Assay Detail

CHEMBL864594

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Binding

Inhibitory activity against cloned human CA12

ChEMBL ↗

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Target

Carbonic anhydrase 12 (CHEMBL3242) ↗

Open DB target context

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Carbonic anhydrase 12 (CHEMBL3242) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Carbonic anhydrase 12

CHEMBL3242

Anchored from Assay target.

Protein identity Carbonic anhydrase 12

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

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

Target

Carbonic anhydrase 12 (CHEMBL3242) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Carbonic anhydrase inhibitors: Valdecoxib binds to a different active site region of the human isoform II as compared to the structurally related cyclooxygenase II "selective" inhibitor celecoxib.

Di Fiore A, Pedone C, D'Ambrosio K, Scozzafava A, De Simone G, Supuran CT.
Bioorg Med Chem Lett (2006) 16 : 437 -442
PubMed 16290146 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
Ki	6	8.02	8.47

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL19	METHAZOLAMIDE	4.0	1	8.47
CHEMBL218490	DORZOLAMIDE	4.0	1	8.46
CHEMBL20	ACETAZOLAMIDE	4.0	1	8.24
CHEMBL865	VALDECOXIB	4.0	1	7.89
CHEMBL118	CELECOXIB	4.0	1	7.75
CHEMBL17	DICHLORPHENAMIDE	4.0	1	7.30

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL19	METHAZOLAMIDE	Ki	=	3.4	nM	8.47
CHEMBL218490	DORZOLAMIDE	Ki	=	3.5	nM	8.46
CHEMBL20	ACETAZOLAMIDE	Ki	=	5.7	nM	8.24
CHEMBL865	VALDECOXIB	Ki	=	13.0	nM	7.89
CHEMBL118	CELECOXIB	Ki	=	18.0	nM	7.75
CHEMBL17	DICHLORPHENAMIDE	Ki	=	50.0	nM	7.30