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Compound Detail

CHEMBL90874

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COc1ccccc1N1CCN(CCCNc2ncccc2C(=O)NC(C)(C)C)CC1

Basic Information

ChEMBL ID CHEMBL90874
Phase Preclinical
Structure Type MOL
InChI Key YPJUOFYBENZLLE-UHFFFAOYSA-N
4
Targets
4
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

425.6
MW (Da)
3.24
ALogP
6
HBA
2
HBD
69.7
PSA (Ų)
0.63
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H35N5O2
MW 425.58
Aromatic Rings 2
Heavy Atoms 31
NP-Likeness -1.64

Activity Summary

Kd 3 meas. best 8.9
Ki 1 meas. best 8.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-1A adrenergic receptor
CHEMBL3637
Kd 8.9 8.9 1.3 1
Alpha-1A adrenergic receptor
CHEMBL4892
Ki 8.8 8.8 1.6 1
Adrenergic receptor alpha-1
CHEMBL2094251
Kd 8.7 8.7 2.0 1
Alpha-1D adrenergic receptor
CHEMBL326
Kd 8.0 8.0 10.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9276013 10.1021/jm970166j Alpha-1A adrenergic receptor 2
9276013 10.1021/jm970166j Adrenergic receptor alpha-1 1
9276013 10.1021/jm970166j Alpha-1D adrenergic receptor 1

Data from ChEMBL 36 via Core Engine