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Compound Detail

CHEMBL357517

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O=C1CC(CN2CCN(c3ncccn3)CC2)Cc2occc21

Basic Information

ChEMBL ID CHEMBL357517
Phase Preclinical
Structure Type MOL
InChI Key FLXRQZHNCDCQLM-UHFFFAOYSA-N
2
Targets
3
Activities
2
Assay Types
0
PK Parameters
12
Publications
0
Known Names

Molecular Properties

312.4
MW (Da)
1.64
ALogP
6
HBA
0
HBD
62.5
PSA (Ų)
0.86
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 C17H20N4O2
MW 312.37
Aromatic Rings 2
Heavy Atoms 23
NP-Likeness -0.84

Activity Summary

Kd 2 meas. best 6.01
Ki 1 meas. best 5.14

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 2B
CHEMBL323
Kd 6.01 5.875 977.2 2
D(2) dopamine receptor
CHEMBL339
Ki 5.14 5.14 7244.4 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11754579 10.1021/jm011014y 5-hydroxytryptamine receptor 2A 2
11754579 10.1021/jm011014y 5-hydroxytryptamine receptor 2B 1
11754579 10.1021/jm011014y 5-hydroxytryptamine receptor 2C 1
11754579 10.1021/jm011014y Serotonin receptor 2a and 2b (5HT2A and 5HT2B) 1
11754579 10.1021/jm011014y Serotonin receptor 2a and 2c (5HT2A and 5HT2C) 1
11101359 10.1021/jm0009890 5-hydroxytryptamine receptor 2A 1
11101359 10.1021/jm0009890 5-hydroxytryptamine receptor 2C 1
11101359 10.1021/jm0009890 D(1A) dopamine receptor 1
11101359 10.1021/jm0009890 D(2) dopamine receptor 1
11101359 10.1021/jm0009890 Unchecked 1
11101359 10.1021/jm0009890 5-hydroxytryptamine receptor 2B 1
11101359 10.1021/jm0009890 Dopamine D2 receptor and serotonin 2a receptor 1

Data from ChEMBL 36 via Core Engine