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Assay Detail

CHEMBL1686237

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

Binding
Inhibition of human recombinant CA5A mitochondrial isoform by stopped-flow CO2 hydration assay
16
Total Activities
16
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 5A, mitochondrial (CHEMBL4789)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

(R)-/(S)-10-camphorsulfonyl-substituted aromatic/heterocyclic sulfonamides selectively inhibit mitochondrial over cytosolic carbonic anhydrases.
Maresca A, Supuran CT.
Bioorg Med Chem Lett (2011) 21 : 1334 -1337
PubMed 21300547 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 7.42 8.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1683474 1 8.23
CHEMBL1683468 1 7.78
CHEMBL1683466 1 7.77
CHEMBL750 ZONISAMIDE 4.0 1 7.70
CHEMBL1683475 1 7.68
CHEMBL18 ETHOXZOLAMIDE 4.0 1 7.60
CHEMBL1683469 1 7.56
CHEMBL1683471 1 7.48
CHEMBL1683472 1 7.45
CHEMBL1683473 1 7.31
CHEMBL20 ACETAZOLAMIDE 4.0 1 7.20
CHEMBL220492 TOPIRAMATE 4.0 1 7.20
CHEMBL1683470 1 7.19
CHEMBL19 METHAZOLAMIDE 4.0 1 7.19
CHEMBL1683467 1 7.16
CHEMBL17 DICHLORPHENAMIDE 4.0 1 6.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1683474 Ki = 5.9 nM 8.23
CHEMBL1683468 Ki = 16.6 nM 7.78
CHEMBL1683466 Ki = 17.1 nM 7.77
CHEMBL750 ZONISAMIDE Ki = 20.0 nM 7.70
CHEMBL1683475 Ki = 21.0 nM 7.68
CHEMBL18 ETHOXZOLAMIDE Ki = 25.0 nM 7.60
CHEMBL1683469 Ki = 27.5 nM 7.56
CHEMBL1683471 Ki = 33.2 nM 7.48
CHEMBL1683472 Ki = 35.3 nM 7.45
CHEMBL1683473 Ki = 48.7 nM 7.31
CHEMBL20 ACETAZOLAMIDE Ki = 63.0 nM 7.20
CHEMBL220492 TOPIRAMATE Ki = 63.0 nM 7.20
CHEMBL1683470 Ki = 64.5 nM 7.19
CHEMBL19 METHAZOLAMIDE Ki = 65.0 nM 7.19
CHEMBL1683467 Ki = 68.6 nM 7.16
CHEMBL17 DICHLORPHENAMIDE Ki = 630.0 nM 6.20