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Compound Detail

CHEMBL1773074

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CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOc2ccc(CCNC[C@H](O)c3ccc(O)c(CO)c3)cc2)ccc1O)C(C)C

Basic Information

ChEMBL ID CHEMBL1773074
Phase Preclinical
Structure Type MOL
InChI Key BBKNEJRUSCLTOC-GTZDIBSYSA-N
2
Targets
2
Activities
2
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

668.9
MW (Da)
7.50
ALogP
7
HBA
5
HBD
105.4
PSA (Ų)
0.06
QED
2
Ro5 Violations
20
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C42H56N2O5
MW 668.92
Aromatic Rings 4
Heavy Atoms 49
NP-Likeness -0.03

Activity Summary

EC50 1 meas. best 6.89
Ki 1 meas. best 9.12

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Muscarinic acetylcholine receptor M3
CHEMBL245
Ki 9.12 9.12 0.8 1
Beta-2 adrenergic receptor
CHEMBL210
EC50 6.89 6.89 129.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 54.0 mL.min-1.g-1 Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
21075627 10.1016/j.bmcl.2010.10.132 Muscarinic acetylcholine receptor M3 2
21075627 10.1016/j.bmcl.2010.10.132 Beta-2 adrenergic receptor 2
21075627 10.1016/j.bmcl.2010.10.132 Liver microsomes 1

Data from ChEMBL 36 via Core Engine