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Compound Detail

CHEMBL545646

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CC1=C(CC2=NCCN2)CCc2ccccc21.Cl

Basic Information

ChEMBL ID CHEMBL545646
Phase Preclinical
Structure Type MOL
InChI Key CIKCFHIGSXCOHB-UHFFFAOYSA-N
Parent Compound CHEMBL1194128
Active Moiety CHEMBL1194128
3
Targets
9
Activities
3
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

226.3
MW (Da)
2.80
ALogP
2
HBA
1
HBD
24.4
PSA (Ų)
0.82
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H19ClN2
MW 262.78
Aromatic Rings 1
Heavy Atoms 17
NP-Likeness 0.27

Activity Summary

IC50 3 meas. best 6.4
Kd 3 meas. best 7.19
Ki 3 meas. best 7.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adrenergic receptor alpha-2
CHEMBL2093864
Ki 7.92 7.92 12.0 2
Adrenergic receptor alpha-2
CHEMBL2093864
Kd 7.19 7.19 64.6 2
Adrenergic receptor alpha-1
CHEMBL1907610
Kd 7.08 7.08 83.2 1
Adrenergic receptor alpha-1
CHEMBL1907610
Ki 6.83 6.83 148.0 1
Rattus norvegicus
CHEMBL376
IC50 6.4 5.0667 400.0 3

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
3039138 10.1021/jm00391a034 Adrenergic receptor alpha-2 4
3039138 10.1021/jm00391a034 Rattus norvegicus 4
3039138 10.1021/jm00391a034 Mus musculus 2
3039138 10.1021/jm00391a034 Adrenergic receptor alpha-1 2
3039138 10.1021/jm00391a034 Unchecked 2

Data from ChEMBL 36 via Core Engine