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Compound Detail

CHEMBL426408

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CC(C)[C@H]1NC(=O)c2cc(cc(NC(=O)CCCCCN)c2)CNC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@H](CCCN=C(N)N)N(C)C1=O.O=C(O)C(F)(F)F.O=C(O)C(F)(F)F

Basic Information

ChEMBL ID CHEMBL426408
Phase Preclinical
Structure Type MOL
InChI Key GPKMDDOTRJJZSK-WRMGOHSWSA-N
Parent Compound CHEMBL1185669
Active Moiety CHEMBL1185669
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

702.8
MW (Da)
-1.52
ALogP
9
HBA
9
HBD
293.5
PSA (Ų)
0.06
QED
2
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C36H52F6N10O12
MW 930.86
Aromatic Rings 1
Heavy Atoms 50
NP-Likeness 0.80

Activity Summary

IC50 1 meas. best 8.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Integrin alpha-IIb/beta-3
CHEMBL2093869
IC50 8.3 8.3 5.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Integrin alpha-IIb/beta-3 IC50 = 5.0 nM 8.3 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