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Compound Detail

CHEMBL4758119

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C[C@](O)(Cn1cc(-c2ccccc2)c(C#N)n1)C(=O)Nc1cnc(C#N)c(C(F)(F)F)c1

Basic Information

ChEMBL ID CHEMBL4758119
Phase Preclinical
Structure Type MOL
InChI Key PEHNMVHNHLVZFJ-FQEVSTJZSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

440.4
MW (Da)
3.10
ALogP
7
HBA
2
HBD
127.6
PSA (Ų)
0.63
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H15F3N6O2
MW 440.39
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -1.20

Activity Summary

IC50 1 meas. best 6.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Androgen receptor
CHEMBL1871
IC50 6.24 6.24 579.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Androgen receptor IC50 = 579.0 nM 6.24 Antagonist activity at recombinant human AR expressed in HEK293 cells assessed a... 33095584

Literature References

PubMed DOI Target Context # Activities
33095584 10.1021/acs.jmedchem.0c00943 Androgen receptor 3

Data from ChEMBL 36 via Core Engine