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Compound Detail

CHEMBL283795

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

Basic Information

ChEMBL ID CHEMBL283795
Phase Preclinical
Structure Type MOL
InChI Key LMFGOELGOHYQNF-UWJYYQICSA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
4
Publications
0
Known Names

Molecular Properties

468.5
MW (Da)
2.69
ALogP
5
HBA
3
HBD
111.6
PSA (Ų)
0.52
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 C25H29FN4O4
MW 468.53
Aromatic Rings 2
Heavy Atoms 34
NP-Likeness -0.63

Activity Summary

IC50 1 meas. best 8.74

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Integrin alpha-V/beta-3
CHEMBL1907598
IC50 8.74 8.74 1.8 1

Pharmacokinetic Data

Parameter Value Units Species
CL 15.0 mL.min-1.kg-1 -
F 44.0 % Eutheria
T1/2 1.5 - -

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Integrin alpha-V/beta-3 IC50 = 1.8 nM 8.74 Inhibition of high affinity radioligand binding to human alphaV-beta3 integrin 11738567

Literature References

PubMed DOI Target Context # Activities
11738567 10.1016/s0960-894x(01)00666-7 ADMET 3
11738567 10.1016/s0960-894x(01)00666-7 Integrin alpha-V/beta-3 1
11738567 10.1016/s0960-894x(01)00666-7 Integrin alpha-IIb/beta-3 1
11738567 10.1016/s0960-894x(01)00666-7 No relevant target 1

Data from ChEMBL 36 via Core Engine