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Compound Detail

CHEMBL508906

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CCCN(CCC)C(=O)[C@H]1CC[C@H](NC(=O)c2cc3cc(Cl)ccc3[nH]2)[C@H](NC(=O)c2nc3c(s2)CN(C)CC3)C1

Basic Information

ChEMBL ID CHEMBL508906
Phase Preclinical
Structure Type MOL
InChI Key QZGLTRCOJZADHH-JKFKMHIGSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
5
Publications
0
Known Names

Molecular Properties

599.2
MW (Da)
4.61
ALogP
6
HBA
3
HBD
110.4
PSA (Ų)
0.33
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 C30H39ClN6O3S
MW 599.20
Aromatic Rings 3
Heavy Atoms 41
NP-Likeness -1.36

Activity Summary

IC50 1 meas. best 8.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
IC50 8.64 8.64 2.3 1

Pharmacokinetic Data

Parameter Value Units Species
AUC - - Macaca mulatta

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X IC50 = 2.3 nM 8.64 Inhibition of human factor 10a 19128974

Literature References

PubMed DOI Target Context # Activities
19128974 10.1016/j.bmc.2008.12.037 Coagulation factor X 1
19128974 10.1016/j.bmc.2008.12.037 Plasma 1
19128974 10.1016/j.bmc.2008.12.037 Unchecked 1
19128974 10.1016/j.bmc.2008.12.037 No relevant target 1
19128974 10.1016/j.bmc.2008.12.037 Rhesus monkey 1

Data from ChEMBL 36 via Core Engine