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Assay Detail

CHEMBL4142230

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

Binding
Inhibition of aromatase (unknown origin) using O-benzyl fluorescein benzyl ester as substrate in presence of NADPH-generating system by fluorescence assay
36
Total Activities
36
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

Synthesis, molecular docking, and QSAR study of sulfonamide-based indoles as aromatase inhibitors.
Pingaew R, Mandi P, Prachayasittikul V, Prachayasittikul S, Ruchirawat S, Prachayasittikul V.
Eur J Med Chem (2018) 143 : 1604 -1615
PubMed 29137864 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 36 5.51 8.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1444 LETROZOLE 4.0 1 8.72
CHEMBL4173941 1 6.16
CHEMBL4161859 1 6.10
CHEMBL4170504 1 5.89
CHEMBL4166016 1 5.85
CHEMBL4176982 1 5.77
CHEMBL4174326 1 5.64
CHEMBL4162572 1 5.64
CHEMBL4173619 1 5.60
CHEMBL157101 KETOCONAZOLE 4.0 1 5.58
CHEMBL4171198 1 5.57
CHEMBL4174637 1 5.57
CHEMBL4159550 1 5.55
CHEMBL4172837 1 5.55
CHEMBL4163649 1 5.50
CHEMBL4160591 1 5.47
CHEMBL4165064 1 5.46
CHEMBL4163983 1 5.46
CHEMBL4159184 1 5.42
CHEMBL4170175 1 5.41
CHEMBL4159524 1 5.40
CHEMBL4162163 1 5.39
CHEMBL4169784 1 5.38
CHEMBL4167098 1 5.36
CHEMBL4166364 1 5.34
CHEMBL4159101 1 5.27
CHEMBL4167430 1 5.26
CHEMBL4169756 1 5.12
CHEMBL4166769 1 5.08
CHEMBL4162907 1 5.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1444 LETROZOLE IC50 = 1.9 nM 8.72
CHEMBL4173941 IC50 = 700.0 nM 6.16
CHEMBL4161859 IC50 = 800.0 nM 6.10
CHEMBL4170504 IC50 = 1300.0 nM 5.89
CHEMBL4166016 IC50 = 1400.0 nM 5.85
CHEMBL4176982 IC50 = 1700.0 nM 5.77
CHEMBL4174326 IC50 = 2300.0 nM 5.64
CHEMBL4162572 IC50 = 2300.0 nM 5.64
CHEMBL4173619 IC50 = 2500.0 nM 5.60
CHEMBL157101 KETOCONAZOLE IC50 = 2600.0 nM 5.58
CHEMBL4171198 IC50 = 2700.0 nM 5.57
CHEMBL4174637 IC50 = 2700.0 nM 5.57
CHEMBL4159550 IC50 = 2800.0 nM 5.55
CHEMBL4172837 IC50 = 2800.0 nM 5.55
CHEMBL4163649 IC50 = 3200.0 nM 5.50
CHEMBL4160591 IC50 = 3400.0 nM 5.47
CHEMBL4165064 IC50 = 3500.0 nM 5.46
CHEMBL4163983 IC50 = 3500.0 nM 5.46
CHEMBL4159184 IC50 = 3800.0 nM 5.42
CHEMBL4170175 IC50 = 3900.0 nM 5.41
CHEMBL4159524 IC50 = 4000.0 nM 5.40
CHEMBL4162163 IC50 = 4100.0 nM 5.39
CHEMBL4169784 IC50 = 4200.0 nM 5.38
CHEMBL4167098 IC50 = 4400.0 nM 5.36
CHEMBL4166364 IC50 = 4600.0 nM 5.34
CHEMBL4159101 IC50 = 5400.0 nM 5.27
CHEMBL4167430 IC50 = 5500.0 nM 5.26
CHEMBL4169756 IC50 = 7600.0 nM 5.12
CHEMBL4166769 IC50 = 8300.0 nM 5.08
CHEMBL4162907 IC50 = 8800.0 nM 5.06
CHEMBL4168266 IC50 = 9800.0 nM 5.01
CHEMBL4167841 IC50 = 9800.0 nM 5.01
CHEMBL4172955 IC50 = 11200.0 nM 4.95
CHEMBL4170393 IC50 = 11900.0 nM 4.92
CHEMBL4174670 IC50 = 11900.0 nM 4.92
CHEMBL4175698 IC50 = 15300.0 nM 4.82