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Assay Detail

CHEMBL3762503

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Binding
Inhibition of human recombinant carbonic anhydrase 9 preincubated for 15 mins by stopped flow CO2 hydration assay
29
Total Activities
29
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

A novel library of saccharin and acesulfame derivatives as potent and selective inhibitors of carbonic anhydrase IX and XII isoforms.
Carradori S, Secci D, De Monte C, Mollica A, Ceruso M, Akdemir A, Sobolev AP, Codispoti R, De Cosmi F, Guglielmi P, Supuran CT.
Bioorg Med Chem (2016) 24 : 1095 -1105
PubMed 26810710 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 29 6.81 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3758979 1 7.75
CHEMBL3759629 1 7.72
CHEMBL3759331 1 7.72
CHEMBL3758923 1 7.66
CHEMBL1391313 1 7.64
CHEMBL20 ACETAZOLAMIDE 4.0 1 7.60
CHEMBL3758428 1 7.58
CHEMBL3759876 1 7.57
CHEMBL3760060 1 7.29
CHEMBL310671 SACCHARIN 3.0 1 6.99
CHEMBL3760047 1 6.79
CHEMBL79350 1 6.76
CHEMBL3758327 1 6.74
CHEMBL1472681 1 6.72
CHEMBL3759518 1 6.71
CHEMBL3758420 1 6.68
CHEMBL1489759 1 6.66
CHEMBL2429920 1 6.65
CHEMBL3759375 1 6.63
CHEMBL3758373 1 6.62
CHEMBL3760113 1 6.58
CHEMBL3759099 1 6.58
CHEMBL3125555 1 6.51
CHEMBL3759608 1 6.27
CHEMBL3759443 1 6.21
CHEMBL3759882 1 5.93
CHEMBL3759447 1 5.80
CHEMBL1351474 ACESULFAME POTASSIUM 3.0 1 5.62
CHEMBL3759567 1 5.61

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3758979 Ki = 18.0 nM 7.75
CHEMBL3759629 Ki = 19.0 nM 7.72
CHEMBL3759331 Ki = 19.0 nM 7.72
CHEMBL3758923 Ki = 22.0 nM 7.66
CHEMBL1391313 Ki = 23.0 nM 7.64
CHEMBL20 ACETAZOLAMIDE Ki = 25.0 nM 7.60
CHEMBL3758428 Ki = 26.0 nM 7.58
CHEMBL3759876 Ki = 27.0 nM 7.57
CHEMBL3760060 Ki = 51.0 nM 7.29
CHEMBL310671 SACCHARIN Ki = 103.0 nM 6.99
CHEMBL3760047 Ki = 161.0 nM 6.79
CHEMBL79350 Ki = 174.0 nM 6.76
CHEMBL3758327 Ki = 184.0 nM 6.74
CHEMBL1472681 Ki = 191.0 nM 6.72
CHEMBL3759518 Ki = 196.0 nM 6.71
CHEMBL3758420 Ki = 210.0 nM 6.68
CHEMBL1489759 Ki = 221.0 nM 6.66
CHEMBL2429920 Ki = 223.0 nM 6.65
CHEMBL3759375 Ki = 234.0 nM 6.63
CHEMBL3758373 Ki = 239.0 nM 6.62
CHEMBL3760113 Ki = 265.0 nM 6.58
CHEMBL3759099 Ki = 261.0 nM 6.58
CHEMBL3125555 Ki = 310.0 nM 6.51
CHEMBL3759608 Ki = 539.0 nM 6.27
CHEMBL3759443 Ki = 616.0 nM 6.21
CHEMBL3759882 Ki = 1169.0 nM 5.93
CHEMBL3759447 Ki = 1570.0 nM 5.80
CHEMBL1351474 ACESULFAME POTASSIUM Ki = 2410.0 nM 5.62
CHEMBL3759567 Ki = 2482.0 nM 5.61