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Compound Detail

CHEMBL416736

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CCc1noc(C2CN=CNC2)n1.O=C(O)C(F)(F)F

Basic Information

ChEMBL ID CHEMBL416736
Phase Preclinical
Structure Type MOL
InChI Key DGWZWAJULKDIKA-UHFFFAOYSA-N
Parent Compound CHEMBL1185481
Active Moiety CHEMBL1185481
4
Targets
4
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

180.2
MW (Da)
0.35
ALogP
5
HBA
1
HBD
63.3
PSA (Ų)
0.71
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C10H13F3N4O3
MW 294.23
Aromatic Rings 1
Heavy Atoms 13
NP-Likeness -1.50

Activity Summary

EC50 2 meas. best 5.0
IC50 2 meas. best 6.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Muscarinic acetylcholine receptor
CHEMBL1907609
IC50 6.0 6.0 1000.0 1
Unchecked
CHEMBL612545
IC50 6.0 6.0 1000.0 1
Muscarinic acetylcholine receptor M3
CHEMBL5105
EC50 5.0 5.0 10000.0 1
Muscarinic acetylcholine receptor M1
CHEMBL3733
EC50 4.92 4.92 12000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9111297 10.1021/jm960467d Muscarinic acetylcholine receptor M1 2
9111297 10.1021/jm960467d Muscarinic acetylcholine receptor M3 2
9111297 10.1021/jm960467d Unchecked 1
9111297 10.1021/jm960467d Rattus norvegicus 1
8464038 10.1021/jm00059a008 Muscarinic acetylcholine receptor 1
8464038 10.1021/jm00059a008 Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine