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Compound Detail

CHEMBL419500

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COc1ccccc1CN[C@H]1C2CCN(CC2)[C@@H]1C(c1ccccc1)c1ccccc1

Basic Information

ChEMBL ID CHEMBL419500
Phase Preclinical
Structure Type MOL
InChI Key FLNYLINBEZROPL-WUFINQPMSA-N
3
Targets
5
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

412.6
MW (Da)
5.08
ALogP
3
HBA
1
HBD
24.5
PSA (Ų)
0.59
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H32N2O
MW 412.58
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness 0.11

Activity Summary

IC50 5 meas. best 9.48

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Substance-P receptor
CHEMBL249
IC50 9.48 6.9867 0.3 3
Substance-P receptor
CHEMBL3942
IC50 8.0 8.0 10.0 1
Substance-P receptor
CHEMBL4027
IC50 6.1 6.1 800.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.1016/S0960-894X(01)81197-5 Substance-P receptor 3
1378901 10.1021/jm00092a009 Cavia porcellus 2
1378901 10.1021/jm00092a009 Substance-P receptor 1
1378901 10.1021/jm00092a009 Rattus norvegicus 1
- 10.1016/S0960-894X(01)81197-5 Substance-K receptor 1
- 10.1016/S0960-894X(01)81197-5 Neuromedin-K receptor 1
16220969 10.1021/jm058225d Substance-P receptor 1
16220969 10.1021/jm058225d Substance-K receptor 1
28710964 10.1016/j.ejmech.2017.06.056 Substance-P receptor 1

Data from ChEMBL 36 via Core Engine