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Compound Detail

CHEMBL256121

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CC#CCn1c(N2CCC[C@@H](N)C2)nc2c(C)nn(Cc3nc(C)c4ccccc4n3)c(=O)c21

Basic Information

ChEMBL ID CHEMBL256121
Phase Preclinical
Structure Type MOL
InChI Key JOAPVBJGWDLSMU-GOSISDBHSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

456.6
MW (Da)
2.15
ALogP
9
HBA
1
HBD
107.8
PSA (Ų)
0.47
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H28N8O
MW 456.55
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -1.39

Activity Summary

IC50 2 meas. best 9.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 9.0 9.0 1.0 1
Muscarinic acetylcholine receptor M1
CHEMBL216
IC50 7.03 7.03 93.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18485703 10.1016/j.bmcl.2008.04.075 Dipeptidyl peptidase 4 1
18485703 10.1016/j.bmcl.2008.04.075 Muscarinic acetylcholine receptor M1 1
18485703 10.1016/j.bmcl.2008.04.075 Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine