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Compound Detail

CHEMBL1916412

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Cc1nc(O[C@H]2C(C)(C)[C@H](NC(=O)c3cnc4ncccn34)C2(C)C)ccc1C#N

Basic Information

ChEMBL ID CHEMBL1916412
Phase Preclinical
Structure Type MOL
InChI Key NZLHNQPBBYMKKJ-WGSAOQKQSA-N
2
Targets
2
Activities
1
Assay Types
5
PK Parameters
12
Publications
0
Known Names

Molecular Properties

404.5
MW (Da)
2.92
ALogP
7
HBA
1
HBD
105.2
PSA (Ų)
0.72
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H24N6O2
MW 404.47
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -1.21

Activity Summary

IC50 2 meas. best 6.84

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Androgen receptor
CHEMBL1871
IC50 6.84 6.84 144.0 1
LNCaP
CHEMBL612518
IC50 6.84 6.84 144.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 8.0 mL.min-1.g-1 Homo sapiens
CL 11.6 mL.min-1.kg-1 Rattus norvegicus
F 31.0 % Rattus norvegicus
Fu 0.62 uM Mus musculus
T1/2 3.6 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
21936524 10.1021/jm201059s LNCaP 4
21955208 10.1021/jm2010942 Rattus norvegicus 3
21955208 10.1021/jm2010942 Aldehyde oxidase 3
21936524 10.1021/jm201059s Androgen receptor 2
35786895 10.1021/acs.jmedchem.2c00716 LNCaP 2
21936524 10.1021/jm201059s Liver microsomes 1
21936524 10.1021/jm201059s DU-145 1
21936524 10.1021/jm201059s No relevant target 1
21936524 10.1021/jm201059s Plasma 1
21936524 10.1021/jm201059s Mus musculus 1
21955208 10.1021/jm2010942 Liver microsomes 1
21955208 10.1021/jm2010942 Hepatocyte 1

Data from ChEMBL 36 via Core Engine