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Assay Detail

CHEMBL4731733

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

ADMET
Inhibition of human carbonic anhydrase 2 incubated for 30 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Carbonic anhydrase 2 (CHEMBL205)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Benzoxaboroles: New Potent Inhibitors of the Carbonic Anhydrases of the Pathogenic Bacterium Vibrio cholerae.
Bonardi A,Nocentini A,Cadoni R,Del Prete S,Dumy P,Capasso C,Gratteri P,Supuran CT,Winum JY
ACS Med Chem Lett (2020) 11 : 2277 -2284
PubMed 33214840 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 6.17 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL20 ACETAZOLAMIDE 4.0 1 7.92
CHEMBL4746021 1 7.05
CHEMBL4172094 1 6.57
CHEMBL4170654 1 6.56
CHEMBL4160012 1 6.36
CHEMBL4161495 1 6.34
CHEMBL443052 TAVABOROLE 4.0 1 6.33
CHEMBL4177136 1 6.32
CHEMBL4175131 1 6.30
CHEMBL4167266 1 6.23
CHEMBL4174083 1 6.15
CHEMBL4163368 1 6.14
CHEMBL4171057 1 6.10
CHEMBL4166821 1 6.08
CHEMBL4174896 1 5.94
CHEMBL4174497 1 5.90
CHEMBL4164241 1 5.90
CHEMBL4757712 1 5.88
CHEMBL4173293 1 5.82
CHEMBL4166580 1 5.81
CHEMBL4176682 1 5.79
CHEMBL4166065 1 5.74
CHEMBL4166184 1 5.65
CHEMBL378506 BENZOXABOROLE 1 5.09
CHEMBL4159776 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL20 ACETAZOLAMIDE Ki = 12.0 nM 7.92
CHEMBL4746021 Ki = 89.0 nM 7.05
CHEMBL4172094 Ki = 272.0 nM 6.57
CHEMBL4170654 Ki = 276.0 nM 6.56
CHEMBL4160012 Ki = 439.0 nM 6.36
CHEMBL4161495 Ki = 456.0 nM 6.34
CHEMBL443052 TAVABOROLE Ki = 462.0 nM 6.33
CHEMBL4177136 Ki = 480.0 nM 6.32
CHEMBL4175131 Ki = 504.0 nM 6.30
CHEMBL4167266 Ki = 590.0 nM 6.23
CHEMBL4174083 Ki = 707.0 nM 6.15
CHEMBL4163368 Ki = 730.0 nM 6.14
CHEMBL4171057 Ki = 797.0 nM 6.10
CHEMBL4166821 Ki = 841.0 nM 6.08
CHEMBL4174896 Ki = 1148.0 nM 5.94
CHEMBL4174497 Ki = 1253.0 nM 5.90
CHEMBL4164241 Ki = 1250.0 nM 5.90
CHEMBL4757712 Ki = 1305.0 nM 5.88
CHEMBL4173293 Ki = 1500.0 nM 5.82
CHEMBL4166580 Ki = 1547.0 nM 5.81
CHEMBL4176682 Ki = 1625.0 nM 5.79
CHEMBL4166065 Ki = 1838.0 nM 5.74
CHEMBL4166184 Ki = 2230.0 nM 5.65
CHEMBL378506 BENZOXABOROLE Ki = 8180.0 nM 5.09
CHEMBL4159776 Ki > 10000.0 nM -