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Assay Detail

CHEMBL657150

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Binding
Inhibition of human carbonic anhydrase II
31
Total Activities
31
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 the tumor-associated isozyme IX with aromatic and heterocyclic sulfonamides.
Vullo D, Franchi M, Gallori E, Pastorek J, Scozzafava A, Pastorekova S, Supuran CT.
Bioorg Med Chem Lett (2003) 13 : 1005 -1009
PubMed 12643899 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 31 7.31 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL268439 1 8.70
CHEMBL18 ETHOXZOLAMIDE 4.0 1 8.10
CHEMBL6685 1 8.10
CHEMBL218490 DORZOLAMIDE 4.0 1 8.05
CHEMBL20 ACETAZOLAMIDE 4.0 1 7.92
CHEMBL6633 1 7.92
CHEMBL19 METHAZOLAMIDE 4.0 1 7.85
CHEMBL6753 1 7.72
CHEMBL7146 1 7.52
CHEMBL266026 1 7.48
CHEMBL17 DICHLORPHENAMIDE 4.0 1 7.42
CHEMBL414 CARZENIDE 2.0 1 7.40
CHEMBL6724 1 7.40
CHEMBL269122 1 7.34
CHEMBL6946 1 7.30
CHEMBL265674 1 7.22
CHEMBL6853 1 7.22
CHEMBL418 2,4-DISULFAMYLTRIFLUOROMETHYLANILINE 1 7.20
CHEMBL268177 1 7.16
CHEMBL266240 1 7.12
CHEMBL6784 1 6.96
CHEMBL7092 1 6.96
CHEMBL268809 1 6.90
CHEMBL6919 1 6.90
CHEMBL6648 1 6.88
CHEMBL7087 1 6.80
CHEMBL419 MAFENIDE 4.0 1 6.77
CHEMBL6852 1 6.62
CHEMBL6705 1 6.53
CHEMBL21 SULFANILAMIDE 4.0 1 6.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL268439 Ki = 2.0 nM 8.70
CHEMBL18 ETHOXZOLAMIDE Ki = 8.0 nM 8.10
CHEMBL6685 Ki = 8.0 nM 8.10
CHEMBL218490 DORZOLAMIDE Ki = 9.0 nM 8.05
CHEMBL20 ACETAZOLAMIDE Ki = 12.0 nM 7.92
CHEMBL6633 Ki = 12.0 nM 7.92
CHEMBL19 METHAZOLAMIDE Ki = 14.0 nM 7.85
CHEMBL6753 Ki = 19.0 nM 7.72
CHEMBL7146 Ki = 30.0 nM 7.52
CHEMBL266026 Ki = 33.0 nM 7.48
CHEMBL17 DICHLORPHENAMIDE Ki = 38.0 nM 7.42
CHEMBL414 CARZENIDE Ki = 40.0 nM 7.40
CHEMBL6724 Ki = 40.0 nM 7.40
CHEMBL269122 Ki = 46.0 nM 7.34
CHEMBL6946 Ki = 50.0 nM 7.30
CHEMBL265674 Ki = 60.0 nM 7.22
CHEMBL6853 Ki = 60.0 nM 7.22
CHEMBL418 2,4-DISULFAMYLTRIFLUOROMETHYLANILINE Ki = 63.0 nM 7.20
CHEMBL268177 Ki = 70.0 nM 7.16
CHEMBL266240 Ki = 75.0 nM 7.12
CHEMBL6784 Ki = 110.0 nM 6.96
CHEMBL7092 Ki = 110.0 nM 6.96
CHEMBL268809 Ki = 125.0 nM 6.90
CHEMBL6919 Ki = 125.0 nM 6.90
CHEMBL6648 Ki = 133.0 nM 6.88
CHEMBL7087 Ki = 160.0 nM 6.80
CHEMBL419 MAFENIDE Ki = 170.0 nM 6.77
CHEMBL6852 Ki = 240.0 nM 6.62
CHEMBL6705 Ki = 295.0 nM 6.53
CHEMBL21 SULFANILAMIDE Ki = 300.0 nM 6.52
CHEMBL7204 Ki = 320.0 nM 6.50