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Compound Detail

CHEMBL168411

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Cn1c(C(=O)[C@H](Cc2cccc(C(=N)N)c2)NC(=O)[C@@H]2CC[C@H]3CN(C(=O)CCc4ccccc4)CC(=O)N32)nc2ccccc21

Basic Information

ChEMBL ID CHEMBL168411
Phase Preclinical
Structure Type MOL
InChI Key AWCMDTMSPRXSSZ-RWPDHJIBSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

619.7
MW (Da)
2.60
ALogP
7
HBA
3
HBD
154.5
PSA (Ų)
0.14
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C35H37N7O4
MW 619.73
Aromatic Rings 4
Heavy Atoms 46
NP-Likeness -0.70

Activity Summary

IC50 2 meas. best 6.35

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
IC50 6.35 6.35 450.0 1
Serine protease 1
CHEMBL209
IC50 4.73 4.73 18680.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin IC50 = 450.0 nM 6.35 Inhibition of human Thrombin 10206546
Serine protease 1 IC50 = 18680.0 nM 4.73 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