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Assay Detail

CHEMBL976458

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of human cloned CA1 by CO2 hydration assay
13
Total Activities
13
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 1 (CHEMBL261)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Inhibition of human mitochondrial carbonic anhydrases VA and VB with para-(4-phenyltriazole-1-yl)-benzenesulfonamide derivatives.
Poulsen SA, Wilkinson BL, Innocenti A, Vullo D, Supuran CT.
Bioorg Med Chem Lett (2008) 18 : 4624 -4627
PubMed 18644716 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 5.76 7.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL750 ZONISAMIDE 4.0 1 7.25
CHEMBL469064 1 7.00
CHEMBL220492 TOPIRAMATE 4.0 1 6.60
CHEMBL469220 1 5.68
CHEMBL513185 1 5.66
CHEMBL445517 1 5.52
CHEMBL222837 1 5.41
CHEMBL469221 1 5.40
CHEMBL468367 1 5.34
CHEMBL513184 1 5.29
CHEMBL468839 1 5.26
CHEMBL512809 1 5.24
CHEMBL467979 1 5.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL750 ZONISAMIDE Ki = 56.0 nM 7.25
CHEMBL469064 Ki = 100.0 nM 7.00
CHEMBL220492 TOPIRAMATE Ki = 250.0 nM 6.60
CHEMBL469220 Ki = 2100.0 nM 5.68
CHEMBL513185 Ki = 2200.0 nM 5.66
CHEMBL445517 Ki = 3000.0 nM 5.52
CHEMBL222837 Ki = 3900.0 nM 5.41
CHEMBL469221 Ki = 4000.0 nM 5.40
CHEMBL468367 Ki = 4600.0 nM 5.34
CHEMBL513184 Ki = 5100.0 nM 5.29
CHEMBL468839 Ki = 5500.0 nM 5.26
CHEMBL512809 Ki = 5800.0 nM 5.24
CHEMBL467979 Ki = 6500.0 nM 5.19