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Assay Detail

CHEMBL658045

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Binding
Inhibitory activity against human cloned isoenzyme carbonic anhydrase II (hCA II), by esterase method.
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Carbonic anhydrase 2 (CHEMBL205)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Carbonic anhydrase inhibitors: inhibition of cytosolic isozymes I and II with sulfamide derivatives.
Casini A, Winum JY, Montero JL, Scozzafava A, Supuran CT.
Bioorg Med Chem Lett (2003) 13 : 837 -840
PubMed 12617903 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 32 7.36 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL167179 1 8.15
CHEMBL18 ETHOXZOLAMIDE 4.0 1 8.10
CHEMBL218490 DORZOLAMIDE 4.0 1 8.05
CHEMBL165878 1 7.96
CHEMBL168514 PHENYLSULFAMIDE 1 7.92
CHEMBL353767 1 7.92
CHEMBL20 ACETAZOLAMIDE 4.0 1 7.92
CHEMBL168778 1 7.89
CHEMBL168511 1 7.89
CHEMBL19 METHAZOLAMIDE 4.0 1 7.85
CHEMBL167048 1 7.82
CHEMBL166340 1 7.80
CHEMBL166446 1 7.77
CHEMBL166708 1 7.72
CHEMBL166686 1 7.68
CHEMBL354323 1 7.68
CHEMBL444608 1 7.57
CHEMBL169486 1 7.50
CHEMBL168910 1 7.44
CHEMBL17 DICHLORPHENAMIDE 4.0 1 7.42
CHEMBL168898 1 7.31
CHEMBL168526 1 6.91
CHEMBL165939 1 6.88
CHEMBL169370 1 6.83
CHEMBL170015 1 6.83
CHEMBL352592 1 6.35
CHEMBL355349 1 6.19
CHEMBL355555 1 6.05
CHEMBL355001 SULFAMIDE 1 4.09
CHEMBL166788 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL167179 Ki = 7.0 nM 8.15
CHEMBL18 ETHOXZOLAMIDE Ki = 8.0 nM 8.10
CHEMBL218490 DORZOLAMIDE Ki = 9.0 nM 8.05
CHEMBL165878 Ki = 11.0 nM 7.96
CHEMBL168514 PHENYLSULFAMIDE Ki = 12.0 nM 7.92
CHEMBL353767 Ki = 12.0 nM 7.92
CHEMBL20 ACETAZOLAMIDE Ki = 12.0 nM 7.92
CHEMBL168778 Ki = 13.0 nM 7.89
CHEMBL168511 Ki = 13.0 nM 7.89
CHEMBL19 METHAZOLAMIDE Ki = 14.0 nM 7.85
CHEMBL167048 Ki = 15.0 nM 7.82
CHEMBL166340 Ki = 16.0 nM 7.80
CHEMBL166446 Ki = 17.0 nM 7.77
CHEMBL166708 Ki = 19.0 nM 7.72
CHEMBL354323 Ki = 21.0 nM 7.68
CHEMBL166686 Ki = 21.0 nM 7.68
CHEMBL444608 Ki = 27.0 nM 7.57
CHEMBL169486 Ki = 32.0 nM 7.50
CHEMBL168910 Ki = 36.0 nM 7.44
CHEMBL17 DICHLORPHENAMIDE Ki = 38.0 nM 7.42
CHEMBL168898 Ki = 49.0 nM 7.31
CHEMBL168526 Ki = 123.0 nM 6.91
CHEMBL165939 Ki = 131.0 nM 6.88
CHEMBL169370 Ki = 148.0 nM 6.83
CHEMBL170015 Ki = 148.0 nM 6.83
CHEMBL352592 Ki = 450.0 nM 6.35
CHEMBL355349 Ki = 647.0 nM 6.19
CHEMBL355555 Ki = 890.0 nM 6.05
CHEMBL355001 SULFAMIDE Ki = 82000.0 nM 4.09
CHEMBL166788 Ki > 100000.0 nM -
CHEMBL355690 Ki > 100000.0 nM -
CHEMBL168408 Ki > 100000.0 nM -