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Compound Detail

CHEMBL262549

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CN1C(=O)[C@@H](CCCCNC(=O)c2ccc(NNC(=O)OC(C)(C)C)nc2)NC(=O)c2cccc(c2)CNC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN=C(N)N.O=C(O)C(F)(F)F.O=C(O)C(F)(F)F

Basic Information

ChEMBL ID CHEMBL262549
Phase Preclinical
Structure Type MOL
InChI Key BMVLVLYYEHPTOX-DXVZVFRVSA-N
Parent Compound CHEMBL1182720
Active Moiety CHEMBL1182720
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

838.9
MW (Da)
-0.78
ALogP
12
HBA
10
HBD
330.8
PSA (Ų)
0.05
QED
3
Ro5 Violations
14
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C42H56F6N12O14
MW 1066.97
Aromatic Rings 2
Heavy Atoms 60
NP-Likeness 0.26

Activity Summary

IC50 1 meas. best 7.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Integrin alpha-IIb/beta-3
CHEMBL2093869
IC50 7.8 7.8 16.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Integrin alpha-IIb/beta-3 IC50 = 16.0 nM 7.8 Inhibition of 125I-fibrinogen binding to alpha IIb beta-3 integrin as inhibition... -

Literature References

PubMed DOI Target Context # Activities
- 10.1016/S0960-894X(97)00083-8 Integrin alpha-IIb/beta-3 1

Data from ChEMBL 36 via Core Engine