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Compound Detail

CHEMBL24981

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COc1ccc(Cl)cc1N1CCN(CCCNc2nccc(C(N)=O)n2)CC1

Basic Information

ChEMBL ID CHEMBL24981
Phase Preclinical
Structure Type MOL
InChI Key NNPHPGSVPQWUHP-UHFFFAOYSA-N
4
Targets
5
Activities
2
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

404.9
MW (Da)
1.86
ALogP
7
HBA
2
HBD
96.6
PSA (Ų)
0.65
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 C19H25ClN6O2
MW 404.90
Aromatic Rings 2
Heavy Atoms 28
NP-Likeness -1.68

Activity Summary

Ki 4 meas. best 8.7
Kd 1 meas. best 8.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-1A adrenergic receptor
CHEMBL229
Ki 8.7 8.65 2.0 2
Adrenergic receptor alpha-1
CHEMBL2094251
Kd 8.6 8.6 2.5 1
Alpha-1D adrenergic receptor
CHEMBL223
Ki 8.6 8.6 2.5 1
Alpha-1B adrenergic receptor
CHEMBL232
Ki 7.9 7.9 12.6 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9135028 10.1021/jm960697s Canis familiaris 2
9135028 10.1021/jm960697s NON-PROTEIN TARGET 1
9135028 10.1021/jm960697s Alpha-1A adrenergic receptor 1
9135028 10.1021/jm960697s Alpha-1B adrenergic receptor 1
9135028 10.1021/jm960697s Alpha-1D adrenergic receptor 1
9135028 10.1021/jm960697s Adrenergic receptor alpha-1 1
9135028 10.1021/jm960697s Unchecked 1
15664832 10.1016/j.bmcl.2004.11.032 Alpha-1A adrenergic receptor 1

Data from ChEMBL 36 via Core Engine