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Compound Detail

CHEMBL301130

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Cn1c(-c2cccnc2)c(CCCCCC(=O)NCCCC[C@H](N[C@@H]2CCc3ccccc3N(CC(=O)[O-])C2=O)C(=O)[O-])c2cc(Cl)ccc21.[K+].[K+]

Basic Information

ChEMBL ID CHEMBL301130
Phase Preclinical
Structure Type MOL
InChI Key KHBPFIYZMHXNGE-MVYNODGQSA-L
Parent Compound CHEMBL1206726
Active Moiety CHEMBL1206726
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

702.2
MW (Da)
5.76
ALogP
7
HBA
4
HBD
153.9
PSA (Ų)
0.10
QED
2
Ro5 Violations
17
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C38H42ClK2N5O6
MW 778.43
Aromatic Rings 4
Heavy Atoms 50
NP-Likeness -0.47

Activity Summary

IC50 2 meas. best 8.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Thromboxane-A synthase
CHEMBL1835
IC50 8.4 8.4 4.0 1
Angiotensin-converting enzyme
CHEMBL4074
IC50 8.22 8.22 6.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
8021921 10.1021/jm00038a011 Rattus norvegicus 3
8021921 10.1021/jm00038a011 Angiotensin-converting enzyme 1
8021921 10.1021/jm00038a011 Thromboxane-A synthase 1

Data from ChEMBL 36 via Core Engine