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Compound Detail

CHEMBL210283

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COc1ccccc1N1CCN(Cc2cn3cc(C)cc(C#N)c3n2)CC1

Basic Information

ChEMBL ID CHEMBL210283
Phase Preclinical
Structure Type MOL
InChI Key VXHLHYPOHKQMNB-UHFFFAOYSA-N
4
Targets
5
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

361.4
MW (Da)
2.85
ALogP
6
HBA
0
HBD
56.8
PSA (Ų)
0.72
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 C21H23N5O
MW 361.45
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -1.89

Activity Summary

Ki 5 meas. best 8.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(4) dopamine receptor
CHEMBL219
Ki 8.89 8.89 1.3 1
D(2) dopamine receptor
CHEMBL217
Ki 5.57 5.475 2700.0 2
D(3) dopamine receptor
CHEMBL234
Ki 5.46 5.46 3500.0 1
D(1A) dopamine receptor
CHEMBL5067
Ki 4.4 4.4 40000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16789750 10.1021/jm060166w Dopamine receptors; D2 & D4 2
16789750 10.1021/jm060166w D(2) dopamine receptor 2
16789750 10.1021/jm060166w Adrenergic receptor alpha-1 1
16789750 10.1021/jm060166w 5-hydroxytryptamine receptor 2A 1
16789750 10.1021/jm060166w 5-hydroxytryptamine receptor 1A 1
16789750 10.1021/jm060166w D(4) dopamine receptor 1
16789750 10.1021/jm060166w D(3) dopamine receptor 1
16789750 10.1021/jm060166w D(1A) dopamine receptor 1

Data from ChEMBL 36 via Core Engine