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Compound Detail

CHEMBL4079233

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CCC(=O)NC1CN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)C1.O=C(O)C(F)(F)F.O=C(O)C(F)(F)F.O=C(O)C(F)(F)F.O=C(O)C(F)(F)F

Basic Information

ChEMBL ID CHEMBL4079233
Phase Preclinical
Structure Type MOL
InChI Key NTDJUQMCJZLDRA-UHFFFAOYSA-N
Parent Compound CHEMBL4115977
Active Moiety CHEMBL4115977
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

950.2
MW (Da)
8.12
ALogP
9
HBA
3
HBD
140.9
PSA (Ų)
0.10
QED
2
Ro5 Violations
16
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C64H75F12N9O13
MW 1406.33
Aromatic Rings 4
Heavy Atoms 70
NP-Likeness -0.49

Activity Summary

Ki 5 meas. best 9.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Muscarinic acetylcholine receptor M2
CHEMBL211
Ki 9.15 9.15 0.7 1
Muscarinic acetylcholine receptor M4
CHEMBL1821
Ki 8.44 8.44 3.6 1
Muscarinic acetylcholine receptor M1
CHEMBL216
Ki 8.15 8.15 7.1 1
Muscarinic acetylcholine receptor M5
CHEMBL2035
Ki 7.11 7.11 77.6 1
Muscarinic acetylcholine receptor M3
CHEMBL245
Ki 6.7 6.7 199.5 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28388054 10.1021/acs.jmedchem.6b01892 Muscarinic acetylcholine receptor M3 1
28388054 10.1021/acs.jmedchem.6b01892 Muscarinic acetylcholine receptor M4 1
28388054 10.1021/acs.jmedchem.6b01892 Muscarinic acetylcholine receptor M5 1
28388054 10.1021/acs.jmedchem.6b01892 Muscarinic acetylcholine receptor M1 1
28388054 10.1021/acs.jmedchem.6b01892 Muscarinic acetylcholine receptor M2 1
28388054 10.1021/acs.jmedchem.6b01892 No relevant target 1

Data from ChEMBL 36 via Core Engine