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Compound Detail

CHEMBL4636550

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Cc1cc(Br)c(NC2=NCCN2)c2ccccc12

Basic Information

ChEMBL ID CHEMBL4636550
Phase Preclinical
Structure Type MOL
InChI Key UYAOIRISFNRFCT-UHFFFAOYSA-N
4
Targets
5
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

304.2
MW (Da)
3.28
ALogP
3
HBA
2
HBD
36.4
PSA (Ų)
0.85
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C14H14BrN3
MW 304.19
Aromatic Rings 2
Heavy Atoms 18
NP-Likeness -0.47

Activity Summary

IC50 4 meas. best 6.75
Kd 1 meas. best 5.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-2C adrenergic receptor
CHEMBL1916
IC50 6.75 6.75 180.0 1
Alpha-1A adrenergic receptor
CHEMBL229
IC50 6.52 6.52 300.0 1
Complement factor B
CHEMBL5731
IC50 5.18 5.18 6600.0 1
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 5.15 5.15 7100.0 1
Complement factor B
CHEMBL5731
Kd 5.0 5.0 10000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32073845 10.1021/acs.jmedchem.9b01870 Complement factor B 2
32073845 10.1021/acs.jmedchem.9b01870 Voltage-gated inwardly rectifying potassium channel KCNH2 1
32073845 10.1021/acs.jmedchem.9b01870 Alpha-1A adrenergic receptor 1
32073845 10.1021/acs.jmedchem.9b01870 Alpha-2C adrenergic receptor 1

Data from ChEMBL 36 via Core Engine