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Assay Detail

CHEMBL854244

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Binding
Binding affinity to human CA2 by ThermoFluor assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Inhibition of carbonic anhydrase-II by sulfamate and sulfamide groups: an investigation involving direct thermodynamic binding measurements.
Klinger AL, McComsey DF, Smith-Swintosky V, Shank RP, Maryanoff BE.
J Med Chem (2006) 49 : 3496 -3500
PubMed 16759092 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 10 5.82 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL417656 1 8.00
CHEMBL24259 PHENYLSULFAMATE 1 6.96
CHEMBL180475 1 6.85
CHEMBL220492 TOPIRAMATE 4.0 1 6.54
CHEMBL172215 1 5.70
CHEMBL168514 PHENYLSULFAMIDE 1 5.34
CHEMBL175644 1 5.00
CHEMBL177425 1 4.90
CHEMBL283695 1 4.60
CHEMBL378292 1 4.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL417656 Kd = 10.0 nM 8.00
CHEMBL24259 PHENYLSULFAMATE Kd = 110.0 nM 6.96
CHEMBL180475 Kd = 140.0 nM 6.85
CHEMBL220492 TOPIRAMATE Kd = 290.0 nM 6.54
CHEMBL172215 Kd = 2000.0 nM 5.70
CHEMBL168514 PHENYLSULFAMIDE Kd = 4550.0 nM 5.34
CHEMBL175644 Kd = 10000.0 nM 5.00
CHEMBL177425 Kd = 12500.0 nM 4.90
CHEMBL283695 Kd = 25000.0 nM 4.60
CHEMBL378292 Kd = 50000.0 nM 4.30