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Compound Detail

CHEMBL2022272

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Clc1ccc2c(c1)N=C(N1CCN(CCc3ccccc3)CC1)c1cccnc1O2

Basic Information

ChEMBL ID CHEMBL2022272
Phase Preclinical
Structure Type MOL
InChI Key KMWUPPLGFWGMEM-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

418.9
MW (Da)
4.78
ALogP
5
HBA
0
HBD
41.0
PSA (Ų)
0.61
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H23ClN4O
MW 418.93
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -0.99

Activity Summary

Ki 4 meas. best 7.72

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 1A
CHEMBL214
Ki 7.72 7.72 19.0 1
D(4) dopamine receptor
CHEMBL219
Ki 7.38 7.38 42.0 1
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 6.75 6.75 180.0 1
Alpha-2A adrenergic receptor
CHEMBL1867
Ki 6.43 6.43 374.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
22268448 10.1021/jm2013419 Unchecked 12
22268448 10.1021/jm2013419 Caudate-putamen 10
22268448 10.1021/jm2013419 Hippocampus 7
22268448 10.1021/jm2013419 D(2) dopamine receptor 4
22268448 10.1021/jm2013419 Serotonin 1a (5-HT1a) receptor/Adrenergic receptor alpha-1 4
22268448 10.1021/jm2013419 D(4) dopamine receptor 1
22268448 10.1021/jm2013419 5-hydroxytryptamine receptor 1A 1
22268448 10.1021/jm2013419 5-hydroxytryptamine receptor 2A 1
22268448 10.1021/jm2013419 Alpha-2A adrenergic receptor 1
22268448 10.1021/jm2013419 No relevant target 1

Data from ChEMBL 36 via Core Engine