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Compound Detail

CHEMBL372222

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Cc1ccc(-c2cc3[nH]c(=O)n(CCN4CCN(c5ccccc5Cl)CC4)c(=O)c3[nH]2)cc1

Basic Information

ChEMBL ID CHEMBL372222
Phase Preclinical
Structure Type MOL
InChI Key DSHAQKQNBSNNEJ-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
16
Publications
0
Known Names

Molecular Properties

464.0
MW (Da)
3.47
ALogP
5
HBA
2
HBD
77.1
PSA (Ų)
0.47
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 C25H26ClN5O2
MW 463.97
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -1.42

Activity Summary

Ki 2 meas. best 7.76

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adrenergic receptor alpha-1
CHEMBL1907610
Ki 7.76 7.76 17.3 1
Adrenergic receptor alpha-1
CHEMBL2094251
Ki 7.76 7.76 17.3 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16216506 10.1016/j.bmcl.2005.09.027 Unchecked 4
15801833 10.1021/jm040870h Unchecked 2
15801833 10.1021/jm040870h Adrenergic receptor alpha-1 1
15801833 10.1021/jm040870h 5-hydroxytryptamine receptor 1A 1
15801833 10.1021/jm040870h D(1A) dopamine receptor 1
15801833 10.1021/jm040870h D(2) dopamine receptor 1
15801833 10.1021/jm040870h Serotonin 1a (5-HT1a) receptor/Adrenergic receptor alpha-1 1
16216506 10.1016/j.bmcl.2005.09.027 Adrenergic receptor alpha-1 1
16216506 10.1016/j.bmcl.2005.09.027 5-hydroxytryptamine receptor 1A 1
16216506 10.1016/j.bmcl.2005.09.027 D(1A) dopamine receptor 1
16216506 10.1016/j.bmcl.2005.09.027 D(2) dopamine receptor 1
16216506 10.1016/j.bmcl.2005.09.027 Alpha-1A adrenergic receptor 1
16216506 10.1016/j.bmcl.2005.09.027 Alpha-1B adrenergic receptor 1
16216506 10.1016/j.bmcl.2005.09.027 Alpha-1D adrenergic receptor 1
16216506 10.1016/j.bmcl.2005.09.027 Alpha adrenergic receptor 1A and 1D 1
16216506 10.1016/j.bmcl.2005.09.027 Alpha adrenergic receptor 1A and 1B 1

Data from ChEMBL 36 via Core Engine