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Compound Detail

CHEMBL555983

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COc1cc2nc(N(C)CCN(C)C(=O)c3ccco3)nc(N)c2cc1OC.Cl

Basic Information

ChEMBL ID CHEMBL555983
Phase Preclinical
Structure Type MOL
InChI Key GRKMDKHBVDNSMQ-UHFFFAOYSA-N
Parent Compound CHEMBL153576
Active Moiety CHEMBL153576
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

385.4
MW (Da)
2.03
ALogP
8
HBA
1
HBD
107.0
PSA (Ų)
0.66
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H24ClN5O4
MW 421.89
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -1.09

Activity Summary

Kd 2 meas. best 7.18

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adrenergic receptor alpha-1
CHEMBL1907610
Kd 7.18 7.18 66.1 1
Rattus norvegicus
CHEMBL376
Kd 5.37 5.37 4265.8 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
3941410 10.1021/jm00151a003 Rattus norvegicus 2
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