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Assay Detail

CHEMBL834886

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Functional
Inhibition constant against human recombinant carbonic anhydrase I
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Carbonic anhydrase 1 (CHEMBL261)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Carbonic anhydrase inhibitors. Synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with boron-containing sulfonamides, sulfamides, and sulfamates: toward agents for boron neutron capture therapy of hypoxic tumors.
Winum JY, Cecchi A, Montero JL, Innocenti A, Scozzafava A, Supuran CT.
Bioorg Med Chem Lett (2005) 15 : 3302 -3306
PubMed 15908201 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 7.02 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL18 ETHOXZOLAMIDE 4.0 1 7.60
CHEMBL189065 1 7.47
CHEMBL189729 1 7.44
CHEMBL364903 1 7.31
CHEMBL190622 1 7.16
CHEMBL190392 1 7.16
CHEMBL373325 1 7.16
CHEMBL193199 1 7.16
CHEMBL189113 1 7.16
CHEMBL191799 1 7.15
CHEMBL190314 1 7.14
CHEMBL193191 1 7.11
CHEMBL190447 1 7.04
CHEMBL192997 1 7.04
CHEMBL190448 1 7.03
CHEMBL20 ACETAZOLAMIDE 4.0 1 6.60
CHEMBL21 SULFANILAMIDE 4.0 1 4.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL18 ETHOXZOLAMIDE Ki = 25.0 nM 7.60
CHEMBL189065 Ki = 34.0 nM 7.47
CHEMBL189729 Ki = 36.0 nM 7.44
CHEMBL364903 Ki = 49.0 nM 7.31
CHEMBL190622 Ki = 70.0 nM 7.16
CHEMBL190392 Ki = 69.0 nM 7.16
CHEMBL373325 Ki = 70.0 nM 7.16
CHEMBL193199 Ki = 69.0 nM 7.16
CHEMBL189113 Ki = 70.0 nM 7.16
CHEMBL191799 Ki = 70.5 nM 7.15
CHEMBL190314 Ki = 72.0 nM 7.14
CHEMBL193191 Ki = 77.0 nM 7.11
CHEMBL190447 Ki = 92.0 nM 7.04
CHEMBL192997 Ki = 91.0 nM 7.04
CHEMBL190448 Ki = 94.0 nM 7.03
CHEMBL20 ACETAZOLAMIDE Ki = 250.0 nM 6.60
CHEMBL21 SULFANILAMIDE Ki = 28000.0 nM 4.55