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Compound Detail

CHEMBL3349354

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N[C@H]1CC[C@H]([C@H](NC(=O)[C@@H]2CC[C@H]3CN(C(=O)CCc4ccccc4)CC(=O)N32)C(=O)c2nccs2)CC1

Basic Information

ChEMBL ID CHEMBL3349354
Phase Preclinical
Structure Type MOL
InChI Key FJLQUAUIJFZSGX-XHVFSLISSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

537.7
MW (Da)
2.16
ALogP
7
HBA
2
HBD
125.7
PSA (Ų)
0.50
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H35N5O4S
MW 537.69
Aromatic Rings 2
Heavy Atoms 38
NP-Likeness -0.80

Activity Summary

IC50 2 meas. best 7.48

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
IC50 7.48 7.48 33.0 1
Serine protease 1
CHEMBL209
IC50 5.05 5.05 8990.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin IC50 = 33.0 nM 7.48 In vitro inhibitory activity against thrombin(FIIa) 9873743
Serine protease 1 IC50 = 8990.0 nM 5.05 In vitro inhibitory activity against trypsin 9873743

Literature References

PubMed DOI Target Context # Activities
9873743 10.1016/s0960-894x(98)00613-1 Prothrombin 1
9873743 10.1016/s0960-894x(98)00613-1 Serine protease 1 1
9873743 10.1016/s0960-894x(98)00613-1 Thrombin & trypsin 1
9873743 10.1016/s0960-894x(98)00613-1 Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine