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Compound Detail

CHEMBL370125

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COc1ccc(-c2cc3c(=O)n(CCN4CCN(c5ccccc5OC)CC4)c(=O)[nH]c3[nH]2)cc1

Basic Information

ChEMBL ID CHEMBL370125
Phase Preclinical
Structure Type MOL
InChI Key QAWYXANRFIWXDP-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

475.6
MW (Da)
2.52
ALogP
7
HBA
2
HBD
95.6
PSA (Ų)
0.43
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 C26H29N5O4
MW 475.55
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -1.03

Activity Summary

Ki 2 meas. best 8.26

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adrenergic receptor alpha-1
CHEMBL2094251
Ki 8.26 8.26 5.5 1
5-hydroxytryptamine receptor 1A
CHEMBL214
Ki 6.95 6.95 113.4 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
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 Unchecked 1

Data from ChEMBL 36 via Core Engine