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Compound Detail

CHEMBL166543

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N=C(N)c1cccc(CC(NC(=O)[C@@H]2CC[C@H]3CN(C(=O)CCc4ccccc4)CC(=O)N32)C(=O)c2nc3ccccc3s2)c1

Basic Information

ChEMBL ID CHEMBL166543
Phase Preclinical
Structure Type MOL
InChI Key GOBFKUOZUDEDMD-VNBODJOOSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

622.8
MW (Da)
3.33
ALogP
7
HBA
3
HBD
149.6
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 C34H34N6O4S
MW 622.75
Aromatic Rings 4
Heavy Atoms 45
NP-Likeness -0.86

Activity Summary

IC50 2 meas. best 7.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
IC50 7.24 7.24 57.0 1
Serine protease 1
CHEMBL209
IC50 6.01 6.01 970.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin IC50 = 57.0 nM 7.24 Inhibition of human Thrombin 10206546
Serine protease 1 IC50 = 970.0 nM 6.01 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