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Assay Detail

CHEMBL1046597

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

Binding
Inhibition of human recombinant cytosolic carbonic anhydrase 1 by stopped-flow CO2 hydration assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Carbonic anhydrase 1 (CHEMBL261)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Carbonic anhydrase inhibitors. Aromatic/heterocyclic sulfonamides incorporating phenacetyl, pyridylacetyl and thienylacetyl tails act as potent inhibitors of human mitochondrial isoforms VA and VB.
Güzel O, Innocenti A, Scozzafava A, Salman A, Supuran CT.
Bioorg Med Chem (2009) 17 : 4894 -4899
PubMed 19539481 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 7.05 7.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL750 ZONISAMIDE 4.0 1 7.25
CHEMBL574779 1 7.22
CHEMBL573859 1 7.22
CHEMBL573127 1 7.21
CHEMBL583971 1 7.21
CHEMBL582841 1 7.20
CHEMBL583171 1 7.17
CHEMBL575660 1 7.17
CHEMBL574245 1 7.15
CHEMBL573381 1 7.14
CHEMBL574780 1 7.14
CHEMBL574783 1 7.12
CHEMBL582965 1 7.12
CHEMBL573335 1 7.11
CHEMBL584387 1 7.08
CHEMBL574782 1 6.97
CHEMBL574246 1 6.79
CHEMBL20 ACETAZOLAMIDE 4.0 1 6.60
CHEMBL220492 TOPIRAMATE 4.0 1 6.60
CHEMBL574021 1 6.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL750 ZONISAMIDE Ki = 56.0 nM 7.25
CHEMBL574779 Ki = 60.0 nM 7.22
CHEMBL573859 Ki = 60.0 nM 7.22
CHEMBL573127 Ki = 61.0 nM 7.21
CHEMBL583971 Ki = 61.0 nM 7.21
CHEMBL582841 Ki = 63.0 nM 7.20
CHEMBL583171 Ki = 68.0 nM 7.17
CHEMBL575660 Ki = 67.0 nM 7.17
CHEMBL574245 Ki = 71.0 nM 7.15
CHEMBL573381 Ki = 73.0 nM 7.14
CHEMBL574780 Ki = 72.0 nM 7.14
CHEMBL574783 Ki = 75.0 nM 7.12
CHEMBL582965 Ki = 75.0 nM 7.12
CHEMBL573335 Ki = 77.0 nM 7.11
CHEMBL584387 Ki = 84.0 nM 7.08
CHEMBL574782 Ki = 108.0 nM 6.97
CHEMBL574246 Ki = 161.0 nM 6.79
CHEMBL20 ACETAZOLAMIDE Ki = 250.0 nM 6.60
CHEMBL220492 TOPIRAMATE Ki = 250.0 nM 6.60
CHEMBL574021 Ki = 263.0 nM 6.58