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Compound Detail

CHEMBL134707

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O=C(O)C(=O)O.Oc1ccc2c(c1)OC(CNCCCOc1cccc3[nH]ccc13)CC2

Basic Information

ChEMBL ID CHEMBL134707
Phase Preclinical
Structure Type MOL
InChI Key CZCGGKGZTISBCH-UHFFFAOYSA-N
Parent Compound CHEMBL1180601
Active Moiety CHEMBL1180601
3
Targets
4
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

352.4
MW (Da)
3.63
ALogP
4
HBA
3
HBD
66.5
PSA (Ų)
0.57
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 C23H26N2O7
MW 442.47
Aromatic Rings 3
Heavy Atoms 26
NP-Likeness 0.27

Activity Summary

Ki 4 meas. best 9.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 1A
CHEMBL273
Ki 9.22 9.22 0.6 1
D(2) dopamine receptor
CHEMBL339
Ki 9.15 8.52 0.7 2
Adrenergic receptor alpha-1
CHEMBL1907610
Ki 8.22 8.22 6.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9435894 10.1021/jm9703653 D(2) dopamine receptor 3
9435894 10.1021/jm9703653 5-hydroxytryptamine receptor 1A 1
9435894 10.1021/jm9703653 Adrenergic receptor alpha-1 1

Data from ChEMBL 36 via Core Engine