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Compound Detail

CHEMBL3577445

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CC12CCC(C(NC(=O)[C@@H](CC3CCCCC3)NC(=O)N[C@@H](Cc3ccc(N)nc3)C(N)=O)C1)C2(C)C

Basic Information

ChEMBL ID CHEMBL3577445
Phase Preclinical
Structure Type MOL
InChI Key ZFFKLIGSDMVSKR-ZSKJDULESA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

512.7
MW (Da)
3.03
ALogP
5
HBA
5
HBD
152.2
PSA (Ų)
0.34
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H44N6O3
MW 512.70
Aromatic Rings 1
Heavy Atoms 37
NP-Likeness 0.41

Activity Summary

IC50 1 meas. best 6.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Carboxypeptidase B2
CHEMBL3419
IC50 6.24 6.24 570.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Carboxypeptidase B2 IC50 = 570.0 nM 6.24 Inhibition of human activated TAFI incubated for 15 mins by microtiter plate rea... 25990761

Literature References

PubMed DOI Target Context # Activities
25990761 10.1021/jm501840b Carboxypeptidase B2 1

Data from ChEMBL 36 via Core Engine