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Assay Detail

CHEMBL1670882

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Binding
Inhibition of human carbonic anhydrase 2 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 2 (CHEMBL205)
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 5.77 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL265674 1 7.22
CHEMBL37537 PROTOCATECHUIC ACID 1 6.33
CHEMBL1668603 1,2-DIMETHOXYBENZENE 1 6.30
CHEMBL95308 3,5-DIHYDROXYBENZOIC ACID 1 6.29
CHEMBL65369 3-HYDROXYBENZOIC ACID 1 6.22
CHEMBL488609 2,6-DIMETHOXYBENZOIC ACID 1 5.99
CHEMBL1668605 1,2,4-TRIMETHOXYBENZENE 1 5.84
CHEMBL1668604 1,4-DIMETHOXYBENZENE 1 5.47
CHEMBL14060 PHENOL 4.0 1 5.26
CHEMBL118903 VERATRIC ACID 1 5.21
CHEMBL52564 O-COUMARIC ACID 1 5.04
CHEMBL23194 SPERMINE 0.5 1 4.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL265674 Ki = 60.0 nM 7.22
CHEMBL37537 PROTOCATECHUIC ACID Ki = 470.0 nM 6.33
CHEMBL1668603 1,2-DIMETHOXYBENZENE Ki = 500.0 nM 6.30
CHEMBL95308 3,5-DIHYDROXYBENZOIC ACID Ki = 510.0 nM 6.29
CHEMBL65369 3-HYDROXYBENZOIC ACID Ki = 600.0 nM 6.22
CHEMBL488609 2,6-DIMETHOXYBENZOIC ACID Ki = 1020.0 nM 5.99
CHEMBL1668605 1,2,4-TRIMETHOXYBENZENE Ki = 1430.0 nM 5.84
CHEMBL1668604 1,4-DIMETHOXYBENZENE Ki = 3350.0 nM 5.47
CHEMBL14060 PHENOL Ki = 5500.0 nM 5.26
CHEMBL118903 VERATRIC ACID Ki = 6180.0 nM 5.21
CHEMBL52564 O-COUMARIC ACID Ki = 9200.0 nM 5.04
CHEMBL23194 SPERMINE Ki = 84000.0 nM 4.08