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Assay Detail

CHEMBL4194334

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

Binding
Inhibition of recombinant human full-length carbonic anhydrase 1 preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay
11
Total Activities
11
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

Exploring Heteroaryl-pyrazole Carboxylic Acids as Human Carbonic Anhydrase XII Inhibitors.
Cadoni R, Pala N, Lomelino C, Mahon BP, McKenna R, Dallocchio R, Dessì A, Carcelli M, Rogolino D, Sanna V, Rassu M, Iaccarino C, Vullo D, Supuran CT, Sechi M.
ACS Med Chem Lett (2017) 8 : 941 -946
PubMed 28947941 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 5.80 7.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2070207 1 7.38
CHEMBL20 ACETAZOLAMIDE 4.0 1 6.60
CHEMBL4212188 1 6.21
CHEMBL19 METHAZOLAMIDE 4.0 1 6.11
CHEMBL17 DICHLORPHENAMIDE 4.0 1 5.92
CHEMBL4208348 1 5.37
CHEMBL4204007 1 5.32
CHEMBL4215693 1 5.27
CHEMBL4207837 1 5.23
CHEMBL4212738 1 5.19
CHEMBL4203483 1 5.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2070207 Ki = 42.0 nM 7.38
CHEMBL20 ACETAZOLAMIDE Ki = 250.0 nM 6.60
CHEMBL4212188 Ki = 620.0 nM 6.21
CHEMBL19 METHAZOLAMIDE Ki = 780.0 nM 6.11
CHEMBL17 DICHLORPHENAMIDE Ki = 1200.0 nM 5.92
CHEMBL4208348 Ki = 4310.0 nM 5.37
CHEMBL4204007 Ki = 4830.0 nM 5.32
CHEMBL4215693 Ki = 5330.0 nM 5.27
CHEMBL4207837 Ki = 5930.0 nM 5.23
CHEMBL4212738 Ki = 6450.0 nM 5.19
CHEMBL4203483 Ki = 6610.0 nM 5.18