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Assay Detail

CHEMBL4002259

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

Binding
Inhibition of recombinant human carbonic anhydrase 1 incubated for 10 mins prior to testing by stopped flow CO2 hydrase 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 1 (CHEMBL261)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological evaluation of cyclic imides incorporating benzenesulfonamide moieties as carbonic anhydrase I, II, IV and IX inhibitors.
Abdel-Aziz AA, Angeli A, El-Azab AS, Abu El-Enin MA, Supuran CT.
Bioorg Med Chem (2017) 25 : 1666 -1671
PubMed 28161252 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 6.42 7.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4078596 1 7.31
CHEMBL4063164 1 7.02
CHEMBL4080077 1 6.75
CHEMBL4079688 1 6.70
CHEMBL20 ACETAZOLAMIDE 4.0 1 6.60
CHEMBL4066940 1 6.41
CHEMBL4091049 1 6.37
CHEMBL4064210 1 6.36
CHEMBL4083255 1 6.36
CHEMBL1905680 1 6.35
CHEMBL4103944 1 6.32
CHEMBL4101260 1 6.31
CHEMBL2414438 1 6.25
CHEMBL4096617 1 6.21
CHEMBL3113927 1 6.06
CHEMBL2424832 1 5.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4078596 Ki = 49.2 nM 7.31
CHEMBL4063164 Ki = 95.7 nM 7.02
CHEMBL4080077 Ki = 179.0 nM 6.75
CHEMBL4079688 Ki = 201.0 nM 6.70
CHEMBL20 ACETAZOLAMIDE Ki = 250.0 nM 6.60
CHEMBL4066940 Ki = 390.0 nM 6.41
CHEMBL4091049 Ki = 425.0 nM 6.37
CHEMBL4064210 Ki = 435.0 nM 6.36
CHEMBL4083255 Ki = 441.0 nM 6.36
CHEMBL1905680 Ki = 446.0 nM 6.35
CHEMBL4103944 Ki = 484.0 nM 6.32
CHEMBL4101260 Ki = 491.0 nM 6.31
CHEMBL2414438 Ki = 562.0 nM 6.25
CHEMBL4096617 Ki = 617.0 nM 6.21
CHEMBL3113927 Ki = 865.0 nM 6.06
CHEMBL2424832 Ki = 5121.0 nM 5.29