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Compound Detail

CHEMBL1773197

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CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCNC(=O)Cc2cccc(CC(C)(C)NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)c2)ccc1O)C(C)C

Basic Information

ChEMBL ID CHEMBL1773197
Phase Preclinical
Structure Type MOL
InChI Key DNVDKAWXAWHRBJ-HIJQYJRJSA-N
5
Targets
5
Activities
2
Assay Types
1
PK Parameters
4
Publications
0
Known Names

Molecular Properties

787.1
MW (Da)
7.05
ALogP
8
HBA
6
HBD
151.2
PSA (Ų)
0.04
QED
3
Ro5 Violations
21
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C45H62N4O6S
MW 787.08
Aromatic Rings 4
Heavy Atoms 56
NP-Likeness -0.48

Activity Summary

EC50 4 meas. best 8.89
Ki 1 meas. best 9.56

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Muscarinic acetylcholine receptor M3
CHEMBL245
Ki 9.56 9.56 0.3 1
NON-PROTEIN TARGET
CHEMBL3879801
EC50 8.89 8.89 1.3 1
Beta-2 adrenergic receptor
CHEMBL5414
EC50 8.68 8.68 2.1 1
Muscarinic acetylcholine receptor M3
CHEMBL5498
EC50 8.28 8.28 5.3 1
Beta-2 adrenergic receptor
CHEMBL210
EC50 8.09 8.09 8.1 1

Pharmacokinetic Data

Parameter Value Units Species
CL 109.0 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 4
21075627 10.1016/j.bmcl.2010.10.132 Beta-2 adrenergic receptor 3
21075627 10.1016/j.bmcl.2010.10.132 NON-PROTEIN TARGET 2
21075627 10.1016/j.bmcl.2010.10.132 Liver microsomes 1

Data from ChEMBL 36 via Core Engine