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Assay Detail

CHEMBL3610380

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

Binding
Inhibition of human recombinant carbonic anhydrase 12 preincubated for 15 mins by stopped flow CO2 hydration method
25
Total Activities
25
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 12 (CHEMBL3242)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Probing the 'bipolar' nature of the carbonic anhydrase active site: aromatic sulfonamides containing 1,3-oxazol-5-yl moiety as picomolar inhibitors of cytosolic CA I and CA II isoforms.
Krasavin M, Korsakov M, Dorogov M, Tuccinardi T, Dedeoglu N, Supuran CT.
Eur J Med Chem (2015) 101 : 334 -347
PubMed 26160114 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 7.22 8.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3608890 1 8.44
CHEMBL3608887 1 8.29
CHEMBL3608871 1 8.21
CHEMBL3608892 1 8.18
CHEMBL3608888 1 8.17
CHEMBL3608874 1 8.16
CHEMBL3608870 1 8.07
CHEMBL3608872 1 8.06
CHEMBL3608891 1 8.06
CHEMBL3608894 1 8.04
CHEMBL3608886 1 8.04
CHEMBL3608885 1 8.03
CHEMBL3608889 1 7.52
CHEMBL3608873 1 7.37
CHEMBL3608880 1 7.20
CHEMBL3608893 1 7.19
CHEMBL3608875 1 6.61
CHEMBL3608876 1 6.42
CHEMBL3608882 1 6.25
CHEMBL3608877 1 5.86
CHEMBL3608881 1 5.55
CHEMBL3608878 1 5.45
CHEMBL3608879 1 5.10
CHEMBL3608883 1 5.07
CHEMBL3608884 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3608890 Ki = 3.6 nM 8.44
CHEMBL3608887 Ki = 5.1 nM 8.29
CHEMBL3608871 Ki = 6.2 nM 8.21
CHEMBL3608892 Ki = 6.6 nM 8.18
CHEMBL3608888 Ki = 6.7 nM 8.17
CHEMBL3608874 Ki = 6.9 nM 8.16
CHEMBL3608870 Ki = 8.5 nM 8.07
CHEMBL3608872 Ki = 8.7 nM 8.06
CHEMBL3608891 Ki = 8.7 nM 8.06
CHEMBL3608894 Ki = 9.2 nM 8.04
CHEMBL3608886 Ki = 9.2 nM 8.04
CHEMBL3608885 Ki = 9.4 nM 8.03
CHEMBL3608889 Ki = 30.3 nM 7.52
CHEMBL3608873 Ki = 42.3 nM 7.37
CHEMBL3608880 Ki = 62.8 nM 7.20
CHEMBL3608893 Ki = 64.4 nM 7.19
CHEMBL3608875 Ki = 245.0 nM 6.61
CHEMBL3608876 Ki = 381.0 nM 6.42
CHEMBL3608882 Ki = 557.0 nM 6.25
CHEMBL3608877 Ki = 1395.0 nM 5.86
CHEMBL3608881 Ki = 2790.0 nM 5.55
CHEMBL3608878 Ki = 3535.0 nM 5.45
CHEMBL3608879 Ki = 7960.0 nM 5.10
CHEMBL3608883 Ki = 8570.0 nM 5.07
CHEMBL3608884 Ki > 10000.0 nM -