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Assay Detail

CHEMBL1031356

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Binding
Inhibition of human recombinant carbonic anhydrase 9 catalytic domain by stopped flow CO2 hydrase assay
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Carbonic anhydrase 9 (CHEMBL3594)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Cloning, expression, post-translational modifications and inhibition studies on the latest mammalian carbonic anhydrase isoform, CA XV.
Hilvo M, Salzano AM, Innocenti A, Kulomaa MS, Scozzafava A, Scaloni A, Parkkila S, Supuran CT.
J Med Chem (2009) 52 : 646 -654
PubMed 19193158 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 38 7.31 8.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL750 ZONISAMIDE 4.0 1 8.29
CHEMBL6685 1 7.85
CHEMBL6633 1 7.80
CHEMBL6919 1 7.68
CHEMBL6784 1 7.66
CHEMBL77517 INDISULAM 2.0 1 7.62
CHEMBL418 2,4-DISULFAMYLTRIFLUOROMETHYLANILINE 1 7.62
CHEMBL7146 1 7.62
CHEMBL20 ACETAZOLAMIDE 4.0 1 7.60
CHEMBL414 CARZENIDE 2.0 1 7.58
CHEMBL865 VALDECOXIB 4.0 1 7.57
CHEMBL19 METHAZOLAMIDE 4.0 1 7.57
CHEMBL360356 1 7.52
CHEMBL6753 1 7.52
CHEMBL266026 1 7.51
CHEMBL6705 1 7.48
CHEMBL7087 1 7.48
CHEMBL18 ETHOXZOLAMIDE 4.0 1 7.47
CHEMBL220491 BRINZOLAMIDE 4.0 1 7.43
CHEMBL456724 1 7.42
CHEMBL266240 1 7.41
CHEMBL265674 1 7.39
CHEMBL328560 SULTHIAME 3.0 1 7.37
CHEMBL26 SULPIRIDE 3.0 1 7.34
CHEMBL73962 BENZOLAMIDE 1 7.33
CHEMBL17 DICHLORPHENAMIDE 4.0 1 7.30
CHEMBL218490 DORZOLAMIDE 4.0 1 7.28
CHEMBL220492 TOPIRAMATE 4.0 1 7.24
CHEMBL419 MAFENIDE 4.0 1 6.99
CHEMBL176495 1 6.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL750 ZONISAMIDE Ki = 5.1 nM 8.29
CHEMBL6685 Ki = 14.0 nM 7.85
CHEMBL6633 Ki = 16.0 nM 7.80
CHEMBL6919 Ki = 21.0 nM 7.68
CHEMBL6784 Ki = 22.0 nM 7.66
CHEMBL77517 INDISULAM Ki = 24.0 nM 7.62
CHEMBL418 2,4-DISULFAMYLTRIFLUOROMETHYLANILINE Ki = 24.0 nM 7.62
CHEMBL7146 Ki = 24.0 nM 7.62
CHEMBL20 ACETAZOLAMIDE Ki = 25.0 nM 7.60
CHEMBL414 CARZENIDE Ki = 26.0 nM 7.58
CHEMBL19 METHAZOLAMIDE Ki = 27.0 nM 7.57
CHEMBL865 VALDECOXIB Ki = 27.0 nM 7.57
CHEMBL360356 Ki = 30.0 nM 7.52
CHEMBL6753 Ki = 30.0 nM 7.52
CHEMBL266026 Ki = 31.0 nM 7.51
CHEMBL6705 Ki = 33.0 nM 7.48
CHEMBL7087 Ki = 33.0 nM 7.48
CHEMBL18 ETHOXZOLAMIDE Ki = 34.0 nM 7.47
CHEMBL220491 BRINZOLAMIDE Ki = 37.0 nM 7.43
CHEMBL456724 Ki = 38.0 nM 7.42
CHEMBL266240 Ki = 39.0 nM 7.41
CHEMBL265674 Ki = 41.0 nM 7.39
CHEMBL328560 SULTHIAME Ki = 43.0 nM 7.37
CHEMBL26 SULPIRIDE Ki = 46.0 nM 7.34
CHEMBL73962 BENZOLAMIDE Ki = 47.0 nM 7.33
CHEMBL17 DICHLORPHENAMIDE Ki = 50.0 nM 7.30
CHEMBL218490 DORZOLAMIDE Ki = 52.0 nM 7.28
CHEMBL220492 TOPIRAMATE Ki = 58.0 nM 7.24
CHEMBL419 MAFENIDE Ki = 103.0 nM 6.99
CHEMBL176495 Ki = 176.0 nM 6.75
CHEMBL21 SULFANILAMIDE Ki = 238.0 nM 6.62
CHEMBL6853 Ki = 245.0 nM 6.61
CHEMBL7092 Ki = 264.0 nM 6.58
CHEMBL6724 Ki = 269.0 nM 6.57
CHEMBL268177 Ki = 285.0 nM 6.54
CHEMBL7204 Ki = 294.0 nM 6.53
CHEMBL574 P-TOLUENESULFONAMIDE Ki = 460.0 nM 6.34
CHEMBL118 CELECOXIB Ki = 16.0 nM -