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Compound Detail

CHEMBL1836647

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O=c1ccc2c([C@@H](O)CNCCCCCCCCCN3CCC(Oc4nn(-c5c(O)cccc5F)c5c4CCCC5)CC3)ccc(O)c2[nH]1

Basic Information

ChEMBL ID CHEMBL1836647
Phase Preclinical
Structure Type MOL
InChI Key MWNIKTJZFRMVQT-UMSFTDKQSA-N
4
Targets
4
Activities
2
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

675.9
MW (Da)
6.04
ALogP
9
HBA
5
HBD
135.9
PSA (Ų)
0.09
QED
2
Ro5 Violations
16
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C38H50FN5O5
MW 675.85
Aromatic Rings 4
Heavy Atoms 49
NP-Likeness -0.44

Activity Summary

EC50 3 meas. best 7.85
Ki 1 meas. best 8.66

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Muscarinic acetylcholine receptor M3
CHEMBL245
Ki 8.66 8.66 2.2 1
Beta-2 adrenergic receptor
CHEMBL210
EC50 7.85 7.85 14.0 1
NON-PROTEIN TARGET
CHEMBL3879801
EC50 7.57 7.57 27.0 1
Cavia porcellus
CHEMBL369
EC50 7.55 7.55 28.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
21863888 10.1021/jm2007535 NON-PROTEIN TARGET 3
21863888 10.1021/jm2007535 Muscarinic acetylcholine receptor M3 2
21863888 10.1021/jm2007535 Beta-2 adrenergic receptor 2
21863888 10.1021/jm2007535 No relevant target 1
21863888 10.1021/jm2007535 Liver microsomes 1
21863888 10.1021/jm2007535 Beta-1 adrenergic receptor 1
21863888 10.1021/jm2007535 Cavia porcellus 1
21863888 10.1021/jm2007535 Caco-2 1

Data from ChEMBL 36 via Core Engine