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Compound Detail

CHEMBL4777693

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Nc1ccc(CNC(=O)N2C(=O)C[C@H]2C(=O)O)cc1.O=C(O)C(F)(F)F

Basic Information

ChEMBL ID CHEMBL4777693
Phase Preclinical
Structure Type MOL
InChI Key PBDSUCKUKNOMFW-FVGYRXGTSA-N
Parent Compound CHEMBL4802346
Active Moiety CHEMBL4802346
2
Targets
4
Activities
1
Assay Types
0
PK Parameters
12
Publications
0
Known Names

Molecular Properties

263.2
MW (Da)
0.16
ALogP
4
HBA
3
HBD
112.7
PSA (Ų)
0.53
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C14H14F3N3O6
MW 377.28
Aromatic Rings 1
Heavy Atoms 19
NP-Likeness -0.50

Activity Summary

IC50 4 meas. best 8.12

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Integrin alpha-4/beta-1
CHEMBL1907599
IC50 8.12 8.09 7.6 2
Integrin alpha-5/beta-1
CHEMBL2095226
IC50 6.48 6.38 331.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27726366 10.1021/acs.jmedchem.6b00576 Integrin alpha-4/beta-1 4
27726366 10.1021/acs.jmedchem.6b00576 Integrin alpha-IIb/beta-3 3
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-5/beta-1 2
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