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Compound Detail

CHEMBL130276

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c1ccc2c(c1)CC2CCN1CCN(c2cccc3c2OCCO3)CC1

Basic Information

ChEMBL ID CHEMBL130276
Phase Preclinical
Structure Type MOL
InChI Key DHYRQVXQZAGWKI-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

350.5
MW (Da)
3.31
ALogP
4
HBA
0
HBD
24.9
PSA (Ų)
0.84
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H26N2O2
MW 350.46
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness -0.57

Activity Summary

Ki 4 meas. best 9.23

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 1A
CHEMBL273
Ki 9.23 9.23 0.6 1
Adrenergic receptor alpha-1
CHEMBL1907610
Ki 7.66 7.66 21.9 1
D(2) dopamine receptor
CHEMBL339
Ki 7.31 7.31 49.0 1
5-hydroxytryptamine receptor 1B
CHEMBL3459
Ki 6.22 6.22 602.6 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
7562940 10.1021/jm00020a020 Rattus norvegicus 5
7562940 10.1021/jm00020a020 5-hydroxytryptamine receptor 1A 2
7562940 10.1021/jm00020a020 Adrenergic receptor alpha-1 2
7562940 10.1021/jm00020a020 D(2) dopamine receptor 2
7562940 10.1021/jm00020a020 5-hydroxytryptamine receptor 1B 1
7562940 10.1021/jm00020a020 Unchecked 1
7562940 10.1021/jm00020a020 Serotonin 1a (5-HT1a) receptor/Adrenergic receptor alpha-1 1

Data from ChEMBL 36 via Core Engine