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Assay Detail

CHEMBL828905

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Binding
Inhibitory constant against human Carbonic anhydrase II
23
Total Activities
23
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: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides incorporating thioureido-sulfanilyl scaffolds.
Puccetti L, Fasolis G, Cecchi A, Winum JY, Gamberi A, Montero JL, Scozzafava A, Supuran CT.
Bioorg Med Chem Lett (2005) 15 : 2359 -2364
PubMed 15837325 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 7.32 8.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL195509 1 8.14
CHEMBL18 ETHOXZOLAMIDE 4.0 1 8.10
CHEMBL364081 1 8.09
CHEMBL196285 1 8.00
CHEMBL195194 1 7.99
CHEMBL20 ACETAZOLAMIDE 4.0 1 7.92
CHEMBL193964 1 7.92
CHEMBL19 METHAZOLAMIDE 4.0 1 7.85
CHEMBL77517 INDISULAM 2.0 1 7.82
CHEMBL7146 1 7.52
CHEMBL266026 1 7.48
CHEMBL17 DICHLORPHENAMIDE 4.0 1 7.42
CHEMBL269122 1 7.34
CHEMBL196198 1 7.34
CHEMBL7087 1 6.80
CHEMBL419 MAFENIDE 4.0 1 6.77
CHEMBL362989 1 6.75
CHEMBL195811 1 6.66
CHEMBL195978 1 6.56
CHEMBL195147 1 6.54
CHEMBL196435 1 6.54
CHEMBL21 SULFANILAMIDE 4.0 1 6.52
CHEMBL365344 1 6.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL195509 Ki = 7.2 nM 8.14
CHEMBL18 ETHOXZOLAMIDE Ki = 8.0 nM 8.10
CHEMBL364081 Ki = 8.1 nM 8.09
CHEMBL196285 Ki = 10.1 nM 8.00
CHEMBL195194 Ki = 10.3 nM 7.99
CHEMBL20 ACETAZOLAMIDE Ki = 12.0 nM 7.92
CHEMBL193964 Ki = 12.0 nM 7.92
CHEMBL19 METHAZOLAMIDE Ki = 14.0 nM 7.85
CHEMBL77517 INDISULAM Ki = 15.0 nM 7.82
CHEMBL7146 Ki = 30.0 nM 7.52
CHEMBL266026 Ki = 33.0 nM 7.48
CHEMBL17 DICHLORPHENAMIDE Ki = 38.0 nM 7.42
CHEMBL269122 Ki = 46.0 nM 7.34
CHEMBL196198 Ki = 46.0 nM 7.34
CHEMBL7087 Ki = 160.0 nM 6.80
CHEMBL419 MAFENIDE Ki = 170.0 nM 6.77
CHEMBL362989 Ki = 180.0 nM 6.75
CHEMBL195811 Ki = 220.0 nM 6.66
CHEMBL195978 Ki = 278.0 nM 6.56
CHEMBL195147 Ki = 290.0 nM 6.54
CHEMBL196435 Ki = 290.0 nM 6.54
CHEMBL21 SULFANILAMIDE Ki = 300.0 nM 6.52
CHEMBL365344 Ki = 640.0 nM 6.19