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Assay Detail

CHEMBL1694074

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

Binding
Inhibition of human placental microsome CYP19 using [1beta-3H] androstenedione as a substrate
35
Total Activities
35
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

Design, synthesis, and biological evaluation of imidazolyl derivatives of 4,7-disubstituted coumarins as aromatase inhibitors selective over 17-α-hydroxylase/C17-20 lyase.
Stefanachi A, Favia AD, Nicolotti O, Leonetti F, Pisani L, Catto M, Zimmer C, Hartmann RW, Carotti A.
J Med Chem (2011) 54 : 1613 -1625
PubMed 21341743 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 35 6.68 7.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1688911 1 7.33
CHEMBL437731 1 7.29
CHEMBL9298 FADROZOLE 2.0 1 7.28
CHEMBL1688915 1 7.17
CHEMBL1688910 1 7.16
CHEMBL1688903 1 7.14
CHEMBL1688902 1 7.14
CHEMBL1688909 1 7.09
CHEMBL1688912 1 6.98
CHEMBL1688891 1 6.95
CHEMBL1688906 1 6.95
CHEMBL1688893 1 6.94
CHEMBL1688898 1 6.90
CHEMBL1688890 1 6.89
CHEMBL1688895 1 6.85
CHEMBL225499 1 6.82
CHEMBL1688907 1 6.79
CHEMBL1688901 1 6.78
CHEMBL1688900 1 6.77
CHEMBL1688897 1 6.75
CHEMBL1688894 1 6.68
CHEMBL1688892 1 6.63
CHEMBL1688896 1 6.57
CHEMBL225472 1 6.55
CHEMBL1688904 1 6.54
CHEMBL1688908 1 6.53
CHEMBL1688916 1 6.50
CHEMBL1688919 1 6.50
CHEMBL1688914 1 6.34
CHEMBL1688899 1 6.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1688911 IC50 = 47.0 nM 7.33
CHEMBL437731 IC50 = 51.0 nM 7.29
CHEMBL9298 FADROZOLE IC50 = 52.0 nM 7.28
CHEMBL1688915 IC50 = 67.0 nM 7.17
CHEMBL1688910 IC50 = 70.0 nM 7.16
CHEMBL1688903 IC50 = 72.0 nM 7.14
CHEMBL1688902 IC50 = 72.0 nM 7.14
CHEMBL1688909 IC50 = 81.0 nM 7.09
CHEMBL1688912 IC50 = 105.0 nM 6.98
CHEMBL1688891 IC50 = 113.0 nM 6.95
CHEMBL1688906 IC50 = 112.0 nM 6.95
CHEMBL1688893 IC50 = 114.0 nM 6.94
CHEMBL1688898 IC50 = 127.0 nM 6.90
CHEMBL1688890 IC50 = 130.0 nM 6.89
CHEMBL1688895 IC50 = 141.0 nM 6.85
CHEMBL225499 IC50 = 150.0 nM 6.82
CHEMBL1688907 IC50 = 164.0 nM 6.79
CHEMBL1688901 IC50 = 165.0 nM 6.78
CHEMBL1688900 IC50 = 169.0 nM 6.77
CHEMBL1688897 IC50 = 178.0 nM 6.75
CHEMBL1688894 IC50 = 207.0 nM 6.68
CHEMBL1688892 IC50 = 235.0 nM 6.63
CHEMBL1688896 IC50 = 267.0 nM 6.57
CHEMBL225472 IC50 = 280.0 nM 6.55
CHEMBL1688904 IC50 = 292.0 nM 6.54
CHEMBL1688908 IC50 = 296.0 nM 6.53
CHEMBL1688916 IC50 = 317.0 nM 6.50
CHEMBL1688919 IC50 = 313.0 nM 6.50
CHEMBL1688914 IC50 = 455.0 nM 6.34
CHEMBL1688899 IC50 = 481.0 nM 6.32
CHEMBL1688917 IC50 = 532.0 nM 6.27
CHEMBL1688905 IC50 = 690.0 nM 6.16
CHEMBL387892 IC50 = 2820.0 nM 5.55
CHEMBL1688913 IC50 = 3750.0 nM 5.43
CHEMBL1688918 IC50 = 4010.0 nM 5.40