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Compound Detail

CHEMBL226849

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N[C@H](COc1cncc(-c2ccc3c(c2)/C(=C\c2ccco2)C(=O)N3)c1)Cc1ccccc1

Basic Information

ChEMBL ID CHEMBL226849
Phase Preclinical
Structure Type MOL
InChI Key RHOXUCVDAMLMFG-NFCNUSAFSA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
2
Publications
0
Known Names

Molecular Properties

437.5
MW (Da)
4.78
ALogP
5
HBA
2
HBD
90.4
PSA (Ų)
0.41
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H23N3O3
MW 437.50
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -0.72

Activity Summary

IC50 1 meas. best 8.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
RAC-alpha serine/threonine-protein kinase
CHEMBL4282
IC50 8.85 8.85 1.4 1

Pharmacokinetic Data

Parameter Value Units Species
AUC - ng.hr.mL-1 Mus musculus
F - % Mus musculus
T1/2 1.15 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
RAC-alpha serine/threonine-protein kinase IC50 = 1.4 nM 8.85 Inhibition of human Akt1 17523610

Literature References

PubMed DOI Target Context # Activities
17523610 10.1021/jm0701019 Mus musculus 3
17523610 10.1021/jm0701019 RAC-alpha serine/threonine-protein kinase 1

Data from ChEMBL 36 via Core Engine