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Compound Detail

CHEMBL197968

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COc1ccccc1N1CCN(CCn2c(=O)[nH]c3[nH]c(-c4ccc(C)cc4)cc3c2=O)CC1

Basic Information

ChEMBL ID CHEMBL197968
Phase Preclinical
Structure Type MOL
InChI Key RMKWPAUMYJFUEG-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

459.6
MW (Da)
2.82
ALogP
6
HBA
2
HBD
86.4
PSA (Ų)
0.46
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H29N5O3
MW 459.55
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -1.12

Activity Summary

Ki 2 meas. best 8.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adrenergic receptor alpha-1
CHEMBL2094251
Ki 8.3 8.3 5.0 1
5-hydroxytryptamine receptor 1A
CHEMBL214
Ki 6.48 6.48 333.3 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16216506 10.1016/j.bmcl.2005.09.027 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