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Compound Detail

CHEMBL543984

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COc1cc2nc(NCC3COc4ccccc4O3)nc(N)c2cc1OC.Cl

Basic Information

ChEMBL ID CHEMBL543984
Phase Preclinical
Structure Type MOL
InChI Key SQUBXEWEVYZMHL-UHFFFAOYSA-N
Parent Compound CHEMBL1192701
Active Moiety CHEMBL1192701
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

368.4
MW (Da)
2.48
ALogP
8
HBA
2
HBD
100.8
PSA (Ų)
0.71
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H21ClN4O4
MW 404.85
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -0.51

Activity Summary

Kd 2 meas. best 7.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adrenergic receptor alpha-1
CHEMBL1907610
Kd 7.22 7.22 60.3 1
Rattus norvegicus
CHEMBL376
Kd 6.17 6.17 676.1 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
2863379 10.1021/jm00147a042 Adrenergic receptor alpha-1 1
2863379 10.1021/jm00147a042 Rattus norvegicus 1
2863379 10.1021/jm00147a042 Unchecked 1

Data from ChEMBL 36 via Core Engine