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Compound Detail

CHEMBL4462252

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CC(C)NC[C@H](O)COc1ccccc1CCn1cc(CNCc2cn(CCc3ccccc3OC[C@@H](O)CNC(C)C)nn2)nn1

Basic Information

ChEMBL ID CHEMBL4462252
Phase Preclinical
Structure Type MOL
InChI Key QOXJTXGLPUKWGZ-ACHIHNKUSA-N
2
Targets
5
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

649.8
MW (Da)
2.12
ALogP
13
HBA
5
HBD
156.4
PSA (Ų)
0.09
QED
2
Ro5 Violations
22
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C34H51N9O4
MW 649.84
Aromatic Rings 4
Heavy Atoms 47
NP-Likeness -0.77

Activity Summary

IC50 3 meas. best 8.69
Ki 2 meas. best 9.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Beta-2 adrenergic receptor
CHEMBL210
Ki 9.05 9.05 0.9 1
Beta-2 adrenergic receptor
CHEMBL210
IC50 8.69 8.51 2.0 2
Beta-1 adrenergic receptor
CHEMBL213
Ki 8.54 8.54 2.9 1
Beta-1 adrenergic receptor
CHEMBL213
IC50 7.71 7.71 19.5 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
31298548 10.1021/acs.jmedchem.9b00595 Beta-2 adrenergic receptor 4
31298548 10.1021/acs.jmedchem.9b00595 Unchecked 2
31298548 10.1021/acs.jmedchem.9b00595 Beta-1 adrenergic receptor 2

Data from ChEMBL 36 via Core Engine