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Compound Detail

CHEMBL424906

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Cc1cccc(Cl)c1NC(=O)c1cnc(Nc2cccc(NCCCn3ccnc3)n2)s1

Basic Information

ChEMBL ID CHEMBL424906
Phase Preclinical
Structure Type MOL
InChI Key SJHDMDLDMVESHW-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
2
PK Parameters
8
Publications
0
Known Names

Molecular Properties

468.0
MW (Da)
5.19
ALogP
8
HBA
3
HBD
96.8
PSA (Ų)
0.29
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H22ClN7OS
MW 467.99
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -2.19

Activity Summary

IC50 3 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
T-cell
CHEMBL614309
IC50 8.7 8.7 2.0 1
PC-3
CHEMBL390
IC50 8.55 8.55 2.8 1
WiDr
CHEMBL614647
IC50 8.39 8.39 4.1 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 74.88 ng.hr.mL-1 Mus musculus
Cmax 88.0 nM Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15615512 10.1021/jm049486a Mus musculus 3
17154512 10.1021/jm060727j T-cell 1
17154512 10.1021/jm060727j Tyrosine-protein kinase Lck 1
15615512 10.1021/jm049486a K562 1
15615512 10.1021/jm049486a PC-3 1
15615512 10.1021/jm049486a MDA-MB-231 1
15615512 10.1021/jm049486a WiDr 1
15615512 10.1021/jm049486a Serum 1

Data from ChEMBL 36 via Core Engine