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Compound Detail

CHEMBL256082

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O=c1cc(C(F)(F)F)c2cc3c(cc2[nH]1)OC[C@@H](Cc1ccccc1)N3CC(F)(F)F

Basic Information

ChEMBL ID CHEMBL256082
Phase Preclinical
Structure Type MOL
InChI Key RJQQBUCAUJOLTN-CYBMUJFWSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

442.4
MW (Da)
4.92
ALogP
3
HBA
1
HBD
45.3
PSA (Ų)
0.59
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H16F6N2O2
MW 442.36
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -0.64

Activity Summary

IC50 1 meas. best 7.29

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Androgen receptor
CHEMBL1871
IC50 7.29 7.29 51.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Androgen receptor IC50 = 51.0 nM 7.29 Antagonist activity at human androgen receptor in CV1 cells by transcriptional a... 18400499

Literature References

PubMed DOI Target Context # Activities
18400499 10.1016/j.bmcl.2008.03.062 Androgen receptor 3

Data from ChEMBL 36 via Core Engine