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Compound Detail

CHEMBL447509

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Cc1ccccc1NC(=O)Nc1ccc(CC(=O)N[C@@H](CCCCNC(=O)/C=C/c2cccnc2)C(=O)N[C@@H](CCCC(=O)O)C(=O)NC2(C(N)=O)CCCCC2)cc1

Basic Information

ChEMBL ID CHEMBL447509
Phase Preclinical
Structure Type MOL
InChI Key OOYFOUHICCOHRQ-CVLSMVSNSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

811.0
MW (Da)
4.11
ALogP
8
HBA
8
HBD
250.8
PSA (Ų)
0.06
QED
2
Ro5 Violations
21
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C43H54N8O8
MW 810.95
Aromatic Rings 3
Heavy Atoms 59
NP-Likeness -0.70

Activity Summary

IC50 1 meas. best 10.43

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Integrin alpha-4/beta-1
CHEMBL1907599
IC50 10.43 10.43 0.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Integrin alpha-4/beta-1 IC50 = 0.037 nM 10.43 Inhibition of human integrin alpha-4-beta-1-mediated MOLT4 cell adhesion to biot... 19072684

Literature References

PubMed DOI Target Context # Activities
16767086 10.1038/nchembio798 Unchecked 17
16767086 10.1038/nchembio798 Integrin alpha-4/beta-1 9
19072684 10.1021/jm800313f Integrin alpha-4/beta-1 1
16767086 10.1038/nchembio798 Integrin alpha2/beta1 1
16767086 10.1038/nchembio798 ITGA6-ITGB1 complex 1
16767086 10.1038/nchembio798 ITGB1-ITGA9 complex 1
16767086 10.1038/nchembio798 Intercellular adhesion molecule (ICAM-1), Integrin alpha-L/beta-2 1
16767086 10.1038/nchembio798 Integrin alpha-M/beta-2 1
16767086 10.1038/nchembio798 Plasma 1
16767086 10.1038/nchembio798 Mus musculus 1

Data from ChEMBL 36 via Core Engine