Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1290837

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

Binding
Inhibition of full length human CA1 cytosolic isoform by stopped-flow CO2 hydration method
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 1 (CHEMBL261)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

7,8-disubstituted- but not 6,7-disubstituted coumarins selectively inhibit the transmembrane, tumor-associated carbonic anhydrase isoforms IX and XII over the cytosolic ones I and II in the low nanomolar/subnanomolar range.
Maresca A, Scozzafava A, Supuran CT.
Bioorg Med Chem Lett (2010) 20 : 7255 -7258
PubMed 21067924 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 5.62 7.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL572366 1 7.11
CHEMBL6466 COUMARIN 4.0 1 5.51
CHEMBL51628 UMBELLIFERONE 1 4.23
CHEMBL1288534 1 -
CHEMBL1288535 1 -
CHEMBL446518 1 -
CHEMBL1288557 1 -
CHEMBL1288558 1 -
CHEMBL1288559 1 -
CHEMBL1288560 1 -
CHEMBL1288593 1 -
CHEMBL1290010 1 -
CHEMBL1290110 1 -
CHEMBL1288594 1 -
CHEMBL1288595 1 -
CHEMBL1288596 1 -
CHEMBL1288620 1 -
CHEMBL1290111 1 -
CHEMBL1290219 1 -
CHEMBL1288621 1 -
CHEMBL1288622 1 -
CHEMBL1288623 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL572366 Ki = 78.0 nM 7.11
CHEMBL6466 COUMARIN Ki = 3100.0 nM 5.51
CHEMBL51628 UMBELLIFERONE Ki = 58400.0 nM 4.23
CHEMBL1288534 Ki > 100000.0 nM -
CHEMBL1288535 Ki > 100000.0 nM -
CHEMBL446518 Ki > 100000.0 nM -
CHEMBL1288557 Ki > 100000.0 nM -
CHEMBL1288558 Ki > 100000.0 nM -
CHEMBL1288559 Ki > 100000.0 nM -
CHEMBL1288560 Ki > 100000.0 nM -
CHEMBL1288593 Ki > 100000.0 nM -
CHEMBL1290010 Ki > 100000.0 nM -
CHEMBL1290110 Ki > 100000.0 nM -
CHEMBL1288594 Ki > 100000.0 nM -
CHEMBL1288595 Ki > 100000.0 nM -
CHEMBL1288596 Ki > 100000.0 nM -
CHEMBL1288620 Ki > 100000.0 nM -
CHEMBL1290111 Ki > 100000.0 nM -
CHEMBL1290219 Ki > 100000.0 nM -
CHEMBL1288621 Ki > 100000.0 nM -
CHEMBL1288622 Ki > 100000.0 nM -
CHEMBL1288623 Ki > 100000.0 nM -