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Compound Detail

CHEMBL497574

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O=C1c2cc3ccccc3n2CCN1CCCCN1CCN(c2ccc(Cl)cc2Cl)CC1

Basic Information

ChEMBL ID CHEMBL497574
Phase Preclinical
Structure Type MOL
InChI Key XLZXIDKEIKKBGP-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

471.4
MW (Da)
5.01
ALogP
4
HBA
0
HBD
31.7
PSA (Ų)
0.47
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H28Cl2N4O
MW 471.43
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -1.50

Activity Summary

Ki 4 meas. best 8.49

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(3) dopamine receptor
CHEMBL234
Ki 8.49 8.49 3.2 1
D(2) dopamine receptor
CHEMBL339
Ki 6.64 6.64 229.0 1
5-hydroxytryptamine receptor 2A
CHEMBL322
Ki 6.52 6.52 300.0 1
D(1A) dopamine receptor
CHEMBL265
Ki 5.37 5.37 4315.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19072656 10.1021/jm800689g Voltage-gated inwardly rectifying potassium channel KCNH2 1
19072656 10.1021/jm800689g Unchecked 1
19072656 10.1021/jm800689g 5-hydroxytryptamine receptor 2A 1
19072656 10.1021/jm800689g 5-hydroxytryptamine receptor 1A 1
19072656 10.1021/jm800689g D(3) dopamine receptor 1
19072656 10.1021/jm800689g D(2) dopamine receptor 1
19072656 10.1021/jm800689g D(1A) dopamine receptor 1

Data from ChEMBL 36 via Core Engine