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Compound Detail

CHEMBL130884

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CC(Nc1ccccc1-c1ccccc1)C1=NCCN1

Basic Information

ChEMBL ID CHEMBL130884
Phase Preclinical
Structure Type MOL
InChI Key QPAIAAWBFFTOPZ-UHFFFAOYSA-N
5
Targets
8
Activities
2
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

265.4
MW (Da)
3.16
ALogP
3
HBA
2
HBD
36.4
PSA (Ų)
0.89
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H19N3
MW 265.36
Aromatic Rings 2
Heavy Atoms 20
NP-Likeness -0.53

Activity Summary

Ki 5 meas. best 7.04
EC50 3 meas. best 7.03

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-2A adrenergic receptor
CHEMBL1867
Ki 7.04 7.04 91.2 1
Alpha-2C adrenergic receptor
CHEMBL1916
EC50 7.03 7.03 93.3 1
Adrenergic receptor alpha-2
CHEMBL2093864
Ki 7.0 7.0 100.0 1
Alpha-2A adrenergic receptor
CHEMBL1867
EC50 6.41 6.41 389.1 1
Alpha-2C adrenergic receptor
CHEMBL1916
Ki 6.15 6.15 708.0 1
Alpha-2B adrenergic receptor
CHEMBL1942
Ki 5.94 5.94 1148.2 1
Alpha-2B adrenergic receptor
CHEMBL1942
EC50 5.42 5.42 3801.9 1
Monoamine oxidase
CHEMBL2095205
Ki 4.9 4.9 12589.2 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11754577 10.1021/jm0110082 Adrenergic receptor alpha-2 3
15566287 10.1021/jm0408215 Alpha-2C adrenergic receptor 3
15566287 10.1021/jm0408215 Alpha-2B adrenergic receptor 3
15566287 10.1021/jm0408215 Alpha-2A adrenergic receptor 3
11754577 10.1021/jm0110082 Monoamine oxidase 1
11754577 10.1021/jm0110082 Adrenergic receptor alpha-1 1
11754577 10.1021/jm0110082 Unchecked 1

Data from ChEMBL 36 via Core Engine