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Compound Detail

CHEMBL299110

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O=C(O)C[C@H](NC(=O)Cn1c(C2CC2)c(Cl)nc(NCc2ccc3c(n2)NCCC3)c1=O)c1cccc(F)c1

Basic Information

ChEMBL ID CHEMBL299110
Phase Preclinical
Structure Type MOL
InChI Key FRCHUTQNZCVLPJ-FQEVSTJZSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

555.0
MW (Da)
3.61
ALogP
8
HBA
4
HBD
138.2
PSA (Ų)
0.30
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H28ClFN6O4
MW 555.01
Aromatic Rings 3
Heavy Atoms 39
NP-Likeness -1.07

Activity Summary

IC50 1 meas. best 8.57

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Integrin alpha-V/beta-3
CHEMBL1907598
IC50 8.57 8.57 2.7 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Integrin alpha-V/beta-3 IC50 = 2.7 nM 8.57 Inhibitory activity against human alpha V beta3 receptor using SPAV3 assay 12729670

Literature References

PubMed DOI Target Context # Activities
12729670 10.1016/s0960-894x(03)00254-3 Integrin alpha-V/beta-3 1
12729670 10.1016/s0960-894x(03)00254-3 No relevant target 1
12729670 10.1016/s0960-894x(03)00254-3 Integrin alpha-IIb/beta-3 1

Data from ChEMBL 36 via Core Engine