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Compound Detail

CHEMBL275946

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N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3ccc(F)cc3)c2c1)C(=O)NCc1ccccc1

Basic Information

ChEMBL ID CHEMBL275946
Phase Preclinical
Structure Type MOL
InChI Key BIGFAABVAZSDBH-UWXQCODUSA-N
4
Targets
4
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

759.9
MW (Da)
5.22
ALogP
6
HBA
7
HBD
169.4
PSA (Ų)
0.04
QED
3
Ro5 Violations
17
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C43H50FN9O3
MW 759.93
Aromatic Rings 5
Heavy Atoms 56
NP-Likeness -1.01

Activity Summary

IC50 3 meas. best 6.52
Kd 1 meas. best 9.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Proteinase-activated receptor 1
CHEMBL3974
Kd 9.15 9.15 0.7 1
Unchecked
CHEMBL612545
IC50 6.52 6.52 300.0 1
Collagenase
CHEMBL2095216
IC50 4.9 4.9 12700.0 1
Prothrombin
CHEMBL204
IC50 4.88 4.88 13300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11297447 10.1021/jm000506s Prothrombin 1
11297447 10.1021/jm000506s Unchecked 1
11297447 10.1021/jm000506s Collagenase 1
11297447 10.1021/jm000506s Proteinase-activated receptor 1 1

Data from ChEMBL 36 via Core Engine