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Assay Detail

CHEMBL4361655

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

Binding
Inhibition of recombinant human carbonic anhydrase 4 incubated for 6 hrs prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay
6
Total Activities
6
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 4 (CHEMBL3729)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and Evaluation of Carbonic Anhydrase Inhibitors with Carbon Monoxide Releasing Properties for the Management of Rheumatoid Arthritis.
Berrino E, Milazzo L, Micheli L, Vullo D, Angeli A, Bozdag M, Nocentini A, Menicatti M, Bartolucci G, di Cesare Mannelli L, Ghelardini C, Supuran CT, Carta F.
J Med Chem (2019) 62 : 7233 -7249
PubMed 31287314 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 7.23 7.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3758522 1 7.33
CHEMBL4586124 1 7.32
CHEMBL4448721 1 7.22
CHEMBL4519372 1 7.21
CHEMBL3322093 1 7.16
CHEMBL308819 1 7.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3758522 Ki = 47.2 nM 7.33
CHEMBL4586124 Ki = 48.3 nM 7.32
CHEMBL4448721 Ki = 59.7 nM 7.22
CHEMBL4519372 Ki = 62.2 nM 7.21
CHEMBL3322093 Ki = 69.2 nM 7.16
CHEMBL308819 Ki = 76.4 nM 7.12