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Assay Detail

CHEMBL915480

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

Binding
Inhibition of human placental microsome CYP19
ChEMBL ↗
79
Total Activities
71
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Aromatase (CHEMBL1978) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Enantioselective nonsteroidal aromatase inhibitors identified through a multidisciplinary medicinal chemistry approach.
Cavalli A, Bisi A, Bertucci C, Rosini C, Paluszcak A, Gobbi S, Giorgio E, Rampa A, Belluti F, Piazzi L, Valenti P, Hartmann RW, Recanatini M.
J Med Chem (2005) 48 : 7282 -7289
PubMed 16279787 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 79 6.59 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL224060 VOROZOLE 2.0 1 8.85
CHEMBL224665 — — 2 8.64
CHEMBL519436 — — 1 8.40
CHEMBL31760 — — 1 8.38
CHEMBL224790 — — 1 8.24
CHEMBL375043 — — 1 7.96
CHEMBL1399 ANASTROZOLE 4.0 1 7.82
CHEMBL31224 — — 1 7.81
CHEMBL31215 S-FADROZOLE — 2 7.77
CHEMBL29482 — — 1 7.74
CHEMBL224391 — — 1 7.74
CHEMBL13784 — — 1 7.55
CHEMBL223717 — — 1 7.52
CHEMBL225053 — — 1 7.43
CHEMBL31456 — — 1 7.42
CHEMBL159073 — — 1 7.40
CHEMBL421149 — — 1 7.37
CHEMBL388187 — — 1 7.36
CHEMBL389433 LIAROZOLE 2.0 1 7.35
CHEMBL223176 — — 1 7.32
CHEMBL374934 — — 1 7.32
CHEMBL522917 — — 2 7.31
CHEMBL1444 LETROZOLE 4.0 1 7.28
CHEMBL224789 — — 1 7.24
CHEMBL223554 — — 1 7.23
CHEMBL225550 — — 1 7.21
CHEMBL421829 — — 1 7.05
CHEMBL224462 — — 1 7.03
CHEMBL388515 — — 1 7.02
CHEMBL223555 — — 1 7.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL224060 VOROZOLE IC50 = 1.413 nM 8.85
CHEMBL224665 — IC50 = 2.3 nM 8.64
CHEMBL224665 — IC50 = 2.291 nM 8.64
CHEMBL519436 — IC50 = 3.981 nM 8.40
CHEMBL31760 — IC50 = 4.169 nM 8.38
CHEMBL224790 — IC50 = 5.754 nM 8.24
CHEMBL375043 — IC50 = 10.96 nM 7.96
CHEMBL1399 ANASTROZOLE IC50 = 15.14 nM 7.82
CHEMBL31224 — IC50 = 15.49 nM 7.81
CHEMBL31215 S-FADROZOLE IC50 = 17.0 nM 7.77
CHEMBL31215 S-FADROZOLE IC50 = 16.98 nM 7.77
CHEMBL29482 — IC50 = 18.2 nM 7.74
CHEMBL224391 — IC50 = 18.2 nM 7.74
CHEMBL13784 — IC50 = 28.18 nM 7.55
CHEMBL223717 — IC50 = 30.2 nM 7.52
CHEMBL225053 — IC50 = 37.15 nM 7.43
CHEMBL31456 — IC50 = 38.02 nM 7.42
CHEMBL159073 — IC50 = 39.81 nM 7.40
CHEMBL421149 — IC50 = 42.66 nM 7.37
CHEMBL388187 — IC50 = 43.65 nM 7.36
CHEMBL389433 LIAROZOLE IC50 = 44.67 nM 7.35
CHEMBL223176 — IC50 = 47.86 nM 7.32
CHEMBL374934 — IC50 = 47.86 nM 7.32
CHEMBL522917 — IC50 = 49.0 nM 7.31
CHEMBL522917 — IC50 = 48.98 nM 7.31
CHEMBL1444 LETROZOLE IC50 = 52.48 nM 7.28
CHEMBL224789 — IC50 = 57.54 nM 7.24
CHEMBL223554 — IC50 = 58.88 nM 7.23
CHEMBL225550 — IC50 = 61.66 nM 7.21
CHEMBL421829 — IC50 = 89.13 nM 7.05
CHEMBL224462 — IC50 = 93.33 nM 7.03
CHEMBL223555 — IC50 = 95.5 nM 7.02
CHEMBL225128 — IC50 = 95.5 nM 7.02
CHEMBL525379 — IC50 = 95.5 nM 7.02
CHEMBL525379 — IC50 = 96.0 nM 7.02
CHEMBL388515 — IC50 = 95.5 nM 7.02
CHEMBL158984 — IC50 = 100.0 nM 7.00
CHEMBL225079 — IC50 = 110.0 nM 6.96
CHEMBL225079 — IC50 = 109.65 nM 6.96
CHEMBL225360 — IC50 = 147.91 nM 6.83
CHEMBL161230 — IC50 = 239.88 nM 6.62
CHEMBL223452 — IC50 = 288.4 nM 6.54
CHEMBL376786 — IC50 = 288.4 nM 6.54
CHEMBL376786 — IC50 = 290.0 nM 6.54
CHEMBL211207 — IC50 = 338.84 nM 6.47
CHEMBL350922 — IC50 = 389.05 nM 6.41
CHEMBL158635 — IC50 = 549.54 nM 6.26
CHEMBL451201 — IC50 = 630.96 nM 6.20
CHEMBL451201 — IC50 = 630.0 nM 6.20
CHEMBL92488 — IC50 = 691.83 nM 6.16