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Compound Detail

CHEMBL370364

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Cc1ccc(-c2cc3c(=O)n(CCN4CCN(c5ccccc5Cl)CC4)c(=O)[nH]c3[nH]2)cc1

Basic Information

ChEMBL ID CHEMBL370364
Phase Preclinical
Structure Type MOL
InChI Key OAUFPDQMACFAMN-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
10
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 -1.31

Activity Summary

Ki 4 meas. best 7.93

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adrenergic receptor alpha-1
CHEMBL2094251
Ki 7.93 7.93 11.7 1
D(1A) dopamine receptor
CHEMBL2056
Ki 6.41 6.41 388.7 1
D(2) dopamine receptor
CHEMBL217
Ki 5.76 5.76 1720.0 1
5-hydroxytryptamine receptor 1A
CHEMBL214
Ki 5.74 5.74 1815.0 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
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