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Assay Detail

CHEMBL4045528

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

Binding
Inhibition of human CA12 pre-incubated for 10 mins by stopped-flow CO2 hydrase assay
16
Total Activities
16
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

Synthesis and carbonic anhydrase inhibition of polycyclic imides incorporating N-benzenesulfonamide moieties.
Angeli A, Abdel-Aziz AA, Nocentini A, El-Azab AS, Gratteri P, Supuran CT.
Bioorg Med Chem (2017) 25 : 5373 -5379
PubMed 28789908 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 7.37 8.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL20 ACETAZOLAMIDE 4.0 1 8.24
CHEMBL4074017 1 7.70
CHEMBL4081833 1 7.58
CHEMBL4084340 1 7.55
CHEMBL4092096 1 7.40
CHEMBL2377778 1 7.37
CHEMBL4099375 1 7.37
CHEMBL4061148 1 7.33
CHEMBL4073974 1 7.33
CHEMBL4098904 1 7.32
CHEMBL2377779 1 7.29
CHEMBL4099996 1 7.13
CHEMBL4072442 1 7.09
CHEMBL4069126 1 7.07
CHEMBL4071301 1 7.07
CHEMBL4099836 1 7.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL20 ACETAZOLAMIDE Ki = 5.7 nM 8.24
CHEMBL4074017 Ki = 19.9 nM 7.70
CHEMBL4081833 Ki = 26.0 nM 7.58
CHEMBL4084340 Ki = 28.3 nM 7.55
CHEMBL4092096 Ki = 39.9 nM 7.40
CHEMBL2377778 Ki = 42.8 nM 7.37
CHEMBL4099375 Ki = 42.8 nM 7.37
CHEMBL4061148 Ki = 46.9 nM 7.33
CHEMBL4073974 Ki = 47.2 nM 7.33
CHEMBL4098904 Ki = 47.7 nM 7.32
CHEMBL2377779 Ki = 51.7 nM 7.29
CHEMBL4099996 Ki = 74.1 nM 7.13
CHEMBL4072442 Ki = 80.5 nM 7.09
CHEMBL4069126 Ki = 84.6 nM 7.07
CHEMBL4071301 Ki = 84.4 nM 7.07
CHEMBL4099836 Ki = 90.3 nM 7.04