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Compound Detail

CHEMBL3809462

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COC(=O)c1cc2cc(CCc3cc(NC(=O)c4ccc(CN5CCC(N(C)C)C5)c(C(F)(F)F)c4)ccc3C)cnc2[nH]1

Basic Information

ChEMBL ID CHEMBL3809462
Phase Preclinical
Structure Type MOL
InChI Key IZPYTCMIIAEYJH-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

607.7
MW (Da)
5.85
ALogP
6
HBA
2
HBD
90.6
PSA (Ų)
0.23
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C33H36F3N5O3
MW 607.68
Aromatic Rings 4
Heavy Atoms 44
NP-Likeness -1.26

Activity Summary

EC50 1 meas. best 6.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
HUVEC
CHEMBL613979
EC50 6.77 6.77 171.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
HUVEC EC50 = 171.0 nM 6.77 Antiangiogenic activity in HUVEC after 72 hrs by MTT assay 27010810

Literature References

PubMed DOI Target Context # Activities
27010810 10.1021/acs.jmedchem.6b00087 HepG2 1
27010810 10.1021/acs.jmedchem.6b00087 HUVEC 1
27010810 10.1021/acs.jmedchem.6b00087 Fibroblast growth factor receptor 2 1
27010810 10.1021/acs.jmedchem.6b00087 Serine/threonine-protein kinase B-raf 1
27010810 10.1021/acs.jmedchem.6b00087 Epidermal growth factor receptor 1
27010810 10.1021/acs.jmedchem.6b00087 Platelet-derived growth factor receptor alpha 1
27010810 10.1021/acs.jmedchem.6b00087 Proto-oncogene tyrosine-protein kinase Src 1
27010810 10.1021/acs.jmedchem.6b00087 Vascular endothelial growth factor receptor 2 1

Data from ChEMBL 36 via Core Engine