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Assay Detail

CHEMBL861560

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Binding
Inhibition of Helicobacter pylori recombinant carbonic anhydrase by stopped-flow CO2 hydrase assay
ChEMBL ↗
47
Total Activities
47
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Carbonic anhydrase (CHEMBL4211) ↗
Type SINGLE PROTEIN
Organism Helicobacter pylori (strain ATCC 700392 / 26695) (Campylobacterpylori)

Publication

Carbonic anhydrase inhibitors: DNA cloning and inhibition studies of the alpha-carbonic anhydrase from Helicobacter pylori, a new target for developing sulfonamide and sulfamate gastric drugs.
Nishimori I, Minakuchi T, Morimoto K, Sano S, Onishi S, Takeuchi H, Vullo D, Scozzafava A, Supuran CT.
J Med Chem (2006) 49 : 2117 -2126
PubMed 16539401 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 47 6.64 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL206295 — — 1 7.92
CHEMBL206657 — — 1 7.89
CHEMBL20 ACETAZOLAMIDE 4.0 1 7.68
CHEMBL204049 — — 1 7.57
CHEMBL204954 — — 1 7.51
CHEMBL266240 — — 1 7.31
CHEMBL204077 — — 1 7.29
CHEMBL203498 — — 1 7.22
CHEMBL381544 — — 1 7.21
CHEMBL425044 — — 1 7.10
CHEMBL6633 — — 1 7.08
CHEMBL360356 — — 1 6.98
CHEMBL7146 — — 1 6.94
CHEMBL266026 — — 1 6.88
CHEMBL220492 TOPIRAMATE 4.0 1 6.76
CHEMBL18 ETHOXZOLAMIDE 4.0 1 6.71
CHEMBL26 SULPIRIDE 3.0 1 6.69
CHEMBL6685 — — 1 6.68
CHEMBL220491 BRINZOLAMIDE 4.0 1 6.68
CHEMBL19 METHAZOLAMIDE 4.0 1 6.65
CHEMBL750 ZONISAMIDE 4.0 1 6.64
CHEMBL268439 — — 1 6.57
CHEMBL73962 BENZOLAMIDE — 1 6.50
CHEMBL206261 — — 1 6.50
CHEMBL7204 — — 1 6.50
CHEMBL203112 — — 1 6.50
CHEMBL265674 — — 1 6.49
CHEMBL7092 — — 1 6.42
CHEMBL17 DICHLORPHENAMIDE 4.0 1 6.42
CHEMBL418 2,4-DISULFAMYLTRIFLUOROMETHYLANILINE — 1 6.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL206295 — Ki = 12.0 nM 7.92
CHEMBL206657 — Ki = 13.0 nM 7.89
CHEMBL20 ACETAZOLAMIDE Ki = 21.0 nM 7.68
CHEMBL204049 — Ki = 27.0 nM 7.57
CHEMBL204954 — Ki = 31.0 nM 7.51
CHEMBL266240 — Ki = 49.0 nM 7.31
CHEMBL204077 — Ki = 51.0 nM 7.29
CHEMBL203498 — Ki = 60.0 nM 7.22
CHEMBL381544 — Ki = 62.0 nM 7.21
CHEMBL425044 — Ki = 79.0 nM 7.10
CHEMBL6633 — Ki = 84.0 nM 7.08
CHEMBL360356 — Ki = 105.0 nM 6.98
CHEMBL7146 — Ki = 114.0 nM 6.94
CHEMBL266026 — Ki = 131.0 nM 6.88
CHEMBL220492 TOPIRAMATE Ki = 172.0 nM 6.76
CHEMBL18 ETHOXZOLAMIDE Ki = 193.0 nM 6.71
CHEMBL26 SULPIRIDE Ki = 204.0 nM 6.69
CHEMBL6685 — Ki = 207.0 nM 6.68
CHEMBL220491 BRINZOLAMIDE Ki = 210.0 nM 6.68
CHEMBL19 METHAZOLAMIDE Ki = 225.0 nM 6.65
CHEMBL750 ZONISAMIDE Ki = 231.0 nM 6.64
CHEMBL268439 — Ki = 268.0 nM 6.57
CHEMBL203112 — Ki = 316.0 nM 6.50
CHEMBL206261 — Ki = 318.0 nM 6.50
CHEMBL73962 BENZOLAMIDE Ki = 315.0 nM 6.50
CHEMBL7204 — Ki = 316.0 nM 6.50
CHEMBL265674 — Ki = 323.0 nM 6.49
CHEMBL7092 — Ki = 378.0 nM 6.42
CHEMBL17 DICHLORPHENAMIDE Ki = 378.0 nM 6.42
CHEMBL418 2,4-DISULFAMYLTRIFLUOROMETHYLANILINE Ki = 412.0 nM 6.38
CHEMBL77517 INDISULAM Ki = 413.0 nM 6.38
CHEMBL6705 — Ki = 426.0 nM 6.37
CHEMBL574 P-TOLUENESULFONAMIDE Ki = 450.0 nM 6.35
CHEMBL6724 — Ki = 452.0 nM 6.34
CHEMBL21 SULFANILAMIDE Ki = 454.0 nM 6.34
CHEMBL268177 — Ki = 510.0 nM 6.29
CHEMBL176495 — Ki = 541.0 nM 6.27
CHEMBL204326 — Ki = 539.0 nM 6.27
CHEMBL6753 — Ki = 549.0 nM 6.26
CHEMBL203534 — Ki = 640.0 nM 6.19
CHEMBL6919 — Ki = 876.0 nM 6.06
CHEMBL419 MAFENIDE Ki = 873.0 nM 6.06
CHEMBL414 CARZENIDE Ki = 1052.0 nM 5.98
CHEMBL6784 — Ki = 1134.0 nM 5.95
CHEMBL7087 — Ki = 1150.0 nM 5.94
CHEMBL6853 — Ki = 1230.0 nM 5.91
CHEMBL218490 DORZOLAMIDE Ki = 4360.0 nM 5.36