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Compound Detail

CHEMBL83649

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O=C(O)C[C@H](NC(=O)CCCCc1ccc2c(n1)NCCC2)c1cccc(F)c1

Basic Information

ChEMBL ID CHEMBL83649
Phase Preclinical
Structure Type MOL
InChI Key HTVBJLAHDXBYNO-IBGZPJMESA-N
1
Targets
3
Activities
1
Assay Types
3
PK Parameters
6
Publications
0
Known Names

Molecular Properties

399.5
MW (Da)
3.62
ALogP
4
HBA
3
HBD
91.3
PSA (Ų)
0.56
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 C22H26FN3O3
MW 399.47
Aromatic Rings 2
Heavy Atoms 29
NP-Likeness -0.54

Activity Summary

IC50 3 meas. best 7.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Integrin alpha-V/beta-3
CHEMBL1907598
IC50 7.64 7.64 22.7 3

Pharmacokinetic Data

Parameter Value Units Species
CL 2.0 mL.min-1.kg-1 Canis lupus familiaris
F 81.0 % Canis lupus familiaris
T1/2 5.5 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12161158 10.1016/s0960-894x(02)00396-7 Canis familiaris 3
12419389 10.1016/s0960-894x(02)00743-6 Integrin alpha-V/beta-3 1
12161158 10.1016/s0960-894x(02)00396-7 Integrin alpha-V/beta-3 1
12161158 10.1016/s0960-894x(02)00396-7 Homo sapiens 1
12161158 10.1016/s0960-894x(02)00396-7 No relevant target 1
15369386 10.1021/jm049874c Integrin alpha-V/beta-3 1

Data from ChEMBL 36 via Core Engine