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Assay Detail

CHEMBL904077

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

Binding
Inhibition of human recombinant carbonic anhydrase 1 by CO2 hydration method
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

Carbonic anhydrase and matrix metalloproteinase inhibitors. Inhibition of human tumor-associated isozymes IX and cytosolic isozyme I and II with sulfonylated hydroxamates.
Nuti E, Orlandini E, Nencetti S, Rossello A, Innocenti A, Scozzafava A, Supuran CT.
Bioorg Med Chem (2007) 15 : 2298 -2311
PubMed 17276072 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 5.78 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL18 ETHOXZOLAMIDE 4.0 1 7.60
CHEMBL77517 INDISULAM 2.0 1 7.51
CHEMBL20 ACETAZOLAMIDE 4.0 1 6.51
CHEMBL19 METHAZOLAMIDE 4.0 1 6.11
CHEMBL226438 1 6.06
CHEMBL227567 1 6.05
CHEMBL227565 1 6.05
CHEMBL17 DICHLORPHENAMIDE 4.0 1 5.92
CHEMBL226439 1 5.39
CHEMBL228176 1 5.23
CHEMBL442057 1 5.05
CHEMBL376841 1 5.05
CHEMBL388982 1 5.01
CHEMBL228229 1 5.01
CHEMBL227566 1 5.00
CHEMBL388309 1 4.99
CHEMBL226149 1 -
CHEMBL373721 1 -
CHEMBL514138 CGS-27023A 1 -
CHEMBL228230 1 -
CHEMBL228231 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL18 ETHOXZOLAMIDE Ki = 25.0 nM 7.60
CHEMBL77517 INDISULAM Ki = 31.0 nM 7.51
CHEMBL20 ACETAZOLAMIDE Ki = 310.0 nM 6.51
CHEMBL19 METHAZOLAMIDE Ki = 780.0 nM 6.11
CHEMBL226438 Ki = 880.0 nM 6.06
CHEMBL227567 Ki = 900.0 nM 6.05
CHEMBL227565 Ki = 890.0 nM 6.05
CHEMBL17 DICHLORPHENAMIDE Ki = 1200.0 nM 5.92
CHEMBL226439 Ki = 4100.0 nM 5.39
CHEMBL228176 Ki = 5900.0 nM 5.23
CHEMBL442057 Ki = 9000.0 nM 5.05
CHEMBL376841 Ki = 8910.0 nM 5.05
CHEMBL388982 Ki = 9700.0 nM 5.01
CHEMBL228229 Ki = 9800.0 nM 5.01
CHEMBL227566 Ki = 10000.0 nM 5.00
CHEMBL388309 Ki = 10200.0 nM 4.99
CHEMBL226149 Ki = 490000.0 nM -
CHEMBL373721 Ki = 156000.0 nM -
CHEMBL514138 CGS-27023A Ki = 281000.0 nM -
CHEMBL228230 Ki = 520000.0 nM -
CHEMBL228231 Ki = 435000.0 nM -