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Compound Detail

CHEMBL3947493

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Cc1cnccc1C(=O)Nc1cccc(C(=O)c2ccc3c(/C=C/c4ccccn4)n[nH]c3c2)c1

Basic Information

ChEMBL ID CHEMBL3947493
Phase Preclinical
Structure Type MOL
InChI Key YSPRURCZYCTTAQ-PKNBQFBNSA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
0
Publications
0
Known Names

Molecular Properties

459.5
MW (Da)
5.32
ALogP
5
HBA
2
HBD
100.6
PSA (Ų)
0.34
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 C28H21N5O2
MW 459.51
Aromatic Rings 5
Heavy Atoms 35
NP-Likeness -1.36

Activity Summary

IC50 1 meas. best 8.11

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
NON-PROTEIN TARGET
CHEMBL3879801
IC50 8.11 8.11 7.7 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 1476.0 ng.hr.mL-1 Mus musculus
Cmax 2193.64 nM Mus musculus
T1/2 1.3 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
NON-PROTEIN TARGET IC50 = 7.7 nM 8.11 Antiproliferative activity against VEGF-stimulated HUVEC cells assessed as reduc... -

Data from ChEMBL 36 via Core Engine