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Compound Detail

CHEMBL231015

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N#Cc1ccc(N2C(=O)[C@@H]3[C@H](O)CCN3C2=O)c(F)c1F

Basic Information

ChEMBL ID CHEMBL231015
Phase Preclinical
Structure Type MOL
InChI Key RGNPRJOXPPHAJR-KCJUWKMLSA-N
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

293.2
MW (Da)
0.74
ALogP
4
HBA
1
HBD
84.6
PSA (Ų)
0.77
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C13H9F2N3O3
MW 293.23
Aromatic Rings 1
Heavy Atoms 21
NP-Likeness -0.59

Activity Summary

EC50 1 meas. best 7.33
Ki 1 meas. best 8.37

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Androgen receptor
CHEMBL1871
Ki 8.37 8.37 4.3 1
Androgen receptor
CHEMBL1871
EC50 7.33 7.33 47.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Androgen receptor Ki = 4.3 nM 8.37 Binding affinity to human AR 17292608
Androgen receptor EC50 = 47.0 nM 7.33 Agonist activity at human AR 17292608

Literature References

PubMed DOI Target Context # Activities
17292608 10.1016/j.bmcl.2007.01.076 Androgen receptor 2

Data from ChEMBL 36 via Core Engine