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Compound Detail

CHEMBL263510

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Cc1n[nH]c2ccc(-c3cncc(OC[C@@H](N)Cc4csc5ccccc45)c3)cc12

Basic Information

ChEMBL ID CHEMBL263510
Phase Preclinical
Structure Type MOL
InChI Key YULFZKNFQQGIAT-IBGZPJMESA-N
2
Targets
2
Activities
2
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

414.5
MW (Da)
5.10
ALogP
5
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 C24H22N4OS
MW 414.53
Aromatic Rings 5
Heavy Atoms 30
NP-Likeness -1.31

Activity Summary

EC50 1 meas. best 6.4
Ki 1 meas. best 8.18

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
RAC-alpha serine/threonine-protein kinase
CHEMBL4282
Ki 8.18 8.18 6.6 1
MIA PaCa-2
CHEMBL614725
EC50 6.4 6.4 400.0 1

Pharmacokinetic Data

Parameter Value Units Species
F 4.2 % Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16678413 10.1016/j.bmcl.2006.04.046 Mus musculus 1
16678413 10.1016/j.bmcl.2006.04.046 RAC-alpha serine/threonine-protein kinase 1
16678413 10.1016/j.bmcl.2006.04.046 MIA PaCa-2 1

Data from ChEMBL 36 via Core Engine