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Compound Detail

CHEMBL1641679

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Cl.c1ccc2c(N=C3NCCN3)n[nH]c2c1

Basic Information

ChEMBL ID CHEMBL1641679
Phase Preclinical
Structure Type MOL
InChI Key MSYWDLFJDMREGG-UHFFFAOYSA-N
Parent Compound CHEMBL1739201
Active Moiety CHEMBL1739201
3
Targets
4
Activities
3
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

201.2
MW (Da)
0.74
ALogP
2
HBA
3
HBD
65.1
PSA (Ų)
0.64
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C10H12ClN5
MW 237.69
Aromatic Rings 2
Heavy Atoms 15
NP-Likeness -0.80

Activity Summary

Ki 2 meas. best 7.41
EC50 1 meas. best 7.09
IC50 1 meas. best 5.49

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adrenergic receptor alpha-2
CHEMBL2093864
Ki 7.41 7.41 39.4 1
Alpha-2A adrenergic receptor
CHEMBL1867
EC50 7.09 7.09 82.0 1
Nischarin
CHEMBL5221
Ki 6.87 6.87 133.6 1
Nischarin
CHEMBL5221
IC50 5.49 5.49 3219.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
21129985 10.1016/j.bmc.2010.11.020 Nischarin 2
21129985 10.1016/j.bmc.2010.11.020 Alpha-2A adrenergic receptor 2
21129985 10.1016/j.bmc.2010.11.020 Adrenergic receptor alpha-1 1
21129985 10.1016/j.bmc.2010.11.020 Adrenergic receptor alpha-2 1
21129985 10.1016/j.bmc.2010.11.020 Unchecked 1

Data from ChEMBL 36 via Core Engine