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Assay Detail

CHEMBL3624595

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Binding
Inhibition of aromatase (unknown origin)
29
Total Activities
29
Compounds Tested
2
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

Recent developments in steroidal and nonsteroidal aromatase inhibitors for the chemoprevention of estrogen-dependent breast cancer.
Ahmad I, Shagufta.
Eur J Med Chem (2015) 102 : 375 -386
PubMed 26301554 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 6.25 7.92
Inhibition 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2179110 1 7.92
CHEMBL41761 1 7.40
CHEMBL3219600 1 7.39
CHEMBL3623225 1 7.00
CHEMBL3623214 1 6.80
CHEMBL3623217 1 6.77
CHEMBL3623213 1 6.75
CHEMBL3621226 1 6.66
CHEMBL3623209 1 6.60
CHEMBL3623208 1 6.38
CHEMBL3623223 1 6.33
CHEMBL3623219 1 6.32
CHEMBL293122 1 6.30
CHEMBL117 CHRYSIN 1 6.30
CHEMBL3623215 1 6.29
CHEMBL3623218 1 6.01
CHEMBL3623216 1 6.00
CHEMBL28 APIGENIN 1 5.92
CHEMBL3623230 1 5.57
CHEMBL2282050 1 5.36
CHEMBL2003274 1 5.28
CHEMBL3623229 1 5.21
CHEMBL274318 FLAVANONE 1 5.10
CHEMBL3623222 1 4.36
CHEMBL3623210 1 -
CHEMBL275638 FLAVONE 2.0 1 -
CHEMBL3623211 1 -
CHEMBL50 QUERCETIN 3.0 1 -
CHEMBL131921 BIOCHANIN 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2179110 IC50 = 12.0 nM 7.92
CHEMBL41761 IC50 = 40.0 nM 7.40
CHEMBL3219600 IC50 = 41.0 nM 7.39
CHEMBL3623225 IC50 = 100.0 nM 7.00
CHEMBL3623214 IC50 = 160.0 nM 6.80
CHEMBL3623217 IC50 = 170.0 nM 6.77
CHEMBL3623213 IC50 = 180.0 nM 6.75
CHEMBL3621226 IC50 = 220.0 nM 6.66
CHEMBL3623209 IC50 = 250.0 nM 6.60
CHEMBL3623208 IC50 = 420.0 nM 6.38
CHEMBL3623223 IC50 = 470.0 nM 6.33
CHEMBL3623219 IC50 = 480.0 nM 6.32
CHEMBL293122 IC50 = 500.0 nM 6.30
CHEMBL117 CHRYSIN IC50 = 500.0 nM 6.30
CHEMBL3623215 IC50 = 510.0 nM 6.29
CHEMBL3623218 IC50 = 970.0 nM 6.01
CHEMBL3623216 IC50 = 1000.0 nM 6.00
CHEMBL28 APIGENIN IC50 = 1200.0 nM 5.92
CHEMBL3623230 IC50 = 2700.0 nM 5.57
CHEMBL2282050 IC50 = 4400.0 nM 5.36
CHEMBL2003274 IC50 = 5200.0 nM 5.28
CHEMBL3623229 IC50 = 6200.0 nM 5.21
CHEMBL274318 FLAVANONE IC50 = 8000.0 nM 5.10
CHEMBL3623222 IC50 = 44000.0 nM 4.36
CHEMBL3623210 Inhibition = 93.3 % -
CHEMBL275638 FLAVONE IC50 = 8000.0 nM -
CHEMBL3623211 Inhibition = 67.9 % -
CHEMBL50 QUERCETIN IC50 = 12000.0 nM -
CHEMBL131921 BIOCHANIN IC50 = 113000.0 nM -