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Compound Detail

CHEMBL3911428

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COc1cccc(C(=O)Nc2cccc(C(=O)c3ccc4c(/C=C/c5ccccn5)n[nH]c4c3)c2)c1

Basic Information

ChEMBL ID CHEMBL3911428
Phase Preclinical
Structure Type MOL
InChI Key VMJJERJLIKJPNQ-WYMLVPIESA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
0
Publications
0
Known Names

Molecular Properties

474.5
MW (Da)
5.62
ALogP
5
HBA
2
HBD
97.0
PSA (Ų)
0.30
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 C29H22N4O3
MW 474.52
Aromatic Rings 5
Heavy Atoms 36
NP-Likeness -1.30

Activity Summary

IC50 1 meas. best 9.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
NON-PROTEIN TARGET
CHEMBL3879801
IC50 9.0 9.0 1.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 2178.0 ng.hr.mL-1 Mus musculus
Cmax 1256.01 nM Mus musculus
T1/2 2.0 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
NON-PROTEIN TARGET IC50 = 1.0 nM 9.0 Antiproliferative activity against VEGF-stimulated HUVEC cells assessed as reduc... -

Data from ChEMBL 36 via Core Engine