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Compound Detail

CHEMBL4238556

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O=C(O)C[C@H](CN1CC[C@@H](CCc2ccc3c(n2)NCCC3)C1)c1cccc(C2CCOCC2)c1

Basic Information

ChEMBL ID CHEMBL4238556
Phase Preclinical
Structure Type MOL
InChI Key XHXYGMZLRLAEDM-QFQXNSOFSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

477.6
MW (Da)
4.85
ALogP
5
HBA
2
HBD
74.7
PSA (Ų)
0.54
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H39N3O3
MW 477.65
Aromatic Rings 2
Heavy Atoms 35
NP-Likeness -0.16

Activity Summary

IC50 2 meas. best 7.9

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Integrin alpha-V/beta-6
CHEMBL2111416
IC50 7.9 7.9 12.6 1
Integrin alpha-V/beta-3
CHEMBL1907598
IC50 6.4 6.4 398.1 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
30215258 10.1021/acs.jmedchem.8b00959 Integrin alpha-V/beta-6 2
30215258 10.1021/acs.jmedchem.8b00959 Voltage-gated inwardly rectifying potassium channel KCNH2 2
30215258 10.1021/acs.jmedchem.8b00959 Integrin alpha-V/beta-3 1
30215258 10.1021/acs.jmedchem.8b00959 Integrin alpha-V/beta-1 1
30215258 10.1021/acs.jmedchem.8b00959 Integrin alpha-V/beta-5 1
30215258 10.1021/acs.jmedchem.8b00959 Integrin alpha-V/beta-8 1
30215258 10.1021/acs.jmedchem.8b00959 No relevant target 1

Data from ChEMBL 36 via Core Engine