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Compound Detail

CHEMBL1916253

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CNC(=O)Cn1ccc(C(=O)N[C@H]2C(C)(C)[C@H](Oc3ccc(C#N)c(Cl)c3)C2(C)C)n1

Basic Information

ChEMBL ID CHEMBL1916253
Phase Preclinical
Structure Type MOL
InChI Key QZVUDGBPCSXUBE-MXVIHJGJSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

443.9
MW (Da)
2.77
ALogP
6
HBA
2
HBD
109.0
PSA (Ų)
0.71
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H26ClN5O3
MW 443.94
Aromatic Rings 2
Heavy Atoms 31
NP-Likeness -1.43

Activity Summary

IC50 1 meas. best 6.79

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Androgen receptor
CHEMBL1871
IC50 6.79 6.79 163.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Androgen receptor IC50 = 163.0 nM 6.79 Antagonist activity at human AR overexpressed in human LNCAP cells by luciferase... 21936524

Literature References

PubMed DOI Target Context # Activities
21936524 10.1021/jm201059s Androgen receptor 2
21936524 10.1021/jm201059s No relevant target 1

Data from ChEMBL 36 via Core Engine