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Assay Detail

CHEMBL932209

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

Binding
Inhibition of human recombinant CA9 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 9 (CHEMBL3594)
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 7.80 8.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL285436 1 8.14
CHEMBL286862 1 8.12
CHEMBL34016 1 8.11
CHEMBL285962 1 8.10
CHEMBL34526 1 8.09
CHEMBL432083 1 8.08
CHEMBL284694 1 8.08
CHEMBL34546 1 8.07
CHEMBL286449 1 8.06
CHEMBL287145 1 8.02
CHEMBL20 ACETAZOLAMIDE 4.0 1 7.60
CHEMBL19 METHAZOLAMIDE 4.0 1 7.57
CHEMBL18 ETHOXZOLAMIDE 4.0 1 7.47
CHEMBL310671 SACCHARIN 3.0 1 6.99
CHEMBL21 SULFANILAMIDE 4.0 1 6.53

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL285436 Ki = 7.3 nM 8.14
CHEMBL286862 Ki = 7.5 nM 8.12
CHEMBL34016 Ki = 7.8 nM 8.11
CHEMBL285962 Ki = 7.9 nM 8.10
CHEMBL34526 Ki = 8.2 nM 8.09
CHEMBL432083 Ki = 8.3 nM 8.08
CHEMBL284694 Ki = 8.4 nM 8.08
CHEMBL34546 Ki = 8.5 nM 8.07
CHEMBL286449 Ki = 8.7 nM 8.06
CHEMBL287145 Ki = 9.6 nM 8.02
CHEMBL20 ACETAZOLAMIDE Ki = 25.0 nM 7.60
CHEMBL19 METHAZOLAMIDE Ki = 27.0 nM 7.57
CHEMBL18 ETHOXZOLAMIDE Ki = 34.0 nM 7.47
CHEMBL310671 SACCHARIN Ki = 103.0 nM 6.99
CHEMBL21 SULFANILAMIDE Ki = 294.0 nM 6.53