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Compound Detail

CHEMBL45422

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CNc1nc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)ccc1C

Basic Information

ChEMBL ID CHEMBL45422
Phase Preclinical
Structure Type MOL
InChI Key QILKJZOYDVAGPZ-UHFFFAOYSA-N
2
Targets
3
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

422.9
MW (Da)
3.96
ALogP
4
HBA
2
HBD
57.3
PSA (Ų)
0.74
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H25ClF2N4O
MW 422.91
Aromatic Rings 2
Heavy Atoms 29
NP-Likeness -1.58

Activity Summary

Ki 2 meas. best 10.4
EC50 1 meas. best 8.67

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 1A
CHEMBL214
Ki 10.4 10.4 0.0 1
5-hydroxytryptamine receptor 1A
CHEMBL273
Ki 10.12 10.12 0.1 1
5-hydroxytryptamine receptor 1A
CHEMBL214
EC50 8.67 8.67 2.1 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10229633 10.1021/jm9806906 Rattus norvegicus 4
10229633 10.1021/jm9806906 5-hydroxytryptamine receptor 1A 2
35939391 10.1021/acs.jmedchem.2c00633 5-hydroxytryptamine receptor 1A 1

Data from ChEMBL 36 via Core Engine