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Assay Detail

CHEMBL3631192

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 at room temperature/6 hrs at 4 deg C by stopped-flow CO2 hydration assay
22
Total Activities
22
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

New natural product carbonic anhydrase inhibitors incorporating phenol moieties.
Karioti A, Ceruso M, Carta F, Bilia AR, Supuran CT.
Bioorg Med Chem (2015) 23 : 7219 -7225
PubMed 26498393 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 7.21 8.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL518243 LITHOSPERMIC ACID 1 8.32
CHEMBL233930 ASTRAGALIN 1 8.31
CHEMBL20 ACETAZOLAMIDE 4.0 1 8.24
CHEMBL8996 ERIODICTYOL 1 7.51
CHEMBL66 (+)-TAXIFOLIN 1 7.49
CHEMBL117 CHRYSIN 1 7.46
CHEMBL457077 SALVIANOLIC ACID A 1.0 1 7.40
CHEMBL309490 GALANGIN 1 7.38
CHEMBL2262641 QUERCETIN-3-O-RHAMNOSIDE 1 7.36
CHEMBL9352 NARINGENIN 1 7.35
CHEMBL250450 ISOQUERCETIN 2.0 1 7.28
CHEMBL131921 BIOCHANIN 1 7.28
CHEMBL379064 ISORHAMNETIN 1 7.26
CHEMBL8145 DAIDZEIN 2.0 1 7.25
CHEMBL151 LUTEOLIN 2.0 1 7.22
CHEMBL266564 TILIROSIDE 1 6.87
CHEMBL150 KAEMPFEROL 1.0 1 6.84
CHEMBL3628130 1 6.40
CHEMBL3628129 1 6.39
CHEMBL399121 HESPERETIN 0.5 1 6.34
CHEMBL541265 SALVIANOLIC ACID B 1 6.34
CHEMBL486386 PUERARIN 2.0 1 6.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL518243 LITHOSPERMIC ACID Ki = 4.8 nM 8.32
CHEMBL233930 ASTRAGALIN Ki = 4.9 nM 8.31
CHEMBL20 ACETAZOLAMIDE Ki = 5.7 nM 8.24
CHEMBL8996 ERIODICTYOL Ki = 31.1 nM 7.51
CHEMBL66 (+)-TAXIFOLIN Ki = 32.5 nM 7.49
CHEMBL117 CHRYSIN Ki = 34.7 nM 7.46
CHEMBL457077 SALVIANOLIC ACID A Ki = 39.8 nM 7.40
CHEMBL309490 GALANGIN Ki = 41.8 nM 7.38
CHEMBL2262641 QUERCETIN-3-O-RHAMNOSIDE Ki = 43.5 nM 7.36
CHEMBL9352 NARINGENIN Ki = 44.3 nM 7.35
CHEMBL250450 ISOQUERCETIN Ki = 52.1 nM 7.28
CHEMBL131921 BIOCHANIN Ki = 52.5 nM 7.28
CHEMBL379064 ISORHAMNETIN Ki = 54.9 nM 7.26
CHEMBL8145 DAIDZEIN Ki = 56.4 nM 7.25
CHEMBL151 LUTEOLIN Ki = 60.3 nM 7.22
CHEMBL266564 TILIROSIDE Ki = 134.3 nM 6.87
CHEMBL150 KAEMPFEROL Ki = 145.9 nM 6.84
CHEMBL3628130 Ki = 399.7 nM 6.40
CHEMBL3628129 Ki = 408.9 nM 6.39
CHEMBL399121 HESPERETIN Ki = 454.1 nM 6.34
CHEMBL541265 SALVIANOLIC ACID B Ki = 453.6 nM 6.34
CHEMBL486386 PUERARIN Ki = 515.0 nM 6.29