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Compound Detail

CHEMBL147824

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CO/N=C(\COCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC(N2CCCC2=O)CC1)c1ccc(Cl)c(Cl)c1

Basic Information

ChEMBL ID CHEMBL147824
Phase Preclinical
Structure Type MOL
InChI Key QBBGNPIZYIFEFU-XOKHWMEBSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

668.5
MW (Da)
7.81
ALogP
5
HBA
0
HBD
54.4
PSA (Ų)
0.14
QED
2
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H33Cl2F6N3O3
MW 668.51
Aromatic Rings 2
Heavy Atoms 44
NP-Likeness -0.88

Activity Summary

Ki 2 meas. best 8.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Substance-K receptor
CHEMBL2327
Ki 8.15 8.15 7.0 1
Substance-P receptor
CHEMBL249
Ki 8.05 8.05 9.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Substance-K receptor Ki = 7.0 nM 8.15 Binding affinity towards NK2 receptor 11229755
Substance-P receptor Ki = 9.0 nM 8.05 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