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Compound Detail

CHEMBL1916250

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CC1(C)[C@H](NC(=O)c2ccn(CCO)n2)C(C)(C)[C@H]1Oc1ccc(C#N)c(Cl)c1

Basic Information

ChEMBL ID CHEMBL1916250
Phase Preclinical
Structure Type MOL
InChI Key HHRVRIGYVNQMQH-WGSAOQKQSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

416.9
MW (Da)
3.01
ALogP
6
HBA
2
HBD
100.2
PSA (Ų)
0.75
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 C21H25ClN4O3
MW 416.91
Aromatic Rings 2
Heavy Atoms 29
NP-Likeness -1.19

Activity Summary

IC50 1 meas. best 6.87

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Androgen receptor
CHEMBL1871
IC50 6.87 6.87 136.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 12.0 mL.min-1.g-1 Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Androgen receptor IC50 = 136.0 nM 6.87 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 Liver microsomes 1
21936524 10.1021/jm201059s No relevant target 1

Data from ChEMBL 36 via Core Engine