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Compound Detail

CHEMBL487986

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O=C(Nc1cccc(SC(F)(F)F)c1)N1CCC(N2CCC(n3c(=O)[nH]c4cc(Cl)ccc43)CC2)CC1

Basic Information

ChEMBL ID CHEMBL487986
Phase Preclinical
Structure Type MOL
InChI Key GIWVDIDTRYDGRF-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

554.0
MW (Da)
5.93
ALogP
5
HBA
2
HBD
73.4
PSA (Ų)
0.39
QED
2
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H27ClF3N5O2S
MW 554.04
Aromatic Rings 3
Heavy Atoms 37
NP-Likeness -1.82

Activity Summary

EC50 1 meas. best 5.44

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Muscarinic acetylcholine receptor M1
CHEMBL216
EC50 5.44 5.44 3600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Muscarinic acetylcholine receptor M1 EC50 = 3600.0 nM 5.44 Agonist activity at muscarinic M1 receptor 18829311

Literature References

PubMed DOI Target Context # Activities
18829311 10.1016/j.bmcl.2008.09.032 Muscarinic acetylcholine receptor M1 2
18829311 10.1016/j.bmcl.2008.09.032 Muscarinic acetylcholine receptor M2 1
18829311 10.1016/j.bmcl.2008.09.032 Muscarinic acetylcholine receptor M3 1
18829311 10.1016/j.bmcl.2008.09.032 Muscarinic acetylcholine receptor M4 1
18829311 10.1016/j.bmcl.2008.09.032 Muscarinic acetylcholine receptor M5 1
18829311 10.1016/j.bmcl.2008.09.032 D(2) dopamine receptor 1

Data from ChEMBL 36 via Core Engine