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Assay Detail

CHEMBL4186813

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

Binding
Inhibition of CYP19A1 (unknown origin)
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

Dihydrobenzisoxazole-4-one compounds are novel selective inhibitors of aldosterone synthase (CYP11B2) with in vivo activity.
Meyers K, Cogan DA, Burke J, Arenas R, Balestra M, Brown NF, Chen Z, Cerny MA, Clifford HE, Colombo F, Fader L, Frederick KS, Guo X, Goldberg D, Hornberger KR, Kugler S, Lord J, Marshall DR, Moss N, Parmentier JH, Richman JR, Schmenk J, Weldon SM, Yu M, Zhang M.
Bioorg Med Chem Lett (2018) 28 : 979 -984
PubMed 29254646 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.30 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL446083 1 7.00
CHEMBL287677 DEXFADROSTAT 2.0 1 6.10
CHEMBL3099695 OSILODROSTAT 4.0 1 5.80
CHEMBL4207995 1 -
CHEMBL4212612 1 -
CHEMBL4211193 1 -
CHEMBL4212918 1 -
CHEMBL4214618 1 -
CHEMBL4207348 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL446083 IC50 = 100.0 nM 7.00
CHEMBL287677 DEXFADROSTAT IC50 = 794.33 nM 6.10
CHEMBL3099695 OSILODROSTAT IC50 = 1584.89 nM 5.80
CHEMBL4207995 IC50 > 31622.78 nM -
CHEMBL4212612 IC50 > 31622.78 nM -
CHEMBL4211193 IC50 > 19952.62 nM -
CHEMBL4212918 IC50 > 31622.78 nM -
CHEMBL4214618 IC50 > 31622.78 nM -
CHEMBL4207348 IC50 > 19952.62 nM -