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Compound Detail

CHEMBL542155

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Cl.OC(c1c[nH]cn1)c1cccc2ccccc12

Basic Information

ChEMBL ID CHEMBL542155
Phase Preclinical
Structure Type MOL
InChI Key XXTOUFHDKGRQIA-UHFFFAOYSA-N
Parent Compound CHEMBL1191106
Active Moiety CHEMBL1191106
5
Targets
5
Activities
3
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

224.3
MW (Da)
2.64
ALogP
2
HBA
2
HBD
48.9
PSA (Ų)
0.70
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 C14H13ClN2O
MW 260.72
Aromatic Rings 3
Heavy Atoms 17
NP-Likeness -0.23

Activity Summary

EC50 2 meas. best 6.43
Ki 2 meas. best 5.05
IC50 1 meas. best 4.21

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adrenergic receptor alpha-2
CHEMBL2095158
EC50 6.43 6.43 375.0 1
Adrenergic receptor alpha-2
CHEMBL2093864
Ki 5.05 5.05 8810.0 1
Adrenergic receptor alpha-1
CHEMBL1907610
Ki 5.03 5.03 9255.0 1
Adrenergic receptor alpha-1
CHEMBL2094251
EC50 4.9 4.9 12692.0 1
Alpha-2A adrenergic receptor
CHEMBL1867
IC50 4.21 4.21 61900.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
7914537 10.1021/jm00041a011 Adrenergic receptor alpha-1 2
7914537 10.1021/jm00041a011 Adrenergic receptor alpha-2 2
7914537 10.1021/jm00041a011 Alpha-2A adrenergic receptor 1
7914537 10.1021/jm00041a011 Adrenergic receptor alpha 1
7914537 10.1021/jm00041a011 Unchecked 1

Data from ChEMBL 36 via Core Engine