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Compound Detail

CHEMBL3985150

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C=C(C)CNC(=O)c1ccccc1Sc1ccc2c(/C=C/c3ccccn3)n[nH]c2c1

Basic Information

ChEMBL ID CHEMBL3985150
Phase Preclinical
Structure Type MOL
InChI Key QZIPJFDHUBMDBB-JLHYYAGUSA-N
1
Targets
1
Activities
1
Assay Types
6
PK Parameters
0
Publications
0
Known Names

Molecular Properties

426.6
MW (Da)
5.59
ALogP
4
HBA
2
HBD
70.7
PSA (Ų)
0.38
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 C25H22N4OS
MW 426.55
Aromatic Rings 4
Heavy Atoms 31
NP-Likeness -1.31

Activity Summary

IC50 1 meas. best 8.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
NON-PROTEIN TARGET
CHEMBL3879801
IC50 8.52 8.52 3.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 546.0 ng.hr.mL-1 Mus musculus
AUC 157.0 ng.hr.mL-1 Mus musculus
Cmax 1357.4 nM Mus musculus
Cmax 180.52 nM Mus musculus
T1/2 1.5 hr Mus musculus
T1/2 14.6 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
NON-PROTEIN TARGET IC50 = 3.0 nM 8.52 Antiproliferative activity against VEGF-stimulated HUVEC cells assessed as reduc... -

Data from ChEMBL 36 via Core Engine