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Compound Detail

CHEMBL186552

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O=C(O)C[C@H](CCCCCCc1ccc2c(n1)NCCC2)c1cncnc1

Basic Information

ChEMBL ID CHEMBL186552
Phase Preclinical
Structure Type MOL
InChI Key DMDDFJFCCZFCKL-KRWDZBQOSA-N
1
Targets
1
Activities
1
Assay Types
9
PK Parameters
4
Publications
0
Known Names

Molecular Properties

368.5
MW (Da)
3.98
ALogP
5
HBA
2
HBD
88.0
PSA (Ų)
0.62
QED
0
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H28N4O2
MW 368.48
Aromatic Rings 2
Heavy Atoms 27
NP-Likeness 0.18

Activity Summary

IC50 1 meas. best 10.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Integrin alpha-V/beta-3
CHEMBL1907598
IC50 10.15 10.15 0.1 1

Pharmacokinetic Data

Parameter Value Units Species
CL 19.0 mL.min-1.kg-1 Cercopithecidae
CL 3.9 mL.min-1.kg-1 Canis lupus familiaris
CL 30.0 mL.min-1.kg-1 Rattus norvegicus
F 46.0 % Cercopithecidae
F 66.0 % Canis lupus familiaris
F 45.0 % Rattus norvegicus
T1/2 2.3 hr Cercopithecidae
T1/2 6.4 hr Canis lupus familiaris
T1/2 4.5 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15369386 10.1021/jm049874c ADMET 10
15369386 10.1021/jm049874c Rattus norvegicus 2
15369386 10.1021/jm049874c Integrin alpha-V/beta-3 1
15369386 10.1021/jm049874c No relevant target 1

Data from ChEMBL 36 via Core Engine