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Compound Detail

CHEMBL1917850

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COc1ccc(-n2nnnc2C(F)(F)F)cc1CN[C@H]1CCN(S(C)(=O)=O)C[C@H]1c1ccccc1

Basic Information

ChEMBL ID CHEMBL1917850
Phase Preclinical
Structure Type MOL
InChI Key RUDMNOHAIPDMCF-OALUTQOASA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

510.5
MW (Da)
2.60
ALogP
8
HBA
1
HBD
102.2
PSA (Ų)
0.52
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 C22H25F3N6O3S
MW 510.54
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -1.64

Activity Summary

IC50 1 meas. best 10.12

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Substance-P receptor
CHEMBL249
IC50 10.12 10.12 0.1 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Substance-P receptor IC50 = 0.075 nM 10.12 Displacement of [125I]BH-SP from NK1 receptor in human IM9 cells after 30 mins b... 21944973

Literature References

PubMed DOI Target Context # Activities
21944973 10.1016/j.bmc.2011.08.070 Substance-P receptor 1
21944973 10.1016/j.bmc.2011.08.070 Cavia porcellus 1
21944973 10.1016/j.bmc.2011.08.070 Liver microsomes 1

Data from ChEMBL 36 via Core Engine