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Assay Detail

CHEMBL1670883

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Binding
Inhibition of human carbonic anhydrase 9 preincubated for 15 mins by CO2 hydration stopped-flow assay
12
Total Activities
12
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 9 (CHEMBL3594)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Kinetic and docking studies of phenol-based inhibitors of carbonic anhydrase isoforms I, II, IX and XII evidence a new binding mode within the enzyme active site.
Durdagi S, Şentürk M, Ekinci D, Balaydın HT, Göksu S, Küfrevioğlu Öİ, Innocenti A, Scozzafava A, Supuran CT.
Bioorg Med Chem (2011) 19 : 1381 -1389
PubMed 21282059 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 5.39 7.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL265674 1 7.39
CHEMBL1668605 1,2,4-TRIMETHOXYBENZENE 1 5.39
CHEMBL1668604 1,4-DIMETHOXYBENZENE 1 5.38
CHEMBL95308 3,5-DIHYDROXYBENZOIC ACID 1 5.36
CHEMBL37537 PROTOCATECHUIC ACID 1 5.35
CHEMBL65369 3-HYDROXYBENZOIC ACID 1 5.34
CHEMBL118903 VERATRIC ACID 1 5.08
CHEMBL1668603 1,2-DIMETHOXYBENZENE 1 5.06
CHEMBL14060 PHENOL 4.0 1 5.06
CHEMBL488609 2,6-DIMETHOXYBENZOIC ACID 1 5.04
CHEMBL23194 SPERMINE 0.5 1 4.88
CHEMBL52564 O-COUMARIC ACID 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL265674 Ki = 41.0 nM 7.39
CHEMBL1668605 1,2,4-TRIMETHOXYBENZENE Ki = 4060.0 nM 5.39
CHEMBL1668604 1,4-DIMETHOXYBENZENE Ki = 4150.0 nM 5.38
CHEMBL95308 3,5-DIHYDROXYBENZOIC ACID Ki = 4410.0 nM 5.36
CHEMBL37537 PROTOCATECHUIC ACID Ki = 4450.0 nM 5.35
CHEMBL65369 3-HYDROXYBENZOIC ACID Ki = 4530.0 nM 5.34
CHEMBL118903 VERATRIC ACID Ki = 8250.0 nM 5.08
CHEMBL1668603 1,2-DIMETHOXYBENZENE Ki = 8630.0 nM 5.06
CHEMBL14060 PHENOL Ki = 8800.0 nM 5.06
CHEMBL488609 2,6-DIMETHOXYBENZOIC ACID Ki = 9070.0 nM 5.04
CHEMBL23194 SPERMINE Ki = 13300.0 nM 4.88
CHEMBL52564 O-COUMARIC ACID Ki > 1000000.0 nM -