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Compound Detail

CHEMBL21284

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CCCC#Cc1noc(C2CN=CNC2)n1.O=C(O)C(F)(F)F

Basic Information

ChEMBL ID CHEMBL21284
Phase Preclinical
Structure Type MOL
InChI Key YHHMFQRQKZKOQM-UHFFFAOYSA-N
Parent Compound CHEMBL1178328
Active Moiety CHEMBL1178328
2
Targets
3
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

218.3
MW (Da)
0.94
ALogP
5
HBA
1
HBD
63.3
PSA (Ų)
0.75
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 C13H15F3N4O3
MW 332.28
Aromatic Rings 1
Heavy Atoms 16
NP-Likeness -0.32

Activity Summary

Ki 2 meas. best 7.76
IC50 1 meas. best 5.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Muscarinic acetylcholine receptor M1
CHEMBL3733
Ki 7.76 7.31 17.4 2
Unchecked
CHEMBL612545
IC50 5.64 5.64 2300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9111297 10.1021/jm960467d Muscarinic acetylcholine receptor M1 4
9111297 10.1021/jm960467d Unchecked 1
9111297 10.1021/jm960467d Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine