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Compound Detail

CHEMBL269537

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COc1cc2nc(N3CCC(CC(=O)NCC4CC4)CC3)nc(N)c2cc1OC

Basic Information

ChEMBL ID CHEMBL269537
Phase Preclinical
Structure Type MOL
InChI Key OHRDRIOXKSBXGK-UHFFFAOYSA-N
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

399.5
MW (Da)
2.36
ALogP
7
HBA
2
HBD
102.6
PSA (Ų)
0.74
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 C21H29N5O3
MW 399.50
Aromatic Rings 2
Heavy Atoms 29
NP-Likeness -1.01

Activity Summary

Ki 2 meas. best 8.97
Kd 1 meas. best 7.25

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adrenergic receptor alpha-1
CHEMBL1907610
Ki 8.97 8.97 1.1 1
Adrenergic receptor alpha-2
CHEMBL2093864
Ki 7.27 7.27 53.3 1
Adrenergic receptor alpha
CHEMBL2095203
Kd 7.25 7.25 56.2 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
2884316 10.1021/jm00389a007 Adrenergic receptor alpha-1 4
2884316 10.1021/jm00389a007 Adrenergic receptor alpha-2 2
2884316 10.1021/jm00389a007 Adrenergic receptor alpha 1

Data from ChEMBL 36 via Core Engine