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Compound Detail

CHEMBL208961

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Cc1cc(-c2cncc(OC[C@@H](N)Cc3c[nH]c4ccccc34)c2)cc2ccncc12

Basic Information

ChEMBL ID CHEMBL208961
Phase Preclinical
Structure Type MOL
InChI Key BHPSGEAUUZMDDL-QFIPXVFZSA-N
1
Targets
1
Activities
1
Assay Types
5
PK Parameters
2
Publications
0
Known Names

Molecular Properties

408.5
MW (Da)
5.04
ALogP
4
HBA
2
HBD
76.8
PSA (Ų)
0.41
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H24N4O
MW 408.51
Aromatic Rings 5
Heavy Atoms 31
NP-Likeness -0.49

Activity Summary

IC50 1 meas. best 6.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
RAC-alpha serine/threonine-protein kinase
CHEMBL4282
IC50 6.0 6.0 995.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 1500.0 ng.hr.mL-1 Mus musculus
AUC - - Mus musculus
CL 2.5 L/hr Mus musculus
F 35.0 % Mus musculus
T1/2 4.5 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 = 995.0 nM 6.0 Inhibition of Akt1 at 5 uM ATP 16603355

Literature References

PubMed DOI Target Context # Activities
16603355 10.1016/j.bmcl.2006.03.041 Mus musculus 6
16603355 10.1016/j.bmcl.2006.03.041 RAC-alpha serine/threonine-protein kinase 1

Data from ChEMBL 36 via Core Engine