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Compound Detail

CHEMBL315956

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O=C(NCc1ccccc1)N[C@@H](CCC(=O)N1CCN(c2cccc(NC3=NCCCN3)c2)CC1)C(=O)O

Basic Information

ChEMBL ID CHEMBL315956
Phase Preclinical
Structure Type MOL
InChI Key RGPCXWUHNLAAMX-QHCPKHFHSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

521.6
MW (Da)
1.83
ALogP
7
HBA
5
HBD
138.4
PSA (Ų)
0.34
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H35N7O4
MW 521.62
Aromatic Rings 2
Heavy Atoms 38
NP-Likeness -1.12

Activity Summary

IC50 1 meas. best 8.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Integrin alpha-V/beta-3
CHEMBL1907598
IC50 8.85 8.85 1.4 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Integrin alpha-V/beta-3 IC50 = 1.4 nM 8.85 Inhibition of binding to human alphaV-beta3 integrin 15109653

Literature References

PubMed DOI Target Context # Activities
15109653 10.1016/s0960-894x(04)00293-8 Integrin alpha-V/beta-3 1
15109653 10.1016/s0960-894x(04)00293-8 Integrin alpha-IIb/beta-3 1
15109653 10.1016/s0960-894x(04)00293-8 Integrin alpha-V/beta-3 and alpha-IIb/beta 3 1
15109653 10.1016/s0960-894x(04)00293-8 Homo sapiens 1

Data from ChEMBL 36 via Core Engine