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Compound Detail

CHEMBL271201

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CC(=O)Nc1ccc(C)c(C(=O)Nc2cnc(Nc3ccc(N4CCN(C)CC4)cc3)nc2)c1

Basic Information

ChEMBL ID CHEMBL271201
Phase Preclinical
Structure Type MOL
InChI Key CAUQFXUMOJTTIX-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

459.6
MW (Da)
3.49
ALogP
7
HBA
3
HBD
102.5
PSA (Ų)
0.52
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H29N7O2
MW 459.55
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -1.72

Activity Summary

IC50 2 meas. best 7.32

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase Lck
CHEMBL258
IC50 7.32 7.32 48.0 1
Mitogen-activated protein kinase 14
CHEMBL260
IC50 7.2 7.2 63.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18321037 10.1021/jm7010996 Tyrosine-protein kinase Lck 1
18321037 10.1021/jm7010996 Angiopoietin-1 receptor 1
18321037 10.1021/jm7010996 Vascular endothelial growth factor receptor 2 1
18321037 10.1021/jm7010996 Mitogen-activated protein kinase 14 1
18321037 10.1021/jm7010996 Tyrosine-protein kinase JAK3 1

Data from ChEMBL 36 via Core Engine