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Compound Detail

CHEMBL433911

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N=C(N)N1CCCC(C[C@H](NC(=O)[C@@H]2CC[C@H]3CN(C(=O)CCc4ccccc4)CC(=O)N32)C(=O)c2nc3ccccc3s2)C1

Basic Information

ChEMBL ID CHEMBL433911
Phase Preclinical
Structure Type MOL
InChI Key XCVRAVMOZULGSZ-UASABWJQSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

629.8
MW (Da)
2.79
ALogP
7
HBA
3
HBD
152.8
PSA (Ų)
0.19
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 C33H39N7O4S
MW 629.79
Aromatic Rings 3
Heavy Atoms 45
NP-Likeness -0.85

Activity Summary

IC50 1 meas. best 6.23

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine protease 1
CHEMBL209
IC50 6.23 6.23 590.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Serine protease 1 IC50 = 590.0 nM 6.23 In vitro inhibitory activity against human trypsin 10206546

Literature References

PubMed DOI Target Context # Activities
10206546 10.1016/s0960-894x(99)00096-7 Prothrombin 1
10206546 10.1016/s0960-894x(99)00096-7 Serine protease 1 1
10206546 10.1016/s0960-894x(99)00096-7 Thrombin & trypsin 1

Data from ChEMBL 36 via Core Engine