBL21 SULFANILAMIDE 4.0 1 7.43
CHEMBL310671 SACCHARIN 3.0 1 6.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL34546 Ki = 2.1 nM 8.68
CHEMBL432083 Ki = 2.8 nM 8.55
CHEMBL34526 Ki = 2.8 nM 8.55
CHEMBL285436 Ki = 3.0 nM 8.52
CHEMBL34016 Ki = 3.2 nM 8.49
CHEMBL19 METHAZOLAMIDE Ki = 3.4 nM 8.47
CHEMBL286862 Ki = 3.9 nM 8.41
CHEMBL286449 Ki = 4.0 nM 8.40
CHEMBL284694 Ki = 4.4 nM 8.36
CHEMBL285962 Ki = 4.8 nM 8.32
CHEMBL20 ACETAZOLAMIDE Ki = 5.7 nM 8.24
CHEMBL287145 Ki = 6.8 nM 8.17
CHEMBL18 ETHOXZOLAMIDE Ki = 22.0 nM 7.66
CHEMBL21 SULFANILAMIDE Ki = 37.0 nM 7.43
CHEMBL310671 SACCHARIN Ki = 633.0 nM 6.20