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Compound Detail

CHEMBL4797755

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NCc1ccc(NC(=O)N2C(=O)CC2CC(=O)NCCC(=O)O)cc1.O=C(O)C(F)(F)F

Basic Information

ChEMBL ID CHEMBL4797755
Phase Preclinical
Structure Type MOL
InChI Key WNJSILFLYVIFJS-UHFFFAOYSA-N
Parent Compound CHEMBL4804104
Active Moiety CHEMBL4804104
2
Targets
4
Activities
2
Assay Types
0
PK Parameters
12
Publications
0
Known Names

Molecular Properties

348.4
MW (Da)
0.26
ALogP
5
HBA
4
HBD
141.8
PSA (Ų)
0.52
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H21F3N4O7
MW 462.38
Aromatic Rings 1
Heavy Atoms 25
NP-Likeness -0.75

Activity Summary

EC50 2 meas. best 8.17
IC50 2 meas. best 8.26

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Integrin alpha-5/beta-1
CHEMBL2095226
IC50 8.26 8.26 5.5 1
Integrin alpha-5/beta-1
CHEMBL2095226
EC50 8.17 8.17 6.7 1
Integrin alpha-IIb/beta-3
CHEMBL2093869
EC50 5.81 5.81 1563.0 1
Integrin alpha-IIb/beta-3
CHEMBL2093869
IC50 5.81 5.81 1563.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27726366 10.1021/acs.jmedchem.6b00576 Integrin alpha-5/beta-1 5
27726366 10.1021/acs.jmedchem.6b00576 Integrin alpha-IIb/beta-3 4
27726366 10.1021/acs.jmedchem.6b00576 Integrin alpha-4/beta-1 4
27726366 10.1021/acs.jmedchem.6b00576 Integrin alpha-V/beta-3 3
27726366 10.1021/acs.jmedchem.6b00576 Integrin alpha-V/beta-5 3
27726366 10.1021/acs.jmedchem.6b00576 Integrin alpha-V/beta-6 3
27726366 10.1021/acs.jmedchem.6b00576 Integrin alpha-L/beta-2 (LFA-1) 2
27726366 10.1021/acs.jmedchem.6b00576 SK-MEL-24 1
27726366 10.1021/acs.jmedchem.6b00576 MCF7 1
27726366 10.1021/acs.jmedchem.6b00576 HT-29 1
27726366 10.1021/acs.jmedchem.6b00576 K562 1
27726366 10.1021/acs.jmedchem.6b00576 HEL 1

Data from ChEMBL 36 via Core Engine