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Compound Detail

CHEMBL478034

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O=c1[nH]c2ccccc2n1C1CCN(C2CCN(Cc3ccccc3[N+](=O)[O-])CC2)CC1

Basic Information

ChEMBL ID CHEMBL478034
Phase Preclinical
Structure Type MOL
InChI Key RCRAYIPXTHUIJR-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

435.5
MW (Da)
3.54
ALogP
6
HBA
1
HBD
87.4
PSA (Ų)
0.49
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H29N5O3
MW 435.53
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -1.42

Activity Summary

EC50 1 meas. best 6.92
IC50 1 meas. best 5.95

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Muscarinic acetylcholine receptor M1
CHEMBL216
EC50 6.92 6.92 120.0 1
D(2) dopamine receptor
CHEMBL217
IC50 5.95 5.95 1130.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Muscarinic acetylcholine receptor M1 EC50 = 120.0 nM 6.92 Agonist activity at muscarinic M1 receptor 18805692
D(2) dopamine receptor IC50 = 1130.0 nM 5.95 Inhibition of dopamine D2 receptor 18805692

Literature References

PubMed DOI Target Context # Activities
18805692 10.1016/j.bmcl.2008.09.023 Muscarinic acetylcholine receptor M1 2
18805692 10.1016/j.bmcl.2008.09.023 D(2) dopamine receptor 1
18805692 10.1016/j.bmcl.2008.09.023 Muscarinic acetylcholine receptor M2 1
18805692 10.1016/j.bmcl.2008.09.023 Muscarinic acetylcholine receptor M3 1
18805692 10.1016/j.bmcl.2008.09.023 Muscarinic acetylcholine receptor M4 1
18805692 10.1016/j.bmcl.2008.09.023 Muscarinic acetylcholine receptor M5 1

Data from ChEMBL 36 via Core Engine