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Assay Detail

CHEMBL5229154

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

Binding
Inhibition of FTO (unknown origin) demethylation activity using m6A7-Broccoli RNA as substrate incubated for 3 mins under shaking condition and measured after 2 hrs by fluorescence based analysis
23
Total Activities
23
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

Alpha-ketoglutarate-dependent dioxygenase FTO (CHEMBL2331065)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Inhibition of AlkB Nucleic Acid Demethylases: Promising New Epigenetic Targets.
Perry GS, Das M, Woon ECY.
J Med Chem (2021) 64 : 16974 -17003
PubMed 34792334 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 5.79 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4572939 1 7.22
CHEMBL465179 1 6.47
CHEMBL5275957 1 6.31
CHEMBL302783 1 6.07
CHEMBL5280834 1 5.94
CHEMBL5274182 1 5.92
CHEMBL5282066 1 5.91
CHEMBL1618358 1 5.90
CHEMBL1370446 METIZOLINE 2.0 1 5.86
CHEMBL1591 DEMECLOCYCLINE 4.0 1 5.86
CHEMBL157351 1 5.79
CHEMBL95 TACRINE 4.0 1 5.77
CHEMBL595227 1 5.66
CHEMBL418068 RHEIN 1 5.66
CHEMBL28626 MORIN 1 5.59
CHEMBL4567838 1 5.58
CHEMBL212579 BENZAMIL 1 5.55
CHEMBL7917 TYRPHOSTIN AG-1478 1 5.52
CHEMBL239800 FENOBAM ANHYDROUS 2.0 1 5.48
CHEMBL289277 EMODIN 1 5.34
CHEMBL945 AMILORIDE 4.0 1 5.32
CHEMBL284028 2,3-DIHYDROXY-6,7-DICHLOROQUINOXALINE 1 5.30
CHEMBL509 MECLOFENAMIC ACID 4.0 1 5.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4572939 IC50 = 60.0 nM 7.22
CHEMBL465179 IC50 = 340.0 nM 6.47
CHEMBL5275957 IC50 = 490.0 nM 6.31
CHEMBL302783 IC50 = 850.0 nM 6.07
CHEMBL5280834 IC50 = 1140.0 nM 5.94
CHEMBL5274182 IC50 = 1200.0 nM 5.92
CHEMBL5282066 IC50 = 1230.0 nM 5.91
CHEMBL1618358 IC50 = 1270.0 nM 5.90
CHEMBL1370446 METIZOLINE IC50 = 1370.0 nM 5.86
CHEMBL1591 DEMECLOCYCLINE IC50 = 1390.0 nM 5.86
CHEMBL157351 IC50 = 1620.0 nM 5.79
CHEMBL95 TACRINE IC50 = 1710.0 nM 5.77
CHEMBL595227 IC50 = 2180.0 nM 5.66
CHEMBL418068 RHEIN IC50 = 2180.0 nM 5.66
CHEMBL28626 MORIN IC50 = 2580.0 nM 5.59
CHEMBL4567838 IC50 = 2600.0 nM 5.58
CHEMBL212579 BENZAMIL IC50 = 2790.0 nM 5.55
CHEMBL7917 TYRPHOSTIN AG-1478 IC50 = 3000.0 nM 5.52
CHEMBL239800 FENOBAM ANHYDROUS IC50 = 3310.0 nM 5.48
CHEMBL289277 EMODIN IC50 = 4530.0 nM 5.34
CHEMBL945 AMILORIDE IC50 = 4740.0 nM 5.32
CHEMBL284028 2,3-DIHYDROXY-6,7-DICHLOROQUINOXALINE IC50 = 4970.0 nM 5.30
CHEMBL509 MECLOFENAMIC ACID IC50 = 7940.0 nM 5.10