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Assay Detail

CHEMBL828908

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Binding
Inhibitory constant against human Carbonic anhydrase IX
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 9 (CHEMBL3594)
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 7.84 8.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL196198 1 8.34
CHEMBL195811 1 8.32
CHEMBL195509 1 8.32
CHEMBL365344 1 8.30
CHEMBL195194 1 8.30
CHEMBL196435 1 8.28
CHEMBL193964 1 8.27
CHEMBL362989 1 8.25
CHEMBL196285 1 8.21
CHEMBL195978 1 8.19
CHEMBL195147 1 8.17
CHEMBL364081 1 8.17
CHEMBL7146 1 7.62
CHEMBL77517 INDISULAM 2.0 1 7.62
CHEMBL20 ACETAZOLAMIDE 4.0 1 7.60
CHEMBL19 METHAZOLAMIDE 4.0 1 7.57
CHEMBL266026 1 7.51
CHEMBL7087 1 7.48
CHEMBL269122 1 7.47
CHEMBL18 ETHOXZOLAMIDE 4.0 1 7.47
CHEMBL17 DICHLORPHENAMIDE 4.0 1 7.30
CHEMBL419 MAFENIDE 4.0 1 6.99
CHEMBL21 SULFANILAMIDE 4.0 1 6.53

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL196198 Ki = 4.6 nM 8.34
CHEMBL195811 Ki = 4.8 nM 8.32
CHEMBL195509 Ki = 4.8 nM 8.32
CHEMBL365344 Ki = 5.0 nM 8.30
CHEMBL195194 Ki = 5.0 nM 8.30
CHEMBL196435 Ki = 5.2 nM 8.28
CHEMBL193964 Ki = 5.4 nM 8.27
CHEMBL362989 Ki = 5.6 nM 8.25
CHEMBL196285 Ki = 6.1 nM 8.21
CHEMBL195978 Ki = 6.4 nM 8.19
CHEMBL195147 Ki = 6.7 nM 8.17
CHEMBL364081 Ki = 6.7 nM 8.17
CHEMBL7146 Ki = 24.0 nM 7.62
CHEMBL77517 INDISULAM Ki = 24.0 nM 7.62
CHEMBL20 ACETAZOLAMIDE Ki = 25.0 nM 7.60
CHEMBL19 METHAZOLAMIDE Ki = 27.0 nM 7.57
CHEMBL266026 Ki = 31.0 nM 7.51
CHEMBL7087 Ki = 33.0 nM 7.48
CHEMBL269122 Ki = 34.0 nM 7.47
CHEMBL18 ETHOXZOLAMIDE Ki = 34.0 nM 7.47
CHEMBL17 DICHLORPHENAMIDE Ki = 50.0 nM 7.30
CHEMBL419 MAFENIDE Ki = 103.0 nM 6.99
CHEMBL21 SULFANILAMIDE Ki = 294.0 nM 6.53