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Compound Detail

CHEMBL144223

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CCOC(=O)C1CCCN(C2CCN(CCC(/C(COCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)=N/OC)c3ccc(Cl)c(Cl)c3)CC2)C1

Basic Information

ChEMBL ID CHEMBL144223
Phase Preclinical
Structure Type MOL
InChI Key DIISULLEIDDLEJ-XVDWRUNBSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

740.6
MW (Da)
8.46
ALogP
7
HBA
0
HBD
63.6
PSA (Ų)
0.09
QED
2
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C34H41Cl2F6N3O4
MW 740.61
Aromatic Rings 2
Heavy Atoms 49
NP-Likeness -1.01

Activity Summary

Ki 2 meas. best 7.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Substance-K receptor
CHEMBL2327
Ki 7.7 7.7 20.0 1
Substance-P receptor
CHEMBL249
Ki 6.93 6.93 117.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Substance-K receptor Ki = 20.0 nM 7.7 Binding affinity towards NK2 receptor 11229755
Substance-P receptor Ki = 117.0 nM 6.93 Binding affinity towards NK1 receptor 11229755

Literature References

PubMed DOI Target Context # Activities
11229755 10.1016/s0960-894x(00)00702-2 Substance-P receptor 1
11229755 10.1016/s0960-894x(00)00702-2 Substance-K receptor 1

Data from ChEMBL 36 via Core Engine