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Compound Detail

CHEMBL127317

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COc1ccccc1N1CCN(CCCCNC(=O)c2ccc3ccccc3n2)CC1

Basic Information

ChEMBL ID CHEMBL127317
Phase Preclinical
Structure Type MOL
InChI Key CDDVHWKFFCJTOZ-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

418.5
MW (Da)
3.58
ALogP
5
HBA
1
HBD
57.7
PSA (Ų)
0.57
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H30N4O2
MW 418.54
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -1.41

Activity Summary

Ki 5 meas. best 8.46

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(3) dopamine receptor
CHEMBL234
Ki 8.46 8.46 3.5 1
D(3) dopamine receptor
CHEMBL3138
Ki 8.32 8.32 4.8 1
D(2) dopamine receptor
CHEMBL217
Ki 7.17 7.17 66.8 1
D(2) dopamine receptor
CHEMBL339
Ki 7.08 7.08 83.0 1
D(1A) dopamine receptor
CHEMBL265
Ki 5.87 5.87 1350.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12930145 10.1021/jm0211220 D(1A) dopamine receptor 1
12930145 10.1021/jm0211220 D(2) dopamine receptor 1
12930145 10.1021/jm0211220 D(3) dopamine receptor 1
12930145 10.1021/jm0211220 5-hydroxytryptamine receptor 1A 1
12930145 10.1021/jm0211220 Alpha-1A adrenergic receptor 1
12930145 10.1021/jm0211220 Alpha-2A adrenergic receptor 1
26203768 10.1021/acs.jmedchem.5b00776 D(2) dopamine receptor 1
26203768 10.1021/acs.jmedchem.5b00776 D(3) dopamine receptor 1
26203768 10.1021/acs.jmedchem.5b00776 Unchecked 1

Data from ChEMBL 36 via Core Engine