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Compound Detail

CHEMBL203362

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O=c1[nH]c2[nH]c(-c3ccccc3)cc2c(=O)n1CCN1CCN(c2ccccc2Cl)CC1

Basic Information

ChEMBL ID CHEMBL203362
Phase Preclinical
Structure Type MOL
InChI Key RCUUBRFHZZUGFH-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

449.9
MW (Da)
3.16
ALogP
5
HBA
2
HBD
77.1
PSA (Ų)
0.49
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 C24H24ClN5O2
MW 449.94
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -1.25

Activity Summary

Ki 4 meas. best 8.33

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adrenergic receptor alpha-1
CHEMBL2094251
Ki 8.33 8.33 4.7 1
D(2) dopamine receptor
CHEMBL217
Ki 6.86 6.86 137.2 1
D(1A) dopamine receptor
CHEMBL2056
Ki 6.29 6.29 516.0 1
5-hydroxytryptamine receptor 1A
CHEMBL214
Ki 5.81 5.81 1540.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16216506 10.1016/j.bmcl.2005.09.027 Unchecked 3
16216506 10.1016/j.bmcl.2005.09.027 Adrenergic receptor alpha-1 1
16216506 10.1016/j.bmcl.2005.09.027 5-hydroxytryptamine receptor 1A 1
16216506 10.1016/j.bmcl.2005.09.027 D(1A) dopamine receptor 1
16216506 10.1016/j.bmcl.2005.09.027 D(2) dopamine receptor 1

Data from ChEMBL 36 via Core Engine