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Compound Detail

CHEMBL203329

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N[C@H](CCc1cnc(Cl)c(/C=C/c2ccncc2)c1)Cc1c[nH]c2ccccc12

Basic Information

ChEMBL ID CHEMBL203329
Phase Preclinical
Structure Type MOL
InChI Key CFYHQUNHGODMIT-GZNAHNRGSA-N
1
Targets
2
Activities
1
Assay Types
4
PK Parameters
3
Publications
0
Known Names

Molecular Properties

402.9
MW (Da)
5.28
ALogP
3
HBA
2
HBD
67.6
PSA (Ų)
0.41
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H23ClN4
MW 402.93
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness -0.13

Activity Summary

IC50 2 meas. best 6.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
RAC-alpha serine/threonine-protein kinase
CHEMBL4282
IC50 6.7 6.7 198.0 2

Pharmacokinetic Data

Parameter Value Units Species
CL 288.33 mL.min-1.kg-1 Mus musculus
Cmax 223.36 nM Mus musculus
F 10.0 % Mus musculus
T1/2 0.2 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16403626 10.1016/j.bmcl.2005.12.017 Mus musculus 5
16403626 10.1016/j.bmcl.2005.12.017 RAC-alpha serine/threonine-protein kinase 1
19497644 10.1016/j.ejmech.2009.04.050 RAC-alpha serine/threonine-protein kinase 1

Data from ChEMBL 36 via Core Engine