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Compound Detail

CHEMBL3629353

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O=C(Nc1ccccc1-c1ccc(O)c(Cl)c1)OC1CCN(CCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1

Basic Information

ChEMBL ID CHEMBL3629353
Phase Preclinical
Structure Type MOL
InChI Key SHHHPTFIRLSTIA-DHUJRADRSA-N
2
Targets
2
Activities
2
Assay Types
2
PK Parameters
3
Publications
0
Known Names

Molecular Properties

691.3
MW (Da)
7.33
ALogP
8
HBA
6
HBD
147.2
PSA (Ų)
0.07
QED
3
Ro5 Violations
16
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C38H47ClN4O6
MW 691.27
Aromatic Rings 4
Heavy Atoms 49
NP-Likeness -0.39

Activity Summary

EC50 1 meas. best 8.43
Ki 1 meas. best 9.14

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Muscarinic acetylcholine receptor M3
CHEMBL245
Ki 9.14 9.14 0.7 1
Beta-2 adrenergic receptor
CHEMBL210
EC50 8.43 8.43 3.7 1

Pharmacokinetic Data

Parameter Value Units Species
CL 23.0 mL.min-1.g-1 Homo sapiens
T1/2 1.95 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26471092 10.1016/j.bmcl.2015.10.008 Beta-2 adrenergic receptor 2
26471092 10.1016/j.bmcl.2015.10.008 Muscarinic acetylcholine receptor M3 2
26471092 10.1016/j.bmcl.2015.10.008 Liver microsome 2

Data from ChEMBL 36 via Core Engine