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Compound Detail

CHEMBL452680

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COc1cc2c(Oc3ccc(-c4cnc(Cc5ccc(C)cc5)n(C)c4=O)cc3F)ccnc2cc1OCCCN1CCOCC1

Basic Information

ChEMBL ID CHEMBL452680
Phase Preclinical
Structure Type MOL
InChI Key ATTJPKDHHQLOJJ-UHFFFAOYSA-N
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

624.7
MW (Da)
5.94
ALogP
9
HBA
0
HBD
87.9
PSA (Ų)
0.17
QED
2
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C36H37FN4O5
MW 624.71
Aromatic Rings 5
Heavy Atoms 46
NP-Likeness -1.03

Activity Summary

IC50 1 meas. best 8.02
Ki 1 meas. best 8.02

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Hepatocyte growth factor receptor
CHEMBL3717
IC50 8.02 8.02 9.6 1
Hepatocyte growth factor receptor
CHEMBL3717
Ki 8.02 8.02 9.6 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Hepatocyte growth factor receptor IC50 = 9.6 nM 8.02 Inhibition of human c-MET 21641696
Hepatocyte growth factor receptor Ki = 9.6 nM 8.02 Inhibition of cMet by HTRF assay 18763753

Literature References

PubMed DOI Target Context # Activities
18763753 10.1021/jm8006189 Hepatocyte growth factor receptor 1
21641696 10.1016/j.ejmech.2011.05.031 Hepatocyte growth factor receptor 1

Data from ChEMBL 36 via Core Engine