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Assay Detail

CHEMBL3135122

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

Binding
Inhibition of human recombinant aromatase expressed in baculovirus infected insect cells using O-benzylfluorescein benzyl ester as substrate after 30 mins
9
Total Activities
9
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

Aromatase (CHEMBL1978)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Flavans from Desmos cochinchinensis as potent aromatase inhibitors
Prachyawarakorn V, Sangpetsiripan S, Surawatanawong P, Mahidol C, Ruchirawat S, Kittakoop P
Medchemcomm (2013) 4 : 1590 -1596
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.82 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1444 LETROZOLE 4.0 1 8.96
CHEMBL3134109 1 7.40
CHEMBL3134113 1 7.10
CHEMBL3134112 1 7.05
CHEMBL3134114 1 6.82
CHEMBL3134115 1 6.22
CHEMBL3134110 1 6.00
CHEMBL3134111 1 4.97
CHEMBL53343 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1444 LETROZOLE IC50 = 1.1 nM 8.96
CHEMBL3134109 IC50 = 40.0 nM 7.40
CHEMBL3134113 IC50 = 80.0 nM 7.10
CHEMBL3134112 IC50 = 90.0 nM 7.05
CHEMBL3134114 IC50 = 150.0 nM 6.82
CHEMBL3134115 IC50 = 600.0 nM 6.22
CHEMBL3134110 IC50 = 1010.0 nM 6.00
CHEMBL3134111 IC50 = 10700.0 nM 4.97
CHEMBL53343 IC50 > 12500.0 nM -