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Compound Detail

CHEMBL210551

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COc1ccccc1N1CCN(Cc2cn3cc(C)cc(-n4cccn4)c3n2)CC1

Basic Information

ChEMBL ID CHEMBL210551
Phase Preclinical
Structure Type MOL
InChI Key CAVSFHXWRJHLEI-UHFFFAOYSA-N
4
Targets
5
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

402.5
MW (Da)
3.16
ALogP
7
HBA
0
HBD
50.8
PSA (Ų)
0.51
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H26N6O
MW 402.50
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -2.21

Activity Summary

Ki 5 meas. best 8.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(4) dopamine receptor
CHEMBL219
Ki 8.8 8.8 1.6 1
D(2) dopamine receptor
CHEMBL217
Ki 6.55 6.415 280.0 2
D(3) dopamine receptor
CHEMBL234
Ki 5.62 5.62 2400.0 1
D(1A) dopamine receptor
CHEMBL5067
Ki 5.06 5.06 8700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
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