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Assay Detail

CHEMBL3874758

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

Binding
Inhibition of human recombinant carbonic anhydrase-1 preincubated for 6 hrs by stopped-flow CO2 hydration assay
13
Total Activities
13
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

Coumarins and other fused bicyclic heterocycles with selective tumor-associated carbonic anhydrase isoforms inhibitory activity.
Bozdag M, Alafeefy AM, Altamimi AM, Vullo D, Carta F, Supuran CT.
Bioorg Med Chem (2017) 25 : 677 -683
PubMed 27939347 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 5.62 6.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL20 ACETAZOLAMIDE 4.0 1 6.60
CHEMBL3976024 1 6.11
CHEMBL3984047 1 4.90
CHEMBL1993421 1 4.86
CHEMBL3914224 1 -
CHEMBL421646 BENZOYLENUREA 1 -
CHEMBL266540 QUINAZOLINONE 1 -
CHEMBL3896854 1 -
CHEMBL3960492 1 -
CHEMBL3986431 1 -
CHEMBL3956977 1 -
CHEMBL3977549 1 -
CHEMBL3928695 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL20 ACETAZOLAMIDE Ki = 250.0 nM 6.60
CHEMBL3976024 Ki = 783.0 nM 6.11
CHEMBL3984047 Ki = 12600.0 nM 4.90
CHEMBL1993421 Ki = 13750.0 nM 4.86
CHEMBL3914224 Ki > 500000.0 nM -
CHEMBL421646 BENZOYLENUREA Ki > 500000.0 nM -
CHEMBL266540 QUINAZOLINONE Ki > 500000.0 nM -
CHEMBL3896854 Ki > 500000.0 nM -
CHEMBL3960492 Ki > 500000.0 nM -
CHEMBL3986431 Ki > 500000.0 nM -
CHEMBL3956977 Ki > 500000.0 nM -
CHEMBL3977549 Ki > 500000.0 nM -
CHEMBL3928695 Ki > 500000.0 nM -